TWI327569B

TWI327569B - Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them

Info

Publication number: TWI327569B
Application number: TW90119473A
Authority: TW
Inventors: Fancelli Daniele; Pittal A Valeria; Varasi Mario
Original assignee: Pharmacia & Upjohn Spa
Priority date: 2001-08-09
Filing date: 2001-08-09
Publication date: 2010-07-21

Description

^27569 吞、發明說明（1) 本發明係有關用作為勃有關雙環咄唑衍生物^^抑制劑之心坐衍生物’特別係組成物及其用作為治療劑法、包含該化合物之醫藥聯疾病之用途。将別用於治療蛋白質激酶失調關蛋白質激酶（PKs)功能失古月θ — A 類癌# Ρ μ μ I θ λ 周疋無數疾病的正字標記。人活：癌基因及前致癌基因皆編碼…。… 關病、神經纖維瘤$ '乾癣、動脈粥狀硬化包增生、肺臟纖維化、關節炎、腎小改月乂及手術後狹窄以及血管再度狹窄。，白質激酶也涉及發炎病情以及病毒及寄生蟲的夤激酶於神經退化病症的病因及發要二蛋白質激酶功能異常或失調可概；二的目前觀點，1 9 9 9，3，459-456。生物學本發明之目的係提供可用於治療作為對抗活性失調引發的宿主疾病之藥劍藉由蛋白質激 1匕。物。本發明之另一目的係提供具有多香疋^ 之化合物。蛋白質激酶抑制活性發明人今日發現雙環°比°坐類具有多重性，因此可用於治療蛋白質激酶失詷白質激蜂抑制活 w關聯疾病。更特別的是，本發明之雙環。比嗅可用於括但非限於癌瘤如膀胱癌、乳癌、結腸癌、^ :裡癌症包肺癌包括小細胞肺癌、食道癌、膽囊癌、癌' 肝癌、胃癌、子宮頸癌、曱狀腺癌、攝蠖腺癌及^ $癌' 胰癌' 皮·膚癌包括鱗狀^27569 吞,发明说明(1) The present invention relates to a heart-sitting derivative 'special line composition" which is used as a bismuth-related bicyclic carbazole derivative inhibitor, and a pharmaceutical combination comprising the same as a therapeutic agent method The use of the disease. It will be used to treat protein kinase dysregulation protein kinase (PKs) function loss of ancient θ - A type of cancer # Ρ μ μ I θ λ 疋疋疋疋疋疋疋疋疋疋疋. Human life: Both oncogenes and pro-oncogenes are encoded... ... Guan disease, neurofibromatosis $ 'dry sputum, atherosclerotic sclerotherapy, pulmonary fibrosis, arthritis, small renal stenosis and postoperative stenosis and vascular stenosis. White matter kinases are also involved in inflammatory conditions and the etiology and development of prase kinases in neurodegenerative disorders of the virus and parasites. Two protein kinase dysfunctions or disorders can be summarized; the current view of the two, 1 9 9 9, 3, 459-456. Biology The object of the present invention is to provide a drug that can be used to treat a host disease caused by an antagonistic activity disorder by protein stimulation. Things. Another object of the present invention is to provide a compound having a polyterpenoid. Protein Kinase Inhibitory Activity The inventors found today that the bicyclic ratio is multiplicative and therefore useful for the treatment of protein kinase deficient white matter bees, which inhibit live w associated diseases. More particularly, the double ring of the present invention. Specific stimuli can be used but not limited to cancers such as bladder cancer, breast cancer, colon cancer, cancer: lung cancer including small cell lung cancer, esophageal cancer, gallbladder cancer, cancer ' liver cancer, stomach cancer, cervical cancer, verrucous adenocarcinoma , salivary gland cancer and ^ $ cancer ' pancreatic cancer ' skin and skin cancer including squamous

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C:\2D-O0DE\91-01\90119473.ptd 第4頁 1327569 五、發明說明（2) · 細胞癌，類淋巴細胞系的造‘ α ^ & 1十此系的k血腫瘤包括白血病、急性淋巴細胞性白血病、急性趾p孙☆ 〜性淋巴母細胞性白血病、B-細胞淋巴瘤、T-細胞淋巴瘤、何木仝 f ^ JJ： Λ .....氏淋巴瘤、非何杰金氏淋巴瘤、髮狀細胞淋巴瘤及伯券姓知汉1日見特氏淋巴瘤（Burkett，s lymphoma);骨髓細胞李之徉虬乐（&血腫瘤包括急性及慢性骨髓生成性白血病、骨髓蓉墟柯 ^ ^ +腿委細眭白血病以及前骨髓細胞性白血 ,r s „ ., ^ 〕腫尾匕括纖維肉瘤及橫紋肌肉瘤；中 _ 渴匕栝玍狀細胞瘤、神經母細胞瘤、神經膠細胞瘤及許旺氏細胎，商·甘a # 十^ A ^ T 土民·，，田胞瘤，其他腫瘤包括黑素細胞瘤、精細胞瘤、畸胎瘤、骨肉瘤、著色性乾皮病、角質棘皮瘤、甲狀腺渡泡癌以及卡波西氏肉瘤。角貝棘 :於蛋白質激酶於細胞增生調節上扮演關鍵角色，此等又比ί 可用於治療多種細胞增生病症例如良性攝護腺肥大、豕族性腺瘤病、息肉病、神經纖維瘤病、乾癬 '動脈粥狀硬化關聯的血營ΗΠ ^ 2ΐΛ a. ^ J s十滑肌細胞增生、肺臟纖維化、關節炎、腎小球性腎炎及手術後狹窄以及血管再度狹窄。本發明化合物如cdk5涉及tau蛋白質磷酸化（生物化學期刊，117，741-749，1 995)提示也可用於治療阿茲海默氏病0 本發明化合物作為細胞凋零程序調節劑也可用於治療癌症、病毒感染、預防Η I V感染個體發展成愛滋病、自體免疫病以及神經退化病症。本發明化合物可用於抑制腫瘤血管生成及轉移。本發明化合物可用作為環素依賴型激酶（cdk)抑制劑也C:\2D-O0DE\91-01\90119473.ptd Page 4 1327569 V. INSTRUCTIONS (2) · Cellular carcinoma, lymphoid lineage-like α ^ & 1 ten-line k-blood tumor including leukemia Acute lymphocytic leukemia, acute toe granulosa ☆ ~ lymphoblastic leukemia, B-cell lymphoma, T-cell lymphoma, He Mutong f ^ JJ: Λ ..... lymphoma, non-He Jie Jin's lymphoma, hair cell lymphoma, and Burdock's surname known as Burk's lymphoma (Burkett, s lymphoma); bone marrow cells Li Zhile (& blood tumors including acute and chronic myelogenous leukemia , bone marrow Rongxu Ke ^ ^ + leg Committee fine leukemia and pre-myeloid cell white blood, rs „., ^ 〕 swollen tail fibrosis and rhabdomyosarcoma; middle _ thirsty sickle cell tumor, neuroblastoma, Glioma cell tumor and Xuwang's fine fetus, Shang·Gan a #十^ A ^ T Tumin·,, Tian tumor, other tumors including melanoma, spermatoma, teratoma, osteosarcoma, coloration Dry skin disease, horny acanthoma, thyroid follicular carcinoma, and Kaposi's sarcoma. Protein kinases play a key role in the regulation of cell proliferation, which in turn can be used to treat a variety of cell proliferative disorders such as benign prostatic hypertrophy, steroidal adenoma, polyposis, neurofibromatosis, cognac 'atherosclerosis Associated blood camp ΗΠ ^ 2ΐΛ a. ^ J s ten-slip muscle cell hyperplasia, pulmonary fibrosis, arthritis, glomerulonephritis and postoperative stenosis and vascular stenosis. The compounds of the invention such as cdk5 are involved in tau protein phosphorylation ( The Journal of Biochemistry, 117, 741-749, 1 995) suggests that it can also be used to treat Alzheimer's disease. 0 The compounds of the present invention are useful as modulators of cell dying procedures and can also be used to treat cancer, viral infections, and prevention of sputum infection. AIDS, autoimmune diseases, and neurodegenerative disorders. The compounds of the invention are useful for inhibiting tumor angiogenesis and metastasis. The compounds of the invention may be used as cyclocycline-dependent kinase (cdk) inhibitors.

C:\2D-C0DE\91-01\90119473.ptd 第5頁 1327569 耳、發明說明（3) . 可用作為其他蛋白質激酶抑制劑例如不词異構形式的蛋白質激酶C、Met、PAK_4、PAK-5、ZC-1.、STLK-2、DDR-2、阿羅拉（Aurora)〗、阿羅拉2、Bub-l、PLK、Chkl、Chk2、 HER2 、rafl 、MEK1 、MAPK 、EGF-R 、PDGF-R 、FGF-R ' IGF-R、VEGF-R、PI3K ' 威爾激酶（weel kinase)、Src、C:\2D-C0DE\91-01\90119473.ptd Page 5 1327569 Ear, invention description (3). It can be used as other protein kinase inhibitors such as protein kinases C, Met, PAK_4, PAK- 5, ZC-1., STLK-2, DDR-2, Aurora, Aurora 2, Bub-l, PLK, Chkl, Chk2, HER2, rafl, MEK1, MAPK, EGF-R, PDGF- R, FGF-R ' IGF-R, VEGF-R, PI3K ' Weel kinase, Src,

Abl、Akt 'ILK 'MK-2 'IKK-2、Cdc7、Nek，因此可有效用於治療其他蛋白質激酶關聯疾病。如此本發明提供一種患有由蛋白質激酶活性變更所引發及/或關聯疾病之哺乳類包括人類之方法，該方法係經/ 對有需要的哺乳類投予治療有效量之一種式（丨）雙環吼唾化合物：Abl, Akt 'ILK 'MK-2 'IKK-2, Cdc7, Nek, is therefore effective for the treatment of other protein kinase-associated diseases. Thus, the present invention provides a method of treating a mammal, including a human, caused by a change in protein kinase activity and/or associated disease, by administering a therapeutically effective amount of a formula (丨) bicyclic 吼 saliva to a mammal in need thereof Compound:

_其中 R及&為相同或相異且分別為氫原子或視需要經取代基團選自 R，、-COR, 、-COOR，、_C0NHR,、-CONR，R"、土 -NH-C( = NH)NHR’、-C(=NH)NHR,、-S02R’、-S〇2NHR，或 -S〇2NR’ R";其中R’及R"為相同成相異且分別係選自氫或視需要經進一步取代之直鏈或分支Ci_Ce烷基、芳基、c广Wherein R and & are the same or different and are respectively a hydrogen atom or, if desired, a substituent group selected from the group consisting of R, -COR, -COOR, _C0NHR, -CONR, R", earth-NH-C ( = NH)NHR', -C(=NH)NHR,, -S02R', -S〇2NHR, or -S〇2NR' R"; where R' and R" are identical and are selected from Hydrogen or a further linear or branched Ci_Ce alkyl, aryl, c-wide

C:\2D-CODE\91-01\90H9473.ptd 第6頁 1327569C:\2D-CODE\91-01\90H9473.ptd Page 6 1327569

13275691327569

業界已知結構與式（丨）化合物相關之雙環衍生物數量有例如參考Gadekar，Sheekrishna M.等人3，醫藥化學期刊；1968 ， 11(3) ，616-fi18 ·袓-抽 , .y ^ ； b 1 b b 18，揭不雙環衍生物，其未顯示何激酶抑制活性，其特徵為於位置〗具有氮取代基。相反地，本發明之目的式（丨）丨_未經取代之雙環咄唑衍生物為新穎化合物，可經由新穎且極為多樣性的固相組合 ^方法’該方法也包含於本發明之範圍。如此本發明提供一種式（丨）雙環β比唑化合物：The number of bicyclic derivatives known in the art to be related to formula (丨) compounds is described, for example, in Gadekar, Sheekrishna M. et al. 3, Med. Chem. 1968, 11(3), 616-fi18 · 袓-抽, .y ^ b 1 bb 18, a bicyclic derivative which does not exhibit any kinase inhibitory activity and is characterized by having a nitrogen substituent at position. In contrast, the object of the present invention, the unsubstituted bicyclic carbazole derivative, is a novel compound which can be incorporated into the present invention via a novel and extremely diverse solid phase combination method. Thus the present invention provides a bicyclic beta-pyrazole compound of the formula:

(CH2)m (CK)n (I)(CH2)m (CK)n (I)

其中' R及R!為相同或相異且分別為氮原子或視需要經取代基 |團選自 R，、-COR，、-COOR，、_c〇NHR，、_C0NR，R"、" -NH-C〇NH)NHR，、_C(=NH)NHR，、-S02R，、-S02NHR，、 -SOjR’ R";其中R’及R"為相同或相異且分別係選自氮成視需要經進一步取代之直鏈或分支C! -Ce烷基、芳基、匸_ G環烷基及芳基q - Ce烷基或r，及r "共同形成q - c6伸烧基鏈；兀土Wherein 'R and R! are the same or different and are each a nitrogen atom or a substituent; the group is selected from R, -COR, -COOR, _c〇NHR, _C0NR, R", " NH-C〇NH)NHR,, _C(=NH)NHR,, -S02R,, -S02NHR,, -SOjR' R"; where R' and R" are the same or different and are selected from nitrogen formation Further substituted straight chain or branched C!-Ce alkyl, aryl, 匸_G cycloalkyl and aryl q-Ce alkyl or r, and r " together form a q-c6 extended alkyl chain; Bauxite

C: \2D-C0DE\91-01\90119473.ptdC: \2D-C0DE\91-01\90119473.ptd

1327569 五、發明說明（6). -----1327569 V. Description of invention (6). -----

Ra ' Rb ' RC ^.Rd Am ^ it 一 # @ έ ^ t或相異且分別係選自氫、視需要Ra ' Rb ' RC ^.Rd Am ^ it a # @ έ ^ t or different and respectively selected from hydrogen, as needed

Li ’ίΓηϋ 或分支鏈以燒基、芳*、芳基c】—Q 说基或-CH2OR基，其φ 〜乂 ΏΑ ώ? # ^ ,4- a, ' τκ疋義如則，或Ra及Rb及/或Rc及Li 'ίΓηϋ or a branched chain with an alkyl group, an aromatic *, an aryl group c——Q or a —CH 2OR group, φ ～乂ΏΑ ώ? # ^ , 4- a, ' τκ疋如如如, or Ra and Rb and / or Rc and

Rd與其鍵結之碳原子 ^ 烷基。 /、同形成一個硯需要經取代之C3-Ce環 m及η各自分別表示〇式等於2(m + ng2) ; — 2之玉數，但規定m + n係小於或及其醫藥可接受性鹽。本發明之目的亦係接视 ^ -V / T \ 受性鹽用作為藥物。種式⑴化合物或其醫藥可接造匕明用D化合物或其醫藥可接受性鹽用於製 ’、於治療患有蛋白質激酶活性變更引發的及/或關聯的疾病病人。 ^發明之目的之式（丨）化合物可有非對稱碳原子，因此可存在呈外消旋混合物或各別光學異構物。如此式（I)化合物的全部可能異構物、及其混合物、及兩種代謝產物、及醫荜可斑為地★Rd is the carbon atom to which it is bonded ^ alkyl. /, forming a 砚, the C3-Ce ring m and η, which need to be substituted, respectively represent a 〇 formula equal to 2 (m + ng2); 2 the number of jade, but the m + n system is less than or its medical acceptability salt. The object of the present invention is also to treat the ^-V / T \ accepting salt as a drug. A compound of the formula (1) or a pharmaceutically acceptable derivative thereof, or a pharmaceutically acceptable salt thereof, is used in the treatment of a patient suffering from a disease caused by a change in protein kinase activity and/or associated. The compound of the formula (丨) for the purpose of the invention may have an asymmetric carbon atom and thus may exist as a racemic mixture or a separate optical isomer. All possible isomers of the compound of formula (I), and mixtures thereof, and two metabolites, and the doctor's advice can be spotted ★

^ #、蒂』接交性生物前驅物（也稱作A 刖驅樂）以及任何包含該等化人為明之範圍。 /α療方法也屬於本發除前述外，容易了解本發明唑已知可於溶液内快速平衡0物之未經取代之環氮0比 ΗΝ-^ #, 蒂" The accommodating biological precursor (also known as A 刖 drive) and any scope that includes such avatars. /α Therapeutic method is also in the present invention. In addition to the foregoing, it is easy to understand the present invention. The azole which is known to rapidly balance the zero in the solution is unsubstituted.

(I) 為兩種互變異構物混合物： \(I) is a mixture of two tautomers:

Rc I ΗΝ m), da) C:\2D-CODE\91-01\901l9473.ptd 1327569 、、發明說明（7) 如此於本發明，若僅指出式（I )化合物的一種互變異構物，則另一種互變異構物（I a )也屬於本發明之範圍，除非特別註明。用於此處，除非另行載明，否則直鏈或分支q -C6烷基就此使用或呈芳基烷基一詞，意圖表示如曱基、乙基、正丙基、異丙基、正丁基、異丁基、第二丁基、第三丁基、正戊基 '正己基等。較佳為G -C4烷基例如曱基、乙基、正丙 _基、異丙基、正丁基、異丁基、第二丁基、第三丁基。當R，及R”共同形成(：4-(：6伸烷基鏈時，R’及R"與其鍵聯之氮原子共同形成一個旅咬或吼°各°定環。 c3-c6環烷基一詞意圖表示環丙基、環丁基、環戊基及環己基。芳基一詞無論就此或呈芳基烷基，意圖表示單-、雙-或多-碳環系及雜環系烴帶有1至4個環部分稠合或藉單鍵彼此鍵結，其中至少一個碳環系或雜環系環為芳香族。芳基之非限制性實例例如為苯基、外基、聯苯基、α或 /5 -萘基、芴基、9，1 0 -二氫蔥基、π比σ定基、°比D坐基、°密D定基、。荅11丼基、°引D朵基、σ米。坐基、味吐并吼。定基、1，2 -亞甲基二氧苯基、"塞唾基、異。塞唾基、吼洛基、吼洛基苯基、呋喃基、苯基σ夫喃基、苯并四氫夫喃基唑基、異$唑基、D比唑基、氧雜蔥基、D塞吩基、苯并°塞吩基、異吲哚琳基、苯并β米。坐基、四吐基、四。坐基苯基、°比洛咬基四。坐Rc I ΗΝ m), da) C:\2D-CODE\91-01\901l9473.ptd 1327569, invention description (7) Thus, in the present invention, if only one tautomer of the compound of formula (I) is indicated, Then another tautomer (I a ) is also within the scope of the invention unless specifically stated. As used herein, unless otherwise stated, a straight or branched q-C6 alkyl group is used herein or is an arylalkyl group, intended to mean, for example, fluorenyl, ethyl, n-propyl, isopropyl, n-butyl. Base, isobutyl, second butyl, tert-butyl, n-pentyl 'n-hexyl, and the like. Preferred is a G-C4 alkyl group such as an anthracenyl group, an ethyl group, a n-propyl group, an isopropyl group, an n-butyl group, an isobutyl group, a second butyl group, and a tert-butyl group. When R, and R" are formed together (: 4-(:6) alkyl chain, R' and R" together with the nitrogen atom to which they are bonded form a bridging or 吼°°° ring. c3-c6 naphthenic The term "base" is intended to mean cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl. The term aryl is used herein to mean arylalkyl, and is intended to mean mono-, di- or poly-carbocyclic and heterocyclic systems. The hydrocarbon has 1 to 4 ring moieties fused or bonded to each other by a single bond, wherein at least one of the carbocyclic or heterocyclic ring is aromatic. Non-limiting examples of the aryl group are, for example, a phenyl group, an external group, and a hydrazine group. Phenyl, α or /5-naphthyl, anthracenyl, 9,10-dihydroinionyl, π-sigma-based, ° ratio D-based, ° dense D-based, 荅11 fluorenyl, ° 引 D Base, σ m. Sitting base, taste vomiting and sputum. Stationary, 1,2-methylenedioxyphenyl, "sodium, iso-sodium, sulphonyl, fluorenyl phenyl, furan Phenyl, phenyl succinyl, benzotetrahydrofuranzolyl, iso-xazolyl, D-pyrazolyl, oxalyl, D-septyl, benzo-septyl, iso-pyrene Base, benzo-β m. sitting base, four thiol, four. sityl phenyl, ° Bilo bite IV. Ride

C:\2D-O0DE\91-01\90119473.ptd 第10頁 1327569 案號 9011(U7.q 五、發明說明（8) _ 基、異吲哚啉基苯基 °比啶基、喳4啉基、 1，2, 3-***基、卜苯顯然如前文指示，或鍵結至C:\2D-O0DE\91-01\90119473.ptd Page 10 1327569 Case No. 9011 (U7.q V. INSTRUCTIONS (8) _ yl, isoindolinylphenyl pyridyl, quinone Base, 1,2,3-triazolyl, benzene, apparently as indicated above, or bonded to

進一步稠合環。 5至7員雜圖表示飽和由雜原子如 5至7員雜 1，3 -二氧伍咬、°比唾琳烷等。環一詞涵或部分飽氮、氧及環視需要圜、π比喃、°底唆、 •、喳啉基、異喳啉基、2,6~二 D比畊基、苯基喳啉基、笨三唾基等' 本基咬赞基、芳基也表示芳香族碳環系非芳香族雜掙i ^ ^ ^ % 户方晋務雜％糸％，典型為5至7員雜蓋芳香族雜環也稱作芳基，進一和5至7員碳環，其中—志夕硫置換。或多個碳原子經苯并縮合或進一步經取代例如包括、咄咯啶、咄咯啉、咪唑啶、d比唑哌畊、嗎啉、四氫呋喃、氮雜雙環壬Further fused ring. The 5 to 7-member hybrid diagram indicates saturation from heteroatoms such as 5 to 7 members, 1,3 - dioxin, bite, and ratio of salicin. The term "circle" or partial nitrogen, oxygen, and cyclonic needs 圜, π 喃、, ° 唆, •, porphyrinyl, isoindolyl, 2,6~2D than argon, phenyl porphyrin, Stupid three-salt base, etc. 'Benji bite, aryl also means aromatic carbocyclic non-aromatic miscellaneous i ^ ^ ^ % household 晋杂糸%%, typically 5 to 7 members Heterocycles are also known as aryl groups, and are substituted with 5 to 7 membered carbon rings, of which - Zhixi sulfur is substituted. Or a plurality of carbon atoms by benzo condensation or further substitution, for example, including, pyrrolidine, porphyrin, imidazolium, d-pyrazole, morpholine, tetrahydrofuran, azabicyclic guanidine

OCT 3 0 2009 I 根，前文提供給R、Rl、R，及R"、Ra、Rb ' Rc及Rd之定義，前述任何基團於任何一個自由位置可進一步視需要藉一或多個基團例如1至6個基團取代，取代基係選自：鹵原子’端基’氧基（ = 0) ’鲮基，氰基’烷基’全氟化烷基，烯基，炔基，環烷基，芳基，雜環基，胺基及其衍生物例 #烷基胺基、二烷基胺基、芳基胺基、二芳基胺基、脲基、烧基脲基或务基服基.；魏基胺基及其衍生物例如曱醯胺基、烷基羰基胺基、烯基羰基胺基、芳基羰基胺基、烷氧羰基胺基、磺醯胺基、烷基磺醯胺基及芳基磺醯胺基，羥基及其衍生物例如烷氧基、芳氧基、烷基羰基氧基、芳基羰基氧基、環烯基氧基或亞烷基胺基氧基；羰基及其衍OCT 3 0 2009 I root, previously provided for the definition of R, Rl, R, and R", Ra, Rb ' Rc and Rd, any of the above groups may further borrow one or more groups as desired in any free position For example, 1 to 6 groups are substituted, the substituent is selected from: a halogen atom 'terminal group' oxy (= 0) 'fluorenyl, cyano 'alkyl' perfluorinated alkyl, alkenyl, alkynyl, ring Alkyl, aryl, heterocyclic, amine and derivatives thereof #alkylamino, dialkylamino, arylamino, diarylamine, ureido, ureidourea or sulfhydryl Kegen.; Wei-based amine and its derivatives such as decylamino, alkylcarbonylamino, alkenylcarbonylamino, arylcarbonylamino, alkoxycarbonylamino, sulfonylamino, alkyl sulfonate Amidino and arylsulfonylamino, hydroxy and its derivatives such as alkoxy, aryloxy, alkylcarbonyloxy, arylcarbonyloxy, cycloalkenyloxy or alkyleneaminooxy Carbonyl and its derivatives

90119473(替換）-2_ptc 第11頁年月曰修(更)正瞀換頁 | 年月 B 修 OCT 3 0 2003 替换頁 1327569 ___索號 90119473 五、發明說明（9) 生物例如烷基羰基、芳基羰基、烷氧鼓，基、芳氧羰基、環烧氧羰基、胺基羰基、烷基胺基羰基、二烷基胺基羰基；硫化衍生物例如烷硫基、芳硫基、烷基磺醯基、芳基磺醯基、烷基亞磺醯基、芳基亞磺醯基、蒡基磺醯基氧基、胺基磺醯基、烷基胺基磺醯基或二烷基胺基磺醯基。若屬適當各個前述取代基可進一步鞟一或多個前述基團取代。90119473 (replacement)-2_ptc Page 11 Year of the month repair (more) 瞀瞀 | Year of the month B repair OCT 3 0 2003 Replacement page 1327569 ___ cable number 90119473 V, invention description (9) organisms such as alkyl carbonyl, aromatic Alkylcarbonyl, alkoxyfluoride, aryloxycarbonyl, cycloalkyloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl; sulfurized derivatives such as alkylthio, arylthio, alkylsulfonate Mercapto, arylsulfonyl, alkylsulfinyl, arylsulfinyl, fluorenylsulfonyloxy, aminosulfonyl, alkylaminosulfonyl or dialkylamine Sulfonyl. If appropriate, each of the aforementioned substituents may be further substituted with one or more of the foregoing groups.

式（I)化合物之醫藥可接受性鹽為與下列無機或有機酸生成之酸加成鹽，例如硝酸、氫氯酸、氫溴酸、硫酸、過氯酸、磷酸、乙酸、三氟乙酸、丙酸、乙醇酸、乳酸、草 :丙二酸、蘋果酸、順丁烯二酸、馬來酸、檸檬酸、笨甲自文、桂皮酸、扁桃酸、甲烷磺酸、羥乙基磺酸及水揚酸，以及與下列無機或有機鹼生成之鹽，例如鹼金屬或鹼 t金屬’特別鈉、鉀、鈣或鎂氫氧化物、碳酸鹽或碳酸氫 =、無環或環狀胺類較佳為甲基胺、乙基胺、二乙基胺、二乙基胺或D底Π定。本發明化合物為式（1)化合物其^為一C0R，或The pharmaceutically acceptable salts of the compounds of formula (I) are the acid addition salts with the following inorganic or organic acids, such as nitric acid, hydrochloric acid, hydrobromic acid, sulfuric acid, perchloric acid, phosphoric acid, acetic acid, trifluoroacetic acid, Propionic acid, glycolic acid, lactic acid, grass: malonic acid, malic acid, maleic acid, maleic acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, isethionate And salicylic acid, and salts with the following inorganic or organic bases, such as alkali metal or alkali t metal 'special sodium, potassium, calcium or magnesium hydroxide, carbonate or hydrogen carbonate =, acyclic or cyclic amines It is preferably methylamine, ethylamine, diethylamine, diethylamine or D. The compound of the present invention is a compound of the formula (1), wherein the compound is a COR, or

sonhr,^Ri 為R 、~C〇R，、-C0NHR，、一C0NR，R"、_s〇2R， s〇2nr，r”，其〇，及r"為相同或相異且係選其W經取代之直鏈或分支鏈院基、芳基、（V 4^ ""方基Cl 一Ce烷基或及R"共同形成(：4-(：6伸烷基广2同或相異且係選自氫或直鏈或分支鏈w燒 :β二;?鍵結之兔原子共同形成C3_C6環烧基；Rc及Rd皆為氫原子，m為〇或1 。Sonhr,^Ri is R, ~C〇R, -C0NHR, a C0NR, R", _s〇2R, s〇2nr,r", and r, and r" are the same or different and are selected Substituted linear or branched chain, aryl, (V 4^ "" square-based Cl-Ce alkyl or R" together (: 4-(:6-alkyl-alkyl 2 or the same The heterologous is selected from hydrogen or a straight chain or a branched chain. w: β2; the bonded rabbit atoms together form a C3_C6 cycloalkyl group; Rc and Rd are both hydrogen atoms, and m is 〇 or 1.

13275691327569

五、發明說明（10) 另一類較佳本發明杷合物為式（I )化合物其中R為乂⑽，或-CONHR，及R丨為r’、_c〇*R，、-C〇NHR，、-c〇NR，R"、 _S〇2R’ ' -S02NHR’ 或-S02NR’R" ’ 其中R’ &R” 為相同或相異且係選自氫或視需要經取代之直鏈或分支鏈c广q烷基、芳基、環烷基及芳基c】烷基或及R"共同形成一個 c4-c6伸烷基鏈；Ra為氫；Rb為-CH2OR，基，其中R’基定義如前；Rc及Rd皆為氫原子；m為0或1 ; η為〇。土另一類較佳本發明化合物為式（I )化合物，其中R為 -COR，或-CONHR，及R1*R，、-COR，、-C0NHR，、二c〇NR’，R"、 -S02『、-S02NHR’或-〇2NR’ R" ’其中R’ &RII為相同或相異且係選自氫或視需要經取代之直鏈或分支鏈匕-匕烷基、〃芳基、C3-C6環烷基及芳基Ci_Ce烷基或R，及R"共同形成一個 C4-C6伸烷基鏈；“、Rc及Rd皆為氫原子；m&n皆為最佳本發明化合物為式（I)化合物其中R為-COR，或 _C〇NHR 及R】為R’、~C〇R’、-C0NHR’、-C0NR，R”、-S0R，盆 :R二二為相同或相異且係選自氩或視需要經取代之2直鏈 R、芳基、c〆6環烷基及芳基w烷基或且俾$自、:二* .個匕"^6伸烧基鍵；Ra及以為相同或相異 β斥二JbL二二&鏈或分支Cl _C3坑基或Ra ARb與其鍵結的 :原子丄同形成—個c“6環化最佳本發明化合 -C0NHR’ 及R,為只’、物為式（I)化合物其中R為-C〇R，或 C〇R,、-C0NHR，、-C0NR，r"、_s〇r，其V. INSTRUCTION DESCRIPTION (10) Another preferred embodiment of the present invention is a compound of formula (I) wherein R is 乂(10), or -CONHR, and R丨 is r', _c〇*R, -C〇NHR, , -c〇NR, R", _S〇2R' ' -S02NHR' or -S02NR'R" 'where R' &R" are the same or different and are selected from hydrogen or a linear or substituted Branching chain c wide q alkyl, aryl, cycloalkyl and aryl c] alkyl or R" together form a c4-c6 alkyl chain; Ra is hydrogen; Rb is -CH2OR, a group, wherein R' The base is as defined above; Rc and Rd are each a hydrogen atom; m is 0 or 1; η is 〇. Another preferred compound of the invention is a compound of formula (I) wherein R is -COR, or -CONHR, and R1 *R,, -COR,, -C0NHR,, two c〇NR', R", -S02『, -S02NHR' or -〇2NR' R" 'where R' & RII are the same or different and are selected A C4-C6 alkylene group formed by hydrogen or, if desired, substituted linear or branched chain fluorenyl-alkyl, aryl, C3-C6 cycloalkyl and aryl Ci_Ce alkyl or R, and R"Chain; ", Rc and Rd are all hydrogen atoms; m&n are the best The compound is a compound of the formula (I) wherein R is -COR, or _C〇NHR and R are R', ~C〇R', -C0NHR', -C0NR, R", -S0R, pot: R two Is the same or different and is selected from argon or optionally substituted 2 linear R, aryl, c〆6 cycloalkyl and aryl w alkyl or 俾$自,: two *. 匕" ^6 stretching base bond; Ra and thinking that the same or different β repulsion JbL bis2 & chain or branch Cl _C3 pit group or Ra ARb bonded with it: atomic 形成 formed - a c "6 cyclization best The present invention combines -C0NHR' and R, which are only compounds of formula (I) wherein R is -C〇R, or C〇R, -C0NHR, -C0NR, r", _s〇r,

第13頁 1327569Page 13 1327569

1327569 五、發明說明（12) 2. N-{5-乙醯基_4，'6 -二氫吡咯并[3, 4-c]吡唑-3 -基}苯基乙醯胺； 3. N-芊基-Ν’ - {3-苯基乙醯胺基-4, 6 -二氫吡咯并 [3，4 - c ] °比。坐-5 -基}脲； 4. ^{5-甲苯石黃醯基-4,6-二氫0比0各并[3,4-〇]°比。坐-3-基}苯基乙醯胺； 5. Ν-乙基-Ν’ - {3 -苯基乙醯胺基-4, 6 -二氫吡咯并 [3,4-(：]°比°坐-5_基}脲； 6. Ν-{5-乙酿基-4，6_二氮。比。各弁[3，4-c] °比〇坐-3-基}-4_(苯基）苯基乙酿胺， 7· Ν-{5~乙酸基_4，6_二氮π比ρ各并[3，4_c] °比〇坐-3- 基}-2_蔡基乙酿胺； 8. N-{5-乙酸基-4，6 -二氫°比°各并[3,4-c] °比。坐-3 -基}-呋喃-2 -羧醯胺； 9. N-{5-乙酸基-4，6 -二氫0比洛并[3,4-c] °比0坐-3-基} - 5 -氣°塞吩-2 -叛臨胺； 10. N-{5_ 乙酿基_4，6 -二氮 °比 °各并[3，4_c] 0比。坐-3_ 基卜6-氣菸鹼醯胺； 11· N-{5-乙酿基-4, 6_二氣D比p各并[3, 4-c] °比。坐-3-基}-苯并咬。南-2 -敌醢胺； 12. N-{5-乙酿基-4，6 -二氫〇比0各并[3, 4-c] B比 °坐-3_ 基} -4-苯氧苯曱醯胺； 13. N-{5-乙酿基_4,6_ 二氣 D 比 0各并[3，4-c] 〇比°坐-3_ 基} -4-第三丁基苯曱醯胺；1327569 V. INSTRUCTIONS (12) 2. N-{5-Ethyl- 4,'6-dihydropyrrolo[3,4-c]pyrazole-3-yl}phenylacetamidamine; N-fluorenyl-Ν'-{3-phenylacetamido-4,6-dihydropyrrolo[3,4 - c] ° ratio. Sodium-5-yl urea; 4. ^{5-toluene xanthine-4,6-dihydro 0 to 0 and [3,4-〇] ° ratio. -3--3-yl}phenylacetamide; 5. Ν-ethyl-Ν' - {3-phenylethylamido-4,6-dihydropyrrolo[3,4-(:]° ratio ° sit -5_urea urea; 6. Ν-{5-ethyl-branched-4,6-dinitrogen. Ratio. Each 弁[3,4-c] ° than 〇 -3- base}-4_( Phenyl)phenylethylamine, 7· Ν-{5~acetic acid _4,6-diaza π ratio ρ[3,4_c] ° ratio 〇-3-yl}-2_Caiji 8. N-{5-acetic acid-4,6-dihydrogen ratio °[3,4-c] ° ratio. sit-3-yl}-furan-2-carboxycarboxamide; 9. N -{5-Acetyl-4,6-dihydro- 0-By-[3,4-c] ° than 0--3-yl} - 5 - gas ° thiophene-2 - tetamine; 10. N -{5_ ethyl ketone_4,6-diaza ratio ° and each [3,4_c] 0 ratio. sit-3_ kib 6-gas nicotine decylamine; 11· N-{5-ethyl aryl- 4, 6_ two gas D ratio p and [3, 4-c] ° ratio. sit-3-yl}-benzoate bite. South-2 - diterpenoid; 12. N-{5-ethyl -4,6-dihydroindole is 0 and each [3, 4-c] B is more than -3 -yl}-4-phenoxybenzamine; 13. N-{5-ethyl ketone _4, 6_ 二气 D ratio 0 and [3,4-c] 〇 ratio ° sitting -3_ base} -4-th-butylbenzamide;

C:\2D-CODE\91-01\90119473.ptd 第15頁 1327569 五、發明說明（13) 14. N-{5-乙蕴基-4，6 -二氫°比0各并[3，4-c] π比0坐-3-基}-胡椒基醯胺； 15. Ν-{5-乙醯基-4,6 -二氫 °比°各并[3,4-c] °比°坐-3-基}-[2-曱基-5-苯基夫喃-3-缓酿胺]; 16. Ν-{5-乙酿基-4，6 -二氫°比。各并[3，4-c] π比0坐-3_ 基}-(喳啉-6-羧醯胺）； 17. Ν_{5-乙酿基_4，6_二氮°比嚷并[3，4-c] 0比°坐_3-基}_[5-(4-氯苯基）n夫Β南-2_魏醯胺]; _ 18. Ν-{5-曱烧石黃醯基-4,6-二氫°比咯并[3,4-c]0比。坐- 3- _基卜4-第三丁基苯曱醯胺； 19. N-{5 -苯石黃醢基- 4,6 -二氫"比17各并[3,4-c] p比。坐- 3-基} -4-第三丁基苯曱醯胺； 20. Ν-{5 -苯曱醯基- 4,6 -二氫"比0各并[3,4-c] 〇比〇坐- 3-基} -4-第三丁基苯曱醯胺； 21. Ν-{5-(1-萘）續醯基- 4,6 -二氫各并[3,4-c]"比嗤 _3_基}_4_第三丁基苯曱酿胺； 22. Ν-{5-(1-萘甲醯基）-4，6 -二氫0比0各并[3,4-c] 〇比口坐 -3-基}-4-第三丁基苯曱醯胺； >2 3..1{5-苯乙醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基} -4-第三丁基苯曱醯胺； 24. N-苯基-Ν’- {3-(4-第三丁基-苯甲醯胺基）-4,6 -二氫n比p各并[3，4 - c ] °比β坐-5 -基}脲； 25. Ν -異丙基-Ν’ - {3-(4-第三丁基-笨曱醯胺基）-4,6-二氫17比11各并[3，4 - c ]吼°坐-5 -基}脲；C:\2D-CODE\91-01\90119473.ptd Page 15 1327569 V. Description of invention (13) 14. N-{5-Bisyl-4,6-dihydrogen ratio 0 and [3, 4-c] π is 0 -3-yl}-piperidinylamine; 15. Ν-{5-ethinyl-4,6-dihydrogen ratio °[3,4-c] ° ratio ° sitting-3-yl}-[2-mercapto-5-phenylfuran-3-yield amine]; 16. Ν-{5-ethyl-branched-4,6-dihydrogen ratio. Each [3,4-c] π is 0 to sit -3_yl}-(porphyrin-6-carboxyguanamine); 17. Ν_{5-ethyl-branched _4,6-diazepine 嚷[ 3,4-c] 0 than ° sitting _3-yl}_[5-(4-chlorophenyl)nfΒ南-2_魏醯amine]; _ 18. Ν-{5-曱烧石黄醯基-4,6-Dihydrogen ratio is [3,4-c] 0 ratio. Sitting - 3- _ kib 4-tert-butyl benzoguanamine; 19. N-{5 - benzotrisyl - 4,6 - dihydro " than 17 and [3,4-c] p ratio . Sodium-3-yl}-4-t-butylbenzamide; 20. Ν-{5-benzoinyl- 4,6-dihydro" ratio 0 and [3,4-c] 〇〇 - - 3-yl} -4-t-butyl benzoguanamine; 21. Ν-{5-(1-naphthalene) hydrazino- 4,6-dihydro-[3,4-c ]"比嗤_3_基}_4_Third butyl benzoate; 22. Ν-{5-(1-naphthylmethyl)-4,6-dihydro 0 to 0 each [3 , 4-c] 〇口 -3- -3- } -4- butyl butyl benzoguanamine; > 2 3..1 {5-phenethyl fluorenyl-4,6-dihydropyrrolo[ 3,4-〇]pyrazol-3-yl}-4-t-butylbenzamide; 24. N-phenyl-indole-{3-(4-t-butyl-benzamide Base)-4,6-dihydron n ratio p and [3,4 - c ] ° ratio β sit-5-yl}urea; 25. Ν-isopropyl-Ν' - {3-(4- Tributyl-codantamine)-4,6-dihydrogen 17 to 11 and [3,4 - c ]吼° sit-5-yl}urea;

C:\2D-OODE\91-Ol\90119473.ptd 第16頁 1327569 五、發明說明（14) 26.1{5-甲烧石黃醯基-4,6-二氫吡0各并[3,4-(：]13比唑-3-基}-4-苯氧苯甲醯胺； 27. N-{5 -苯曱醯基_4，6 -二氫吼11各并[3，4-c] 0比。坐- 3-基}-4-苯氧苯曱醯胺； 28. N-{5-(1-萘甲醯基）-4,6 -二氫吡咯并[3,4-c]吡唑 -3-基}-4_苯氧苯曱酿胺， 29. N-異丙基-N’-{3-(4-苯氧-苯曱醯胺基）-4,6 -二氫 °比p各并[3，4 - c ] D比。坐-5 -基}脲； 30. N-{5-乙酸基-4，6_ 二氫°比°各并[3，4-c] °比。坐-3-基}_[2_(2 -秦基）丙酿胺]， 31. N_異丙基-N’_{3_胡椒基缓酿胺基）_4，6_二氮吼11各并[3,4-〇]°比°坐-5-基}脲； 32. N -環己基-Ν’-{3-(4-第三丁基-苯甲醯胺基）-4, 6-二氫B比p各并[3，4 - c ] °比α坐-5 -基}脲； 33. Ν-乙基-Ν’-{3-(4-第三丁基-苯曱醯胺基）-4,6 -二氫°比ρ各并[3，4 - c ] °比°坐-5 -基}脲； 34. Ν-(2,6 -二乙基苯基）-Ν’-{3-(4-第三丁基-苯甲醯胺基）-4，6 -二氫吼Β各并[3, 4-c] D比哇-5-基}脲； 35. N -環己基-N’-{3-(2-乙基-丁醯胺基）-4,6 -二氫吡口各并[3，4 - c ] °比°坐-5 -基}脲； 36. N-(2,6 -二乙基苯基）-N’-{3-(胡椒基羧醯胺基）-4, 6 -二氫"比11 各并[3，4-c]°比吐-5-基}脲； 37. N-2-曱氧苯基-Ν’ - {3-(2 -萘-2-基-丙醯胺基）-4,6-二氫D比p各并[3，4 - c ]吼°坐-5 -基}脲；C:\2D-OODE\91-Ol\90119473.ptd Page 16 1327569 V. INSTRUCTIONS (14) 26.1{5-甲烧石黄醯基-4,6-Dihydropyridinium each [3,4-( :]13-pyrazol-3-yl}-4-phenoxybenzamide; 27. N-{5-benzoinyl_4,6-dihydroindole 11 and [3,4-c] 0 Sodium 3-yl}-4-phenoxybenzamine; 28. N-{5-(1-naphthomethyl)-4,6-dihydropyrrolo[3,4-c]pyridinium Zyridin-3-yl}-4-phenoxybenzoquinone, 29. N-isopropyl-N'-{3-(4-phenoxy-benzoguanamine)-4,6-dihydrogen Ratio of p to [3,4 - c ] D ratio. sit -5 -yl}urea; 30. N-{5-acetoxy-4,6_ dihydrogen ratio °[3,4-c] ° Ratio. sit -3-yl}_[2_(2-methyl-yl)propanolamine], 31. N_isopropyl-N'_{3_piperidinylamino)_4,6-diazepine 11 each [3,4-〇]° ratio °-5-yl}urea; 32. N-cyclohexyl-Ν'-{3-(4-t-butyl-benzylamino)-4 , 6-dihydrogen B ratio p and [3,4 - c ] ° ratio α sit-5-yl} urea; 33. Ν-ethyl-Ν'-{3-(4-t-butyl-benzene Amidino)-4,6-dihydrogen ratio ρ[3,4 - c ] ° ratio ° sit-5-yl}urea; 34. Ν-(2,6-diethylphenyl) -Ν'-{3-(4-Terbutyl-benzamide -4,6-dihydroindole each [3,4-c] D than wow-5-yl}urea; 35. N-cyclohexyl-N'-{3-(2-ethyl-butyl) Amino)-4,6-dihydropyrrole each [3,4 - c ] ° ratio ° sit-5-yl}urea; 36. N-(2,6-diethylphenyl)-N' -{3-(Pepperylcarboxycarboxamido)-4,6-dihydro" ratio 11 [3,4-c]° ratio 吐-5-yl}urea; 37. N-2-oxime Phenyl-Ν'-{3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydrogen D is more than p[3,4 - c ]吼°-5-yl} Urea

C:\2D-00DE\91-01\90119473.ptd 第17頁 1327569 五、發明說明（15) 38. N-(l -苯基）乙基-N’-{3-(2 -萘-2 -基-丙醯胺基）-4, 6 -二氫吼洛并[3,4-c]°比。坐-5-基}脲； 39· N-{5-苯基醯胺基-4, 6 -二氫°比°各并[3, 4-c] °比°坐- 3- 基}-3-(2 -萘-2-基）-丙酷胺； 40. N-(2,5 -二甲基苯基）-N’_{3-(4-第三丁基-苯曱醯胺基）-4，6 -二氫吼11 各并[3,4-c] °比°坐-5-基}脲； 41. N-(2,5 -二曱基苯基）-N’-{3-(2-乙基-丁醯胺基）-4，6 -二氫吼p各并[3,4-c]吼°圭-5-基}脲； 42. N-(4-氟苄基）-N’-{3-(2-乙基-丁醯胺基）-4,6 -二 _氫D比B各并[3，4 - c ] °比°坐-5 -基}脲； 43. N-{5-亨基石黃醢基- 4,6 -二氫吼17各并[3,4-c] D比哇- 3-基}-4-第三丁基苯曱醯胺；- 44. N-2 -氯苯基-N’-{3-(2 -萘-2 -基-丙醯胺基）-4,6 -二氫°比各并[3，4 - c ]吼°坐-5 -基}脲； 45_ N-{5 -胺基獄基-4,6 -二氫吼0各并[3，4-c] B比。坐- 3- 基}-2-(2-萘基）-丙醯胺； 46. N-{5-(3-甲基-丁醯基）-4,6 -二氫吡咯并[3,4-c] 。坐-3 -基}_4-苯氧苯甲酿胺； # 47. 1{5-(2-苯基-噻唑-4-基）乙醯基-4,6-二氫吡咯并 [3，4-c]吡唑-3 -基卜4 -苯氧苯甲醯胺； 48. N-{5-(2-°塞吩基-乙醜基）-4, 6 -二氫0比0各并[3,4-c] 吡唑-3-基}-4-第三丁基苯曱醯胺； 49. Ν-{5-(3-πΛ 咬基-乙醯基）-4，6 -二氫 D比 11 各并[3,4-c] 吡唑-3-基}-4-第三丁基苯甲醯胺；C:\2D-00DE\91-01\90119473.ptd Page 17 1327569 V. INSTRUCTIONS (15) 38. N-(l-Phenyl)ethyl-N'-{3-(2-naphthalene-2 -yl-propionylamino)-4,6-dihydroindolo[3,4-c]° ratio. Sodium-5-yl}urea; 39·N-{5-phenylamidoamine-4,6-dihydrogen ratio °[3, 4-c] °°°-3-base}-3 -(2-naphthalen-2-yl)-propanolamine; 40. N-(2,5-dimethylphenyl)-N'_{3-(4-t-butyl-benzoguanamine -4,6-dihydroindole 11 each [3,4-c] ° ratio -5-yl}urea; 41. N-(2,5-dimercaptophenyl)-N'-{ 3-(2-ethyl-butylammonium)-4,6-dihydroindole p-[3,4-c]吼°-5-yl}urea; 42. N-(4-fluorobenzyl) -N'-{3-(2-ethyl-butylammonium)-4,6-di-hydrogen D ratio B and [3,4 - c ] ° ratio ° sit-5-yl}urea 43. N-{5-Henkestone xanthene- 4,6-dihydroindole 17 and [3,4-c] D than wow-3-yl}-4-t-butylbenzamide;- 44. N-2 -Chlorophenyl-N'-{3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydrogen ratio [3,4 - c ]吼° Sodium-5-yl}urea; 45_N-{5-amine-based Pegyl-4,6-dihydroindole 0 and [3,4-c] B ratio. Sodium 3-yl}-2-(2-naphthyl)-propanamine; 46. N-{5-(3-methyl-butenyl)-4,6-dihydropyrrolo[3,4-c ]. -3 -yl}_4-phenoxybenzamide; #47. 1{5-(2-phenyl-thiazol-4-yl)ethenyl-4,6-dihydropyrrolo[3,4 -c]pyrazole-3-pyrimidine-4-phenoxybenzamide; 48. N-{5-(2-°Sepyl-Ethyl)-4,6-dihydrogen 0 to 0 each [3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 49. Ν-{5-(3-πΛ 咬-乙醯基)-4,6 -二Hydrogen D ratio 11 and [3,4-c]pyrazol-3-yl}-4-t-butylbenzamide;

C:\2D-C0DE\91-01\90119473.ptd 第18頁 1327569 五、發明說明（16) 50. N-.{5_窄基石黃酷基-4，6_二氫0比0各并[3，4-c]吼11坐_3-基}-4-苯氧苯曱醯胺；· 51_ N-{5-(2-曱基丙基）羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3 -基卜4-第三丁基苯甲醯胺； 52. N-{5-(2 -苯基_ °比0坐-4-基）乙酿基-4，6_二氫°比。各并 [3,4-c]吡唑-3-基}-4_第三丁基苯曱醯胺； 53. N-{5-(2 -噻吩基-乙醯基）-4,6-二氫。比咯并[3,4-(：] 吡唑-3 -基} - 4 -苯氧苯曱醯胺； 54. N-{5-(苯并[1，3]二氧伍圜-5 -基）乙醯基-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基卜3-甲基丁醢胺； 55. Ν-{5-(1_萘）磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑 -3 -基卜環丙基羧醯胺； 56. N-{ 5-(2-甲氧苯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3-(2-萘-2-基）-丙醯胺； - 57. Ν-{5-(2-β夫喃曱醯基）-4, 6 -二氫0比°各并[3,4-c] 口比唑_3-基}-3-(2-萘-2-基）-丙醯胺； 58.1{5-[5-(1-嗎啉基甲基）呋喃-2-羰基]-4,6-二氫吡咯并[3, 4-c]吡唑-3-基}-4_第三丁基苯曱醯胺； 59. Ν-{5-{4-[2-(1-吡咯啶基）乙氧]苯基}乙醯基-4,6- 二氫吡咯并[3, 4-c]吡唑-3-基}-4-第三丁基苯甲醯胺； 60· N-{5-(卜H-苯并***-5 -羰基）-4,6 -二氫吼咯并[3, 4-c]咄唑-3-基}-4_第三丁基苯曱醯胺； 61,~-{5-(°比咯-3-羰基）乙醯基-4,6-二氫咄咯并 [3,4-c]。比唑-3-基}-4-第三丁基苯曱醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 18 1327569 V. Description of invention (16) 50. N-.{5_Narrow bedrock yellow base-4,6_dihydrogen 0 to 0 each [3,4-c]吼11 sits _3-yl}-4-phenoxybenzamine;· 51_ N-{5-(2-mercaptopropyl)carbonyl-4,6-dihydropyrrole [3,4-(:]pyrazol-3-ylpyr-4-tert-butylbenzylideneamine; 52. N-{5-(2-phenyl-~° ratio 0--4-yl) a ratio of -4,6-dihydrogen. Each [3,4-c]pyrazol-3-yl}-4_t-butylbenzamide; 53. N-{5-(2-thiophene -ethylamino)-4,6-dihydro.pyrolo[3,4-(:]pyrazol-3-yl}-4-phenoxybenzamine; 54. N-{5-( Benzo[1,3]dioxoindol-5-yl)ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl-3-methylbutyramine; 55. Ν-{5-(1_naphthalene)sulfonyl-4,6-dihydropyrrolo[3,4-indolyl]oxazol-3-pyridylcarboxycarboxamide; 56. N-{ 5-(2-methoxyphenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-(2-naphthalen-2-yl)-propanamide; - 57. Ν-{5-(2-β-fucainyl)-4,6-dihydrogen 0 ratio °[3,4-c] portazole-3-3}-3-(2 -naphthalen-2-yl)-propanamine; 58.1{5-[5-(1-morpholinylmethyl)furan-2- Carbonyl]-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4_t-butylbenzamide; 59. Ν-{5-{4-[2- (1-pyrrolidinyl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide 60·N-{5-(Bu H-benzotriazol-5-carbonyl)-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-4_third Butyl benzoguanamine; 61,~-{5-(°-pyrrol-3-carbonyl)ethenyl-4,6-dihydroindolo[3,4-c].pyrazol-3-yl }-4-tert-butylbenzamide;

C:\2D-GODE\91-01\90119473.ptd 第19頁 1327569 五、發明說明（17) ' 62. N-{5-{4-[2 -氧基-2-U- °比咯啶基）乙氧]苯基}乙醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 63. N-{5_(4-曱基續酿胺基_苯基）乙酿基_4，6_二氫°比咯并[3,4-c]咄唑-3-基卜4-苯氧苯曱醯胺； 64. ^{5-[2-(6-氧基-1(61〇-嗒啡基}乙醯基-4,6-二氫吡咯并[3, 4-c]吡唑-3 -基}-4-苯氧苯曱醯胺； 65.1^-{5-(3-胺基甲醯基甲氧-苯基）乙醯基-4,6-二氫 Λ。比咯并[3,4-c]吡唑-3-基}-4-笨氧苯曱醯胺；讎66. N-{5-(4-胺基曱醯基甲氧-苯基）乙醯基-4,6-二氫口比咯并[3, 4-c]吼唑-3-基卜4-苯氧苯曱醯胺； 6 7· N-{ 5-[4-(1-吡咯啶基）苯基]乙醯基-4, 6 -二氫吡咯并[3,4-c]吼唑-3-基}-4_苯氧苯曱醯胺； 68. N-{5 -胺基甲醯氧基乙醯基-4, 6 -二氫吡11 各并 [3,4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 69. N-{5-{4-[2-(4-甲基哌畊-2 -基）乙氧]苯基}乙醯基 -4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-苯氧苯曱醯胺； 70. Ν-{5-{4-[2-(1-吡咯啶基）乙氧]苯基}乙醯基-4,6-‘二氫咄咯并[3, 4-c]咄唑-3 -基卜4-苯氧苯曱醯胺； 71· N-{5-{4-[2 -氧基-2-(1-吼咯啶基）乙氧]苯基}乙醯基-4,6-二氮°比洛并[3，4-c]D比0坐_3_基}_4-第三丁基苯甲醢胺； 72. N_{5_(4_曱基石黃酿胺基-苯基）乙酿基_4，6_二氮°比咯并[3,4-c]吼唑-3-基}-4-第三丁基苯甲醯胺；C:\2D-GODE\91-01\90119473.ptd Page 19 1327569 V. INSTRUCTIONS (17) ' 62. N-{5-{4-[2-Oxo-2-U-°bibromopyridine Ethyl]phenyl}ethenyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 63. N-{ 5-(4-indolyl arylamino-phenyl) ethyl bromo-4,6-dihydro-pyrolo[3,4-c]oxazol-3-yl-4-phenylphenoxybenzamine 64. ^{5-[2-(6-Alkoxy-1(61〇-嗒- yl)}ethinyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl }-4-phenoxybenzamine; 65.1^-{5-(3-aminocarbamimidomethoxy-phenyl)ethinyl-4,6-dihydroanthracene. -c]pyrazol-3-yl}-4- phenoxybenzamine; 雠66. N-{5-(4-aminomercaptomethoxy-phenyl)ethenyl-4,6- Dihydrogen-n-butyr[3,4-c]oxazol-3-ylbu-4-phenoxybenzamine; 6 7·N-{ 5-[4-(1-pyrrolidinyl)phenyl] Ethyl 4-(6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-phenoxyphenyl hydrazide; 68. N-{5-aminomethyl methoxy ethoxylate Mercapto-4,6-dihydropyrrole 11 each [3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 69. N-{5-{4-[2- (4-methylpipedin-2-yl)ethoxy]phenyl}ethinyl-4,6-dihydropyridyl [3,4-(:]pyrazol-3-yl}-4-phenoxybenzamine; 70. Ν-{5-{4-[2-(1-pyrrolidinyl)ethoxy] Phenyl}ethenyl-4,6-'dihydroindolo[3,4-c]indazol-3-yl-4-phenoxybenzamine; 71·N-{5-{4- [2-oxy-2-(1-pyridyridyl)ethoxy]phenyl}ethinyl-4,6-diaza°Bilo[3,4-c]D is 0 _3_ __4-t-butyl benzamide; 72. N_{5_(4_曱石石黄-amino-phenyl) ethyl ketone _4,6-diazepine ratio [3,4- c] oxazol-3-yl}-4-t-butylbenzamide;

C:\2D-C0DE\91-01\90119473.ptd 第20頁 1327569 五、發明說明（18) 7 3. N - {. 5 -(吡啶-3 -羰基）-4，6 -二氫p比咯并[3，4 - c ]吡唑 -3-基卜4-第三丁基苯甲醯胺； 74. N-{5-(吼啶-3-羰基）-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-4-第三丁基苯曱醯胺； 75_ N-{5-( D比啶-4-羰基）-4,6 -二氫吼11各并[3,4-c] D比0坐 -3-基}-4-第三丁基苯曱醯胺； 76. N-{ 5-(2-甲基-咄啶-3 -羰基）-4, 6 -二氫吡咯并 [3,4-(：]°比唑-3-基}-4-第三丁基苯曱醯胺； 77. N-{ 5-(2 -硫曱基-吡啶-3 -羰基）-4, 6 -二氫吼咯并 [3，4-c] 0比°坐-3-基}_4-第三丁基苯曱酿胺； 7 8. N - { 5 - ( °比 D井-2 -叛基）-4，6 -二氫 °比 p各并[3，4 - c ] »比。坐 _3-基}_4_第二丁基苯曱酿胺， 79. N-{5-(3 -呋喃曱醯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-4-苯氧苯甲醯胺； 80. Ν-{5-(2-σ塞吩甲醯基）-4,6 -二氫0比略并[3,4-c] °比唑-3-基}-4-苯氧苯甲醯胺； 81. N-{5-(7-曱氧-苯并呋喃-2-羰基）-4,6 -二氫吡咯并 [3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 82. N-{5-(苯并呋喃-2 -羰基）-4,6 -二氫吼咯并[3,4-c] 吡唑-3-基}-4-第三丁基苯曱醯胺； 83. N-{5-(2 -呋喃曱醯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-4-第三丁基苯甲醯胺； 84. N-{5-(3-0夫喃曱醯基）-4,6 -二氫吼口各并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 20 1327569 V. INSTRUCTIONS (18) 7 3. N - {. 5 -(pyridine-3-carbonyl)-4,6-dihydrop ratio [3,4 - c ]pyrazol-3-yl b 4-t-butylbenzamide; 74. N-{5-(acridin-3-carbonyl)-4,6-dihydropyrrole And [3, 4-c]pyrazol-3-yl}-4-t-butylbenzamide; 75_ N-{5-(D-pyridyl-4-carbonyl)-4,6-dihydroindole 11 each [3,4-c] D is 0--3-yl}-4-t-butylbenzamide; 76. N-{ 5-(2-methyl-acridin-3-carbonyl -4,6-dihydropyrrolo[3,4-(:]°pyrazol-3-yl}-4-t-butylbenzamide; 77. N-{ 5-(2-sulfuronium) -Pyridin-3-carbonyl)-4,6-dihydroindolo[3,4-c] 0 ratio °-3-yl}_4-tert-butylbenzoate; 7 8. N - { 5 - ( ° ratio D well - 2 - rebel) -4,6 - dihydrogen ratio p and [3,4 - c ] » ratio. sit _3-base}_4_second butyl benzoquinone Amine, 79. N-{5-(3-furanyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide 80. Ν-{5-(2-σ 塞醯醯 ))-4,6-dihydro 0 is slightly more than [3,4-c] ° oxazol-3-yl}-4-phenoxybenzene Methionine; 81. N-{5-(7-oxime-benzo Furan-2-carbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 82. N-{5-(benzene And furan-2-carbonyl)-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 83. N-{5- (2-furopyryl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 84. N-{5- (3-0-v-amyl)-4,6-dihydropurine each [3,4-c]pyrazol-3-yl}-4-t-butylbenzamide;

C:\2D-00DE\91-01\90119473.ptd 第21頁 1327569 五、發明說明（19) 85_ N-{5-(2 -呋喃曱醯基）-4, 6-二氫吡咯并[3, 4-c]吡 β坐-3_基}-4_苯氧苯甲酿胺； 86. Ν-{5-(3 -噻吩曱醯基）-4, 6-二氫吡咯并[3, 4-c] 口比唑-3-基}-4-第三丁基苯甲醯胺； 87. Ν-{5-(喳4啉-2 -羰基）-4, 6 -二氫吡咯并[3, 4-c]吡。坐-3-基}_4 -苯氧苯曱醯胺； 88· Ν-{5-(2 -噻吩基）乙醯基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基}-4-第三丁基苯甲醯胺； 89. Ν-{5-(嗜琳-6-幾基）-4,6 -二氫D比ρ各并[3,4-c]D比0坐、-3-基}_4-第三丁基苯甲酿胺； 90· N-{5 -（3-0夫喃甲醯基）-4, 6-二氫n比口各并[3, 4-c] D比唑-3-基}-4 -苯氧苯曱醯胺； 9 1 · N - { 5 - ( °比啡-2 -幾基）-4，6 -二氫 °比 p各并[3，4 - c ] °比。坐 _3_基}-4_苯氧苯曱驢胺； 92. N-{5-[2-(6-氧基-1(6H)-嗒畊基}乙醯基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 93.1{5-(4-胺基曱醯基曱氧-苯基）乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 94. N-{5 -胺基曱醯基乙酸基- 4,6 -二氫0比0各并[3,4-c] 吡唑-3 -基} - 4 -第三丁基苯曱醯胺； 95. N-{5-{4-[2-(4-曱基哌畊-2 -基）乙氧]苯基}乙醯基 -4，6-二氮'1比|1各并[3，4_(3]11比〇坐-3_基}-4_第三丁基苯曱酿胺； 96. N-{5-(2-曱基磺醯胺基噻唑-4 -碳基）-4,6 -二氫吡C:\2D-00DE\91-01\90119473.ptd Page 21 1327569 V. INSTRUCTIONS (19) 85_ N-{5-(2-Furylmercapto)-4,6-dihydropyrrolo[3 , 4-c]pyridyl-β-yl}-4-phenoxybenzamide; 86. Ν-{5-(3-thiophenanthryl)-4,6-dihydropyrrolo[3, 4-c] Oroxazol-3-yl}-4-t-butylbenzamide; 87. Ν-{5-(喳4 oxalin-2-carbonyl)-4,6-dihydropyrrolo[ 3, 4-c]pyridyl. -3--3-yl}_4-phenoxybenzamine; 88·Ν-{5-(2-thiophenyl)ethenyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole- 3-based}-4-t-butylbenzamide; 89. Ν-{5-((琳-6-yl)-4,6-dihydro D ratio ρ[3,4-c ]D is more than 0, -3-yl}_4-t-butylbenzamide; 90·N-{5-(3-0-bucamyryl)-4,6-dihydron ratio And [3, 4-c] D-pyrazol-3-yl}-4-phenoxybenzamine; 9 1 · N - { 5 - ( ° than cyano-2 -yl)-4,6 - II The ratio of hydrogen to p is [3,4 - c ] ° ratio. Sitting on _3_yl}-4_phenoxybenzamine; 92. N-{5-[2-(6-oxy-1(6H)-indole)}ethinyl-4,6-di Hydroquino[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 93.1{5-(4-aminoindenyloxy-phenyl)acetamidine 4-,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 94. N-{5-aminomercaptoacetate - 4,6-dihydrogen 0 to 0 each [3,4-c]pyrazol-3-yl}-4-tetrabutylbenzamide; 95. N-{5-{4-[2 -(4-mercaptopiperidin-2-yl)ethoxy]phenyl}ethenyl-4,6-diaza'1 ratio|1 each [3,4_(3]11 than 〇--3_ Base}-4_t-butylphenyl hydrazine; 96. N-{5-(2-mercaptosulfonylthiazol-4-carboyl)-4,6-dihydropyridyl

C:\2D-CODE\91-01\90119473.ptd 第22頁 1327569 五、發明說明（20) 咯并[3,4-c]吡唑-3-墓}-4-第三丁基笨甲醯胺； 97. N-{5-(苯并呋喃-2 -羰基）-4,6 -二氫吡咯并[3,4-c] 吡唑-3“基}-4-苯氧苯甲醯胺； 98. N-{5-(吡啶-2 -羰基）-4, 6 -二氫吼咯并[3, 4-c]吡唑 -3_基}-4·•苯氧苯曱酿胺； 99. N_{5-(2-甲基比咬-3_戴基）-4，6 -二氫D比°各并 [3,4-c]吡唑-3-基卜4-苯氧苯甲醯胺； 10 0. N-{5-(喳啉-4 -羰基）-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基}-4 -苯氧苯甲醢胺； 101. N_{5—[4_(1_0比口各°定_2_嗣）苯曱醯基]一4，6 -二氮0比咯并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 102. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4_第三丁基苯甲酿胺； 103. N -正丁基-Ν’ - {3-(2 -秦-2_ 基-丙酿胺基）_4, 6_ 二氫°比ρ各并[3，4 - c ] °比。坐-5 _基}脲； 104. Ν-異丙基-Ν’ - {3-(2 -萘-2 -基-丙醯胺基）-4, 6 -二氫°比ρ各并[3，4 - c ] °比°坐-5 -基}脲； 105. Ν-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 _3_基卜2 -秦基丙酿胺； 106. Ν-{5-乙氧叛基-4，6_二氮ρ比D各弁[3，4-c] 0比0坐- 3-基}-3_(2 -蔡-2_基）_丙酿胺； 107. N-{5-(3-曱基丁醯基）-4,6 -二氫吡咯并[3,4-c] 口比唑-3-基卜3-(2 -萘-2 -基）-丙醯胺； 108.1'1-{5-胺基叛基曱基-4,6-二氫〇比17各并[3,4-(：]11比唑C:\2D-CODE\91-01\90119473.ptd Page 22 1327569 V. INSTRUCTIONS (20) S-[3,4-c]pyrazole-3-tomb}-4-t-butyl phenyl Indoleamine; 97. N-{5-(benzofuran-2-carbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-3"yl}-4-phenoxybenzidine Amine; 98. N-{5-(pyridine-2-carbonyl)-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}-4·•phenoxybenzoquinone 99. N_{5-(2-methyl ratio bit-3-Daki)-4,6-dihydro D ratio °[3,4-c]pyrazol-3-ylbu-4-phenyloxide Benzalamine; 10 0. N-{5-(porphyrin-4-carbonyl)-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-phenoxybenzene Methionine; 101. N_{5—[4_(1_0 比各 _2 _2 嗣 _2 _2 ] ] ] ] ] ] ] ] ] ] ] 4 4 4 4 4 4 4 - - - - - - - - - - - - - - 3-yl}-4-t-butylbenzamide; 102. N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl} -4_T-butylbenzamide; 103. N-n-butyl-indole-{3-(2-methyl-2-yl-propylamino)_4,6-dihydrogen ratio ρ[ 3,4 - c ] ° ratio. sit -5 _ ki) urea; 104. Ν-isopropyl-Ν' - {3-(2 -naphthalen-2-yl-propionamido)-4, 6 - The dihydrogen ratio ρ is [3,4 - c ] ° ° sit-5-yl}urea; 105. Ν-{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole_3_ylbu-2-methylidene Brewing amine; 106. Ν-{5-ethoxyoxin-4,6_diazo ρ ratio D 弁[3,4-c] 0 to 0 sitting - 3-base}-3_(2 - Cai-2 _ base)_ propylamine; 107. N-{5-(3-indolyl decyl)-4,6-dihydropyrrolo[3,4-c] oxazole-3-ylbu 3-(2 -naphthalen-2-yl)-propanthamine; 108.1'1-{5-amino thiopurinyl-4,6-dihydroindole ratio 17 and [3,4-(:]11 azole

C:\2D-C0DE\91-01\90119473.ptd 第23頁 1327569 五、發明說明（21) -3 -基}-3-(2 -萘_2_基）-丙醯胺； 109. N-{5-(吡咯-3 -基羰基）-4,6-二氫吡咯并[3,4-<:] 吡唑-3-基}-3-(2-萘-2-基）-丙醯胺； 110. N-{5-乙氧徵基-4, 6 -二氫°比11 各并[3, 4-c] D比。坐- 3-基} -4-第三丁基苯曱醯胺； 111. N_{5 -異戍基- 4,6 -二氮 D 比 B各并[3,4-c] °比。坐-3-基} -4-第三丁基苯曱醯胺； 112. ^丁基1’-{3-(4-第三丁基-苯甲醯胺基）-4,6-二赢氫°比17各并[3，4 - c ] °比。坐-5 -基} ; —113. N-{5-(吲哚-2-基）羰基-4,6-二氫吡咯并[3,4-c] 吡唑-3-基}-4-第三丁基苯甲醯胺； 1 14. 1^-{5-(1-曱基-吲哚-3-基）乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 115.1^-{5-[4-(1-咪唑基曱基）苯曱醯基]-4,6-二氫吡咯并[3,4-c]吼唑-3-基}-4-苯氧苯曱醯胺； 116. !^_{5-[4-(卜咪唑基曱基）苯甲醯基]-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 117. N-{5-[4-(l-p比口各0定-2-酮）苯曱醯基]-4,6 -二氫。比 I®咯并[3,4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 118. N-{5-(2 -嗎啉基甲基-5 -呋喃曱醯基）-4,6 -二氫吡咯并[3,4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 119. N-{5-(5 -乙醯胺基-2 -呋喃曱醯基）-4,6 -二氫吡咯并[3，4-c] π比0坐-3-基}-3-(2 -蔡-2-基）-丙酿胺； 120. Ν-{5-(4-甲基-c底啡-1-基）乙醯基-4，6 -二氫0比口各C:\2D-C0DE\91-01\90119473.ptd Page 23 1327569 V. INSTRUCTIONS (21) -3 -yl}-3-(2-naphthalene-2-yl)-propanamide; 109. N -{5-(pyrrole-3-ylcarbonyl)-4,6-dihydropyrrolo[3,4-<:]pyrazol-3-yl}-3-(2-naphthalen-2-yl)- Propylamine; 110. N-{5-ethoxyxy-4,6-dihydrogen ratio 11 and [3, 4-c] D ratio. Sodium-3-yl}-4-t-butylbenzamide; 111. N_{5-isodecyl- 4,6-diaza D ratio B [3,4-c] ° ratio. Benzyl-3-yl}-4-tert-butylbenzamide; 112. ^Butyl 1'-{3-(4-t-butyl-benzamide)-4,6-win The ratio of hydrogen to 17 is [3,4 - c ] ° ratio. -5-(indol-2-yl)carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4- Tert-butylbenzamide; 1 14. 1^-{5-(1-indolyl-indol-3-yl)ethenyl-4,6-dihydropyrrolo[3,4-c] Pyrazol-3-yl}-4-t-butylbenzamide; 115.1^-{5-[4-(1-imidazolylhydrazyl)phenylhydrazino]-4,6-dihydropyrrole [3,4-c]oxazol-3-yl}-4-phenoxybenzamine; 116. !^_{5-[4-(b-imidazolyl)benzoyl]-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 117. N-{5-[4-(lp ratio 0 each -2- Keto)phenylhydrazine]-4,6-dihydrogen. Ratio of I®-[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 118. N-{5-(2- morpholinylmethyl-5-furanium -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 119. N-{5-(5-acetamido- 2-furanyl)-4,6-dihydropyrrolo[3,4-c] π ratio 0--3-yl}-3-(2-Cai-2-yl)-propanol; 120 Ν-{5-(4-Methyl-c-endo-1-yl)ethenyl-4,6-dihydro- 0

.C:\2D-C0DE\91-01\90119473.ptd 第24頁 1327569 五、發明說明（22) 并[3, 4-c]吡唑-3 -基}- 3-(2 -萘-2 -基）-丙醯胺； 121.1^-{5-(哌啶-1-基）乙醯基_4,6-二氫吡咯并 [3，4_c]'D比。坐_3_ 基}-3-(2_ 秦_2 -基）-丙酿胺； 122.1^-{5-(咄咯啶-1-基羰基）曱基-4,6-二氫吡咯并 [3,4-c]吡唑-3-基}-3-(2 -萘-2 -基）-丙醯胺； 123. N-{5-乙醯基-4, 6 -二氫。比。各并[3，4-c] °比°坐_3_ -基）苯基乙酿胺； 124_1{5-乙醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-2 -（（4_π比口各咬_1-基）苯基）丙臨胺， 125. N-{5-乙醯基-4,6_二氫吡咯并[3,4-c]吡唑-3-基}·_(4_(2_氧基_D比略π定_1_基）苯基）乙酿胺， 126. Ν-{5-乙醯基-4,6 -二氫 °比°各并[3，4-c] °比°坐-3-基}_2-(4_(2-氧基_Ditn各。定_1_基）苯基）丙酿胺， 127. N-2-曱氧苯基-Ν’-{2-[4-(2 -氧基-吡咯啶-1-基）苯基]-丙臨胺基_4，6 -二氫°比°各并[3，4-c] °比°坐-5-基}脈； 128. N-2，4-二氟苯基- Ν’ - {2-[4-(2 -氧基-p比 p各。定-I-基）苯基]-丙醯胺基-4,6 -二氫各并[3，4-c] °比°坐-5-基} 脲； 129· N-(l -苯基）乙基-N’-{2-[4-(2 -氧基-吡咯啶-1-基）苯基]-丙酿胺基-4，6 -二氫π比略并[3，4-c] °比。坐-5-基} 脲； 130. Ν-2-甲氧苯基-Ν’-{2-(4 -吡咯啶-卜基-苯基）-丙醯胺基-4，6 -二氫吼D各并[3,4-c] D比。坐-5-基}脲； 131. N-2，4 -二氟苯基- Ν’ - {2-(4 - °比°各 σ定-I-基-苯基）-.C:\2D-C0DE\91-01\90119473.ptd Page 24 1327569 V. INSTRUCTIONS (22) And [3, 4-c]pyrazol-3-yl}- 3-(2-naphthalene-2 -yl)-propanamide; 121.1^-{5-(piperidin-1-yl)ethenyl-4,6-dihydropyrrolo[3,4_c]'D ratio. _3_基}-3-(2_Qin-2-yl)-propanol; 122.1^-{5-(indolyl-1-ylcarbonyl)indolyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-3-(2-naphthalen-2-yl)-propanamine; 123. N-{5-ethenyl-4,6-dihydrogen. ratio. Each [3,4-c] ° ratio sits _3_-yl) phenylethylamine; 124_1{5-acetamido-4,6-dihydropyrrolo[3,4-indolyl]pyrazole- 3-yl}-2 -((4_π 口各 _1 _1 yl) phenyl) propionine, 125. N-{5-ethenyl-4,6-dihydropyrrolo[3,4- c]pyrazol-3-yl}·_(4_(2_oxy_D ratio slightly π定_1_yl)phenyl)benzamine, 126. Ν-{5-ethinyl-4,6 - dihydrogen ratio ° and [3,4-c] ° ratio of sitting-3-yl}_2-(4_(2-oxy-Ditn each)-1-phenyl) phenylamine, 127. N-2-nonyloxyphenyl-indole-{2-[4-(2-oxy-pyrrolidin-1-yl)phenyl]-propanylamino-4,6-dihydrogen ratio °[3,4-c] °°°-5-base} vein; 128. N-2,4-difluorophenyl-Ν' - {2-[4-(2-oxy-p)比·I-yl)phenyl]-propionylamino-4,6-dihydro-[3,4-c] ° ratio °-5-yl} urea; 129· N-( l-Phenyl)ethyl-N'-{2-[4-(2-oxy-pyrrolidin-1-yl)phenyl]-propanyl-4,6-dihydro-π ratio slightly [ 3,4-c] ° ratio. Sodium-5-yl}urea; 130. Ν-2-methoxyphenyl-Ν'-{2-(4-pyrrolidine-buyl-phenyl)-propanin-4,6-dihydroanthracene D each and [3,4-c] D ratio. Sodium-5-yl urea; 131. N-2,4-difluorophenyl- Ν' - {2-(4 - ° ratio σ - -I-yl-phenyl)-

C: \2ϋ-ω〇Ε\91 -01 \90119473 .ptd 第25頁 1327569 五、發明說明（23) 丙酿胺基_4，6-二氫°比°各并[3，4-c] 11比吐-5-基}脈； 132. N-(l -苯基）乙基-N’-{2-(4 -吡咯啶-卜基-苯基）-丙龜胺基- 4,6 -二氫吼11各并[3,4-c]吼°坐-5_基}脲； 1 33. N-{5 -苯基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-2-(4-吡咯啶-1-基-苯基）丙醯胺； 1 34. N-2-曱氧苯基-Ν’ -{ [4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲； 1 3 5, N-2-氯苯基-Ν’ - { [4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基-4,6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲；零136. N_(l -苯基）乙基-Ν’ - {[4-(2 -氧基-吡咯啶-卜基）-苯基]-乙醯胺基-4,6-二氫°比洛并[3,4-c]吼°坐-5-基}脲； 137. N -正丁基-N’-{[4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基- 4,6 -二氫吡咯并[3, 4-c]呲唑-5-基}脲； 138· N-{ 5 -苯基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}_4-(2_氧基_ 0比D各σ定_1-基）-苯基-乙酿胺； 139. Ν -正丁基-Ν’-{2-[4-(2 -氧基-吡咯啶-卜基）-苯基]-丙醯胺基-4，6-二氫°比略并[3，4-c] °比°坐-5-基}脲； 140. Ν-{5 -苯基續醯基-4, 6 -二氫吼°各并[3,4-c] °比。坐 ^•3-基}-2-[4-(2 -氧基-吼咯啶-卜基）-笨基]-丙醯胺； 141. N-{5 -胺基羰基- 4,6 -二氫°比°各并[3,4-c] D比嗤- 3-基}-4-(2 -氧基-B比基）_苯基-乙酿胺； 142. Ν -正丁基- Ν’ _{2-(4-°比略°定-1_基-苯基）_丙酿胺基- 4,6 -二氫°比D各并[3,4-c]吼°坐-5-基丨脲； 143. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑- 3-C: \2ϋ-ω〇Ε\91 -01 \90119473 .ptd Page 25 1327569 V. Description of invention (23) Acrylamino 4,6-dihydrogen ratio °[3,4-c] 11 than spit-5-yl} vein; 132. N-(l-phenyl)ethyl-N'-{2-(4-pyrrolidinyl-p-phenyl)-propaninyl-4,6 - indoline 11 and [3,4-c]吼°-5-yl}urea; 1 33. N-{5-phenylsulfonyl-4,6-dihydropyrrolo[3, 4 -c]pyrazol-3-yl}-2-(4-pyrrolidin-1-yl-phenyl)propanamine; 1 34. N-2-nonyloxyphenyl-Ν'-{ [4-( 2-oxy-pyrrolidin-1-yl)-phenyl]-acetamido-4,6-dihydroindolo[3,4-c]pyrazole-5-yl}urea; 1 3 5 , N-2-chlorophenyl-Ν' - { [4-(2-oxy-pyrrolidin-1-yl)-phenyl]-acetamido-4,6-dihydropyrrolo[3, 4-c]pyrazol-5-yl}urea; zero 136. N_(l-phenyl)ethyl-Ν'-{[4-(2-oxy-pyrrolidinyl)-phenyl]- Acetylamino-4,6-dihydro-pyrolo[3,4-c]吼°-5-yl}urea; 137. N-n-butyl-N'-{[4-(2 - Oxy-pyrrolidin-1-yl)-phenyl]-acetamido- 4,6-dihydropyrrolo[3,4-c]indazol-5-yl}urea; 138· N-{ 5 -phenylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyridyl Azole-3 -yl}_4-(2_oxy~ 0 to D each sigma 1-1-yl)-phenyl-ethylamine; 139. Ν-n-butyl-Ν'-{2-[4- (2-oxy-pyrrolidinyl-buyl)-phenyl]-propionylamino-4,6-dihydrogen ratio slightly [3,4-c] ° ratio °-5-yl}urea; 140. Ν-{5-Phenyl fluorenyl-4,6-dihydroindole ° [3,4-c] ° ratio. ^^3-yl}-2-[4-(2-oxy-indolyl-buyl)-phenyl]-propanamine; 141. N-{5-aminocarbonyl- 4,6- Dihydrogen ratio °[3,4-c] D is more than 3-(3-yl}-4-(2-oxy-B-yl)-phenyl-ethylamine; 142. Ν-n-butyl - Ν' _{2-(4-° ratio °1_yl-phenyl)_ propylamino- 4,6-dihydrogen ratio D and [3,4-c]吼° -5-carbazide; 143. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-

C:\2D-CODE\91-01\90119473.ptd 第26頁 1327569 五、發明說明（24) 基}-2-(4-吡咯啶-1-基）-苯基-丙醯胺； 144. N-2-甲氧苯基-N;-{(4-°比咯啶-1-基-苯基）-乙醯胺基-4，6 -二氫吼p各并[3, 4-c] π比吐-5-基}脲； 145. Ν-2-氯苯基- Ν’ - {(4 - °比11各π定-1-基-苯基）-乙酸胺基- 4，6 -二氫吼11各并[3,4-(：]°比°坐-5-基}脲； 146. N-(l -苯基）乙基-Ν’ - {(4 -°比咯啶-1-基-苯基）-乙酿胺基-4，6 -二氫°比π各并[3，4 - c ]吼。坐-5 -基}脲； 147. Ν -正丁基-Ν’ - {(4 -D比咯啶-1-基-苯基）-乙醯胺基 -4，6 -二氫n比D各并[3，4 - c ] D比β坐-5 -基}脲； 1 4 8. Ν - { 5 -苯基項醯基-4，6 -二氫Β比洛并[3，4 - c ] D比。坐 -3-基}-(4-吡咯啶-1-基-苯基）-乙醯胺； 149. Ν-乙基-Ν’-{[4-(2 -氧基-咄咯啶-1-基）-苯基]-乙酿胺基-4，6 -二氫D比略并[3，4 - c ] °比σ坐-5 -基}脲； 150. Ν-異丙基-Ν’-{[4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲； 151. Ν-{5-(2 -呋喃甲醯基）-4,6_二氫咄咯并[3,4-c] 唑-3-基}-4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺； 152. N-{5-(2-曱氧苯基）-4,6 -二氫咄咯并[3,4-c]吼唑 -3-基}-4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺； 153. N-{5 -胺基羰基曱基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-4-(2 -氧基-D比基）_苯基-乙酿胺； 154. Ν-異丙基-Ν’ - {(4-。比咯啶-1-基-苯基）-乙醯胺基 -4,6-二氫°比洛并[3,4-(：]°比°坐-5-基}脲； 155. Ν-乙基-Ν’ -{(4 -吡咯啶-1-基-苯基）-乙醯胺基-4,C:\2D-CODE\91-01\90119473.ptd Page 26 1327569 V. Description of the invention (24) yl}-2-(4-pyrrolidin-1-yl)-phenyl-propanamide; 144. N-2-methoxyphenyl-N;-{(4-°pyrrolidin-1-yl-phenyl)-acetamido-4,6-dihydroindole p[3, 4-c π 吐 -5-5-yl} urea; 145. Ν-2-chlorophenyl- Ν' - {(4 - ° ratio 11 π -1- phenyl-phenyl)-acetic acid amine - 4,6 - indoline 11 each [3,4-(:]° ratio °-5-yl}urea; 146. N-(l-phenyl)ethyl-Ν' - {(4 -°bibromopyridine) -1-yl-phenyl)-ethanoamine-4,6-dihydrogen ratio π[3,4 - c ]吼.sodium-5-yl}urea; 147. Ν-n-butyl- Ν'-{(4-D-Byryl-1-yl-phenyl)-acetamido-4,6-dihydron ratio D and [3,4 - c ] D ratio β sit-5 -脲-urea; 1 4 8. Ν - { 5 -phenyl-indenyl-4,6-dihydroindolebiol[3,4 - c ] D ratio. Sodium-3-yl}-(4-pyrrole Acridine-1-yl-phenyl)-acetamide; 149. Ν-ethyl-Ν'-{[4-(2-oxy-indolyl-1-yl)-phenyl]-ethonamide Base-4,6-dihydrogen D ratio slightly [3,4 - c ] ° ratio σ sit-5-yl}urea; 150. Ν-isopropyl-Ν'-{[4-(2-oxyl) -pyrrolidin-1-yl)-phenyl]-醯-amino-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea; 151. Ν-{5-(2-furanylmethyl)-4,6-dihydrogen咄[3,4-c]oxazol-3-yl}-4-(2-oxy-pyrrolidin-1-yl)-phenyl-acetamide; 152. N-{5-(2- Phenoxyphenyl)-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-4-(2-oxy-pyrrolidin-1-yl)-phenyl-B Guanidine; 153. N-{5-aminocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-4-(2-oxy-D ratio base ) phenyl-ethylamine; 154. Ν-isopropyl-Ν' - {(4-.pyrrolidin-1-yl-phenyl)-acetamido-4,6-dihydrogen ratio洛和[3,4-(:]°°°-5-yl}urea; 155. Ν-ethyl-Ν'-{(4-pyrrolidin-1-yl-phenyl)-acetamido -4,

C:\2D-00DE\91-01\90119473.ptd 第27頁 1327569 五、發明說明（25) 6 -二氫吼11各并[3，4-c]吼°坐-5-基}脲； 156. N-{5-胺基羰基甲基-4, 6-二氫咄咯并[3, 4-c]吡唑 -3-基}-(4-咄咯啶-1-基-苯基）-乙醯胺； 157. N-{5-(3-曱基丁醯基）-4，6 -二氫〇比 p各并[3,4-c] 0 比唑-3-基}-4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺； 158. N -正丁基-Ν’ - {3-(2 -萘-2 -基）乙醯胺基-4, 6 -二氫 0比0各并[3，4 - c ] °比°坐-5 -基}脲； 159. Ν -正丁基-Ν’ - {3-(3-曱基-苯基）乙醯胺基-4, 6 -二氫D比ρ各并[3，4 - c ] °比°坐-5 -基}脲； 160. Ν_正丁基_Ν’ _{3_(3_氟-苯基）乙酿胺基-4，6_二氯 0比Β各并[3，4 - c ] °比°坐-5 -基}脲； 161. Ν -正丁基-Ν’ - {3-(3 -吡啶基）乙醯胺基-4, 6 -二氫 0比略并[3，4 - c ] °比。坐-5 -基}脲； 162_ Ν -正丁基-Ν’-{3-(雙環[4.2.0.]辛1，3,5_ 三烯-7-缓酿胺基）-4，6_二氫吼17各并[3，4-~c] °比。坐-5-基}脈； 163. N -正丁基-Ν’ - {3 -苯氧乙醯胺基-4, 6 -二氫吡咯并 [3, 4-c]吡唑-5-基}脲； 164. Ν -正丁基-Ν’ - {3-(4-曱基-苯基）乙醯胺基-4, 6 -二氫吼17各并[3，4 - c ] D比°坐-5 -基}脲； 165. N -正丁基_N’ _{3_(4_敦-苯基）乙酿胺基-4，6 -二氮 0比°各并[3，4 - c ]吼。坐-5 -基}脲； 166. N_正丁基-Ν’ _{3_(3，4_二氣-苯基）乙酿胺基-4, 6_ 二氫吼11各并[3，4 - c ] °比。坐-5 -基}脲； 167. Ν -正丁基-Ν’ - {3-(4 -三氟甲氧-苯基）乙醯胺基-4,C:\2D-00DE\91-01\90119473.ptd Page 27 1327569 V. Description of the invention (25) 6-Dihydroindole 11 and [3,4-c]吼°-5-yl}urea; 156. N-{5-Aminocarbonylmethyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-(4-oxaridin-1-yl-phenyl - acetamidine; 157. N-{5-(3-mercaptobutyl fluorenyl)-4,6-dihydroindole ratio p and [3,4-c] 0 thiazol-3-yl}-4- (2-oxy-pyrrolidin-1-yl)-phenyl-acetamide; 158. N-n-butyl-indole-{3-(2-naphthalen-2-yl)ethynylamino-4 , 6 - dihydrogen 0 to 0 each [3,4 - c ] ° ratio ° sit -5 -yl} urea; 159. Ν - n-butyl-Ν' - {3-(3-mercapto-phenyl Ethylamino-4,6-dihydrogen D ratio ρ[3,4 - c ] ° ratio ° sit-5-yl}urea; 160. Ν_n-butyl _Ν' _{3_(3 _Fluoro-phenyl)ethinyl-4,6-dichloro- 0 Β[3,4 - c ] ° ratio ° sit-5-yl}urea; 161. Ν-n-butyl-Ν' - {3-(3-Pyridinyl)acetamido-4,6-dihydrogen 0 is a ratio of [3,4 - c] °. Sodium-5-yl}urea; 162_ Ν-n-butyl-Ν'-{3-(bicyclo[4.2.0.] octane 1,3,5-triene-7-sweetylamino)-4,6_ The indoline 17 is each [3,4-~c] ° ratio. Sitting on a 5-kilo} vein; 163. N-n-butyl-Ν' - {3-phenoxyethylamino-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl Urea; 164. Ν-n-butyl-Ν' - {3-(4-mercapto-phenyl)acetamido-4,6-dihydroindole 17 each [3,4 - c ] D ratio ° sitting -5 -yl}urea; 165. N-n-butyl _N' _{3_(4_Den-phenyl) ethanoamine-4,6-diaza 0°°[3,4 - c ]吼. Sodium-5-yl urea; 166. N_n-butyl-Ν' _{3_(3,4_di-phenyl)ethanoyl-4,6-dihydroindole 11 each [3,4 - c ] ° ratio. Sodium-5-yl}urea; 167. Ν-n-butyl-Ν' - {3-(4-trifluoromethoxy-phenyl)acetamido-4,

C:\2D-OODE\91-01W0119473.ptd 第28頁 1327569 五、發明說明（26) 6 -二氫D比D各并[3，4 - c ] °比°坐-5 -基}脲； 168. N -正丁基-N’-U1。-甲基-苯基）乙醯胺基_4,6-二氫°比B各并[3，4 - c ]吼°坐-5 -基}脲； 169. N -正丁基-Ν’ - {3-(2 -溴-苯基）乙醯胺基-4, 6 -二氫 °比ρ各并[3，4 - c ]吼。坐-5 -基}脲； 170. Ν -正丁基-Ν’ - {3-(2, 5 -二氟-苯基）乙醯胺基-4, 6-二氫°比D各并[3，4 - c ] °比D坐-5 _基}脲； 171. N-正丁基-Ν’-{3-(4-(吡咯啶-1-基-羰基曱氧）-苯基）乙醢胺基- 4,6 -二氫°比。各并[3,4-(：]°比°坐-5-基}脲； 172. N -正丁基-N’-{3-(3-(胺基羰基甲氧）-苯基）乙醯胺基-4，6 -二氫吼13各并[3,4-c] °比。坐-5-基}脲； 173. N -正丁基-N’-{3-(°比啶-4 -基-乙醯胺基）-4,6 -二氫°比σ各并[3，4 - c ] °比°坐-5 -基}脲； 174. Ν -正丁基-Ν’-{3-(4-(嗎啉-1-基）-苯基）乙醯胺基 -4，6 -二氫。比Β各并[3，4 - c ] °比。坐-5 -基}脲； 175. Ν-正丁基-Ν’-{3-(2-氟-苯基）乙醯胺基-4,6 -二氫 0比11各并[3，4 - c ]吼°坐-5 -基}脲； 176. N -正丁基-Ν’ - {3-(3, 5 -二氟-苯基）乙醯胺基-4,6-二氫吼11各并[3，4 - c ] π比。坐-5 -基}脲； 177. Ν -正丁基-Ν’ - {3-(6 -氧基-6Η-嗒畊-1-基）乙醯胺基-4，6 -二氫吼11 各并[3,4-c]吼°坐-5-基}脲； 17 8. N-{5-曱基咄啶曱醯基-4, 6 -二氫吡咯并[3, 4-c]。比唑-3-基}-4-(2 -氧基唑啶-3 -基）-苯基-乙醯胺； 179. N-{5-(噻吩-2 -基）乙醯基-4, 6 -二氫吡咯并C:\2D-OODE\91-01W0119473.ptd Page 28 1327569 V. INSTRUCTIONS (26) 6-Dihydrogen D ratio D and [3,4 - c ] ° ratio ° sit-5-yl} urea; 168. N-n-butyl-N'-U1. -Methyl-phenyl)ethylammonium _4,6-dihydrogen ratio B and [3,4 - c ]吼° sit-5-yl}urea; 169. N-n-butyl-Ν' - {3-(2-Bromo-phenyl)acetamido-4,6-dihydrogen ratio ρ and [3,4 - c ]吼. Sodium-5-yl}urea; 170. Ν-n-butyl-Ν'-{3-(2,5-difluoro-phenyl)acetamido-4,6-dihydrogen ratio D and [ 3,4 - c ] ° ratio D sitting -5 _ yl} urea; 171. N-n-butyl-Ν'-{3-(4-(pyrrolidin-1-yl-carbonyl anthraceneoxy)-phenyl) Acetylamino-4,6-dihydrogen ratio. Each [3,4-(:]° ratio °-5-yl}urea; 172. N-n-butyl-N'-{3-(3-(aminocarbonylmethoxy)-phenyl)醯Amino-4,6-dihydroindole 13 each [3,4-c] °. Sodium-5-yl}urea; 173. N-n-butyl-N'-{3-(° pyridine -4 -yl-acetamido)-4,6-dihydrogen ratio σ[3,4 - c ] ° ratio ° sit-5-yl}urea; 174. Ν-n-butyl-Ν' -{3-(4-(morpholin-1-yl)-phenyl)acetamidoamine-4,6-dihydrogen. Specific enthalpy [3,4 - c ] ° ratio. Sit-5-yl Urea; 175. Ν-n-butyl-Ν'-{3-(2-fluoro-phenyl)acetamidoamine-4,6-dihydrogen 0 to 11 each [3,4 - c ]吼° Sodium-5-yl}urea; 176. N-n-butyl-indole-{3-(3,5-difluoro-phenyl)acetamido-4,6-dihydroindole 11 each [3 , 4 - c ] π ratio. sit-5-yl}urea; 177. Ν-n-butyl-Ν' - {3-(6-oxy-6Η-嗒耕-1-yl)acetamido- 4,6-dihydroindole 11 each [3,4-c]吼°-5-yl}urea; 17 8. N-{5-mercaptoacridinyl-4,6-dihydropyrrole And [3, 4-c]. Biazol-3-yl}-4-(2-oxoxazolidin-3-yl)-phenyl-acetamide; 179. N-{5-(thiophene-2 -yl)ethinyl-4,6-dihydropyrrole

C:\2D-C0DE\91-01\90119473.ptd 第29頁 1327569 五、發明說明（27) [3, 4-c]吡唑-3 -基}-4-(2_氧基-巧唑啶」3 -基）-苯基-乙醯胺； 180. N-{5-(2 -呋喃曱醯基）-4,6 -二氫吡口各并[3,4-c] °比。坐_3-基}_4-(2_氧基-$°坐咬_3 -基苯基-乙酿胺； 181. N-{5-(2-乙氧乙醯基）-4,6 -二氫吡咯并[3,4-c]吼。坐_3_基}_4-(2 -氧基-吃峻0定-3 -基）-苯基-乙酿胺； 182. N-{5-(3-曱基-丁醯基）-4,6 -二氫吡咯并[3,4-c] 。比唑-3 -基}-4-( 2 -氧基-$唑啶-3-基）-苯基-乙醯胺； A 183. N-{5 - 丁醯基-4,6-二氫吡咯并[3,4-c]吡唑-3- _基}-4-(2-氧基-g唑啶-3-基）-苯基-乙醯胺； 184. N-異丙基-N’-{3-[4-(2 -氧基唑啶-3 -基）-苯基 -乙醯胺基]-4，6 -二氫°比°各并[3，4 - c ] D比。坐-5 -基}脲； 185. N-(正丁基）-N’-{3-[4-(2-氧基唑啶-3 -基）-苯基-乙酿胺基]-4, 6 -二氫D比咯并[3，4 - c ] °比〇坐-5 -基}服； 186· N-{5-乙氧幾基-4,6 -二氫吼。各并[3，4-c] D比0坐_3_ 基卜4-(2-氧基唑啶-3-基）-苯基-乙醯胺； 187.1^-異丙基-!^’-{3-[2-(3-氧基-3,4,4&，8&-四氫 -2H-苯并[1，4]烯嚐畊-6 -基）乙醯胺基]-4, 6 -二氫吡咯并 3，4 - c ] °比。坐-5 -基}脲； 18 8. N-異丙基-Ν’ - {3-(3 -溴-苯曱醯胺基）-4,6 -二氫略并[3，4 - c ]吼。坐-5 -基}脲； 189. N-{5 -苯續醯基-4，6 -二氫p比11 各并[3, 4-c]吼°坐- 3-基丨_ 3 - >臭苯曱酿胺； 190. Ν-{5-乙酿基-4, 6 -二氫。比°各并[3,4-c] 0比。坐- 3-C:\2D-C0DE\91-01\90119473.ptd Page 29 1327569 V. INSTRUCTIONS (27) [3, 4-c]pyrazol-3-yl}-4-(2-oxy-cinazole Acridine "3 -yl)-phenyl-acetamide; 180. N-{5-(2-furanyl)-4,6-dihydropyryldi[3,4-c]. Sit _3-yl}_4-(2_oxy-$° sitbit _3-phenylene-ethylamine; 181. N-{5-(2-ethoxyethyl)-4,6- Dihydropyrrolo[3,4-c]indole. sitting on the _3_yl}_4-(2-oxy-acesulfame-decyl-yl)-phenyl-ethylamine; 182. N-{5 -(3-mercapto-butenyl)-4,6-dihydropyrrolo[3,4-c].Bizozol-3 -yl}-4-(2-oxy-$oxazol-3-yl) -phenyl-acetamide; A 183. N-{5-butenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-(2-oxy- G zirdin-3-yl)-phenyl-acetamide; 184. N-isopropyl-N'-{3-[4-(2-oxoxazolidine-3-yl)-phenyl-B醯Amino]-4,6-dihydrogen ratio °[3,4 - c ] D ratio. Sodium-5-yl}urea; 185. N-(n-butyl)-N'-{3- [4-(2-Oxyloxazol-3-yl)-phenyl-ethanoyl]-4,6-dihydro-D is more than s-[3,4 - c] ° } service; 186· N-{5-ethoxyxo-4,6-dihydroindole. Each [3,4-c] D is 0 to sit _3_ kib 4-(2- oxazolidine- 3-yl)-phenyl-acetamide; 187.1^-isopropyl-!^'-{3-[2-(3-oxy-3,4,4&,8&-tetrahydro-2H- Benzo[1,4]ene tastes -6-yl)acetamido]-4,6-dihydropyrrolo 3,4 - c] °. -5-yl}urea; 18 8. N-isopropyl-Ν' - {3-(3-bromo-benzoguanidino)-4,6-dihydro-s-[3,4-c]吼Sodium-5-yl}urea; 189. N-{5-Benzene fluorenyl-4,6-dihydrop ratio 11 and [3, 4-c]吼° sit- 3-base 丨 3 - > Odor Benzene Amine; 190. Ν-{5-Ethyl-4,6-dihydrogen. Ratio °[3,4-c] 0 ratio. Sit - 3-

C:\2D-OODE\91-Ol\90119473.ptd 第30頁 1327569 五、發明說明（28) 基}-[4-(1~吡咯啶-2-酮）苯甲醯胺]; 191. N-乙基-Ν’ -{ 3-(3 -溴-苯曱醯胺基）-4, 6 -二氫咄咯并[3, 4-c]吡唑-5-基}脲； 192.1^-{5-(8-喳啉）磺醯基-4,6-二氫咄咯并[3,4-(：]0比唑-3-基}-對曱苯曱醯胺； 19 3. N-苯基-Ν’ -{ 3-(3 -溴-苯甲醯胺基）-4, 6 -二氫吡咯并[3,4-c]p比吐-5-基}脲； 194. N-{5 -苯磺乙醯基-4,6-二氫呲咯并[3,4-〇:]吡唑 _ 3 _基} - 3 - >臭苯曱酿胺； 195. N_{5-甲烧石黃醯基- 4,6 -二氫°比°各并[3,4-c] °比唑 _ 3 -基} - 3 - >臭苯曱酿胺； 196. N-異丙基-N’-{3-[4-(1-吡咯啶-2-酮）-苯基醯胺基]-4，6 -二氫D比p各并[3,4-c]吼°坐-5_基}脲； 197. N-{5-(8 -喳啉）羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基卜對甲苯曱醯胺； 198· Ν-{5-(1-萘）磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-4-苯基苯曱醯胺； 199. Ν-{5-(1-萘曱醯基）-4,6 -二氫吼咯并[3,4-c]吡唑 _3-基}-4_苯基苯曱酸胺； 200. N-{5-(卜萘曱醯基）-4,6 -二氫咄咯并[3,4-c]吡唑 -3-基}-4 -苯氧苯曱醯胺； 201. N_苯基-Ν’ _{3_(4_苯基-苯曱酸胺基）_4，6_二氮〇比口各并[3，4 - c ] °比°坐-5 -基}脲； 2 02. N-{5 -苯基乙醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑C:\2D-OODE\91-Ol\90119473.ptd Page 30 1327569 V. Description of the invention (28) Base}-[4-(1~pyrrolidin-2-one)benzamide]; 191. N -ethyl-Ν'-{ 3-(3-bromo-benzoguanamine)-4,6-dihydroindolo[3,4-c]pyrazole-5-yl}urea; 192.1^- {5-(8-porphyrin)sulfonyl-4,6-dihydroindolo[3,4-(:]0-pyrazol-3-yl}-p-benzoquinone; 19 3. N -phenyl-Ν'-{3-(3-bromo-benzylamino)-4,6-dihydropyrrolo[3,4-c]p than oxa-5-yl}urea; 194. N -{5 - phenylsulfonyl-4,6-dihydroindolo[3,4-anthracene]pyrazole-3-yl}- 3 - > odor benzoquinone; 195. N_{5 - 甲石石黄醯基 - 4,6 - dihydrogen ° ° each [3,4-c] ° ratio azole 3 -yl} - 3 - > odor benzoquinone; 196. N-isopropyl -N'-{3-[4-(1-pyrrolidin-2-one)-phenylguanidino]-4,6-dihydrogen D is more than p[3,4-c]吼° _. U-{5-(8-carboline)carbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl-p-toluidine; 198·Ν-{5-(1-naphthalene)sulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-phenylbenzamide; 199 . Ν-{5-(1-Naphthyl)-4,6-dihydroindole [3,4-c]pyrazole-3-yl}-4-phenylphthalic acid amine; 200. N-{5-(b-naphthyl)-4,6-dihydroindole[3 , 4-c]pyrazol-3-yl}-4-phenoxybenzamine; 201. N_phenyl-Ν' _{3_(4-phenyl-benzoic acid amine)_4,6_ Diazolidine is more than [3,4 - c ] ° ratio ° sit-5-yl}urea; 2 02. N-{5-phenylethenyl-4,6-dihydroindole[3 , 4-c]pyrazole

C:\2D-0ODE\91-01\90119473.ptd 第31頁 1327569 五、發明說明（29) -3_基}_4_苯基苯曱酿胺， 203. ^{5-(1-萘）磺醯基-4,6-二氫吡11各并[3,4-(：]吡唑 -3-基卜對曱苯甲醯胺； 204. Ν-{5-(1-萘甲醯基）-4,6 -二氫吼咯并[3,4-c]吼唑 -3-基卜對甲苯曱醯胺； 205. N-{5_ 乙酿基-4,6 -二氫 D 比口各并[3，4-c] D 比0坐-3_ 基}-3-苯氧苯曱醯胺； 206. N-[5-(4 -氯-2, 5 -二氟苯甲醯基）-4,6 -二氫吡咯并 [3, 4-c]咄唑-3 -基]-2-(2 -萘基）乙醯胺； —207. N-{5-[第三丁基羧酸根]-4,6-二氫吡咯并[3,4-〇] 吡唑-3-基}-2-(2 -萘基）乙醯胺； 2 08. N-{5-[ (1-曱基環丙基）羰基]-4, 6 -二氫η比咯并[3, 4-c]吡唑-3-基}-2-(2_萘基）乙醯胺； 2 0 9. Ν-[5-(環丁基羰基）-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基]_2-(2_秦基）乙酿胺； 210. Ν-[5-(2 -氟苯甲醯基）-4,6 -二氫吡咯并[3,4-c]吡唑-3-基]-2-(2-萘基）乙醯胺； 211. N-[5-(咄啶-3 -基羰基）-4, 6 -二氫吡咯并[3, 4-c] 4吡唑-3-基]-2-(2-萘基）乙醯胺； 212.1{5-[(2,2,2,3，-四甲基環丙基）羰基]-4,6-二氫吡咯并[3, 4-c]咄唑-3 -基}-2-(2 -萘基）乙醢胺； 213. N-[5-(2,4,5 -三氟苯曱醯基）-4,6 -二氫吼咯并[3, 4-c]吡唑-3-基]-2-(2 -萘基）乙醯胺； 214. N-[5-(2-曱基戊-4 -烯醯基）-4,6 -二氫吡咯并C:\2D-0ODE\91-01\90119473.ptd Page 31 1327569 V. Description of Invention (29) -3_Base}_4_Phenylbenzoquinone, 203. ^{5-(1-naphthalene) Sulfosyl-4,6-dihydropyridinyl 1 [3,4-(:]pyrazol-3-yl b-p-benzamide; 204. Ν-{5-(1-naphthomethyl fluorenyl) -4,6-dihydroindolo[3,4-c]oxazol-3-yl-p-toluidine; 205. N-{5_ ethoxylated-4,6-dihydro D ratio Each [3,4-c] D is more than 0 -3 -yl-3-phenoxybenzamine; 206. N-[5-(4-chloro-2,5-difluorobenzhydryl) -4,6-dihydropyrrolo[3,4-c]oxazol-3-yl]-2-(2-naphthyl)acetamide; -207. N-{5-[Third butylcarboxylate Acidate]-4,6-dihydropyrrolo[3,4-indolepyrazol-3-yl}-2-(2-naphthyl)acetamidamine; 2 08. N-{5-[ (1- Mercaptocyclopropyl)carbonyl]-4,6-dihydron-pyrolo[3,4-c]pyrazol-3-yl}-2-(2-naphthyl)acetamide; 2 0 9. Ν-[5-(Cyclobutylcarbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl]_2-(2-methyl)ethene; 210. Ν- [5-(2-Fluorobenzylidene)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 211. N-[5-(acridin-3-ylcarbonyl)-4,6-dihydropyrrolo[3 , 4-c] 4pyrazol-3-yl]-2-(2-naphthyl)acetamide; 212.1{5-[(2,2,2,3,-tetramethylcyclopropyl)carbonyl] -4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}-2-(2-naphthyl)acetamide; 213. N-[5-(2,4,5 - Trifluorophenylhydrazino)-4,6-dihydroindolo[3,4-c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 214. N-[5 -(2-mercapto-4-indolyl)-4,6-dihydropyrrole

C:\2D-O0DE\91-01\90119473.ptd 第32頁 1327569 五、發明說明（30) [3, 4-c]吼唑-3 -基]-2-(2 -萘基）乙醯胺； 215. N-[5-(環丙基乙醯基）_4, 6 -二氫°比°各并[3，4-c] 唑-3-基]-2-(2-萘基）乙醯胺； 216. N-[5-(5 -氟-2-曱基苯曱醯基）-4,6 -二氫吡咯并 [3, 4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 217. N-{5-[2-氟-5-(三氟曱基）苯曱醯基]-4,6 -二氫吡咯并[3,4-c] °比唑-3-基}-2-(2 -萘基）乙醯胺.； 218. N-{5-[(3-曱氧環己基）羰基]-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基}-2-(2 -萘基）乙醯胺； 219. N-[5-(2, 4 -二氯-5-氟苯甲醯基）-4,6 -二氫吡咯并 [3，4-c]吼唑-3 -基]-2-(2 -萘基）乙醯胺； 220.1-[5-(2-氯-4,5-二氟苯曱醯基）-4,6-二氫吡咯并 [3，4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 221.1^-{5-[4-(111-咪唑-1-基）苯甲醯基]-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-2-(2 -萘基）乙醯胺； 222. N_{5-[4-(胺基確酿基）丁酸基]-4, 6 -二氣β比13各并 [3,4-c]吼唑-3-基}-2-(2 -萘基）乙醯胺； 223. Ν-{5-[(8 -氧基-5，6，7，8-四氫萘-2-基）獄基]- 4，6 -二氫π比17各并[3, 坐-3-基丨- 2- (2 -萘基）乙醯胺； 224_ N-(5-丙酮醯基- 4,6 -二氫吼11各并[3,4-c] °比。坐- 3- 基）-2-(2_蔡基）乙酸胺； 225. N-[5-(2,2 -二曱基丙醯基）-4,6 -二氫吡咯并 [3，4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 226. N_(5_ 丁 _2_ 酿基 _4，6_ 二氮吼 17各并[3，4_c] π 比 °坐 _3_C:\2D-O0DE\91-01\90119473.ptd Page 32 1327569 V. INSTRUCTIONS (30) [3, 4-c]carbazole-3-yl]-2-(2-naphthyl)acetamidine Amine; 215. N-[5-(cyclopropylethylhydrazino)-4,6-dihydrogen ratio [3,4-c]oxazol-3-yl]-2-(2-naphthyl) Acetamine; 216. N-[5-(5-fluoro-2-mercaptophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl]-2 -(2-naphthyl)acetamidamine; 217. N-{5-[2-fluoro-5-(trifluoromethyl)benzoinyl]-4,6-dihydropyrrolo[3,4- c] ° oxazol-3-yl}-2-(2-naphthyl)acetamide. 218. N-{5-[(3-oxocyclohexyl)carbonyl]-4,6-dihydropyrrole And [3,4-c]oxazol-3-yl}-2-(2-naphthyl)acetamide; 219. N-[5-(2,4-dichloro-5-fluorobenzhydryl) -4,6-dihydropyrrolo[3,4-c]oxazol-3-yl]-2-(2-naphthyl)acetamide; 220.1-[5-(2-chloro-4,5) -difluorophenylindenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 221.1^-{5- [4-(111-Imidazol-1-yl)benzylidenyl]-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-(2-naphthyl)B Indoleamine; 222. N_{5-[4-(amino-based)butyric acid]-4,6-digas β ratio 13 and [3,4-c [oxazol-3-yl}-2-(2-naphthyl)acetamide; 223. Ν-{5-[(8-oxy-5,6,7,8-tetrahydronaphthalen-2-yl) ) Prison base]- 4,6-dihydro-π ratio 17 and [3, sit-3-ylindole-2-(2-naphthyl)acetamide; 224_ N-(5-acetone fluorenyl-4, 6-dihydroindole 11 each [3,4-c] ° ratio. Sodium 3-yl)-2-(2_caiyl)acetic acid amine; 225. N-[5-(2,2 - diterpene) Benzyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 226. N_(5_丁_2_ Base _4,6_ diazepine 17 and [3,4_c] π ratio ° sitting_3_

C:\2D-CODE\91-01\90119473.ptd 第33頁 1327569 五、發明說明（31) 基）-2-(2-萘基）乙醯胺； 227. N-[5-(3 -碘-4-甲基苯甲醯基）-4,6 -二氫吡咯并 [3, 4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 228. N-{5-[(苄基氧）乙醯基]-4,6-二氫吡咯并[3,4-(：] 吡唑-3-基卜2-(2-萘基）乙醯胺； 229. N-{5-(2-氟-2 -苯基乙醯基）-4,6 -二氫吡咯并 [3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 230. N-{5-(2-氟-2 -苯基乙醯基）-4,6 -二氫吼咯并 23,4-〇]吡唑-3-基}-4-苯氧苯甲醯胺；攀231. N-{5-(2-°塞吩基-乙蕴基）-4,6 -二氫吼11 各并 [3,4-c]吡唑-3-基}-4-(4-甲基哌啡基）苯甲醯胺； 232. N-{5-(3-甲基-丁醯基）-4,6 -二氫吡咯并[3,4-c] 吡唑-3-基}-4-(4_甲基哌啡基）苯曱醯胺； 233. N-{5-(2-呋喃曱醯基）-4,6 -二氫咄咯并[3,4-c] 吡唑-3-基}-4-(4-甲基哌D井基）苯曱醯胺； 234. N-{5 -苯基乙醯基-4, 6 -二氫吼17各并[3,4-c] 0比0坐 -3-基}-4-(4-曱基哌畊基）苯甲醯胺； 235. N-{ 5 -苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-0基} - 4-(4-曱基哌畊基）苯曱醯胺； 236. N-(2，6_ 二乙基苯基）- N’_{3-[4-(4_ 曱基旅 D丼基）苯甲醯胺]-4,6 -二氫吡咯并[3, 4-c]吡唑-5-基}脲； 237. N-乙基-N’-{3-[4-(4-曱基哌。丼基）苯曱醯胺] -4，6 -二氫D比17各并[3，4 - c ] °比°坐-5 -基}脲； 238. N-{5-(2-氟-2 -苯基乙醯基）-4,6_二氫咄咯并C:\2D-CODE\91-01\90119473.ptd Page 33 1327569 V. INSTRUCTIONS (31) yl)-2-(2-naphthyl)acetamide; 227. N-[5-(3 - Iodo-4-methylbenzhydryl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 228. N -{5-[(benzyloxy)ethenyl]-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-ylbu 2-(2-naphthyl)acetamide; 229. N-{5-(2-Fluoro-2-phenylethyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butyl Phenylguanamine; 230. N-{5-(2-fluoro-2-phenylethenyl)-4,6-dihydroindolo[23,4-indolyl]pyrazol-3-yl}-4 -phenoxybenzamide; Climbing 231. N-{5-(2-°Shenyl-ethylidene)-4,6-dihydroindole 11 each [3,4-c]pyrazole-3 -yl}-4-(4-methylpipephinyl)benzamide; 232. N-{5-(3-methyl-butenyl)-4,6-dihydropyrrolo[3,4-c Pyrazol-3-yl}-4-(4-methylpipephinyl)benzamide; 233. N-{5-(2-furanyl)-4,6-dihydroindole [3,4-c]pyrazol-3-yl}-4-(4-methylpiperidinyl)benzamide; 234. N-{5-phenylethenyl-4,6-di Hydroquinone 17 and [3,4-c] 0 to 0--3-yl}-4-(4-mercaptopiperidinyl)benzene Indoleamine; 235. N-{5-phenylsulfonyl-4,6-dihydropyrrolo[3,4-c]indazol-3-0yl}-4-(4-mercapto-peptidyl) Benzoylamine; 236. N-(2,6-diethylphenyl)-N'_{3-[4-(4_ fluorenyl D-yl) benzylideneamine]-4,6-dihydrogen Pyrrolo[3,4-c]pyrazol-5-yl}urea; 237. N-ethyl-N'-{3-[4-(4-mercaptopiperazinyl)benzamide] - 4,6-dihydrogen D ratio 17 and [3,4 - c ] ° ratio ° sit-5-yl}urea; 238. N-{5-(2-fluoro-2-phenylethenyl)- 4,6_dihydroindole

C:\2D-CODE\91-01\90119473.ptd 第34頁 1327569 五、發明說明（32) [3, 4-c]"比唑-3-基卜[4-U- °比咯啶-2-酮）苯甲醯胺]; 239. N-{5-(2-氟-2 -苯基乙醯基）-4,6 -二氫吡咯并 [3, 4-c]吡唑-3 -基}-4-(4-曱基哌畊基）苯曱醯胺； 240. N-{5-(2 -噻吩基乙醯基）-4,6-二氫°比咯并[3,4-〇] 吡唑-3-基}-胡椒基醯胺； 241. N-{5-(3-曱基-丁醯基）-4,6 -二氫吡咯并[3,4-c] 吼唑-3 _基卜胡椒基醯胺； 242. N - {5-(2 -呋喃曱醯基）-4, 6 -二氫吡咯并[3,4-c] 。比唑-3 -基}-胡椒基醯胺； 243. N-{5 -苯基乙醯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑 - 3 -基} _胡椒基酿胺； 244. N-{5 -苯磺醯基）-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基}-胡椒基醯胺； 245. ^{5-(2_三氟曱基）苯磺醯基-4,6-二氫吼咯并[3, 4 - c ]吼°坐-3 -基}-胡椒基醢胺； 246. N-乙基-Ν’ -{3 -胡椒基羧醯胺基-4, 6 -二氫咄咯并 [3，4 - c ]吡唑-5 -基}脲； 247.1^1-{5-乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-乙醯胺； 248. ^{5-乙醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基丨-環丙烷羧醯胺； 249. Ν-{5-乙醯基-4, 6 -二氫°比口各并[3, 4-c] D比0坐- 3-基}-異丁醯胺； 250. N-{5-乙醯基-4,6-二氫吡咯并[3,4-〇]°比唑-3-C:\2D-CODE\91-01\90119473.ptd Page 34 1327569 V. INSTRUCTIONS (32) [3, 4-c]"Bizozol-3-ylbu [4-U- °Byridine -2-keto)benzamide> 239. N-{5-(2-fluoro-2-phenylethenyl)-4,6-dihydropyrrolo[3,4-c]pyrazole- 3-based}-4-(4-mercaptopiperidinyl)benzamide; 240. N-{5-(2-thiophenylethenyl)-4,6-dihydrogen ratio[3 , 4-〇]pyrazol-3-yl}-piperidinylamine; 241. N-{5-(3-indolyl-butenyl)-4,6-dihydropyrrolo[3,4-c]indole Azole-3 _ kib-pepyl decylamine; 242. N - {5-(2-furanyl)-4,6-dihydropyrrolo[3,4-c]. Benzazole-3-yl}-piperonyl decylamine; 243. N-{5-phenylethenyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl} _ Piperamine; 244. N-{5-phenylsulfonyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-piperidinamide; 245. ^{ 5-(2-trifluoroindolyl)benzenesulfonyl-4,6-dihydroindolo[3,4-c]吼°-3-yl}-piperidinamide; 246. N-B Ν-Ν' -{3 -piperonylcarboxylamido-4,6-dihydroindolo[3,4-c]pyrazol-5-yl}urea; 247.1^1-{5-ethenyl -4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-acetamide; 248. ^{5-Ethyl-4,6-dihydropyrrolo[3, 4-〇]pyrazol-3-ylindole-cyclopropanecarboxamide; 249. Ν-{5-ethinyl-4,6-dihydrogen ratio [3, 4-c] D ratio 0 Sodium 3-yl}-isobutylamine; 250. N-{5-ethenyl-4,6-dihydropyrrolo[3,4-indole]pyrazole-3-

C:\2D-C0DE\91-01\90119473.ptd 第35頁 1327569 五、發明說明（33) 基}-環戊烷羧醯胺； 251. N-{5-乙酸基-4，6_ 二氫 nbB各并[3, 4-c] °比。坐- 3-基}-苯曱醯胺； 252. N-{5-乙酿基-4，6 -二氫吼17各并[3，4-c] σ比 °坐-3-基}-曱基吡啶甲醯胺； 253. Ν-{5_ 乙酿基- 4，6 -二氛 D 比0各并[3，4-c] 0 比0坐 _3-基}-菸鹼醯胺； 254. N-{5-乙酸基-4，6 -二氫各并[3,4-c] °比。坐-3-基}-異菸鹼醯胺； —255. Ν-{5-乙醯基-4,6 -二氫 0比°各并[3，4-(：]°比°坐-3- 基}-3-曱基-2-呋喃甲醯胺； 256. Ν-{5-乙醯基-4，6 -二氫"比°各并[3,4-c] °比。坐- 3-基} - °塞吩-2 -叛酿胺； 257. N-{5-乙醯基-4，6 -二氫 °比°各并[3, 4-c] D比。坐- 3-基} - °塞吩-3 -叛酿胺； 258. N-{5-乙醢基-4，6 -二氫吼11各并[3，4-c]吼。坐- 3-基卜鄰-甲苯曱醯胺； 259· N-{5-乙醯基-4，6 -二氫 °比 p各并[3,4-c] °比°坐- 3- I®基卜間-甲苯甲醯胺； 260. N-{5-乙醯基-4，6 -二氫口比嘻并[3, 4-c]吼。坐- 3-基卜對-甲苯甲醯胺； 261. N-{5-乙醯基-4，6 -二氫0比口各并[3，4-c] °比0坐- 3-基卜水楊醯胺； 262. N-{5-乙醢基-4, 6 -二氫 π比 17各并[3，4-c] °比。坐- 3-C:\2D-C0DE\91-01\90119473.ptd Page 35 1327569 V. INSTRUCTIONS (33) BASE}-Cyclopentane Carboxamide; 251. N-{5-Acetyl-4,6-Dihydrogen nbB is each [3, 4-c] ° ratio. Sodium 3-yl}-benzoguanamine; 252. N-{5-ethyl-branched-4,6-dihydroindole 17 and [3,4-c] σ ratio ° sitting-3-yl}- Mercaptopyridylcarboxamide; 253. Ν-{5_ 乙-- 4,6-di-environment D ratio 0 and [3,4-c] 0 to 0 sit _3-yl}-nicotinamide; 254. N-{5-Acetyl-4,6-dihydrogen [3,4-c] ° ratio. -3--3-yl}-isonicotinium amide; —255. Ν-{5-ethenyl-4,6-dihydrogen 0°°[3,4-(:]°°° sitting-3 - yl}-3-mercapto-2-furancarboxamide; 256. Ν-{5-ethinyl-4,6-dihydro" ratio °[3,4-c] ° ratio. - 3-yl} - ° phenophene-2 - Atherosamine; 257. N-{5-ethenyl-4,6-dihydrogen ratio ° and [3, 4-c] D ratio. Sit - 3-yl}- °Cet-3 - Azoine; 258. N-{5-Ethyl-4,6-dihydroindole 11 and [3,4-c]pyrene. Sodium-3-yl Bu-o-toluidine; 259· N-{5-ethenyl-4,6-dihydrogen ratio p and [3,4-c] ° ratio sit - 3- I® 基卜- Toluidine; 260. N-{5-ethinyl-4,6-dihydrogen hydrazino[3,4-c] oxime. s--3-yl-p-toluamylamine; 261. N-{5-ethinyl-4,6-dihydrogen 0 is a ratio of [3,4-c] ° to 0-position - 3-ylbu salicylamine; 262. N-{5-acetamidine Base-4,6-dihydroπ ratio to 17 and [3,4-c] ° ratio. Sit - 3-

C:\2D-CODE\91-01\90119473.ptd 第36頁 1327569 五、發明說明（34) 基}-2-氟苯甲醯胺/ 26 3. N-{5-乙醯基-4, 6 -二氫 0比 p各并[3, 4-c] D比0坐- 3-基卜3 -氟苯甲醯胺； 264. N-{5-乙酿基-4，6 -二氫吼17各并[3, 4-c] °比 σ坐- 3-基}-4-氟苯甲醯胺； 265· Ν-{5-乙酿基-4，6_ 二氮0比 11 各并[3，4-c] D比0坐- 3-基} - π塞吩-2 _乙酿胺； 266. Ν-{5-乙醯基-4，6 -二氫。比 °各并[3, 4-c] D比。坐- 3-基} - °塞吩-3 _乙酿胺； 267. N_{5~ 乙酿基_4，6 -二氮 p比咯并[3，4_c] °比〇坐-3-基}-苯基丙炔醯胺； 268. ^{5-乙醯基-4,6-二氫吡咯并[3,4-。]咄唑-3-基}_3_氛基苯甲酿胺； 269.1^-{5-乙醢基-4，6-二氫0比°各并[3,4-(：]吼°坐-3-基丨_4_氛基苯曱酿胺； 270. N-{5-乙酿基-4, 6 -二氫各并[3, 4-c] n比0坐- 3- 基卜反-桂皮醯胺； 2 71. N-{5-乙醯基-4，6 -二氫 17 比 11 各并[3, 4-c] °比。坐- 3-基} _順-桂皮酿胺； 272. N-{5-乙驢基-4, 6 -二氫0比 D各并[3, 4-c]吼〇坐- 3-基卜3 - ( 3 -吼啶基）丙烯醯胺； 273. \-{5-乙醯基-4,6-二氫0比口各并[3,4-(：]11比〇坐-3-基}_3-(4 -吡啶基）丙烯醯胺； 274. N-{5-乙醢基-4, 6 -二氫吼17各并[3,4-c] D比唑- 3-C:\2D-CODE\91-01\90119473.ptd Page 36 1327569 V. INSTRUCTIONS (34) BASE}-2-Fluorobenzamide/26 3. N-{5-Ethyl-4 6-dihydrogen 0 to p each [3, 4-c] D is 0-position - 3-kib 3-fluorobenzamide; 264. N-{5-ethyl-branched-4,6-dihydrogen吼17 each [3, 4-c] ° ratio σ sitting - 3-yl}-4-fluorobenzamide; 265· Ν-{5-ethyl aryl-4,6-dinitrogen 0 to 11 each [3,4-c] D is 0-position - 3-yl} - π-cetin-2 _ethidamine; 266. Ν-{5-ethinyl-4,6-dihydrogen. Ratio to [3, 4-c] D ratio. Sit-3-yl}- °cephene-3 _ethylamine; 267. N_{5~ ethoxylated _4,6-diaza p is more than [3,4_c] ° 〇-3-yl }-Phenylpropynylamine; 268. ^{5-Ethyl-4,6-dihydropyrrolo[3,4-. ] oxazol-3-yl}_3_ aryl benzoylamine; 269.1^-{5-ethenyl-4,6-dihydrogen 0 ratio °[3,4-(:]吼° sitting- 3-based 丨_4_ aryl benzoquinone; 270. N-{5-ethyl aryl-4,6-dihydro each [3, 4-c] n ratio 0 sitting - 3-kib - cinnamylamine; 2 71. N-{5-ethenyl-4,6-dihydrogen 17 to 11 each [3, 4-c] ° ratio. Sodium - 3-yl} _ cis-cassia 272. N-{5-Ethyl-4,6-dihydrogen 0 to D and [3, 4-c]吼〇-3-ylbu 3 -(3-anridino)propenylamine ; 273. \-{5-Ethyl-4,6-dihydrogen 0 is a ratio of [3,4-(:]11 to -3--3-yl}_3-(4-pyridyl)propene oxime Amine; 274. N-{5-ethenyl-4,6-dihydroindole 17 and [3,4-c] D-pyrazole-3-

第37頁 C:\2D-C0DE\91-01\90119473.ptd 1327569 五、發明說明（35) 基}-2-苯基丙醯胺； 275.1^-{5-乙醯基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-鄰-甲苯基乙醯胺； 276. N-{5-乙醯基-4, 6 -二氫 °比°各并[3, 4-c] °比〇坐- 3-基}-間-甲苯基乙醯胺； 277. ^{5-乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-對-甲苯基乙醯胺； 278. N-{5-乙醯基-4,6-二氫吡咯并[3,4-cレ比唑-3-基}-鄰-茴香醯胺； 279. N-{5-乙酿基_4，6_ 二說11 比 p各并[3，4-c] 0 比吐_3_ 基}-3-曱氧苯甲醯胺； 2 8 0. N-{5_ 乙酿基_4，6_ 二氮吼11各弁[3，4_c]吼°坐 _3_ 基}-對-茴香蕴胺； 281. N-{5-乙醯基-4，6 -二氫0比 p各并[3，4-c] ° 比。坐- 3-基}-苯氧乙醯胺； 282_ N-{5-乙醯基-4，6 -二氫 D比 p各并[3, 4-c] 0比°坐-3-基}_2_氣苯基乙酿胺， 283. N_{5-乙酿基_4，6_ 二氫吼。各并[3，4_c] D比 π坐 _3_ 基}_3_氣苯基乙酿胺； 284. N-{5-乙醯基-4, 6 -二氫吼11各并[3, 4-c] 〇比0坐-3-基}_4_氣苯基乙酿胺； 285· N-{5-乙醯基-4，6 -二氫 °比°各并[3，4-c] °比吐-3-基}-3_(2_嚷吩基）丙稀酿胺； 286. N-{5-乙醢基-4，6-二氫°比洛并[3, 4-c] °比°坐- 3-Page 37 C:\2D-C0DE\91-01\90119473.ptd 1327569 V. INSTRUCTIONS (35) BASE}-2-Phenylpropylamine; 275.1^-{5-Ethyl-4,6- Dihydropyrrolo[3,4-(:]oxazol-3-yl}-o-tolylacetamide; 276. N-{5-ethenyl-4,6-dihydrogen ratio [3, 4-c] ° 〇 - - 3-yl}-m-tolylacetamide; 277. ^{5-Ethyl-4,6-dihydropyrrolo[3,4-(: Pyrazol-3-yl}-p-tolylacetamide; 278. N-{5-ethenyl-4,6-dihydropyrrolo[3,4-cindolozol-3-yl} - o-anisoleamine; 279. N-{5-ethyl-branched _4,6_ 2 said 11 than p and [3,4-c] 0 than spit_3_yl}-3-oxobenzophenone Amine; 2 8 0. N-{5_ 乙式基_4,6_ diazepine 11 弁[3,4_c]吼° _3_ base}-p-fennelamine; 281. N-{5-B Mercapto-4,6-dihydrogen 0 to p and [3,4-c] ° ratio. Sodium-3-yl}-phenoxyacetamide; 282_ N-{5-ethenyl-4,6 - Dihydrogen D ratio p and [3, 4-c] 0 ratio °-3-yl}_2_ gas phenyl ethylamine, 283. N_{5-ethyl aryl 4,6-dihydroanthracene. Each [3,4_c] D is π sitting on _3_ base}_3_gas phenylethylamine; 284. N-{5-ethinyl-4,6-dihydroindole 11 each [3, 4- c] 〇 ratio 0 -3-yl}_4_gas phenylethylamine; 285· N-{5-ethinyl-4,6-dihydrogen ratio °[3,4-c] ° ratio -3-yl }-3_(2_嚷) acrylamide; 286. N-{5-ethenyl-4,6-dihydro-pyro[3, 4-c] °°°- 3-

C:\2D-C0DE\91-01\90119473.ptd 第38頁 1327569 五、發明說明（36) 基}-3-(3-噻吩基）丙烯醯胺； 287. N-{5-乙醯基_4,6 -二氫°比口各并[3,4-c]吡唑-3-基卜3-(2-噻吩基）丙醯胺； 288.1^-{5-乙醯基-4,6-二氮°比咯并[3,4-(：]°比唑-3-基}-2_氯苯曱酿胺； 289. N-{5-乙酿基-4，6_ 二氫°比0各并[3，4-c] D比。坐-3-基}-3-氯苯曱驢胺； 290· N-{5-乙醯基-4，6 -二氫 °比°各并[3,4-c]吼°坐- 3-基}-4-氯苯曱醯胺； 291. N-{5-乙酿基-4，6_ 二氫 °比0各并[3，4_c] π比0坐-3_ 基卜1 -哌啶丙醯胺； 292_ Ν-{5-乙龜基-4,6 -二氫吼0各并[3,4-c]n 比。坐- 3- 基卜2 -乙醯基苯甲醯胺； 293. N-{5-乙醯基-4，6 -二氫 D比 p各并[3, 4-c] °比哇- 3-基卜4-乙醯基苯曱醯胺； 294. N-{5-乙醯基-4, 6 -二氫吡p各并[3, 4-c]吼。坐- 3-基卜卜萘曱醯胺； 295. N-{5-乙醯基-4，6 -二氫 10比°各并[3,4-(：]11比°坐-3-基} - 2 -萘曱醯胺； 296. N-{5-乙醯基-4，6 -二氫吼 11 各并[3,4-c] °比。坐- 3-基}-3-苯曱醯基丙醯胺； 297. N-{5_ 乙酿基-4, 6 -二氫吼11各并[3，4_c] D 比。坐 _3_ 基}-4-乙醯胺基苯曱醯胺； 298· N-{5-乙醢基-4,6 -二氫吼17各并[3,4-c] p 比唾- 3-C:\2D-C0DE\91-01\90119473.ptd Page 38 1327569 V. INSTRUCTIONS (36) yl}-3-(3-thienyl)propenylamine; 287. N-{5-ethenyl _4,6-dihydrogen ratio of each [3,4-c]pyrazol-3-ylbu-3-(2-thienyl)propanamine; 288.1^-{5-ethenyl-4, 6-diaza ratio: [3,4-(:]°pyrazol-3-yl}-2_chlorobenzoquinone; 289. N-{5-ethyl-branched-4,6-dihydrogen Ratio of 0 to [3,4-c] D. Sodium-3-yl}-3-chlorophenylamine; 290·N-{5-ethenyl-4,6-dihydrogen °° And [3,4-c]吼°-3-yl}-4-chlorophenylamine; 291. N-{5-ethyl-branched-4,6-dihydrogen ratio 0 and [3,4_c ] π ratio 0 sitting -3_ kib 1 -piperidine propylamine; 292_ Ν-{5-ethanetosyl-4,6-dihydroindole 0 each [3,4-c]n ratio. sitting - 3 - kib 2 - ethenylbenzamide; 293. N-{5-ethinyl-4,6-dihydro D ratio p and [3, 4-c] ° than wow - 3-kib 4-ethylmercaptobenzamine; 294. N-{5-ethinyl-4,6-dihydropyridinyl[3,4-c]indole. Amine; 295. N-{5-ethenyl-4,6-dihydrogen 10 ratios each [3,4-(:]11 ratio °-3--3-}-2-naphthylamine; 296 . N-{5-Ethyl-4,6-dihydroanthracene 1 1 each [3,4-c] ° ratio. Sodium 3-yl}-3-phenylmercaptopropylamine; 297. N-{5_ ethyl-branched-4,6-dihydroindole 11 each [3,4_c] D ratio. Sit _3_ ki}-4-acetamidobenzoin; 298· N-{5-ethinyl-4,6-dihydroanthracene 17 [3,4 -c] p than saliva - 3-

C: \2D-OODE\91 -01 \90119473.ptd 第39頁 1327569 五、發明說明（37) 基}-2,5 -二曱氧苯曱醯胺； . 299. N-{5-乙醯基_4，6_ 二氫吼51 各并[3，4-c] °比。坐-3_ 基}-2,6 -二甲氧苯曱醯胺； 300. N-{5-乙醯基-4，6 -二氫各并[3, 4-c] ° 比0坐- 3-基}-3, 4-二曱氧苯甲醯胺； 301. N-{5-乙酿基-4，6 -二氫吼 17各并[3, 4-c] 0 比。坐- 3-基}-3,5 -二甲氧苯甲醯胺； 302. N-{5_ 乙酿基_4，6 -二氫°比0各并[3，4-c] °比°坐_3_ _基} - 3-(2 -噻吩曱醯基）-丙醯胺； ,303. N_{5_ 乙酿基_4，6_ 二氮 D比 D各弁[3，4-c] π 比0坐-3_ 基}-1-秦基乙酿胺； 304. Ν_{5_ 乙酿基-4，6_ 二氮 °比略弁[3，4_c] D比。坐-3_ 基} -4 -苯基笨曱醯胺； 305· N-{5-辛基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}- 乙醯胺； 306. N-{5-苄基-4,6-二氫咄咯并[3,4-c]咄唑-3-基}-環丙烷羧醯胺； 307. ^1-{5-苄基-4,6-二氫咄咯并[3,4-〇]°比唑-3-基}-0異丁醯胺； 308. N-{5-罕基-4, 6 -二氫 n 比 p各并[3,4-c] 0 比〇坐-3-基}-環戊烷羧醯胺； 309. N-{5-苄基-4，6 -二氫0比。各并[3, 4-c] 0 比。坐-3-基}-苯曱醯胺； 310. N_{5_ 爷基 _4，6_ 二氫 D 比 0各并[3，4-c] 0 比0坐-3_基}-C: \2D-OODE\91 -01 \90119473.ptd Page 39 1327569 V. Description of the invention (37) yl}-2,5-dioxaphthalamide; .299. N-{5-acetamidine The base_4,6_dihydroindole 51 is each [3,4-c] ° ratio. Sitting -3_yl}-2,6-dimethoxybenzamine; 300. N-{5-ethinyl-4,6-dihydro each [3, 4-c] ° than 0 sitting - 3 -yl}-3,4-dioxabenzoguanamine; 301. N-{5-ethenyl-4,6-dihydroindole 17 and [3, 4-c] 0 ratio. Sodium 3-yl}-3,5-dimethoxybenzamide; 302. N-{5_ ethoxylated _4,6-dihydrogen ratio 0 and [3,4-c] ° ratio ° Sit _3_ _ yl} - 3-(2-thiophenanthryl)-propanamide; , 303. N_{5_ Ethyl _4,6_ dinitrogen D ratio D 弁 [3,4-c] π Sitting on -3_ base}-1-methyl-based ethylamine; 304. Ν_{5_ ethyl-branched-4,6_ dinitrogen ° ratio slightly [3,4_c] D ratio. -3 -yl-phenyl-p-nonylamine; 305 · N-{5-octyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-acetamidine Amine; 306. N-{5-benzyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-cyclopropanecarboxamide; 307. ^1-{5- Benzyl-4,6-dihydroindolo[3,4-indene]pyrazol-3-yl}-0 Isobutylamine; 308. N-{5-Hanyl-4,6-dihydrogen n is more than p and [3,4-c] 0 is more than 〇-3-yl}-cyclopentane carboxamide; 309. N-{5-benzyl-4,6-dihydro 0 ratio. Each [3, 4-c] 0 ratio. Sodium-3-yl}-benzoguanamine; 310. N_{5_ 贵基 _4,6_ dihydrogen D ratio 0 and [3,4-c] 0 is 0 to 0 -3 base}-

C:\2D-CODE\91-01\90119473.ptd 第40頁 1327569 五、發明說明（38) 甲基吡啶曱醯胺； 311. N-{5-辛基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-菸鹼醯胺； 312. N-{5-辛基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}-異菸鹼醯胺； 313. N-{5-辛基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-3-甲基-2-呋喃甲醯胺； 314. N-{5-爷基- 4,6 -二氫 D 比 11 各并[3，4-c] 0 比0坐-3_基}-噻吩-2 -羧醯胺； 315. \-{5-苄基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-噻吩-3 -羧醢胺； 316· N-{5-苄基-4,6-二氫 °比咯并[3,4-c]吡唑-3 -基}- 鄰-曱苯曱醯胺； 317· N-{5-辛基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}- 間-曱苯曱醯胺； 318. N-{5-窄基-4, 6 -二氫吡咯并[3, 4-c]吡哇-3 -基}-對-曱苯曱醯胺； 319· N-{5-苄基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}- 苯基乙醯胺； 320. N-{5-苄基-4,6-二氫吼咯并[3,4-c]吡唑-3-基}- 水楊醢胺； 321.1^-{5-苄基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}_2-氟苯曱酿胺； 322. N-{5-苄基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-C:\2D-CODE\91-01\90119473.ptd Page 40 1327569 V. INSTRUCTIONS (38) Methylpyridinium; 311. N-{5-octyl-4,6-dihydropyrrole [3,4-c]pyrazol-3-yl}-nicotinium amide; 312. N-{5-octyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 }.-Isonicotinium amide; 313. N-{5-octyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-methyl-2-furan Methionine; 314. N-{5-aryl- 4,6-dihydro D ratio 11 each [3,4-c] 0 to 0--3-yl}-thiophene-2-carboxycarboxamide; 315. \-{5-Benzyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-thiophene-3-carboxycarboxamide; 316·N-{5-benzyl -4,6-dihydro-pyrolo[3,4-c]pyrazol-3-yl}-o-nonylphthalamide; 317·N-{5-octyl-4,6-dihydrogen Pyrrolo[3,4-c]pyrazol-3-yl}-m-nonylbenzamide; 318. N-{5-narrow-based-4,6-dihydropyrrolo[3,4-c] Pyra-3-yl}-p-nonylbenzamide; 319·N-{5-benzyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}- Phenylacetamide; 320. N-{5-benzyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-salicylide; 321.1^-{5 -benzyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}_2-fluorobenzoquinone ; 322. N- {5- benzyl-4,6-dihydro-pyrrolo [3,4-○:] pyrazol-3

C:\2D-C0DE\91-01\90119473.ptd 第41頁 1327569 五、發明說明（39) 基}-3-氟苯曱醯胺； 323. N-{5-辛基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3-基}-4-氟苯曱醯胺； 324. \-{5-苄基-4,6-二氫吼咯并[3,4-〇]。比唑-3-基}-11塞吩-2 -乙醯胺； 32 5. N-{5-芊基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}- 噻吩-3-乙醯胺； 326. N-{5-苄基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}- 苯基丙炔醯胺； —327. N-{5-苄基-4,6-二氫吡咯并[3,4-c]咄唑-3- 基}-3-氰基苯曱醯胺； 328. N-{5-爷基-4，6 -二氫吼11各并[3,4-c] D比。坐- 3-基卜4-氰基苯曱醯胺； 329. N-{5-苄基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-反_桂皮酿胺； 330. N_{5-辛基 _4，6_ 二氮 D比洛弁[3，4-c] 11比0坐- 3_ 基}-順-桂皮酿胺； 331. N-{5-苄基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3-基} - 3 _ ( 3 - °比σ定基）丙稀酿胺； 332. Ν-{5-亨基-4，6 -二氫 D比 ρ各并[3,4-c]"比〇坐-3-基} - 3 - ( 4 - n比啶基）丙烯醯胺； 333. ^{5-辛基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-2 -苯基丙醯胺； 334. N-{5-苄基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-C:\2D-C0DE\91-01\90119473.ptd Page 41 1327569 V. Description of the invention (39) yl}-3-fluorobenzamide; 323. N-{5-octyl-4, 6- Dihydroindolo[3,4-c]pyrazol-3-yl}-4-fluorobenzamide; 324. \-{5-benzyl-4,6-dihydroindole[3, 4-〇]. Bisazo-3-yl}-11-cepan-2-acetamide; 32 5. N-{5-mercapto-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl }- thiophene-3-acetamide; 326. N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-phenylpropynylamine; — 327. N-{5-Benzyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-3-cyanobenzoquinone; 328. N-{5- The genomic-4,6-dihydroindole 11 has a [3,4-c] D ratio. Sodium 3-yl-4-cyanobenzoguanamine; 329. N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-trans_ Cassia sulphate; 330. N_{5-octyl _4,6_ dinitrogen D belovin [3,4-c] 11 to 0 sitting - 3_ ki}-cis-cinnamamine; 331. N-{5 -benzyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl} - 3 _ (3 - ° ratio σ base) acrylamide; 332. Ν-{5- Henki-4,6-dihydrogen D ratio ρ和[3,4-c]" 〇 -3--3-yl} - 3 - ( 4 - n-pyridyl) acrylamide; 333. ^{ 5-octyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-2-phenylpropanamine; 334. N-{5-benzyl-4,6 -dihydropyrrolo[3,4-indolylpyrazol-3-yl}-

C:\2D-CODE\91-01\90119473.ptd 第42頁 1327569 五、發明說明（40) 鄰-曱苯基乙醯胺；’ 33 5_ N-{5-苄基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3 -基}- 間-曱苯基乙醯胺； 336. ^{5-苄基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}- 對-曱苯基乙醯胺； 337. N-{5-芊基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}- 鄰-茴香醯胺； 338.1{5-苄基-4,6-二氫吡咯并[3,4-(：]咄唑-3- 基}-3-曱氧苯甲醯胺； 33 9. N-{5-苄基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3 -基}-對-茴香醯胺； 34 0. N-{5 -苄基-4, 6 -二氫吡咯并[3, 4-c]吡。坐-3 -基}- 苯氧乙醯胺； 341. N-{5 -爷基-4, 6 -二氫咄咯并[3, 4-c]咄唑-3- 基}_2_氣苯基乙酿胺； 342· N-{5-苄基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3- 基}_3_氣苯基乙酿胺； 343. N-{5-辛基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}-4-氣苯基乙酸胺； 344. N-{5-苄基-4，6 -二氫 °比口各并[3, 4-c] 0比嗤-3-基}-3-(2-°塞吩基）丙烯醯胺； 345· N-{5-苄基-4,6-二氫吡咯并[3,4-c]吡唑-3- 基}_3_(3_。塞吩基）丙稀酿胺； 346. N-{5 -苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-C:\2D-CODE\91-01\90119473.ptd Page 42 1327569 V. INSTRUCTIONS (40) o-Methylphenyl acetamide; '33 5_ N-{5-benzyl-4, 6 - two Hydroquino[3,4-c]pyrazol-3-yl}-m-indolephenylacetamide; 336. ^{5-benzyl-4,6-dihydropyrrolo[3,4- (:]oxazol-3-yl}-p-indole phenylacetamide; 337. N-{5-mercapto-4,6-dihydropyrrolo[3,4-c]pyrazole-3- }--o-anisoleamine; 338.1 {5-benzyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-3-indolylbenzamide; 33 9. N-{5-Benzyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-p-anisylamine; 34 0. N-{5-benzyl -4,6-dihydropyrrolo[3,4-c]pyridinium-sodium-3-yl}-phenoxyacetamide; 341. N-{5-y-yl-4,6-dihydroindole [3,4-c]oxazol-3-yl}_2_qiphenylphenylamine; 342· N-{5-benzyl-4,6-dihydroindolo[3,4-c]pyridin Zyridin-3-yl}_3_gasphenylethylamine; 343. N-{5-octyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4- Gas phenylacetic acid amine; 344. N-{5-benzyl-4,6-dihydrogen ratio each [3, 4-c] 0 to indole-3-yl}-3-(2-° stopper Phenyl) acrylamide; 345· N-{5-benzyl-4,6-dihydropyrrolo[ 3,4-c]pyrazol-3-yl}_3_(3_.sepeno)propanol; 346. N-{5-benzyl-4,6-dihydropyrrolo[3,4-( :]Pyrazole-3-

C:\2D-00DE\91-01\90119473.ptd 第43頁 1327569 五' 發明說明（41) 基} -3-(2-噻吩基）丙醯胺； ' 347. N-{5-亨基-4,6-二氫吡咯并[3,4-c]°比唑-3-基}-2-氯苯甲醯胺； 348. N-{5 -节基 _4，6 -二氫 °比0各并[3，4-c] ° 比0坐-3_ 基}_3-氯苯曱酿胺； 349.1^-{5-辛基-4,6-二氫吡咯并[3,4-。]吡唑-3-基} -4-氯苯甲醯胺； 350. N-{5-窄基-4,6-二氫咄咯并[3,4-c]咄唑-3- 基}-l-°底β定丙醯胺；，351. N-{5-苄基-4,6 -二氫吡咯并[3,4-c]吡唑-3- 基}-2-乙醯基苯曱醯胺； 352· N-{5-亨基-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基} -4-乙醯基苯曱醯胺； 353. N_{5~ 辛基_4，6 -二氫 D比 p各弁[3，4_c] °比°坐-3-基} -1 -萘曱醯胺； 354. N_{5-辛基 _4，6_ 二氮 °比洛弁[3，4_c]吼〇坐-3-基}-2 -萘曱醯胺； 355. \-{5-苄基-4,6-二氫吡咯并[3,4-。]吡唑-3-¥基} - 3-苯甲醯基丙醯胺； 356_ N-{5-苄基-4,6-二氫吡咯并[3,4-c]°比唑-3- 基}-4-乙醯胺基苯曱醯胺； 357.1^-{5-罕基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-2, 5-二曱氧苯甲醯胺； 358. N-{5-辛基-4,6-二氫吡咯并[3,4-〇]咄唑-3-C:\2D-00DE\91-01\90119473.ptd Page 43 1327569 V' Description of invention (41) yl}-3-(2-thienyl)propanamide; '347. N-{5-Henki -4,6-dihydropyrrolo[3,4-c]°boxazol-3-yl}-2-chlorobenzamide; 348. N-{5 -gangyl-4,6-dihydrogen More than 0 each [3,4-c] ° than 0 sitting -3_yl}_3-chlorophenyl hydrazine; 349.1^-{5-octyl-4,6-dihydropyrrolo[3,4-. Pyrazol-3-yl}-4-chlorobenzamide; 350. N-{5-Narrow-based-4,6-dihydroindolo[3,4-c]oxazol-3-yl} -l-° bottom β decylamine; 351. N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-ethenyl Benzoylamine; 352· N-{5-Henyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-ethenylbenzamide; 353. N_{5~ octyl_4,6-dihydrogen D ratio p 弁[3,4_c] ° ratio ° sits-3-yl} -1 -naphthylamine; 354. N_{5-octyl _4 , 6_ dinitrogen phloindole [3,4_c] 吼〇-3-yl}-2-naphthylamine; 355. \-{5-benzyl-4,6-dihydropyrrolo[3, 4-. Pyrazol-3-carbyl}-3-benzylidenepropionamine; 356_ N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]°bazole-3- } -4- 醯醯醯 35 35 35 35 ^ 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 35 - dioxobenzoguanamine; 358. N-{5-octyl-4,6-dihydropyrrolo[3,4-indolyl]carbazole-3-

C:\2D-OODE\9卜01\90119473_ptd 第44頁 1327569 五、發明說明（42) 基卜2, 6-二曱氧苯曱醯胺； 359.1^1-{5-辛基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3, 4-二曱氧苯甲醯胺； 360.1'1-{5-苄基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-3, 5-二甲氧苯甲醯胺； 361. N_{5_ 辛基_4，6_ 二氮口比11各弁[3，4_c] D比 σ坐-3_ 基}-3-(2 -噻吩甲醯基）-丙醯胺； 362· Ν-{5 -苄基-4,6-二氫°比咯并[3,4-c]吡唑-3- 基}_2_秦基乙酸胺； 363. Ν-{5 -苄基-4,6 -二氫吡咯并[3,4-c]咄唑-3-基}-1-蔡基乙酿胺； 364. N-{5_ 辛基 _4，6_ 二氮 D 比 17各弁[3，4_c] °比°坐 _3-基}-4-苯基苯曱醯胺； 365. N-{5 -苯基乙基-4，6 -二氮11比p各并[3，4_c] 0比°坐- 3-基}-乙醯胺； 366. N-{5 -苯基乙基_4，6-二氮°比洛弁[3，4_c] σ比.°坐-3 -基}-環丙烷羧醯胺； 367. Ν-{5_苯基乙基-4，6_二氮〇比口各并[3,4-c]。比。坐-3_ 基}-異丁醯胺； 368· N_{5_苯基乙基-4，6-二氣°比。各并[3，4_C] π比0坐-3_ 基}-環戊烷羧醯胺； 369. ^{5-苯基乙基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}-苯甲醯胺； 370. Ν_{5_ 苯基乙基_4，6_ 二氮各并[3，4_c] ϋ比0坐-3-C:\2D-OODE\9 Bu 01\90119473_ptd Page 44 1327569 V. Description of the invention (42) Kib 2,6-dioxabenzoquinone; 359.1^1-{5-octyl-4,6 -dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3,4-dioxaxybenzamide; 360.1'1-{5-benzyl-4,6-dihydropyrrole And [3,4-(:]oxazol-3-yl}-3, 5-dimethoxybenzamide; 361. N_{5_ octyl_4,6-diazide ratio 11 弁 [3, 4_c] D is σ sitting -3_yl}-3-(2-thiophenemethyl)-propanamine; 362·Ν-{5-benzyl-4,6-dihydrogen ratio [3,4 -c]pyrazol-3-yl}_2-methylglycolic acid amine; 363. Ν-{5-benzyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}- 1-蔡基乙乙胺; 364. N-{5_ octyl_4,6_ dinitrogen D ratio 17 弁[3,4_c] ° ratio _3-yl}-4-phenylbenzamide; 365 N-{5-Phenylethyl-4,6-diaza 11 ratio p and [3,4_c] 0 ratio ° sit--3-yl}-acetamide; 366. N-{5-phenyl Ethyl_4,6-diaza° 弁弁 [3,4_c] σ ratio. ° sit-3-yl}-cyclopropane carboxamide; 367. Ν-{5_phenylethyl-4,6 _Diazinium is more than [3,4-c]. Sit-3_yl}-isobutylamine; 368· N_{5_phenylethyl-4,6-diox ratio. [3,4_C] π ratio 0 sitting -3_yl}-cyclopentane carboxamide; 369. ^{5-phenylethyl-4,6-dihydroindole[3,4-(:]咄Zyrid-3-yl}-benzamide; 370. Ν_{5_ phenylethyl_4,6-diaza each [3,4_c] ϋ is 0 -3-

C:\2D-C0DE\91-01\90119473.ptd 第45頁 1327569 五、發明說明（43) 基}-曱基吼啶曱醯胺； 371.1^{5-苯基乙基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基卜菸鹼醯胺； 372. ^{5-苯基乙基-4,6-二氫口比咯并[3,4-(：]"比唑-3-基}-異菸鹼醯胺； 373. ^{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]咄唑-3-基} - 3 -曱基-2 _ π夫喃甲酿胺； 374.1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-噻吩-2-羧醯胺； • 375. Ν-{5-苯基乙基-4,6-二氫咄咯并[3,4-c]吡唑-3- 基卜噻吩-3 -羧醯胺； 376. N-{5 -苯基乙基-4,6-二氫D比咯并[3,4-c]吡唑-3- 基}-鄰-甲苯甲醯胺； 377.1{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基卜間-曱苯甲醯胺； 378. N-{ 5 -苯基乙基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-對-甲苯曱醯胺； 379. N_{5_苯基乙基_4，6_二氮口比17各并[3，4_c] 〇比0坐- 3-W基卜苯基乙醯胺； 380. N-{5_苯基乙基_4，6_二氮吼口各并[3，4_c] D比0坐-3_ 基}-水楊醯胺； 381. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡哇-3-基}-2-氟苯曱酿胺； 382_ N-{5 -苯基乙基-4,6-二氫咄咯并[3,4-〇]吡唑-3-C:\2D-C0DE\91-01\90119473.ptd Page 45 1327569 V. INSTRUCTIONS (43) BASE}-Mercaptoacridamine; 371.1^{5-phenylethyl-4,6- Dihydroindolo[3,4-(:]oxazol-3-ylpyramine decylamine; 372. ^{5-phenylethyl-4,6-dihydroperoxyl[3,4 -(:]"Bizozol-3-yl}-isonicotinamine amide; 373. ^{5-Phenylethyl-4,6-dihydropyrrolo[3,4-indolyl]carbazole-3 -yl} - 3 -mercapto-2 _ π 喃甲酿 ;; 374.1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]carbazole-3- }--thiophene-2-carboxamide; 375. Ν-{5-phenylethyl-4,6-dihydroindolo[3,4-c]pyrazole-3-ylthiophene-3 - Carboxylamidine; 376. N-{5-Phenylethyl-4,6-dihydro D-pyrolo[3,4-c]pyrazol-3-yl}-o-tolylcarbamide; 377.1 {5-Phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-ylbu-indolylbenzamide; 378. N-{5-phenylethyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-p-toluidine; 379. N_{5_phenylethyl-4,6-diaza ratio 17 each [3,4_c] 〇 is 0 to sit - 3-W phenyl phenyl acetamide; 380. N-{5_phenylethyl _4,6-diazide oxime [3,4_c ] D is 0 to sit -3_ base}- Salicylamine; 381. N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-c]pyran-3-yl}-2-fluorobenzoquinone; 382_ N -{5-phenylethyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-

C:\2D-OODE\91-01\90119473.ptd 第46頁 1327569 五、發明說明（44) 基}_3-默苯曱酿胺； 383. ^1-{5-苯基乙基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-4-氟苯曱醯胺； 384. N-{ 5 -苯基乙基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-噻吩-2-乙醯胺； 385.1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-噻吩-3-乙醯胺； 386.1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-。]吡唑-3-基}-苯基丙炔醯胺； 387.^{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3-氰基苯曱醯胺； 388.1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-氰基苯曱酿胺； 389. ^{5-苯基乙基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基}-反-桂皮醯胺； 390. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基卜順-桂皮醯胺； 391. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}_3_(3_c比咬基）丙稀趨胺， 392_ N-{5 -苯基乙基-4,6-二氫咄咯并[3,4-c]咄唑-3-基}-3-(4-吡啶基）丙烯醯胺； 393. N-{5_苯基乙基_4，6_二氫D比0各并[3, 4-c] °比°坐- 3-基}-2-苯基丙醯胺； 394. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-C:\2D-OODE\91-01\90119473.ptd Page 46 1327569 V. INSTRUCTIONS (44) BASE}_3- benzophenone amine; 383. ^1-{5-phenylethyl-4, 6-dihydroindolo[3,4-(:]pyrazol-3-yl}-4-fluorobenzamide; 384. N-{ 5 -phenylethyl-4,6-dihydropyrrole And [3, 4-c]pyrazol-3-yl}-thiophene-2-acetamide; 385.1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(: ]oxazol-3-yl}-thiophene-3-acetamide; 386.1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-.]pyrazol-3-yl} -Phenylpropynylamine; 387.^{5-Phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-cyanobenzoquinone Amine; 388.1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-cyanobenzoquinone; 389. ^{ 5-phenylethyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-trans-cintoinamide; 390. N-{5-phenylethyl-4 , 6-dihydropyrrolo[3,4-c]pyrazole-3-ylbus- cinnamate; 391. N-{5-phenylethyl-4,6-dihydropyrrolo[3, 4-c]pyrazol-3-yl}_3_(3_c ratio) amidamine, 392_ N-{5-phenylethyl-4,6-dihydroindole[3,4-c] Oxazol-3-yl}-3-(4-pyridyl)propenylamine; 393. N- {5_Phenylethyl_4,6-dihydrogen D is 0 and each is [3, 4-c] °°°-3-yl}-2-phenylpropanamide; 394. N-{5 -Phenylethyl-4,6-dihydropyrrolo[3,4-indole]pyrazole-3-

C:\2D-C0DE\91-01\90119473.ptd 第47頁 1327569 五、發明說明（45) 基}-鄰-曱笨基乙醯胺； 395.1'1-{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]°比唑-3-基}-間-甲笨基乙醯胺； 396. N_{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3- 基}-對-曱苯基乙醯胺； 397.1^{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-鄰-茴香醯胺； 398.1^-{5-苯基乙基-4,6-二氫°比咯并[3,4-〇]吡唑-3-基}-3-甲氧苯甲醯胺； ,399.1^-{5-苯基乙基-4,6-二氫吼咯并[3,4-〇]吡唑-3-基}-對-茴香醯胺； 400.1^-{5-苯基乙基-4,6-二氫吼咯并[3,4-(：]吡唑-3-基}-苯氧乙醯胺； 401. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-2-氟苯基乙酿胺； 402. N-{5_苯基乙基-4，6 -二氮吼13各弁[3，4-c]吼*1坐_3_ 基}-3-氣苯基乙酿胺； 403.1{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]咄唑-3-¥基卜4-氟苯基乙醯胺； 404. N_{5_苯基乙基-4，6_二氮0比17各并[3，4_c]吼°坐_3_ 基}_3_(2_ °塞吩基）丙稀酿胺； 405. ?^-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3_(3_°塞吩基）丙稀酿胺； 406. N-{5 -苯基乙基-4,6-二氫咄咯并[3,4-〇:]吡唑-3-C:\2D-C0DE\91-01\90119473.ptd Page 47 1327569 V. INSTRUCTIONS (45) Base}-o-indoleylacetamide; 395.1'1-{5-phenylethyl-4 ,6-dihydropyrrolo[3,4-〇]°bazol-3-yl}-m-methylphenylacetamide; 396. N_{5-phenylethyl-4,6-dihydropyrrole And [3,4-c]pyrazol-3-yl}-p-indole phenylacetamide; 397.1^{5-phenylethyl-4,6-dihydropyrrolo[3,4-(: Pyrazol-3-yl}-o-anisoleamine; 398.1^-{5-phenylethyl-4,6-dihydropyr-[3,4-indolylpyrazol-3-yl} -3-methoxybenzamide; 399.1^-{5-phenylethyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-p-anise Amine; 400.1^-{5-phenylethyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-phenoxyacetamide; 401. N-{5 -Phenylethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-fluorophenylethylamine; 402. N-{5_phenylethyl- 4,6-diazepine 13 弁[3,4-c]吼*1 sits _3_ yl}-3-phenylphenylethylamine; 403.1{5-phenylethyl-4,6-dihydro Pyrrolo[3,4-(:]carbazole-3-¥ kib4-fluorophenylacetamide; 404. N_{5_phenylethyl-4,6-diaza 0 to 17 each [ 3,4_c]吼°Sit _3_ base}_3_(2_ ° Acetylamine; 405. ?^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3_(3_°secenyl) Acetylamine; 406. N-{5-phenylethyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-

C:\2D-CODE\91-01\90119473.ptd 第48頁 1327569 五、發明說明（46) 基卜3 - ( 2 -噻吩基）丙醯胺； 407. N-{5-苯基乙基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}_2-氯苯曱酿胺； 408. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}_3-氯苯曱酿胺； 409. N_{5_苯基乙基_4，6_二氮0比0各弁[3，4-c] °比〇坐- 3-基}_4-氯苯曱酷胺； 410. N_{5_苯基乙基_4，6 -二氮吼11 各并[3，4-c] °比。坐- 3-基}-1-°底。定丙醯胺； 411. ^{5-苯基乙基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-2-乙醯基苯甲醯胺； 412. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基卜4-乙醯基苯曱醯胺； 413. N-{5 -苯基乙基-4，6 -二氫π比n各并[3，4-c] °比σ坐-3-基} - ：!-萘甲醯胺； 414. Ν-{5 -苯基乙基- 4,6 -二氫D比11 各并[3,4-c] η比唾- 3-基}-2 -蔡曱酿胺； 415. Ν-{5_苯基乙基_4，6_二氮π比D各弁[3，4_c] 0比。坐-3_ 基}-3 -苯曱醯基丙醯胺； 416· N_{5_苯基乙基_4，6_二氮〇比0各并[3，4-c] 〇比。坐-3_ 基}-4-乙醯胺基苯曱醯胺； 417. N-{5-苯基乙基-4, 6 -二氫0比B各并[3, 4-c] 0比°坐- 3-基}-2, 5-二甲氧苯曱醯胺； 418. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-C:\2D-CODE\91-01\90119473.ptd Page 48 1327569 V. INSTRUCTIONS (46) Kib 3 - (2-Thienyl)propanamide; 407. N-{5-phenylethyl -4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}_2-chlorobenzoquinone; 408. N-{5-phenylethyl-4,6-dihydropyrrole And [3,4-c]pyrazol-3-yl}_3-chlorobenzoquinone; 409. N_{5_phenylethyl_4,6-diaza 0 to 0 弁[3,4- c] ° than squat - 3-yl}_4-chlorobenzoquinone; 410. N_{5_phenylethyl-4,6-diazepine 11 each [3,4-c] ° ratio. Sit - 3-base}-1-° bottom. Propylamine; 411. ^{5-Phenylethyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazol-3-yl}-2-ethenylbenzamide; 412. N-{5-Phenylethyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-ylbu-4-ethenylbenzamide; 413. N-{5 -Phenylethyl-4,6-dihydroπ ratio n[3,4-c] ° ratio σ-3-yl} - :!-naphthylcarboxamide; 414. Ν-{5 - benzene Benzyl- 4,6-dihydro D ratio 11 and [3,4-c] η than sal-3-(yl)-2-caxene; 415. Ν-{5_phenylethyl_ 4,6_Dinitrogen π is more than D [3,4_c] 0 ratio. Sitting -3_yl}-3-phenylmercaptopropylamine; 416·N_{5_phenylethyl_4,6-diazonium is more than 0 and [3,4-c] isomer ratio. Sitting -3_yl}-4-acetamidophenylamine; 417. N-{5-phenylethyl-4,6-dihydrogen 0 to B and [3, 4-c] 0 ratio Sodium 3-yl}-2, 5-dimethoxybenzamine; 418. N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazole- 3-

C:\2D-C0DE\91-01\90119473.ptd 第49頁 1327569 五、發明說明（47) 基}-2,6 -二曱氧苯曱醯胺； 419. N-{5_ 苯基乙基-4，6-.二氫0比 11 各并[3，4-c] σ 比0坐-3-基} -3, 4-二甲氧苯甲醯胺； 420. Ν-{5 -苯基乙基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-3,5 -二曱氧苯曱醯胺； 421. Ν_{5 -苯基乙基-4，6_二氫口比洛并[3，4-c] 0比0坐_3 -基}-3-(2-噻吩曱醯基）-丙醯胺； 422. Ν-{5 -苯基乙基-4,6-二氫咄咯并[3,4-c]吡唑-3-_基}_2_蔡基乙酿胺； I 423_ Ν_{5_ 苯基乙基-4，6 -二氮0比 11 各并[3, 4-c]吼11 坐_3- 基}_1_秦基乙驢胺； 424. Ν-{5 -苯基乙基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}_4_苯基苯曱酿胺； 425. Ν-{5-曱烧石黃酸基-4,6-二氫°比洛并[3,4-c] η比0坐 _3_基}_乙酿胺； 426. Ν-{5-曱烧石黃酿基- 4,6 -二氫〇比°各并[3，4-c] 0比0坐 -3-基}_環丙烧魏酿胺； 427. Ν-{5_曱烧石黃酿基-4，6_二氮D比口各弁[3，4_c] 11比0坐 3 _基}_異丁酿胺； 428· N-{5-曱烷磺醯基-4,6-二氫吼咯并[3,4-(：]吡唑 _3_基}-環戍烧叛酿胺； 429. N-{5-曱烧石黃醯基-4, 6 -二氫D比略并[3, 4-。]0比°坐 -3-基卜苯曱醯胺； 430. N-{ 5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑C:\2D-C0DE\91-01\90119473.ptd Page 49 1327569 V. INSTRUCTIONS (47) BASE}-2,6-Dioxabenzoylamine; 419. N-{5_phenylethyl -4,6-. Dihydrogen 0 to 11 each [3,4-c] σ is 0 -3-yl} -3,4-dimethoxybenzamide; 420. Ν-{5 - benzene Ethylethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3,5-dioxabenzoquinone; 421. Ν_{5-phenylethyl- 4,6_ dihydrogen piroxi[3,4-c] 0 to 0 sitting _3 -yl}-3-(2-thienyl)-propanamine; 422. Ν-{5-benzene Ethylethyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}_2_caffeylamine; I 423_ Ν_{5_ phenylethyl-4,6-diaza 0 to 11 each [3, 4-c] 吼 11 sitting _3- yl}_1_methyl acetamide; 424. Ν-{5-phenylethyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}_4_phenylbenzoquinone; 425. Ν-{5-曱石石石酸-4,6-dihydropyrazine[3,4- c] η is 0 _3_基}_乙胺胺; 426. Ν-{5-曱烧石黄毛- 4,6-dihydroindole ratio °[3,4-c] 0 ratio 0 sit-3-yl}_cyclopropane-burning styrene; 427. Ν-{5_ 曱石石黄 -4,6_二氮 D ratio 弁 [3,4_c] 11 to 0 sit 3 _基}_Isobutylamine 428· N-{5-nonanesulfonyl-4,6-dihydroindolo[3,4-(:]pyrazole-3-yl}-cycloindole Amine; 429. N-{ 5-曱烧石黄醯基-4,6-dihydrogen D ratio slightly [3, 4-.]0 ratio °-3--3-phenylbenzamide; 430. N-{ 5-decanesulfonyl -4,6-dihydropyrrolo[3,4-c]carbazole

C:\2D-CODE\91-01\901l9473.ptd 第50頁 1327569 五、發明說明（48) -3 -基}-曱基吡啶甲醯胺； 431. N-{5-曱烧石黃醯基-4,6-二氫吡咯并[3,4-<:]11比唑 _3_基卜於鹼醯胺； 432. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基}_異菸鹼醯胺； 433. N_{5_甲烧石黃酿基_4，6_二氮nitp各并[3，4_c] 口比〇坐 -3 -基卜3-曱基-2 -呋喃曱醯胺； 434. N-{5-曱烧石黃醯基- 4,6 -二氫吼0各并[3,4-c] 0比。坐 -3-基}-°塞吩-2-叛酿胺； 435. ^1-{5-曱烧石黃醯基-4，6-二氫吼11各并[3,4-(：]°比〇坐 -3-基}_°塞吩_3-叛酿胺； 436. N-{5-曱烧石黃龜基- 4,6 -二氫吼0各并[3，4-c] °比口坐 -3-基卜鄰-甲苯甲醯胺； 437· N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-(：]°比唑 -3-基}-間-曱苯曱醯胺； 438_ N-{5-曱烷磺醢基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-對-曱苯甲醯胺； 439· N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-<:]吡唑 _3_基}_苯基乙酿胺； 440. N_{5_甲烧項酿基_4，6_二氮°比0各并[3,4_c]D比°坐 _3_.基}_水楊酿胺； 441. N-{5_甲烧石黃酿基-4，6_二氮°比°各并[3，4_c] °比〇坐 -3-基}-2_氣苯甲酿胺； 442. N-{5-甲烧確醯基-4，6 -二氫°比°各并[3，4-c] °比〇坐C:\2D-CODE\91-01\901l9473.ptd Page 50 1327569 V. INSTRUCTIONS (48) -3 -yl}-mercaptopyridinecarboxamide; 431. N-{5-曱烧石黄醯基- 4,6-dihydropyrrolo[3,4-<:]11-pyrazole_3_baseb in base decylamine; 432. N-{5-methanesulfonyl-4,6-dihydropyrrole [3,4-(:]pyrazol-3-yl}-isonicotinamine amide; 433. N_{5_甲烧石黄煮基_4,6_二氮nitp each [3,4_c] 〇3 - kib 3-mercapto-2-furanamine; 434. N-{5-曱石石黄醯基- 4,6-dihydroindole 0 and [3,4-c] 0 -3-. °. ° 〇 -3- 基基 _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _. ° ° than the mouth -3- kib-o-toluidine; 437 · N-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-(:] ° azole - 3-yl}-m-p-benzoylamine; 438_ N-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-p- Benzamethyleneamine; 439· N-{5-methanesulfonyl-4,6-dihydropyrrolo[3,4-<:]pyrazole-3-yl}-phenylethylamine; 440 N_{5_甲烧项粉基_4,6_Dinitrogen ° ratio 0 and [3,4_c]D ratio ° sitting_3_.基}_水杨胺胺; 441. N-{5_甲The burnt stone yellow base 4,6_ dinitrogen ° ° and each [3,4_c] ° ratio -3- -3- base} -2_ gas benzoyl amine; 442. N-{5-甲烧Mercapto-4,6-dihydrogen ratio °[3,4-c] °

C:\2D-C0DE\91-01\90119473.ptd 第51頁 1327569 五、發明說明（49) -3 -基丨_3-氣苯曱酿胺， 443· N-{5-曱烧石黃醯基-4, 6 -二氫吡D各并[3, 4-c] °比唑 -3_基}_4_氣苯曱酿胺； 444. N-{5-甲烧石黃醒基-4，6 -二氫D比0各并[3, 4-c] D比0坐 -3 -基}_B塞吩-2_乙酸胺； 445_ N-{5-甲烧石黃醯基-4，6 -二氫D比D各并[3，4-c] °比〇坐 -3-基}-噻吩-3-乙醯胺； 446.1'1-{5-甲烧績醯基-4,6-二氫']比(1各并[3，4-(：]吼〇坐 -3_基}_苯基丙快酿胺； _ 447. N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-c]吡唑 -3 -基}-3-氰基苯甲酸胺； 448. N-{5-曱院石黃醢基- 4,6 -二氫0比0各并[3,4-c] 0比0坐 -3-基}-4-氰基苯曱醯胺； 449. N-{5-曱烧石黃醢基_4,6_二氫°比口各并[3,4-c] °比。坐 -3-基卜反-桂皮醯胺； 450.1{5-曱烧續醯基-4，6-二氫〇比1?各并[3,4-〇]°比'1坐 -3 -基}-順-桂皮醯胺； 4 51, N - { 5 -曱烧石黃醢基-4，6 -二氫0比p各并[3，4 - c ] D比0坐 3_基}_3_(3_11比°定基）丙稀酿胺； 452_ N-{5-曱烧續醯基- 4，6 -二氫吼11 各并[3，4-c] 0比0坐 -3-基}-3-(4-°比啶基）丙烯醯胺； 453. N - { 5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_2_苯基丙酿胺； 454.1'1-{5-甲烧石黃醯基-4,6-二氫1>比咯并[3,4-(：]0比〇坐C:\2D-C0DE\91-01\90119473.ptd Page 51 1327569 V. Description of Invention (49) -3 -Based on _3-Benzene Benzene, 443· N-{5-曱烧石黄醯基-4,6-dihydropyridyl D each [3, 4-c] ° azole-3_yl}_4_ gas benzoquinone; 444. N-{5-甲烧石黄醒基-4,6 - Dihydrogen D is 0 and each is [3, 4-c] D is 0-position -3 -yl}_B-cephene-2-acetic acid amine; 445_ N-{5-methyst-xanthine-4,6-dihydrogen D Ratio D to [3,4-c] ° 〇-3-yl}-thiophene-3-acetamide; 446.1'1-{5-甲烧醯基-4,6-dihydro'] Ratio (1 each [3,4-(:]吼〇--3_yl}}-phenylpropanol; _ 447. N-{5-decanesulfonyl-4,6-dihydropyrrole And [3,4-c]pyrazol-3-yl}-3-cyanobenzoic acid amine; 448. N-{5-曱院石黄醢基- 4,6-dihydrogen 0 to 0 each [3, 4-c] 0 to 0--3-yl}-4-cyanobenzoquinone; 449. N-{5-曱烧石黄醢基_4,6_ dihydrogen ratio each [3,4 -c] ° ratio. sit -3- kebu anti-cassia amide; 450.1 {5- 曱醯醯 -4 -4 4,6- dihydropyrene ratio 1? each [3,4-〇] ° ratio ' 1 sit -3 -yl}-cis-cassia amide; 4 51, N - { 5 - 曱石石醢基-4,6-dihydrogen 0 ratio p and [3,4 - c ] D ratio 0 sit 3 _基}_3_(3 _11 ratio ° base) acrylamide; 452_ N-{5-曱醯醯 - - 4,6-dihydroindole 11 each [3,4-c] 0 to 0 -3-yl}-3 -(4-°-pyridyl) acrylamide; 453. N - { 5-decanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole_3_yl}_2_ Phenylpropanolamine; 454.1'1-{5-carbide xanthine-4,6-dihydrogen 1> than s-[3,4-(:]0

C:\2D-C0DE\91-01\90119473.ptd 第52頁 1327569 五、發明說明（50) -3 -基}-鄰-甲苯基乙酿胺； 455. N - { 5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_間-曱苯基乙酿胺； 4 5 6. N-{5-甲烷磺醯基_4, 6 -二氫吼咯并[3, 4-c]吡唑 -3 -基卜對-曱苯基乙醯胺； 457. N-{5-曱烷石黃醯基-4,6-二氫吡咯并[3,4-(：]°比唑 -3-基}-鄰-茴香醯胺； 458. N-{5-甲烧石黃醯基-4, 6 -二氫0比0各并[3, 4-c] 0比唑 -3-基}-3-曱氧苯甲醯胺； 459.1'1-{5-曱烧石黃醯基-4,6-二氫0比0各并[3,4-(：]51比唑 -3 -基}-對-茴香醯胺； 460.1^-{5-曱烧續醯基-4,6-二氫吡洛并[3,4-〇]。比唑 _3_基}_苯氧乙酿胺； 4 61. N - { 5 -曱烧石黃醢基-4，6 -二氫0比0各并[3，4 - c ] 0比。坐 _3_基}_2_氣苯基乙酿胺； 462.1'1-{5-甲烧石黃蕴基-4，6-二氫0比11各并[3,4-(：]0比°坐 _3_基}_3_氣苯基乙蕴胺； 463. N-{5-曱烧續醯基-4, 6 -二氫0比口各并[3, 4-c] °比唑 -3-基}_4-敗苯基乙酿胺； 464. N-{5-曱烧石黃醯基- 4,6 -二氫吼11 各并[3,4-c] °比唑 -3-基}-3-(2-噻吩基）丙烯醯胺； 465. N-{5-曱烧績醯基-4, 6 -二氫吼0各并[3,4-c] 0比0坐 _3_基丨_3_(3_D塞吩基）丙稀隨胺； 466. N-{5-曱烷磺醯基-4,6-二氫咄咯并[3,4-〇]°比唑C:\2D-C0DE\91-01\90119473.ptd Page 52 1327569 V. INSTRUCTIONS (50) -3 -yl}-o-tolylamine; 455. N - { 5-decanesulfonate 4-,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-m-p-phenylphenylamine; 4 5 6. N-{5-methanesulfonyl-4 6-dihydroindolo[3,4-c]pyrazole-3-ylpyridin-p-phenylethylamine; 457. N-{5-decane fluorenyl-4,6-dihydropyrrole [3,4-(:]°pyrazol-3-yl}-o-anisylamine; 458. N-{5-methorphanate xanthyl-4,6-dihydrogen 0 to 0 each [3, 4 -c] 0-pyrazol-3-yl}-3-oxophenanthramine; 459.1'1-{5-曱石石黄醯基-4,6-dihydro 0-0 each [3,4-( :]51-pyrazol-3-yl}-p-anisylamine; 460.1^-{5-曱醯醯 -4 -4-4,6-dihydropyrolo[3,4-〇]. _基}_phenoxyethylamine; 4 61. N - { 5 - 曱石石醢基-4,6 - dihydrogen 0 to 0 each [3,4 - c ] 0 ratio. Sit _3_ base} _2_ gas phenyl ethylamine; 462.1'1-{5-methyst huangyunji-4,6-dihydrogen 0 to 11 each [3,4-(:]0 than ° sitting_3_base}_3 _ phenyl phenyl amide; 463. N-{5-曱醯醯 -4 -4 4,6 - dihydrogen 0 than each of the [3, 4-c] ° than azole-3-yl} _ 4 Phenyl Ethylamine; 464. N-{5-曱烧石黄醯基- 4,6-dihydroindole 11 each [3,4-c] ° oxazol-3-yl}-3-(2-thienyl) Acrylamide; 465. N-{5-曱曱醯 -4 4,6-dihydroindole 0 each [3,4-c] 0 to 0 sitting _3_ 丨 _3_ (3_D seno Acetylene with amine; 466. N-{5-nonanesulfonyl-4,6-dihydroindolo[3,4-〇]° azole

C:\2D-0QDE\91-01\90119473.ptd 第53頁 1327569 五、發明說明（51) _3_基}_3_(2_°塞吩基）丙酿胺， 4 67· N-{ 5-甲烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_2-氯苯曱酿胺； 4-6 8. N-{5-曱烷磺醯基-4, 6 -二氫吡洛并[3, 4-c]咄唑 -3_基丨- 3-氯苯甲酿胺； 469. N-{5-曱烧石黃醯基-4,6 -二氫D比洛并[3,4-c] 0比。坐 -3_基}_4_氯苯曱酿胺； 470. N-{5-曱烧石黃酿基-4，6 -二氫0比0各并[3，4-c] 〇比。坐 -3 -基} - 1 -哌啶丙醯胺； _ 471. N_{5-曱烧石黃酷基-4，6_二氮D比p各并[3，4-c] 〇比。坐 -3_基}-2_乙酿基苯曱酿胺； 472. N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-4-乙醯基苯甲醯胺； 473. N-{5-曱烧石黃醢基-4，6 -二氫°比〇各并[3，4-c] °比。坐 -3-基}-1-萘曱醯胺； 474. N_{5-曱烧石黃酿基-4，6_二氯吼11各并[3，4_c]。比口坐 -3-基}-2 -萘曱醯胺； 475.1^-{5-曱炫1石黃醯基-4，6-二氫〇比17各并[3，4-(：]〇比〇坐 (|-3-基}-3 -苯甲醯基丙醯胺； 476. N-{5-甲烧石黃醯基- 4,6 -二氫〇比°各并[3，4-c] 0比°坐 -3-基}-4-乙醯胺基苯曱醯胺； 477. N-{5-曱烧石黃醯基-4，6 -二氫"比0各并[3，4-c] °比。坐 _3-基}-2,5_二甲氧苯甲酿胺； 478. N-{ 5-曱烷磺醯基-4, 6 -二氫咣咯并[3, 4-c]。比唑C:\2D-0QDE\91-01\90119473.ptd Page 53 1327569 V. INSTRUCTIONS (51) _3_BASE}_3_(2_°Sepyl) propylamine, 4 67· N-{ 5-methane Sulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}_2-chlorobenzoquinone; 4-6 8. N-{5-decanesulfonyl- 4,6-dihydropyrazolo[3,4-c]carbazole-3_ylindole-3-chlorobenzamide; 469. N-{5-曱石石黄醯基-4,6-dihydrogen D is more than [3,4-c] 0 ratio. Sit -3_yl}_4_ chlorophenyl hydrazine; 470. N-{5- 曱石黄 -4 -4,6 - dihydrogen 0 to 0 each [3,4-c] 〇 ratio. -3 -yl} - 1 -piperidine propylamine; _ 471. N_{5-曱石石黄基基-4,6_二氮 D ratio p and [3,4-c] 〇 ratio. Sitting on -3_yl}-2_ethyl phenyl hydrazine; 472. N-{5-decanesulfonyl-4,6-dihydropyrrolo[3,4-indole]pyrazole-3- } -4- -4- 醯苯苯 ; ; ; 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473 473. Sodium-3-yl}-1-naphthylamine; 474. N_{5-曱石石黄-基-4,6-dichloroindole 11 each [3,4_c].比-3-yl}-2-naphthylamine; 475.1^-{5-曱炫1石黄醯基-4,6-dihydroindole ratio 17 and [3,4-(:]〇比〇 Sodium (|-3-yl}-3-benzhydrylpropionamide; 476. N-{5-methyst-xanthine- 4,6-dihydroindole ratio °[3,4-c] 0 Ratio °-3-yl}-4-acetamidophenylamine; 477. N-{5-曱石石黄醯基-4,6-dihydro" ratio 0 and [3,4-c ° °. Sit _3-yl}-2,5-dimethoxybenzoic acid; 478. N-{ 5-decanesulfonyl-4,6-dihydroindole[3, 4- c].

C:\2D-0QDE\91-01\90119473.ptd 第54頁 1327569 五、發明說明（52) _3_基}_2，6_二甲氧苯曱酿胺； 479· N-{5-曱院續醯基-4，6 -二氫0比0各并[3, 4-c] 〇比°坐 -3_基}-3，4_二曱氧苯曱酿胺； 480· N-{5-甲烧石黃醯基- 4,6 -二氫D比洛并[3,4-c] 0比0坐 _3_基}_3，5_二曱氧苯曱酿胺； 4 81. N - { 5 -曱烧石黃醯基-4，6 -二氫0比17各并[3, 4 - c ] 0比0坐 -3 -基}-3-(2-噻吩甲醯基）-丙醯胺； 482. N-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_2_秦基乙酿胺； 483. N-{5-曱烧績醯基-4，6 -二氫吼17各并[3，4-c] 0比。坐 -3-基}-：1-萘基乙醯胺； 484_ N-{5-曱烧績醯基-4，6 -二氫0比洛并[3，4-c]"比。坐 -3-基}-4-苯基苯曱醯胺； 485. N-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3,4-c]吡唑 -3-基卜乙醯胺； 486. N-{5-乙基胺基羰基_4,6-二氫吡咯并[3,4-〇]°比唑 -3-基}-環丙烧缓酿胺； 487. N-{5-乙基胺基幾基-4，6 -二氫D比p各并[3，4-c] °比〇坐 -3-基}-異丁醯胺； 488. N_{5_乙基胺基幾基-4，6_二氫吼11 各并[3，4-c] B比0坐 _3-基}-環戍烧叛酿胺； 489. N-{5_乙基胺基幾基_4，6_二氫0比p各弁[3，4-c] 0比。坐 _3_基}_苯甲酿胺； 490. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 Ϊ mC:\2D-0QDE\91-01\90119473.ptd Page 54 1327569 V. INSTRUCTIONS (52) _3_BASE}_2,6_Dimethoxybenzoate; 479· N-{5-曱院Continued fluorenyl-4,6-dihydrogen 0 to 0 each [3, 4-c] 〇 ratio ° sitting -3 yl}-3,4_dioxabenzoquinone; 480· N-{5 - 甲石石黄醯基 - 4,6-dihydro D, piroxi[3,4-c] 0 to 0, _3_yl}_3,5-dioxabenzoquinone; 4 81. N - { 5 - anthraquinone-4,6-dihydrogen 0 to 17 each [3, 4 - c ] 0 to 0 sitting -3 -yl}-3-(2-thienylmethyl)-propanamide; 482. N-{5-decanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_2-methylglycolamine; 483. N-{5-曱曱 -4 -4 4,6-dihydroindole 17 and [3,4-c] 0 ratio. Sodium-3-yl}-:1-naphthylacetamide; 484_ N-{5-曱曱醯 -4-4,6-dihydro- 0 bis-[3,4-c]" ratio. -3--3-yl}-4-phenylbenzamide; 485. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl乙乙胺胺; 486. N-{5-ethylaminocarbonyl_4,6-dihydropyrrolo[3,4-indene]pyrazol-3-yl}-cyclopropanol slow-acting amine; 487 N-{5-ethylamino benzyl-4,6-dihydro D ratio p and [3,4-c] ° ratio 〇-3-yl}-isobutylamine; 488. N_{ 5_ethylamino benzyl-4,6-dihydroindole 11 each [3,4-c] B is 0 _3-yl}-cyclic anthraquinone; 489. N-{5_ Ethylamino group _4,6-dihydro 0 is more than p 弁[3,4-c] 0 ratio. Sit _3_基}_benzamide; 490. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole Ϊ m

ψ,)·}ψ,)·}

C:\2D-C0DE\91-01\90119473.ptd 第55頁 1327569 五、發明說明（53) _3_基}-曱基吡啶曱醯胺； 4 91. N-{ 5-乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-菸鹼醯胺； 492. N-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑 -3_基}_異於驗酿胺； 493. N-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 -3-基}-3-曱基-2 -呋喃甲醯胺； 4 94. N-{ 5-乙基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3 -基}-11塞吩-2-叛酿胺； ® 495. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑 -3-基}-噻吩-3-羧醯胺； 496. N-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 -3 -基}-間-曱苯曱醯胺； 497. N-{5-乙基胺基羰基-4,6_二氫吡咯并[3,4-c]吡唑 _3-基}-對-曱苯曱醯胺； 498. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基丨-水揚酿胺； 499. N-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 3-基丨-2-氟苯甲酿胺； 500. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}-3_氟苯曱酿胺； 501. N-{5-乙基胺基幾基- 4,6 -二氫吼0各并[3,4-c]吼。坐 -3-基}-4-氟苯甲醯胺； 502. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 55 1327569 V. Description of the invention (53) _3_yl}-mercaptopyridine amide; 4 91. N-{ 5-ethylaminocarbonyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-nicotinium amide; 492. N-{5-ethylaminocarbonyl-4,6-dihydroanthracene And [3,4-(:]pyrazole-3-yl}- is different from the amine; 493. N-{5-ethylaminocarbonyl-4,6-dihydroindole[3,4- 〇]pyrazol-3-yl}-3-mercapto-2-furomylamine; 4 94. N-{ 5-ethylaminocarbonyl-4,6-dihydroindole[3, 4- c]pyrazol-3-yl}-11-cetin-2-reactive amine; ® 495. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyridinium Zyridin-3-yl}-thiophene-3-carboxamide; 496. N-{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl }-m-p-benzoylamine; 497. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-p-nonylbenzene Indoleamine; 498. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole_3_ylindole-water-enhanced amine; 499. N-{ 5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-indolylpyrazole-3-ylindole-2-fluorobenzamide; 500. N-{5-ethylamino Carbonyl-4,6-dihydrogen咯[3,4-〇]pyrazole-3-yl}-3-fluorobenzamide; 501. N-{5-ethylaminomethyl- 4,6-dihydroindole 0 each [ 3,4-c]吼. sit-3-yl}-4-fluorobenzamide; 502. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-( :]Pyrazole

C:\2D-G0DE\91-01\90119473.ptd 第56頁 1327569 五、發明說明（54) -3-基}-噻吩-2-乙醢胺； 503. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]咄唑 -3-基}-°塞吩-3-乙酿胺； 504. N-{5-乙基胺基羰基-4, 6 -二氫吡11 各并[3,4-c]咄唑 _3_基}_苯基丙快酿胺； 505. N-{5-乙基胺基羰基- 4,6 -二氫吼17各并[3,4-〇]吼°坐 -3_基}-3 -氮基苯曱酿胺； 506· N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3-基}-4-氰基苯曱醯胺； 507. ^{5-乙基胺基幾基-4,6-二氫°比11各并[3,4-(：]11比峻 -3 -基}-反-桂皮醯胺； 508. N-{5-乙基胺基幾基-4，6 -二氫吼11 各并[3,4-c] °比°坐 -3 -基}-順-桂皮醯胺； 509. N-{5_乙基胺基幾基- 4,6 -二氫π比0各并[3,4-c]°比0坐 _3_基}_3_(3_11比。定基）丙稀酿胺； 510. N-{5-乙基胺基幾基- 4,6 -二氫吼11 各并[3，4-c]0比。坐 -3-基}-3-(4 -吡啶基）丙烯醯胺； 511. N-{5-乙基胺基数基- 4,6 -二氫0比各并[3，4-c] °比°坐 -3_基}_2_苯基丙酿胺； 512. N-{5-乙基胺基羰基- 4,6 -二氫D比洛并[3,4-c]吡。坐 _3_基}-鄰-甲苯基乙酿胺； 513. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_間-曱苯基乙酿胺； 514. ^{5-乙基胺基羰基-4,6-二氫吡>1各并[3,4-(：]°比〇坐C:\2D-G0DE\91-01\90119473.ptd Page 56 1327569 V. INSTRUCTIONS (54) -3-yl}-thiophene-2-acetamide; 503. N-{5-ethylamino group Carbonyl-4,6-dihydropyrrolo[3,4-indole-3-oxazol-3-yl}-°cetin-3-ethylamine; 504. N-{5-ethylaminocarbonyl-4, 6-dihydropyrrole 11 each [3,4-c]carbazole-3-yl}}phenylpropanol; 505. N-{5-ethylaminocarbonyl-4,6-dihydroanthracene 17 each [3,4-〇]吼°-3_yl}-3-nitrobenzoquinone; 506· N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[ 3,4-〇]pyrazole-3-yl}-4-cyanobenzoquinone; 507. ^{5-ethylamino benzyl-4,6-dihydrogen ratio 11 and [3, 4-(:]11 than ternary-3-yl}-trans-cinsinamide; 508. N-{5-ethylaminomethyl-4,6-dihydroindole 11 each [3,4-c ° ° ° ° -3 -} cis - cinnamylamine; 509. N-{5_ethylamino benzyl- 4,6-dihydro π ratio 0 and [3,4-c] ° _3_基}_3_(3_11 ratio. base) acrylamide; 510. N-{5-ethylamino-based - 4,6-dihydroindole 11 each [3,4-c 0 ratio. sit-3-yl}-3-(4-pyridyl)propenylamine; 511. N-{5-ethylamino group- 4,6-dihydro- 0 ratio each [3,4 -c] ° than ° sitting - 3_yl}_2_phenylpropanol; 512. N-{5-ethylaminocarbonyl- 4,6-dihydro D-pyrolo[3,4-c]pyridine. sitting _3_yl} - o-tolylamine; 513. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3-yl}-m-phenylene Ethylamine; 514. ^{5-ethylaminocarbonyl-4,6-dihydropyridin>1 each [3,4-(:]°

C:\2D-00DE\91-0l\90119473.ptd 第57頁 1327569 五、發明說明（55) -3-基}_對-甲苯基乙酿胺； 515. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]咄唑 -3-基}-鄰-茴香醯胺； 516. N-{5-乙基胺基幾基-4, 6 -二氫0比略并[3,4-c] D比。坐 -3-基}-3-曱氧苯甲醯胺； 517. N-{5-乙基胺基幾基- 4,6 -二氫°比p各并[3,4-c] 0比嗤 _3-基}-對-茴香醯胺； 518. N-{5_乙基胺基幾基-4，6 -二氮0比0各并[3,4-c] D比。坐 _3_基}_苯氧乙酿胺； • 519. N-{5-乙基胺基幾基- 4，6 -二氫°比°各并[3,4-〇]°比°坐 _3_基}-2-氣苯基乙酿胺； 520. N-{5-乙基胺基叛基-4,6 -二氫吼11 各并[3，4-(^]°比〇坐 _3-基}_3-說苯基乙酿胺； 521. ^1-{5-乙基胺基徵基-4，6-二氫〇比°各并[3,4-(：]°比。坐苯基乙酿胺； 522. N-{5-乙基胺基幾基-4，6 -二氛0比π各并[3, 4-c] °比〇坐 -3 -基丨- 3- (2 -噻吩基）丙烯醯胺； 523. N-{5-乙基胺基幾基-4,6-二氫°比洛并[3,4-c] °比。坐 <·-3-*}-3-(3-噻吩基）丙烯醯胺； 524. Ν-{5-乙基胺基Μ基- 4,6 -二氫σ比ρ各并[3,4-c] °比0坐 _3_基}-3_(2_°塞吩基）丙酿胺； _3-基}-2 -氯苯曱酿胺； 526. N-{5-乙基胺基徵基-4,6 -二氫吼11各并[3,4-c] °比〇坐C:\2D-00DE\91-0l\90119473.ptd Page 57 1327569 V. Description of the invention (55) -3-yl}-p-tolylamine; 515. N-{5-ethylamino Carbonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-o-anisylamine; 516. N-{5-ethylamino group-4,6- Dihydrogen 0 is slightly more than [3,4-c] D ratio. Sodium-3-yl}-3-indolylbenzamide; 517. N-{5-ethylamino group - 4,6 - Dihydrogen ratio p and [3,4-c] 0 to 嗤-3-yl}-p-anisamine; 518. N-{5-ethylaminomethyl-4,6-diaza 0 Ratio of 0 to [3,4-c] D. Sit _3_yl}-phenoxyethylamine; • 519. N-{5-ethylaminomethyl- 4,6-dihydrogen ratio °[3,4-〇]°°°坐_3_基}-2-Phenylphenylethylamine; 520. N-{5-Ethylamino-based 4-,6-dihydroindole 11 each [3,4-(^]° 〇 _3-基}_3- phenyl phenylamine; 521. ^1-{5-ethylamino ketone-4,6-dihydro 〇 ° ° ° ° [3,4- (:] ° ratio. sit phenyl acetaminophen; 522. N-{5-ethylamino group - 4,6 - two atmosphere 0 to π each [3 , 4-c] ° 〇 -3 -3 - 丨 - 3- (2-thienyl) acrylamide; 523. N-{5-ethylamino benzyl-4,6-dihydropyrrol And [3,4-c] ° ratio. Sitting <·-3-*}-3-(3-thienyl)propenylamine; 524. Ν-{5-ethylamino fluorenyl- 4,6-dihydro σ ratio ρ[3, 4-c] ° sits at 0 _3_base}-3_(2_°secenyl) propylamine; _3-yl}-2-chlorophenyl hydrazine; 526. N-{5-ethylamino征基-4,6-dihydroindole 11 and [3,4-c] °

C:\2D-CODE\91-01\9O119473.ptd 第58頁 1327569 五、發明說明（56) -3 -基丨-3 -氣苯甲酿胺； 527· N-{5-乙基胺基截基-4，6-二氫吼洛并[3,4-(：]°比吐 -3-基}-4-氯苯曱醯胺； 528. N-{5-乙基胺基羰基- 4,6 -二氫°比0各并[3,4-c]D比唑 -3 -基} - ；1 -哌啶丙醯胺； 529. N-{5-乙基胺基羰基-4,6-二氫吡11各并[3,4-(：]吡唑 _3_基}_2_乙酿基苯甲酿胺， 530. N-{5-乙基胺基幾基- 4,6 -二氫π比17各并[3,4-c] °比〇坐 -3-基}-4-乙醯基苯甲醯胺； 531. N-{5-乙基胺基幾基- 4,6 -二氫吼17各并[3,4-c] °比0坐 -3 -基} - ：1 -萘甲醯胺； 532. N-{5-乙基胺基幾基- 4,6 -二氫°比略并[3,4-c] °比°坐 -3-基}-2-萘曱醯胺； 533.1^-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吼唑 -3-基}-3 -苯甲醯基丙醯胺； 534. N-{5_乙基胺基幾基-4,6 -二氮吼11 各并[3,4-c] °比。坐 -3-基}-4-乙醯胺基苯甲醯胺； 535. N-{5-乙基胺基数基- 4,6 -二氫吼°各并[3,4-c]吼〇坐 _3-基}-2，5_二曱氧苯甲酿胺； 536· N_{5_乙基胺基獄基-4，6_二氮°比^各并[3，4-c] °比〇坐 -3-基}-2,6 -二曱氧苯曱醢胺； 537. N-{5-乙基胺基叛基-4，6 -二氫"比°各并[3,4-c] D比。坐 -3-基}-3,4 -二甲氧苯甲醯胺； 538. N-{5-乙基胺基獄基-4, 6 -二氫°比°各并[3,4-c] D比0坐C:\2D-CODE\91-01\9O119473.ptd Page 58 1327569 V. INSTRUCTIONS (56) -3 -Based-3 - gas benzoic acid; 527 · N-{5-ethylamino group Truncate-4,6-dihydroindolo[3,4-(:]°pyt-3-yl}-4-chlorophenylguanamine; 528. N-{5-ethylaminocarbonyl- 4,6-dihydrogen ratio 0 and [3,4-c]D-pyrazol-3-yl}-;1-piperidinepropionamide; 529. N-{5-ethylaminocarbonyl-4 , 6-dihydropyrrole 11 and [3,4-(:]pyrazole-3-yl}_2-ethyl benzoylbenzamine, 530. N-{5-ethylaminomethyl--4, 6-dihydroπ ratio 17 and [3,4-c] ° 〇-3-yl}-4-ethenylbenzamide; 531. N-{5-ethylamino group- 4,6-dihydroindole 17 each [3,4-c] ° is 0--3 -yl} - :1 -naphthylamine; 532. N-{5-ethylamino group - 4 ,6-dihydrogen ratio slightly [3,4-c] ° ratio of sitting-3-yl}-2-naphthylamine; 533.1^-{5-ethylaminocarbonyl-4,6-di Hydropyrrolo[3,4-(:]oxazol-3-yl}-3-benzhydrylpropionamide; 534. N-{5-ethylaminomethyl-4,6-diazaindole 11 each [3,4-c] ° ratio. sit-3-yl}-4-acetamidobenzamide; 535. N-{5-ethylamino group- 4,6-dihydrogen吼° Each [3,4-c] 吼〇 _ 3-yl}-2,5-dioxobenzoic acid; 536· N_{5_ethylamine-based prison, 4,6-diaza ratio, each [3,4-c] ° ratio Sputum-3-yl}-2,6-dioxabenzoylamine; 537. N-{5-ethylamino-based t-group-4,6-dihydro" ratio °[3,4 -c] D ratio. Sodium-3-yl}-3,4-dimethoxybenzamide; 538. N-{5-ethylamine-prison-4,6-dihydrogen ratio [3,4-c] D is sitting at 0

C:\2D-C0DE\91-01\90119473.ptd 第59頁 1327569 五、發明說明（57) -3-基} -3, 5-二曱氧苯曱醯胺； 539. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-3-(2-噻吩曱醯基）-丙醯胺； 540. N-{5-乙基胺基羰基-4,6-二氫°比咯并[3,4-(：]吡唑 -3_基}_2 -秦基乙酿胺； 541. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-1-秦基乙酿胺； 542· N-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑 -3-基}-4 -苯基苯甲醯胺；寒543. N-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-。]咄唑 -3 -基}-乙醯胺； 544. N-{5 -苯基胺基羰基-4, 6 -二氫吼11 各并[3,4-c]吼°坐 _3_基}-環丙烧叛酿胺； 545. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-異丁醯胺； 546. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇:]吼唑 _ 3 -基} _環戊烧叛胺； 547. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑丨3 -基}-苯甲醯胺； 548. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基}-曱基吡啶曱醯胺； 549. N-{5 -苯基胺基幾基-4, 6 -二氫D比略并[3,4-c] π比嗤 _3-基}-於驗酿胺； 550. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 59 1327569 V. INSTRUCTIONS (57) -3-yl}-3,5-dioxabenzophenamine; 539. N-{5- Ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-(2-thienyl)-propanamine; 540. N-{ 5-ethylaminocarbonyl-4,6-dihydropyrolo[3,4-(:]pyrazol-3-yl}_2-methylglycolamine; 541. N-{5-ethyl Aminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-1-methylenylamine; 542·N-{5-ethylaminocarbonyl-4, 6-dihydroindolo[3,4-(:]pyrazol-3-yl}-4-phenylbenzamide; cold 543. N-{5-phenylaminocarbonyl-4,6- Dihydropyrrolo[3,4-.]oxazol-3-yl}-acetamide; 544. N-{5-phenylaminocarbonyl-4,6-dihydroindole 11 each [3,4 -c]吼° sit _3_基}-cyclopropanol; 545. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole- 3-based}-isobutylamine; 546. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]carbazole-3-indolyl}-cyclopentene Oreline; 547. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-benzamide; 548. N-{5 -phenylamine Carbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-mercaptopyridiniumamine; 549. N-{5-phenylaminomethyl-4,6- Dihydrogen D ratio slightly [3,4-c] π is more than 嗤3-3-}} in the amine; 550. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-〇]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第60頁 1327569 五 '發明說明（58) -3 -基卜異於驗醯胺； 551. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-3-曱基-2 -呋喃曱醯胺； 552. N-{5 -苯基胺基羰基_4,6 -二氫吡咯并[3,4-c]吡唑 _ 3 _基} _ D塞吩_ 2 _叛酿胺； 553. N-{5 -苯基胺基幾基-4，6_二氫吼17各并[3，4-c] °比〇坐 -3-基卜噻吩-3-羧醯胺； 554. N-{5 -苯基胺基羰基-4,6-二氫°比咯并[3,4-(：]吡唑 -3-基}-鄰-曱苯曱醯胺； 555. N-{5 -苯基胺基幾基- 4,6 -二氫吼11各并[3,4-c] °比°坐 -3-基}-間-曱苯甲醯胺； 556· N-{5 -苯基胺基獄基-4, 6 -二氫吼17各并[3,4-c] °比°坐 -3 -基}-對-曱苯甲醯胺； 557.1^-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-苯基乙醯胺； 55 8. N-{ 5 -苯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c]咄唑 -3 -基}-水楊酿胺； 559. N-{5 -苯基胺基羰基-4,6-二氫"比咯并[3,4-〇]°比唑 -3 -基}-2-氟苯甲酿胺； 560. N-{5 -苯基胺基幾基-4，6 -二氫吼11 各并[3,4-c] °比°坐 -3-基}-3-敗苯甲酿胺； 561. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基} -4-氟苯甲醯胺； 562. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 60 1327569 V'Inventive Description (58) -3 - kibdiamine valeramine; 551. N-{5-phenylaminocarbonyl-4 , 6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-indolyl-2-furaniumamine; 552. N-{5-phenylaminocarbonyl-4, 6-dihydropyrrolo[3,4-c]pyrazole _ 3 _ yl} _ D seleno _ 2 _ apoein; 553. N-{5-phenylamino group-4,6_2 Hydroquinone 17 each [3,4-c] ° 〇 -3- thiophene-3-carboxamide; 554. N-{5-phenylaminocarbonyl-4,6-dihydrogen ratio [3,4-(:]pyrazol-3-yl}-o-nonylphthalamide; 555. N-{5-phenylamino-yl- 4,6-dihydroindole 11 [3,4-c] ° ratio -3-yl}-m-benzamide; 556· N-{5-phenylamine-based prison-4,6-dihydroindole 17 each [ 3,4-c] ° ratio -3 -yl}-p-nonylbenzamide; 557.1^-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-( :]pyrazol-3-yl}-phenylacetamide; 55 8. N-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-c]carbazole-3 - aryl}-hydropenic amine; 559. N-{5-phenylaminocarbonyl-4,6-dihydro"bido[3,4-〇]°bizozol-3 -yl}-2 -Fluorobenzoic Amine; 560. N-{5-Phenylamino-yl-4,6-dihydroindole 11 each [3,4-c] °°--3-yl}-3-phenylene stearamide 561. N-{5-Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-fluorobenzamide; 562. N- {5-Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole

C:\2D-O0DE\91-01\9O119473.ptd 第61頁 1327569 五、發明說明（59) -3 -基}-噻吩-2-乙醯胺； 5 63. N-{5-苯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3 -基}-噻吩-3-乙醯胺； 564. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-苯基丙快酿胺； 565. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇:]吡唑 -3_基}-3_氮基苯曱酿胺； 5 6 6. N-{ 5-苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-氰基苯曱醯胺； _ 567. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基卜反-桂皮醯胺； 56 8. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3 -基}-順-桂皮醯胺； 569. N-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 _3 -基}_3-(3_ 0比。定基）丙稀酿胺； -570. N-{5 -苯基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑 -3 -基} - 3 - ( 4 -咄啶基）丙烯醯胺； 5 71. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 3-基}_2_苯基丙酿胺； 572. N-{5 -苯基胺基幾基-4, 6 -二氫吡ϋ各并[3, 4-c]吼嗤 -3 -基}-鄰-曱苯基乙醯胺； 573. Ν-{5-苯基胺基羰基-4,6-二氫吼咯并[3,4-〇:]吡唑 _3_基}-間-甲苯基乙酿胺； 574.1'1-{5-苯基胺基羰基-4,6-二氫吡11各并[3,4-(：]吡唑C:\2D-O0DE\91-01\9O119473.ptd Page 61 1327569 V. Description of the invention (59) -3 -yl}-thiophene-2-acetamide; 5 63. N-{5-phenylamine Alkylcarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-thiophene-3-acetamide; 564. N-{5-phenylaminocarbonyl-4,6 - dihydropyrrolo[3,4-c]pyrazol-3-yl}-phenylpropanol; 565. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-〇:]pyrazole-3-yl}-3_nitrobenzoquinone; 5 6 6. N-{ 5-phenylaminocarbonyl-4,6-dihydropyrrolo[3, 4 -c]pyrazol-3-yl}-4-cyanobenzoquinone; _ 567. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyridinium Azole-3 - kib-trans-cinnamate; 56 8. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]indazol-3-yl}-cis - cinnamylamine; 569. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}_3-(3-0 ratio. Propylene amine; -570. N-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-3-(4-pyrene) Pyridyl) acrylamide; 5 71. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_2_phenylpropane Amine; 572. N-{5-phenylaminomethyl-4,6-dihydropyridinium[3,4-c]indole-3-yl}-o-indolephenylacetamide; 573. Ν-{5-Phenylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl}-m-tolylylylamine; 574.1'1- {5-Phenylaminocarbonyl-4,6-dihydropyrrole 11 and [3,4-(:]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第62頁 1327569 五、發明說明（60) - 3 -基}-對-甲苯基乙醯胺； 5 7 5. N-{ 5-苯基胺基羰基-4, 6 -二氫》比咯并[3, 4-c]吡唑 _3-基}-鄰-菌香酿胺； 576. N-{5-苯基胺基羰基-4,6-二氮。比咯并[3,4-〇]°比唑 -3-基}-3-甲氧苯甲醯胺； 577. N-{5 -苯基胺基羰基-4, 6 -二氫D比p各并[3, 4-c] °比。坐 -3-基}-對-窗香酸胺； 578. N-{5-苯基胺基羰基- 4,6 -二氫。比11各并[3,4-c] ^比峻 _3_基}_苯氧乙酿胺； 579· N-{5-苯基胺基裁基- 4,6 -二氫°比°各并[3,4-c]吼°坐 -3-基}_2_說苯基乙酿胺； 580. N-{5-苯基胺基毅基- 4,6 -二氫°比嘻并[3,4-c] n比。坐苯基乙酿胺； 581. N_{5 -苯基胺基幾基-4，6 -二氳吼11 各并[3, 4-c] D比。坐 -3 -基}-4_氣苯基乙酿胺； 582. N-{5-苯基胺基戴基- 4,6 -二氫D比洛并[3,4-c]吼。坐 -3_基}_3_(2-°塞吩基）丙稀酿胺； 583. N-{5-苯基胺基幾基- 4,6 -二氫°比°各并[3,4-c]吼〇坐 _3_基}_3_(3_°塞吩基）丙稀酿胺； 584. N-{5-苯基胺基幾基- 4,6 -二氫吼11各并[3,4-c] °比〇坐 -3-基}-3-(2-噻吩基）丙醯胺； 585. N-{5 -苯基胺基裁基- 4,6 -二氫。比11 各并[3,4-c] D比0坐 _3-基}-2 -氯苯曱酿胺； 586. ^{5-苯基胺基幾基-4，6-二氫11比11各并[3,4-(：]°比11坐C:\2D-C0DE\91-01\90119473.ptd Page 62 1327569 V. INSTRUCTIONS (60) - 3 -yl}-p-tolylacetamide; 5 7 5. N-{ 5-phenyl Aminocarbonyl-4,6-dihydro"pyrolo[3,4-c]pyrazole-3-yl}-ortho-bacteria; 576. N-{5-phenylaminocarbonyl-4 , 6-diaza. Bis-[3,4-〇]°boxazol-3-yl}-3-methoxybenzamide; 577. N-{5-phenylaminocarbonyl-4,6-dihydro D ratio p Each [3, 4-c] ° ratio. Sodium-3-yl}-p-cosmic acid amine; 578. N-{5-phenylaminocarbonyl-4,6-dihydrogen. Ratio of 11 [3,4-c] ^ than _ 3_ _ _ phenoxy ethoxylate; 579 · N-{5-phenylamino group - 4,6 - dihydrogen ° ° And [3,4-c]吼° sitting-3-yl}_2_ said phenylethylamine; 580. N-{5-phenylamino-yl- 4,6-dihydrogen 嘻[ 3,4-c] n ratio. Phenylbenzamine; 581. N_{5-Phenylamino-yl-4,6-diindole 11 each [3, 4-c] D ratio. Sodium-3 -yl}-4_ phenyl phenylacetamide; 582. N-{5-phenylaminodyl- 4,6-dihydro D-piro[3,4-c]indole. Sitting -3_yl}_3_(2-°secenyl) acrylamide; 583. N-{5-phenylamino-yl- 4,6-dihydrogen ratio °[3,4- c] 吼〇3_基}_3_(3_°塞基基) acrylamide; 584. N-{5-phenylamino-yl- 4,6-dihydroindole 11 each [3, 4-c] ° 〇-3-yl}-3-(2-thienyl)propanamine; 585. N-{5-phenylamino-based 4,6-dihydrogen. Ratio of 11 [3,4-c] D to 0 _3-yl}-2-chlorophenyl hydrazine; 586. ^{5-Phenylamino-based-4,6-dihydro-11 ratio 11 each [3,4-(:]° is sitting at 11

C:\2D-OODE\91-Ol\90119473.ptd 第63頁 1327569 五、發明說明（61) -3 -基}-3 -氣苯甲醯胺； 587. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基} -4-氣苯甲醯胺； 588. N-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基} - 1 -哌啶丙醯胺； 589. N-{5-笨基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吼唑 -3 -基}-2-乙醯基苯甲醯胺； .590. N-{5 -苯基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-4-乙醯基苯曱醯胺； _591.1^-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]咄唑 -3-基}-1-蔡曱酿胺； 592. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-2 -萘甲醯胺； 593. N-{5 -苯基胺基羰基-4,6 -二氫咣咯并[3,4-c]吡唑 _3_基}_3_苯甲酿基丙酿胺； 594. N-{5 -苯基胺基数基_4，6 -二氮吼11各并[3，4-c] D比0坐 -3_基}_4_乙酿胺基苯甲酿胺， 595.1'1-{5_苯基胺基羰基-4,6-二氫吡>1各并[3,4-(：]1?比〇坐二甲氧苯曱醢胺； 596. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吼唑 -3-基}-2,6 -二曱氧苯曱醯胺； 597. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3_基}_3，4_二曱氧苯曱酿胺， 598. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑C:\2D-OODE\91-Ol\90119473.ptd Page 63 1327569 V. INSTRUCTIONS (61) -3 -yl}-3 - gasbenzamide; 587. N-{5-phenylamino group Carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-oxabenzamide; 588. N-{5-phenylaminocarbonyl-4,6- Dihydropyrrolo[3,4-indolepyrazol-3-yl}-1 -piperidinepropanamine; 589. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]carbazole-3-yl}-2-ethinylbenzamide; .590. N-{5-phenylaminocarbonyl-4,6-dihydroindole[3, 4 -c]pyrazol-3-yl}-4-ethenylbenzamide; _591.1^-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-anthracene] Oxazol-3-yl}-1-cainine; 592. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl} -2 -naphthylamine; 593. N-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}_3_benzyl Acrylic amine; 594. N-{5-phenylamino group _4,6-diazaindole 11 each [3,4-c] D ratio 0 sitting -3_yl}_4_ethylamino benzene Artemisamine, 595.1'1-{5-phenylaminocarbonyl-4,6-dihydropyridin>1 each [3,4-(:]1? than benzoquinone; 596. Ν-{5-Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-2,6-dioxabenzoquinone; 597. Ν -{5-Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazole-3-yl}_3,4-dioxabenzoquinone, 598. Ν-{5 -phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole

C:\2D-CODE\91-01\90119473.ptd 第64頁 1327569 五、發明說明（62) -3-基}-3,5 -二曱氧苯曱醯胺； 599. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]。比唑 -3-基}-3-(2-噻吩甲醯基）-丙醯胺； 600. N-{5 -苯基胺基羰基-4, 6 -二氫吼13各并[3,4-c] °比唑 -3_基}_2_秦基乙酿胺； 6 01. N-{5 -苯基胺基羰基-4, 6 -二氫。比咯并[3, 4-c]吼唑 _3_基}_1-秦基乙酿胺； 602. N-{5 -苯基胺基羰基-4,6-二氫咄咯并[3,4-〇]咄唑 _3_基}_4-苯基苯甲酿胺； 603. N-{5-辛基胺基鑛基_4, 6_二氮°比°各并[3,4-c] 0比0坐 _ 3 -基}-乙酿胺； 604. N-{5-¥基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 _基}-環丙烧叛酿胺； 60 5. Ν·-{5-窄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-異丁醯胺； 606. Ν-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}-環戊烧叛醯·胺； 607. Ν-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 -3_基}_苯曱酿胺； 608. Ν-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]。比唑 -3 -基}-甲基吡啶甲醯胺； 609. Ν-{5-辛基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基}-菸鹼醯胺； 610· Ν-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑C:\2D-CODE\91-01\90119473.ptd Page 64 1327569 V. INSTRUCTIONS (62) -3-yl}-3,5-dioxabenzoylamine; 599. N-{5 - Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]. Biazo-3-yl}-3-(2-thienylmethyl)-propanamine; 600. N-{5-phenylaminocarbonyl-4,6-dihydroindole 13 each [3,4 -c] °Bizozol-3_yl}_2_Qinyl Ethylamine; 6 01. N-{5-Phenylaminocarbonyl-4,6-dihydrogen. Bis-[3,4-c]carbazole _3_yl}_1-methylglycolamine; 602. N-{5-phenylaminocarbonyl-4,6-dihydroindole[3, 4-〇]carbazole_3_yl}_4-phenylbenzamide; 603. N-{5-octylamine-based mineral base_4,6-diaza ratio °[3,4- c] 0 to 0 sitting _ 3 -yl}-ethylamine; 604. N-{5-¥ylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3 _ }--cyclopropanol; 4 5. Ν·-{5-narrowylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-isobutyl Indoleamine; 606. Ν-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}-cyclopentanthrene repellent amine; 607. Ν-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-indolylpyrazole-3-yl}_benzoquinone; 608. Ν-{5-benzylamine Alkylcarbonyl-4,6-dihydropyrrolo[3,4-(:].pyrazol-3-yl}-methylpyridinecarboxamide; 609. Ν-{5-octylaminocarbonyl-4, 6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-nicotinium amide; 610·Ν-{5-benzylaminocarbonyl-4,6-dihydroindole[ 3,4-〇]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第65頁 1327569 五、發明說明（63) _3_基}_異於驗S莲胺， 611. N-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-3-曱基-2 -呋喃曱醯胺； 612. N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑 _3-基}_°塞吩_2_缓醯胺； 613. N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-噻吩-3 -羧醯胺； 614. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基卜鄰-甲苯甲醯胺； ® 615. N-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑 _3_基}_間-曱苯曱酿胺， 616. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-對-曱苯曱醯胺； 617. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_水楊酿胺； 618. N-{5-苄基胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吡唑 _3_基}_2_敦苯曱蕴胺； 619. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 3_基}-3_敗苯曱酿胺； 620. N-{5-苄基胺基羰基-4,6-二氫咣咯并[3,4-〇:]吡唑 _3 -基}_4_氣苯甲酿胺； 621. N-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-噻吩-2-乙醯胺； 622. N-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 65 1327569 V. INSTRUCTIONS (63) _3_BASE}_ 于验莲胺, 611. N-{ 5-Benzylaminocarbonyl- 4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-mercapto-2-furanamine; 612. N-{5-benzylaminocarbonyl-4, 6-dihydropyrrolo[3,4-c]carbazole-3-yl}_°Cetene-2_retinamide; 613. N-{5-benzylaminocarbonyl-4,6-dihydrogen Pyrrolo[3,4-c]pyrazol-3-yl}-thiophene-3-carboxycarboxamide; 614. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4 -(:]pyrazol-3-yl-o-tolylamine; ® 615. N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyridyl Azole_3_yl}-m-indole benzoic acid, 616. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl }-p-nonylbenzamide; 617. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazole-3-yl}} 618. N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}_2_dendrazin; 619. N-{ 5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazole-3-yl}-3-benzophenone; 620. N-{5-benzylaminocarbonyl -4,6- Hydroquinone [3,4-〇:]pyrazole-3-yl}_4_ gas benzoylamine; 621. N-{ 5-benzylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-thiophene-2-acetamide; 622. N-{ 5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyridinium Azole

C:\2D-OODE\91-Ol\90119473.ptd 第66頁 1327569 五、發明說明（64) _3_基}_°塞吩-3_乙酿胺； 623. N-{5-辛基胺基叛基_4，6 -二氮吼17各弁[3，4-c] °比0坐 _3_基}-苯基丙快酿胺； 624. [{5-亨基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}_3-氮基苯甲驢胺； 625. N-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}-4 -氮基苯甲酿胺； 626. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-〇]咣唑 -3-基卜反-桂皮醯胺； 627.1^{5-芊基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 -3 -基}-順-桂皮醯胺； 628· N-{5-苄基胺基羰基-4,6-二氫吼咯并[3,4-(：]吡唑 _3_基}-3-(3-11比咬基）丙稀酿胺； 629. N-{5-苄基胺基羰基-4,6-二氫吼咯并[3,4-〇]吡唑 _3_基}-3_(4_°比°定基）丙稀酿胺； 630. N-{5-苄基胺基羰基-4,6-二氫吼咯并[3,4-〇]吼唑 _3_基}_2-苯基丙酿胺； 631. N_{5_窄基胺基獄基_4，6_二氫吼1^各并[3,4_c] °比〇坐 _3_基}_鄰-曱苯基乙酿胺； 632. N-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-〇:]吡唑 _3_基}_間-甲苯基乙酿胺； 633. N-{5-苄基胺基羰基_4,6_二氫吡咯并[3,4-c]吡唑 _3_基}_對-曱苯基乙酿胺； 634. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑C:\2D-OODE\91-Ol\90119473.ptd Page 66 1327569 V. INSTRUCTIONS (64) _3_BASE}_°Cetamine-3_Ethylamine; 623. N-{5-octylamine Baseline _4,6-diazepine 17 弁[3,4-c] ° than 0 _3_ yl}-phenylpropanol; 624. [{5-Henylaminocarbonyl- 4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}_3-nitrobenzamide; 625. N-{5-decylaminocarbonyl-4,6-di Hydropyrrolo[3,4-(:]pyrazole-3-yl}-4-azabenzamide; 626. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[ 3,4-〇]carbazole-3-kib-trans-cinnamate; 627.1^{5-decylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3 -yl}-cis-cinnamate; 628· N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazole-3-yl}-3- (3-11 than bite base) acrylamide; 629. N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl}- 3_(4_°°° base) acrylamide; 630. N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]carbazole_3_yl}_2 -Phenylpropanol; 631. N_{5_Narrow-based amine-based prison base_4,6-dihydroindole 1^ each [3,4_c] ° than 〇3_基}_o- benzene Ethylamine 632. N-{5-Benzylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl}-m-tolylyl-brontan; 633. N- {5-Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-p-indolephenylethylamine; 634. N-{5-benzyl Aminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第 67 頁 1327569 五、發明說明（65) -3 -基}-鄰-茴香醯胺； 635. N-{5-辛基胺基羰基-4,6-二氫吡咯并[3,4-(：]咄唑 -3-基}-3-曱氧苯曱醯胺； 636. N-{5-辛基胺基獄基-4，6 -二氮13比0各并[3，4-c] 17比。坐 -3 -基}-對-茴香醯胺； 637· N-{5-苄基胺基幾基- 4，6 -二氫吼。各并[3,4-c]吼〇坐 -3_基}_笨氧乙酿胺； 638. N-{5-笮基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}~*2_氣苯基乙酷胺； ® 639. N-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-〇:]吡唑 _3-基}-3-氟苯基乙酿胺； 640. N-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑苯基乙酿胺； 641. N-{5-亨基胺基截基-4，6_二氫D比p各并[3，4-c] °比°坐 _3_基}_3_(2-°塞吩基）丙稀酿胺； 642· .N-{5-罕基胺基叛基-4，6 -二氫吼*1 各并[3，4-c] D比0坐 _3_基}-3_(3_°塞吩基）丙稀酿胺； 643. N-{5 -苄基胺基獄基- 4,6 -二氫吼11各并[3,4-c] °比〇坐 3-基}-3_(2-。塞11分基）丙酿胺； 644. N-{5-窄基胺基鑛基- 4,6 -二氫°比°各并[3,4-c] D比嗅 _3-基}-2_氣苯曱酿胺； 645.1^-{5-苄基胺基獄基-4，6-二氫〇比17各并[3,4-(：]'1比。圭 _3-基}-3-氯苯甲酿胺； 646. N-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 67 1327569 V. INSTRUCTIONS (65) -3 -yl}-o-anisoleamine; 635. N-{5-octylaminocarbonyl- 4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-3-indolephthalamide; 636. N-{5-octylamine-based prison-4,6 - dinitrogen 13 to 0 each and [3,4-c] 17 ratio. sitting -3 -yl}-p-anisylamine; 637 · N-{5-benzylamino group - 4,6 - two Hydroquinone. Each [3,4-c] stilbene-3_yl}- oxohydroethene; 638. N-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-(:]pyrazol-3-yl}~*2_qiphenylethylamine; ® 639. N-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4 -〇:]pyrazole-3-yl}-3-fluorophenylethylamine; 640. N-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4-indole]pyridinium Oxazol phenylethylamine; 641. N-{5-Hexylamine-based cleaving-4,6-dihydrogen D ratio p and [3,4-c] ° ratio ° _3_基}_3_( 2-°Septyl)propanolamine; 642· .N-{5-罕基胺基基基-4,6-dihydroanthracene*1 Each [3,4-c] D is 0 _ 3_基}-3_(3_°secenyl) acrylamide; 643. N-{5-benzylamine-based prison- 4,6-dihydroindole 11 each [3,4-c] ° Than sitting on 3-base}- 3_(2-. plug 11 base) propylamine; 644. N-{5-narrow-based amine-based group - 4,6-dihydrogen ratio °[3,4-c] D ratio sniffing 3-yl}-2_ gas benzoquinone; 645.1^-{5-benzylamine-prison-4,6-dihydroindole ratio 17 and [3,4-(:]'1 ratio. _3-yl}-3-chlorobenzamide; 646. N-{ 5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第68頁 1327569 五、發明說明（66) _3-基}-4-氯苯曱醯胺； 647. N-{5-辛基胺基幾基_4，6_二氫°比0各并[3，4_c]吼0坐 -3 -基卜卜哌啶丙醯胺； 648. N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_2_乙蕴基苯甲酿胺； 649. N-{5-芊基胺基羰基-4,6-二氫吼咯并[3,4-(：]咄唑 _3-基}_4_乙酿基苯曱酿胺； 650. N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基} - ：!-萘曱醯胺； 651. N-{5-窄基胺基羰基-4,6-二氫咣咯并[3,4-〇]吡唑 -3 -基} - 2 -萘甲醯胺； 652. N-{5-芊基胺基羰基-4,6-二氫吼咯并[3,4-〇]吼唑 _3-基}_3 -苯曱酿基丙酿胺； 653. N-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-〇]°比唑 -3-基}_4_乙酿胺基苯曱臨胺； 654. N-{5-芊基胺基叛基-4，6 -二氫吼11 各并[3，4-c] °比。坐 _3-基}_2，5_二曱氧苯甲酸胺； 655. N-{5-苄基胺基幾基-4, 6 -二氫吼11 各并[3,4-c] °比0坐 _3_基}_2，6_二曱氣苯甲酿胺； 656. N-{5-苄基胺基叛基-4，6 -二氫〇比0各并[3，4-c] °比〇坐 -3-基}-3, 4-二曱氧苯甲醯胺； 657. N-{5-苄基胺基幾基-4, 6 -二氫吼°各并[3,4-c]。比哇 _3_基丨_3，5_二曱氧苯甲酿胺； 658. N-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 68 1327569 V. Description of the invention (66) _3-yl}-4-chlorobenzamide; 647. N-{5-octylamino group The ratio of _4,6_dihydrogen is 0 and each [3,4_c] 吼0 is 3--3-pibpiridinamide; 648. N-{5-benzylaminocarbonyl-4,6- Dihydropyrrolo[3,4-c]pyrazole-3-yl}_2-ethylidenebenzamide; 649. N-{5-decylaminocarbonyl-4,6-dihydroindole [3,4-(:]carbazole-3-yl}_4_ethyl phenyl benzoate; 650. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4 -(:]pyrazol-3-yl}-:!-naphthylamine; 651. N-{5-Narrow-based carbonyl-4,6-dihydroindolo[3,4-indole]pyridinium Oxazol-3-yl}-2-naphthylamine; 652. N-{5-decylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]carbazole-3-yl} _3 - Benzene aryl aryl amine; 653. N-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4-〇]°bazol-3-yl}_4_ Aminophenyl hydrazine amine; 654. N-{5-decylamino thiol-4,6-dihydroindole 11 each [3,4-c] ° ratio. sitting _3-yl}_2,5 _ Dioxabenzoic acid amine; 655. N-{5-benzylaminomethyl-4,6-dihydroindole 11 each [3,4-c] ° than 0 sitting _3_ base}_2, 6_ Helium benzoic acid; 656. N-{5-benzylamino-based defensyl-4,6-dihydroindole ratio 0 and [3,4-c] ° 〇-3-yl}-3 , 4-dioxabenzoguanamine; 657. N-{5-benzylaminomethyl-4,6-dihydroindole °[3,4-c]. Wow_3_ylindole _3,5_dioxabenzoylamine; 658. N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第69頁 1327569 五、發明說明（67) -3 -基}-3-(2-噻吩甲醯基）-丙醯胺； 659. N-{5 -苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}_2-秦基乙酿胺； 660. N-{5-芊基胺基羰基-4,6-二氫咄咯并[3,4-〇:]吡唑 _3_基}-1_秦基乙酸胺； 661. N-{5-芊基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑 _3_基}_4_苯基苯曱酿胺， 662. N-{5 -苯曱醯基胺基羰基-4,6-二氫"比咯并[3,4-(：] 吡唑-3-基}-乙醯胺； 663. N-{5_苯曱疏基胺基叛基_4，6 -二氮D比略并[3，4_c] 咄唑-3-基卜環丙烷羧醯胺； 664. N-{5 -苯甲酿基胺基獄基_4，6 -二氫D比略并[3，4-c] 口比唑-3 -基}_異丁醯胺； 665. N-{5 -苯甲醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] "比唑-3-基卜環戊烷羧醯胺； 666. N-{5 -苯曱醯基胺基羰基-4,6-二氫。比咯并[3,4-〇] 吡唑-3-基}-苯甲醯胺； 667. N-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇:] 丨•吡唑_ 3 -基}-甲基〇比啶甲醯胺； 668. N-{5 -苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-(：] 。比。坐-3 -基}-於驗醯胺； 669. N-{ 5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 〇比吐-3 -基}-異於驗酿胺； 670. N-{5 -苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-〇]C:\2D-C0DE\91-01\90119473.ptd Page 69 1327569 V. INSTRUCTIONS (67) -3 -yl}-3-(2-thienylmethyl)-propanamide; 659. N- {5-Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}_2-methylideneamine; 660. N-{5-decylamine Alkylcarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl}-1-methylglycolic acid amine; 661. N-{5-decylaminocarbonyl-4, 6-Dihydroindolo[3,4-(:]pyrazole-3-yl}_4_phenylbenzoquinone, 662. N-{5-benzoylaminocarbonyl-4,6- Dihydro"pyrolo[3,4-(:]pyrazol-3-yl}-acetamide; 663. N-{5_benzoquinone-based thiol-4,6-diaza D略略和[3,4_c] oxazol-3-ylcyclopropanecarboxamide; 664. N-{5-benzamide-based phenyl group 4,6-dihydrogen D ratio slightly [3, 4-c] Oroxazol-3 -yl}-isobutylamine; 665. N-{5-Benzyldecylaminocarbonyl-4,6-dihydropyrrolo[3,4-c] " Bisazo-3-ylbucyclopentane carboxamide; 666. N-{5-phenylhydrazinocarbonyl-4,6-dihydro.pyrolo[3,4-indole]pyrazole-3 -yl}-benzamide; 667. N-{5-benzhydrylaminocarbonyl-4,6-dihydropyrrolo[3,4-indole:]pyrazole-3 -yl}-methylpyridinium carbamide; 668. N-{5-benzhydrylaminocarbonyl-4,6-dihydroindole[3,4-(:]. 3 -yl}-in the case of decylamine; 669. N-{ 5 -benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyridylpyr-3-yl}-iso EST. 670. N-{5-benzhydrylaminocarbonyl-4,6-dihydroindolo[3,4-anthracene]

C:\2D-CODE\91-01\90119473.ptd 第70頁 1327569 五、發明說明（68) 吡唑-3 -基} - 3 -曱基-2 -呋喃曱醯胺； 671. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3,4-c] 吡唑-3-基}-噻吩-2-羧醯胺； 672. N-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-(：] π比°坐-3 -基} - °塞吩_ 3 _缓酿胺； 673. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c] 吼唑-3 -基}-鄰-甲苯甲醯胺； 674. N-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吼唑-3-基}-間-曱苯曱醯胺； 675. N-{5 -苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-〇] 。比唑-3 -基}-對-甲苯曱醯胺； 676. N-{5 -苯曱醯基胺基羰基-4, 6-二氫吡咯并[3,4-c] 吡唑-3-基}-苯基乙醯胺； 677. N-{5_苯曱酿基胺基幾基_4，6_二氮°比0各弁[3，4_c] 0比°坐-3 _基} _水楊酿胺； 678. N-{5 -苯曱酿基胺基幾基-4，6 -二氫°比咯并[3，4-c] 。比唑-3 -基} - 2 -氟苯甲醯胺； 679. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇:] 吡唑-3-基}-3-氟苯曱醯胺； 680. N_{5_苯曱酿基胺基截基- 4，6_二氮0比σ各弁[3，4-c] 吡唑-3-基}_4-氟苯甲醯胺； 681. N-{5_苯曱酿基胺基截基_4，6_二氮比略弁[3，4-c] 。比唾-3 -基} - °塞吩-2 -乙醯胺； 682. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇]C:\2D-CODE\91-01\90119473.ptd Page 70 1327569 V. INSTRUCTIONS (68) Pyrazol-3-yl}-3-indol-2-furanamine; 671. N-{ 5-Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-thiophene-2-carboxamide; 672. N-{5-benzoquinone Mercaptoalkylcarbonyl-4,6-dihydroindole[3,4-(:] π ratio ° sitting -3 -yl} - ° phenanthrene _ 3 _ slow-acting amine; 673. N-{5 - Benzoylaminocarbonyl-4,6-dihydroindolo[3,4-c]carbazole-3-yl}-o-tolylcarbamide; 674. N-{5-benzhydryl Aminocarbonyl-4,6-dihydropyrrolo[3,4-indole-3-oxazol-3-yl}-m-nonylphenylamine; 675. N-{5-phenylhydrazinocarbonyl- 4,6-dihydroindolo[3,4-indole].Bizozol-3-yl}-p-toluidine; 676. N-{5-benzoylaminocarbonyl-4, 6 -dihydropyrrolo[3,4-c]pyrazol-3-yl}-phenylacetamide; 677. N-{5_benzoquinoneamino group _4,6-diaza ratio 0弁[3,4_c] 0°°坐-3 _基} _水杨胺胺; 678. N-{5-Benzene arylamino group-4,6-dihydrogen ratio 3,4-c].Bizozol-3 -yl}-2-fluorobenzamide; 679. N-{5-benzoylaminocarbonyl-4,6- Dihydropyrrolo[3,4-anthracene]pyrazol-3-yl}-3-fluorobenzamide; 680. N_{5_benzoquinone-based amine- 4,6-diaza 0 σ[3,4-c]pyrazol-3-yl}_4-fluorobenzamide; 681. N-{5_benzoquinone-based amino group _4,6-diaza ratio弁[3,4-c]. than saliva-3 -yl}- °cephen-2-acetamide; 682. N-{5-benzoylaminocarbonyl-4,6-dihydropyrrole [3,4-〇]

C:\2D-O0DE\91-01\90119473.ptd 第71頁 1327569 五、發明說明（69) 吡唑-3 -基}-噻吩-3 -乙醯胺； 683. ^{5-苯曱醯基胺基羰基-4,6-二氫°比咯并[3,4-<:] 吼唑-3 -基}-苯基丙炔醯胺； 684. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3-基}-3_氰基苯曱醯胺； 685,1^-{5-苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-(：] 吡唑-3-基}-4-氰基苯甲醯胺； 686. N - {5_苯曱酿基胺基徵基-4,6 -二氫D比11 各并[3,4-c] 咄唑-3-基}-反-桂皮醯胺；泰687. N-{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-c] 口比唑-3 -基}-順-桂皮醯胺； 688. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基} - 3 - ( 3 -咄啶基）丙烯醯胺； 689. N-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-〇] 吡唑-3 -基} - 3 - ( 4 -吡啶基）丙烯醯胺； 690. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 吡唑-3_基}-2-苯基丙醯胺； 691. N-{5_苯曱酿基胺基叛基_4，6_二氮吼17各并[3，4_c] •吡唑-3 -基}-鄰-甲苯基乙醯胺； 692. N-{5 -苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-(：] 11比σ坐-3 _基} _間-曱苯基乙酿胺； 693. Ν-{5 -苯曱醯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c] 。比唑-3-基}-對-曱苯基乙醯胺； 694. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇]C:\2D-O0DE\91-01\90119473.ptd Page 71 1327569 V. INSTRUCTIONS (69) Pyrazol-3-yl}-thiophene-3-acetamide; 683. ^{5-benzoquinone Aminocarbonyl-4,6-dihydropyrano[3,4-<:]carbazol-3-yl}-phenylpropynylamine; 684. N-{5-benzoinyl Aminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-cyanobenzoguanamine; 685,1^-{5-benzoguanamine Carbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-4-cyanobenzamide; 686. N - {5_benzoquinoneamino Significant-4,6-dihydrogen D ratio 11 and [3,4-c]oxazol-3-yl}-trans-cinsamine; 687. N-{5-benzoguanidinocarbonyl -4,6-dihydropyrrolo[3,4-c] oxazole-3-yl}-cis-cinnamate; 688. N-{5-benzoylaminocarbonyl-4,6- Dihydropyrrolo[3,4-indene]pyrazol-3-yl}-3-(3-oxalyl)propenylamine; 689. N-{5-phenylhydrazinocarbonyl-4,6 - dihydroindolo[3,4-indolyl]pyrazol-3-yl}-3-(4-pyridyl)propenylamine; 690. N-{5-benzoguanidinocarbonyl-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-phenylpropanamine; 691. N-{5_benzoquinone-based thiol _4,6_diazepine 17 and [3,4_c] •pyrazol-3-yl}-o-tolylacetamide; 692. N-{5-benzoylaminocarbonyl-4,6 - dihydroindolo[3,4-(:]11 than σ sitting-3-yl} _ m-indole phenylethylamine; 693. Ν-{5-phenylhydrazine carbonyl-4, 6-dihydroindolo[3,4-c].pyrazol-3-yl}-p-indole phenylacetamide; 694. Ν-{5-phenylhydrazinocarbonyl-4,6 -dihydropyrrolo[3,4-〇]

C:\2D-C0DE\91-01\90119473_ptd 第72頁 1327569 五、發明說明（70) 吡唑-3-基}-鄰-茴香醯胺； 695. N-{5 -苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-〇] 吡唑-3-基}-3-曱氧苯甲醯胺； 696. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫"比咯并[3,4-c] °比°坐-3 -基}-對-茴香醯胺； 697. N-{5 -苯曱酿基胺基幾基_4，6_二氫0比°各并[3，4-c] °比唑-3-基}-苯氧乙醯胺； 698. N-{5 -苯曱醯基胺基羰基-4,6-二氫°比咯并[3,4-〇] 咄唑-3-基}-2-氟苯基乙醯胺； 699. N-{5 -苯甲醢基胺基羰基-4,6-二氫吼咯并[3,4-〇] 吡唑-3-基}-3-氟苯基乙醯胺； 700. N_{5_苯甲酿基胺基獄基_4，6_二氮D比p各并[3，.4-c] 吡唑-3 _基} - 4 -氟苯基乙醯胺； 701. N-{5 -苯甲酿基胺基截基-4，6_二氮0比0各并[3，4-c] 吡唑-3 -基} - 3 - ( 2 -噻吩基）丙烯醯胺； 702. N-{5 -苯曱酿基胺基Μ基-4,6-二氫π比17各并[3,4-c] 吡唑-3 -基} - 3 - ( 3 -噻吩基）丙烯醯胺； 703. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3 -基} - 3 - ( 2 -噻吩基）丙醯胺； 704. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] "比唑-3-基}-2 -氯苯曱醯胺； 70 5. N-{5 -苯甲醯基胺基羰基-4, 6-二氫η比咯并[3, 4-c] 咄唑_3-基}-3 -氯苯曱醯胺； 706. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-叫C:\2D-C0DE\91-01\90119473_ptd Page 72 1327569 V. INSTRUCTIONS (70) Pyrazol-3-yl}-o-anisylamine; 695. N-{5-benzhydrylamino Carbonyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-3-indolylbenzamide; 696. N-{5-benzoguanidinocarbonyl- 4,6-dihydro"bi[3,4-c] ° ratio -3 -yl}-p-anisylamine; 697. N-{5-benzoquinoneamino group _ 4,6-dihydrogen 0 ratio °[3,4-c] ° oxazol-3-yl}-phenoxyacetamide; 698. N-{5-benzoguanamine carbonyl-4, 6-Dihydro-pyrolo[3,4-indole]oxazol-3-yl}-2-fluorophenylacetamidamine; 699. N-{5-benzhydrylaminocarbonyl-4,6 - dihydroindolo[3,4-indolyl]pyrazol-3-yl}-3-fluorophenylacetamidamine; 700. N_{5_benzylamine-based prison base_4,6_two The ratio of nitrogen to D is [3,.4-c]pyrazol-3-yl}-4-fluorophenylacetamide; 701. N-{5-benzamide-amino--4,6 _Dinitrogen 0 to 0 and [3,4-c]pyrazol-3-yl}-3-(2-thienyl)propenylamine; 702. N-{5-benzoquinone-based fluorenyl -4,6-dihydroπ ratio 17 and [3,4-c]pyrazol-3-yl}-3-(3-thienyl)propenylamine; 703. N-{5-benzene Mercaptoalkylcarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-(2-thiophenyl)propanamine; 704. N-{5 - Benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4-c] "pyrazol-3-yl}-2-chlorobenzoin; 70 5. N-{5-benzene Mercapto-aminocarbonyl-4,6-dihydro-n-pyrolo[3,4-c]carbazole-3-yl}-3-chlorobenzoin; 706. Ν-{5-benzamide Aminocarbonyl-4,6-dihydropyrrolo[3,4-called

C:\2D-C0DE\91-Ol\90119473.ptd 第73頁 1327569 五、發明說明（71) 吡唑-3 -基}-4-氯苯曱醯胺； 707. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 0比β坐-3 -基} -1 - °底σ定丙醯胺； 708. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-(：] 咄唑-3 -基} - 2 -乙醯基苯曱醯胺； 709. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基} - 4 -乙醯基苯曱醯胺； 710. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-(：] 比唑-3 -基} - 1 -萘甲醯胺；箏711. Ν-{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-。] 吡唑-3 -基} - 2 -萘甲醯胺； 712. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3 -基} - 3 -苯甲醯基丙醯胺； 713. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-〇] 吡唑-3 -基} - 4 -乙醯胺基苯曱醯胺； 714. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基卜2, 5 -二甲氧苯甲醯胺； 715. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 比唑-3-基}-2,6 -二曱氧苯曱醯胺； 716. Ν-{ 5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 吼唑-3-基}-3, 4 -二曱氧苯甲醯胺； 717. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基} - 3，5 -二甲氧苯曱醯胺； 718. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-〇]C:\2D-C0DE\91-Ol\90119473.ptd Page 73 1327569 V. Description of the invention (71) Pyrazole-3-yl}-4-chlorophenylamine; 707. N-{5-benzoquinone Mercaptoalkylcarbonyl-4,6-dihydropyrrolo[3,4-indene] 0 is more than β-s-yl}-1 - ° 醯醯醯醯 ;; 708. Ν-{5 - phenylhydrazine Mercaptoalkylcarbonyl-4,6-dihydroindolo[3,4-(:]carbazol-3-yl}-2-ethoxybenzamide; 709. Ν-{5-benzoquinone Mercaptoaminocarbonyl-4,6-dihydropyrrolo[3,4-indenepyrazol-3-yl}-4-ethoxybenzhydrylamine; 710. Ν-{5-benzhydryl Aminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-1 -naphthylcarboxamide; Zheng 711. Ν-{5-benzoguanamine Carbonyl-4,6-dihydropyrrolo[3,4-.]pyrazol-3-yl}-2-naphthylcarboxamide; 712. Ν-{5-benzoylaminocarbonyl-4,6 -dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-ylbenzhydrylpropionamide; 713. Ν-{5-benzoylaminocarbonyl-4,6- Dihydroindolo[3,4-indene]pyrazol-3-yl}-4-ethaneaminobenzamide; 714. Ν-{5-benzoylaminocarbonyl-4,6- Dihydropyrrolo[3,4-indolyl]pyrazole-3-yl b 2,5-dimethoxybenzamide; 715. Ν-{5 - Benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4-indole]biazol-3-yl}-2,6-dioxabenzoquinone; 716. Ν-{ 5 - Benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-3,4-dioxabenzoguanamine; 717. Ν-{5 - Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolepyrazol-3-yl}-3,5-dimethoxybenzamide; 718. Ν-{5 - Benzylaminocarbonyl-4,6-dihydroindolo[3,4-anthracene]

C:\2D-CODE\91-01\90119473.ptd 第74頁 1327569 五、發明說明（72) 吡唑-3 -基}-3-( 2 -噻吩甲醯基）-丙醯胺； 719. N-{5 -苯甲醯基胺基羰基-4, 6 -二氫咄咯并[3, 4-c] °比唑-3-基卜2-萘基乙醯胺； 7 20. N-{ 5 -苯甲醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 吡唑-3 -基} - ；1 -萘基乙醯胺； 721. N-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基} - 4 -苯基苯曱醯胺； 722.1^1-{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-乙醯胺； 723. N-{5_胺基叛基-4，6_二氮吼17各并[3，4_c]吼11坐- 3-基}-環丙烷羧醯胺； 724. N_{5_胺基幾基_4，6_二氮°比°各并[3，4_c] °比°坐- 3-基}-異丁醯胺； 725. N-{5 -胺基叛基_4，6 -二氮D比p各并[3，4-c]吼吐-3-基}-環戊烷羧醯胺； 726· N-{5_胺基幾基-4，6_二氫D比略并[3,4-c] °比°坐-3-基}-苯甲醯胺； 727. N_{5_ 胺基幾基_4，6_ 二氮 D比 17各弁[_3，4-c] B比。坐- 3-基}-甲基吼啶甲醯胺； 728· N-{5 -胺基獄基-4, 6 -二氫吼11 各并[3,4-c]吼°坐- 3-基}-於驗醯胺； 729.1{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}_異菸鹼醯胺； 730. N-{5_胺基幾基_4，6_二氮吼11 各并[3，4_c] °比°坐- 3-C:\2D-CODE\91-01\90119473.ptd Page 74 1327569 V. INSTRUCTIONS (72) Pyrazol-3-yl}-3-(2-thiophenanthryl)-propanamide; 719. N-{5-benzylidenylaminocarbonyl-4,6-dihydroindolo[3,4-c] °pyrazol-3-ylpy-2-naphthylacetamide; 7 20. N- {5-Benzyldecylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-;1-naphthylacetamide; 721. N-{5 - Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-indene]pyrazol-3-yl}-4-phenylphenylamine; 722.1^1-{5-aminocarbonyl -4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-acetamide; 723. N-{5-amino-based t-group-4,6-diazepine 17 And [3,4_c]吼11-sodium 3-yl}-cyclopropanecarboxamide; 724. N_{5_amino-based _4,6-diazepine ratio °[3,4_c] ° ratio ° sit-3-yl}-isobutylamine; 725. N-{5-amino-t-radyl-4,6-diaza D ratio p and [3,4-c]indole-3-yl} -cyclopentane carboxamide; 726· N-{5_amino-based-4,6-dihydrogen D ratio slightly [3,4-c] ° ratio sit-3-yl}-benzamide Amine; 727. N_{5_amino-based _4,6-dinitrogen D ratio 17 弁[_3,4-c] B ratio. Sodium-3-yl}-methyl acridine carbenamide; 728· N-{5-amino-p-phenyl-4,6-dihydroindole 11 each [3,4-c]吼°-3-yl}-in the case of the amine; 729.1{5-aminocarbonyl -4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-isonicotinamine amide; 730. N-{5-aminodoyl_4,6-diazaindole 11 each [3,4_c] ° ratio ° sitting - 3-

C:\2D-C0DE\91-Ol\90119473.ptd 第75頁 1327569 五、發明說明（73) 基} -3-曱基-2-呋喃甲醯胺； 731. N-{5 -胺基羰基- 4,6 -二氫°比°各并[3,4-c] D比。坐- 3-基} -11塞吩-2-缓酿胺； 732. ^{5-胺基羰基-4,6-二氫咄咯并[3,4-〇:]吡唑-3-基} - 17塞吩-3 _叛酿胺； 733. N-{5 -胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3-基卜鄰-甲苯曱醯胺； 734. N-{5 -胺基幾基-4，6 -二氫π比11 各并[3，4-c]吼°坐-3-基}-間-甲苯曱醯胺； • 735. N-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基卜對-曱苯曱醯胺； 736. N_{5 -胺基獄基_4，6_二氮吼0各弁[3,4-c] D比π坐-3_ 基}-苯基乙醯胺； 737. Ν-{5 -胺基幾基-4，6 -二氫D比ρ各并[3, 4-c] ρ比D坐-3-基}-水楊醯胺； 738. N_{5_胺基截基-4，6 -二氯π比p各并[3，4-c] π比。坐- 3-基丨-2-說苯曱蕴胺； 739. Ν-{5 -胺基截基-4，6 -二氫吼17各并[3，4-c] °比°坐- 3-氟苯甲醯胺； 740. N-{5 -胺基幾基-4，6 -二氫D比p各并[3，4-c] D比°坐- 3-基}-4-氟苯曱醯胺； 741. N-{5 -胺基獄基-4，6_二氮D比p各并[3，4_c] °比。坐_3_ 基卜噻吩-2-乙醯胺； 742. N-{5 -胺基羰基- 4,6 -二氫n比洛并[3,4-c] °比唾- 3-C:\2D-C0DE\91-Ol\90119473.ptd Page 75 1327569 V. INSTRUCTIONS (73) BASE -3-Mercapto-2-furancarboxamide; 731. N-{5-Aminocarbonyl - 4,6-dihydrogen ratio ° and [3,4-c] D ratio. Sodium-3-yl}-11-phene-2-lowering amine; 732. ^{5-Aminocarbonyl-4,6-dihydroindolo[3,4-anthracene]pyrazol-3-yl } - 17 phenophene-3 _ apoein; 733. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-ylbu-p-toluene Amine; 734. N-{5-amino-based-4,6-dihydroπ ratio 11 each [3,4-c] 坐坐-3-yl}-m-toluidine; N-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-ylbu-p-benzoquinone; 736. N_{5-amine prison Base _4,6_diazepine 0 弁[3,4-c] D is π sitting -3_yl}-phenyl acetamide; 737. Ν-{5-amino-based-4,6- Dihydrogen D ratio ρ and [3, 4-c] ρ ratio D sitting-3-yl}-salimentide; 738. N_{5_amino-based cleaving-4,6-dichloroπ ratio p And [3,4-c] π ratio. Sitting - 3-ylindole-2- benzoquinone; 739. Ν-{5-amino-based - 4,6-dihydroindole 17 each [3,4-c] °°° - 3 -Fluorobenzamide; 740. N-{5-amino-based-4,6-dihydro D ratio p and [3,4-c] D ratio °-3-yl}-4-fluoro Benzoylamine; 741. N-{5-amine-based Pegyl-4,6-dinitrogen D ratio p and [3,4_c] ° ratio. Sit _3_ thiophene-2-acetamide; 742. N-{5-aminocarbonyl- 4,6-dihydron-bi-l-[3,4-c] ° than saliva- 3-

C:\2D-C0DE\91-01\90119473.ptd 第76頁 1327569 五、發明說明（74) 基}-噻吩-3-乙醯胺； 743· N-{5 -胺基羰基-4, 6 -二氫吼17各并[3,4-c] D比。坐- 3- 基}-苯基丙炔醯胺； 744. N-{5 -胺基幾基-4，6 -二氫吼σ各并[3, 4-c] D比°坐-3-基}_3 -氰基苯曱酿胺； 745. N-{5 -胺基羰基-4, 6 -二氫吼p各并[3,4-c] °比°坐- 3-基}-4_氰基苯曱酿胺； 746. N_{5_胺基幾基-4, 6 -二氫D比B各并[3，4-c] °比°坐-3-基丨•反-桂皮酿胺； 747· N_{5 -胺基幾基_4，6_二氮D比11 各并[3，4-c] °比°坐_3- 基} _順-桂皮酿胺； 748.1'1_{5-胺基幾基_4，6-二氮11比'3各并[3，4_(3]1：1比51坐-3_ 基}_3_(3_51比°定基）丙稀酿胺； 749. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基}-3-(4 -吡啶基）丙烯醯胺； 750· N_{5_胺基幾基_4，6 -二氮。比17各弁[3，4-c] °比°坐-3_ 基}-2 -苯基丙醯胺； 751. N-{5 -胺基数基- 4,6 -二氫°比°各并[3,4-c] °比°坐- 3-基}-鄰-曱苯基乙醯胺； 752. N-{5 -胺基幾基- 4,6 -二氫°比°各并[3,4-c] 13比嗤- 3-基}-間-甲苯基乙醯胺； 753. N-{5 -胺基幾基_4，6 -二氫吼13各并[3,4-c] D比。坐- 3-基}-對-曱苯基乙醯胺； 754. N-{5 -胺基 Μ 基- 4,6 -二氫吼11各并[3,4-c] °比。坐- 3-C:\2D-C0DE\91-01\90119473.ptd Page 76 1327569 V. INSTRUCTIONS (74) BASE}-thiophene-3-acetamide; 743· N-{5-aminocarbonyl-4, 6 - Dihydroanthracene 17 each [3,4-c] D ratio. Sodium-3-yl}-phenylpropynylamine; 744. N-{5-amino-based-4,6-dihydroindole σ[3, 4-c] D ratio ° sitting-3- __3-cyanobenzoquinone; 745. N-{5-aminocarbonyl-4,6-dihydroindole p each [3,4-c] ° ratio sit--3-yl}-4 _ cyanobenzoquinone; 746. N_{5_amino-based 4-, 6-dihydro D ratio B and [3,4-c] ° ratio sit-3-yl 丨 • anti-cassia Amine amine; 747· N_{5-amino-based _4,6-dinitrogen D ratio 11 each [3,4-c] ° ratio _3-base} _ cis-cinnamamine; 748.1' 1_{5-amino-based _4,6-diaza 11 ratio '3 each [3,4_(3]1:1 ratio 51 sitting -3_ base}_3_(3_51 ratio ° base) acrylamide; 749. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-3-(4-pyridyl)propenylamine; 750·N_{ 5_Amino-based _4,6-diaza. Ratio of 17 弁[3,4-c] °°°-3_yl}-2-phenylpropanamide; 751. N-{5-amine Base group - 4,6-dihydrogen ratio °[3,4-c] ° ratio -3 -yl}-o-indole phenylacetamide; 752. N-{5-amino group - 4,6 - dihydrogen ° ° each [3,4-c] 13 than 嗤-3-yl}-m-tolyl acetamide; 753. N-{5-amino group _4 , 6-dihydroanthracene 13 [3,4-c] D ratio. Sodium 3-yl}-p-indole phenylacetamide; 754. N-{5-aminoindolyl-4,6-dihydroindole 11 each [3 , 4-c] ° ratio. Sitting - 3-

C:\2D-C0DE\91-01\90119473.ptd 第77頁 1327569 五、發明說明（75) 基卜鄰-茴香醯胺； 7 5 5. N-{ 5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c] π比唑-3- 基}-3-曱氧苯曱醯胺； 756. Ν-{5 -胺基数基-4，6 -二氫D比ρ各并[3，4-c] °比°坐- 3-基卜對-茴香醯胺； 757.1^-{5-胺基截基-4，6-二氫吼1}各并[3，4-(：]11比°坐-3-基}-苯氧乙醯胺； 758. Ν-{5 -胺基叛基-4，6-二氫吼。各并[3，4-c] π比°坐-3-基}-2-氟苯基乙醯胺； 759. Ν-{5 -胺基截基-4，6 -二氫 11 比 0各并[3, 4-c] °比。坐-3-基}-3-氟苯基乙醯胺； 760. Ν_{5_胺基幾基_4，6_二氮11比ρ各并[3，4-c] D比π坐- 3-基} -4-氟苯基乙醯胺； 761. Ν-{5 -胺基幾基-4，6 -二氮°比ρ各并[3.，4_c] D比。坐- 3-基}-3-(2-11塞吩基）丙稀酿胺； 762. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3_ 基}-3-(3-噻吩基）丙烯醯胺； 763· N-{5 -胺基幾基-4，6 -二氮吼13各并[3，4-c] °比。坐- 3-|基}-3-(2-°塞吩基）丙醯胺； 764. N-{5 -胺基幾基-4，6_二氫°比p各并[3，4-c]吼°坐-3-基}-2 -氣苯曱酿胺； 765. N-{5 -胺基裁基-4，6 -二氯吼1*各并[3，4-c] π比°坐- 3-基}_3-氣苯曱酿胺； 766. Ν-{5 -胺基幾基-4，6 -二氫°比°各并[3，4-c] D比D坐- 3-C:\2D-C0DE\91-01\90119473.ptd Page 77 1327569 V. INSTRUCTIONS (75) Keb o-anisamide; 7 5 5. N-{ 5 -aminocarbonyl-4, 6 - Dihydroindolo[3,4-c] π-pyrazol-3-yl}-3-oxobenzoquinone; 756. Ν-{5-amino-based-4,6-dihydro-D ratio ρ Each [3,4-c] ° ratio sits - 3-kib-p-anisamine; 757.1^-{5-amino-based -4,6-dihydroanthracene 1} each [3,4 -(:]11°°-3-yl}-phenoxyacetamide; 758. Ν-{5-amino thio- 4,6-dihydroindole. each [3,4-c] π Ratio °-3-yl}-2-fluorophenylacetamide; 759. Ν-{5-amino-based cleaving-4,6-dihydrogen 11 to 0 and [3, 4-c] ° ratio坐-3-yl}-3-fluorophenylacetamide; 760. Ν_{5_amino-based _4,6-dinitrogen 11 ratio ρ and [3,4-c] D than π 3- 3-yl}-4-fluorophenylacetamide; 761. Ν-{5-amino-based-4,6-diaza ratio ρ and [3.,4_c] D ratio. Sit - 3 -yl}-3-(2-11-thenyl)propanolamine; 762. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl }-3-(3-thienyl)propenylamine; 763· N-{5-amino-based-4,6-diazaindole 13 each [3,4-c] ° ratio. Sitting - 3- |基}-3-(2 -°Cenyl)propanamide; 764. N-{5-amino-based-4,6-dihydrogen ratio p and [3,4-c]吼°-3-yl}-2 - gas benzoquinone; 765. N-{5-amino-based 4,6-dichloroindole 1* each [3,4-c] π ratio ° sitting - 3-yl}_3-benzene Brewing amine; 766. Ν-{5-amino benzyl-4,6-dihydrogen ratio °[3,4-c] D ratio D sitting - 3-

C: \2D-00DE\91-01\90119473.ptd 第78頁 1327569 五、發明說明（76) 基}-4 -氯苯甲醯胺； 767. ^{5-胺基羰基-4,6-二氫吡咯并[3,4-叫吡唑-3-基} - 1 -哌啶丙醯胺； 768. N_{5_胺基叛基_4，6_二氮D比p各弁[3，4_c] π比。坐- 3-基}-2-乙醯基苯曱醯胺； 769.1'1-{5-胺基叛基_4，6-二氫11比洛并[3,4-〇]11比°坐-3-基}-4-乙醯基苯曱醯胺； 770. Ν-{5 -胺基羰基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}_l_蔡曱酿胺； 771. Ν-{5 -胺基幾基- 4,6 -二氫吼11各并[3,4-c] β比唾- 3-基}-2 -萘曱醯胺； 772. Ν-{5 -胺基幾基-4，6 -二氫D比π各并[3, 4-c]吼嗤- 3-基}-3 -苯甲醯基丙醯胺； 773. Ν-{5 -胺基叛基- 4,6 -二氯吼13各并[3，4-c] D比°坐-3-基}-4-乙醯胺基苯甲醯胺； 774. N-{5 -胺基截基-4，6_二氮D比17各并[3，4-c] B比唾- 3-基}-2, 5-二曱氧苯甲醯胺； 775. N-{5 -胺基羰基-4, 6 -二氫吼11 各并[3, 4-c] 17比唾- 3-基}-2,6 -二曱氧苯曱醯胺； 776_^{5-胺基叛基-4，6-二氫吼洛并[3,4-〇]11比°坐-3-基}-3, 4-二曱氧苯甲醯胺； 777. N_{5_胺基幾基-4, 6_二氫吼17各并[3，4-c] π比β坐-3-基}-3, 5-二曱氧苯甲醯胺； 778. Ν-{5 -胺基幾基-4，6_二氫°比0各并[3，4**c] °比。坐- 3-C: \2D-00DE\91-01\90119473.ptd Page 78 1327569 V. Description of the invention (76) yl}-4-chlorobenzamide; 767. ^{5-Aminocarbonyl-4,6- Dihydropyrrolo[3,4-pyrazol-3-yl}-1 -piperidinepropanamine; 768. N_{5_Amino-based defensyl-4,6-diaza D ratio p弁[3 , 4_c] π ratio. Sodium 3-yl}-2-ethylmercaptobenzamine; 769.1'1-{5-amino-based thiol-4,6-dihydro- 11 bis-[3,4-〇]11 -3-yl}-4-ethylmercaptobenzamine; 770. Ν-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl} _l_蔡曱胺胺; 771. Ν-{5-amino-based- 4,6-dihydroindole 11 and [3,4-c] β-pyria-3-yl}-2-naphthoquinone Amine; 772. Ν-{5-amino-based-4,6-dihydro D ratio π-[3,4-c]吼嗤-3-yl}-3-benzhydryl propylamine; 773. Ν-{5-amino-based thio- 4,6-dichloroindole 13 and [3,4-c] D ratio °-3-yl}-4-acetamidobenzamide; 774. N-{5-amino-inter)-4,6-diaza D ratio 17 and [3,4-c] B than sal-3-yl}-2, 5-dioxabenzoguanamine 775. N-{5-aminocarbonyl-4,6-dihydroindole 11 each [3,4-c] 17-pyran-3-yl}-2,6-dioxabenzoylamine; 776_^{5-Amino-Rexyl-4,6-dihydroindolo[3,4-indenyl]11-pyridin-3-yl}-3,4-dioxabenzoguanamine; 777. N_{5-amino-based group-4,6-dihydroindole 17 and [3,4-c] π ratio β-s--3-yl}-3, 5-dioxalylbenzamide; 778. Ν-{5-aminol group-4,6-dihydrogen ratio 0 and [3,4**c] ° ratio. Sitting - 3-

C:\2D-00DE\91-01\90119473.ptd 第79頁 1327569 五、發明說明（77) 基}-3-(2 -噻吩曱醯基）-丙醯胺； 779. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}_2_秦基乙酿胺， 7 80. N-{ 5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基}_1_秦基乙酿胺， 781. Ν-·{5 -胺基羰基- 4,6 -二氫D比咯并[3,4-c]吼°坐- 3- 基} -4 -苯基苯曱醯胺； 7 8 2. N - { 5 -胺基石黃醯基-4, 6 -二氫°比D各并[3, 4 - c ] °比°坐 -3_基}_乙酿胺， • 783. N-{5 -胺基續臨基-4,6-二氫吼°各并[3,4-〇:]°比口坐 -3 _基} _環丙烧叛酿胺； 7 8 4 · N - { 5 -胺基績醯基-4，6 _二氫°比p各并[3，4 - c ] °比。坐 _3-基}_異丁酿胺； 785. N_{5_胺基石黃酿基_4，6_二氮B比略弁[3，4-c]。比〇坐 -基}_環戊烧叛酿胺； 7 8 6 . N - { 5 -胺基續醯基-4, 6 -二氫D比咯并[3，4 - c ] °比。坐 _3_基}_苯曱酿胺， 787. N-{5 -胺基續醯基- 4,6 -二氫°比°各并[3,4-c]"比〇坐彳I- 3 -基}-曱基吡啶曱醯胺； 788. N-{5 -胺基磺醯基-4,6-二氫咄咯并[3,4-〇]°比唑 -3_基}-於驗酿胺； 789. N-{5 -胺基續醯基-4, 6 -二氫吼17各并[3, 4-c]吼°坐 _3 -基}_異於驗酿胺； 790· N-{5 -胺基磺醯基-4,6 -二氫咄咯并[3,4-c]咄唑C:\2D-00DE\91-01\90119473.ptd Page 79 1327569 V. INSTRUCTIONS (77) yl}-3-(2-thiophenanthryl)-propanamide; 779. N-{5 - Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}_2-methylglycolamine, 7 80. N-{5-aminocarbonyl-4,6- Dihydropyrrolo[3,4-c]pyrazol-3-yl}_1-methylglycolamine, 781. Ν-·{5-aminocarbonyl- 4,6-dihydro D ratio 咯[3 , 4-c] 吼 ° sits - 3-yl} -4 -phenylbenzoguanamine; 7 8 2. N - { 5 -aminophthalazinyl-4,6-dihydrogen ratio D and [3, 4 - c ] ° ratio ° -3 - base} - ethylamine, • 783. N-{5 -Amino-based imyl-4,6-dihydroanthracene [3,4-〇:] ° than the mouth sitting -3 _ _} _ Cyclopropyl burnt amine; 7 8 4 · N - { 5 - Amino thiol-4,6 _ dihydrogen ratio p and [3,4 - c ] ° ratio. Sit _3-yl}_isobutylenamine; 785. N_{5_amine stone yellow wine base_4,6_diaza B ratio slightly [3,4-c]. 〇 - - 基}_cyclopentan-burning amine; 7 8 6 . N - { 5 -amino sulfonyl-4,6-dihydro D than octoh [3,4 - c ] ° ratio. Sit _3_基}_Benzene amide, 787. N-{5-Amino thiol- 4,6-dihydrogen ratio °[3,4-c]"Comparative 彳I - 3 -yl}-decylpyridinium; 788. N-{5-aminosulfonyl-4,6-dihydroindolo[3,4-indole]pyrazole-3_yl} - in the test of amine; 789. N-{5-amino sulfhydryl-4,6-dihydroindole 17 and [3, 4-c] 吼 ° _3 - yl} _ different from the amine 790· N-{5-Aminosulfonyl-4,6-dihydroindolo[3,4-c]carbazole

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A 1327569 五、發明說明（78) -3-基}-3-甲基-2-呋喃曱醯胺； 791. N-{5 -胺基續醯基- 4,6 -二氫°比°各并[3,4-c] D比。坐 -3 -基}-噻吩-2 -羧醯胺； 792.1{5-胺基罐醯基-4,6-二氮吼11各并[3,4-〇]吼〇坐 _3-基}-°塞吩_3_綾酿胺； 793. N-{5 -胺基績醯基- 4,6 -二氫°比嘻并[3,4-c] 11比唆 -3 -基}-鄰-甲苯甲醯胺； 794.1^-{5-胺基續醯基-4,6-二氫°比'1各并[3,4-(：]°比唑 _3_基}_間-甲苯甲酿胺；A 1327569 V. Description of the invention (78) -3-yl}-3-methyl-2-furanium amide; 791. N-{5-aminol-decyl- 4,6-dihydrogen ratio And [3,4-c] D ratio. -3 -yl}-thiophene-2-carboxycarboxamide; 792.1{5-amine-based cans-4,6-diazaindole 11 and [3,4-〇]吼〇__yl} - ° 吩 _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _. O-toluamylamine; 794.1^-{5-amino sulfonyl-4,6-dihydrogen ratio '1 each [3,4-(:]° azole _3_ yl}}- Toluene

795. N-{5 -胺基績醯基-4,6-二氫°比洛并[3,4-c] °比唑 -3-基}-對-甲苯曱醯胺； 796.1'1_{5-胺基項醯基-4,6-二氫11比洛并[3,4-(：]11比。坐 _3_基}-苯基乙酿胺； 797. N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}_水揚酿胺； 798. N-{5 -胺基續酿基- 4,6 -二氫吼17各并[3,4-c] 17比0坐 _3-基}-2-氟苯曱酿胺；795. N-{5-Amino-alkyl-4,6-dihydro-pyrolo[3,4-c] °biazol-3-yl}-p-toluidine; 796.1'1_{ 5-amino group fluorenyl-4,6-dihydro 11 piroxi[3,4-(:]11 ratio. sitting _3_yl}-phenylethylamine; 797. N-{5-amine Alkyl sulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}-hydrogen amine; 798. N-{5-amino aryl- 4,6 - indoline 17 and [3,4-c] 17 to 0 sit _3-yl}-2-fluorobenzoquinone;

799. N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3-基}-3-氣苯曱醢胺； 800. N-{5 -胺基續酿基- 4,6 -二氫π比B各并[3,4-c] °比唑 _3_基}-4_氟苯甲酿胺； 801. N-{5 -胺基績S篮基- 4,6 -二氫吼17各并[3,4-c] °比唑 -3-基}-噻吩-2-乙醯胺； 8〇2.1^-{5-胺基續醋基-4,6-二氫吡0各并[3,4-(：]°比唑799. N-{5-Aminosulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}-3-phenanthridine; 800. N-{ 5-Amino aryl-based 4,6-dihydro π ratio B and [3,4-c] ° azole -3-yl}-4 fluorobenzamide; 801. N-{5 - Amine based S basket - 4,6-dihydroindole 17 each [3,4-c] ° oxazol-3-yl}-thiophene-2-acetamide; 8〇2.1^-{5-amine Continuation of vinegar-4,6-dihydropyridinium each [3,4-(:]° azole

C:\2D-G0DE\91-01\90119473.ptd 第81頁 1327569 五、發明說明（79) -3 -基}_D塞吩-3-乙蕴胺； 803. N-{5 -胺基磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑 _3_基}_苯基丙快酿胺， 804. N-{5 -胺基項醢基- 4,6 -二氫°比°各并[3,4-c] B比。坐 -3-基}-3-氰基苯曱醯胺； 805. N_{5_胺基項酿基- 4,6 -二氫°比0各并[3，4-c] °比°坐 -3-基}-4-氰基苯曱醯胺； 806. N_{5_胺基續酿基_4，6_二氮°比洛弁[3，4_c] D比。坐 -3-基}-反-桂皮醯胺；鲁807.1^-{5-胺基續醯基-4,6-二氫吼洛并[3,4-。]吼唾 - 3 _基}-順-桂皮酿胺； 808. N-{5 -胺基續醢基-4,6 -二氫吼11 各并[3，4-c] °比°坐 -3_基}_3_(3_ β比π定基）丙稀酿胺； 809. Ν_{5 -胺基項基-4，6 -二氣Β比11 各并[3，4-c] D比0坐 -3-基}-3-(4 -吡啶基）丙烯醯胺； 810.1{5-胺基項酿基-4,6-二氫吼11各并[3,4-(：]°比。坐 -3_基}_2_苯基丙酿胺； 8 1 1 · N - { 5 -胺基續醯基-4，6 -二氫吼13各并[3，4 - c ] D比0坐 13 -基}-鄰-曱苯基乙醯胺； 8 1 2. N - { 5 -胺基石黃醯基-4, 6 -二氫°比p各并[3，4 - c ] °比〇坐 -3_基}_間-甲苯基乙酿胺； 813. N-{5 -胺基續醯基-4，6 -二氫°比p各并[3，4-c] °比°坐 -3 -基}-對-曱苯基乙醯胺； 814. N-{5 -胺基續醯基-4，6 -二氫π比p各并[3，4-c]吼〇坐C:\2D-G0DE\91-01\90119473.ptd Page 81 1327569 V. Description of the invention (79) -3 -yl}_D-cetin-3-ethylamine; 803. N-{5-aminosulfonate Mercapto-4,6-dihydroindolo[3,4-(:]pyrazole-3-yl}}phenylpropanol, 804. N-{5-amine-based fluorenyl- 4, 6-Dihydrogen ratio °[3,4-c] B ratio. Sodium-3-yl}-3-cyanobenzoquinone; 805. N_{5_Amine-based base - 4,6 - dihydrogen ratio of 0 and [3,4-c] ° ratio of s--3-yl}-4-cyanobenzoquinone; 806. N_{5_amine continuation base _4,6_ Dinitrogen pyrrole [3,4_c] D ratio. Sodium-3-yl}-trans-cinnafloxacin; Lu 807.1^-{5-amino thiol-4,6-dihydroindolo[ 3,4-.]吼 - - 3 _ yl}-cis-cinnamin; 808. N-{5-amino sulfhydryl-4,6-dihydroindole 11 each [3,4-c] ° ratio ° sitting -3_base}_3_(3_β ratio π-base) acrylamide; 809. Ν_{5 -amino group-4,6-diox ratio 11 and [3,4-c D is 0--3-yl}-3-(4-pyridyl)propenylamine; 810.1{5-amino-branched-4,6-dihydroindole 11 each [3,4-(: ]° ratio. sit -3_yl}_2_phenyl propylamine; 8 1 1 · N - { 5 -amino thiol-4,6-dihydroindole 13 each [3,4 - c ] D is sitting at 0 13-yl}-o-nonylphenyl acetamidine; 8 1 2. N - { 5 -amino sulphate xanthyl-4,6-dihydrogen ratio p and [3,4 - c ] ° than squat - 3_基}_m-tolylethylamine; 813. N-{5-amino group thiol-4,6-dihydrogen ratio p and [3,4-c] ° ratio sit-3 -yl}-p-indole phenylacetamide; 814. N-{5-amino thiol-4,6-dihydro π ratio p and [3,4-c] 吼〇

C:\2D-OODE\91-Ol\90119473.ptd 第82頁 1327569 五、發明說明（80) _3_基卜鄰香酿胺； 815. N-{5 -胺基磺醯基-4, 6 -二氫呲咯并[3, 4-c]吡唑 -3-基卜3-曱氧苯甲醯胺； 816.1^1-{5-胺基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基}-對-茴香趨胺； 817. N-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_苯氧乙酿胺； 818_ N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑苯基乙酿胺； 819. N-{5-胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c] °比唑 _3_基}_3_氟!苯基乙酿胺； 8 2 0 . N - { 5 -胺基磺醯基-4，6 -二氫吡咯并[3，4 - c ]吡唑 _3-基}-4-氣苯基乙龜胺； 821. N-{5 -胺基磺醯基-4, 6_二氫吡咯并[3, 4-c]吡唑 _3_基}_3_(2_°塞吩基）丙稀酸胺； 822. N-{5 -胺基續醯基-4, 6 -二氫°比。各并[3, 4-c] °比唑 _3_基}_3_(3_°塞吩基）丙稀酿胺， 823. N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}·_3_(2-°塞吩基）丙酿胺； 824. Ν-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-〇]°比唑 _3-基}-2-氯苯曱酿胺； 825. Ν-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}-3-氯苯曱酿胺； 826. \-{5-胺基確醯基-4,6-二氫咄11各并[3,4-(：]吼唑C:\2D-OODE\91-Ol\90119473.ptd Page 82 1327569 V. INSTRUCTIONS (80) _3_基卜邻香香胺; 815. N-{5-Aminosulfonyl-4, 6-II Hydroquino[3,4-c]pyrazol-3-ylbu-3-oxooxybenzamide; 816.1^1-{5-aminosulfonyl-4,6-dihydropyrrolo[3 , 4-(:]pyrazol-3-yl}-p-anisine; 817. N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole _3_基}_phenoxyethylamine; 818_ N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazolephenylethylamine; 819. N -{5-Aminosulfonyl-4,6-dihydropyrrolo[3,4-c] °biazole_3_yl}_3_fluoro!phenylethylamine; 8 2 0 . N - { 5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-4-phenylphenylthiocyanamide; 821. N-{5-aminosulfonate Mercapto-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_3_(2_°secenyl)acrylic acid amine; 822. N-{5-amino group -4,6-dihydrogen ratio. Each [3, 4-c] ° azole _3_ yl}_3_(3_°secenyl) acrylamide, 823. N-{5-amino sulfonate Mercapto-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}·_3_(2-°secenyl) propylamine; 824. Ν-{5 - Sulfosyl-4,6-dihydropyrrolo[3,4-indenyl]-pyrimidin-3-yl}-2-chlorobenzoquinone; 825. Ν-{5-aminosulfonyl- 4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-3-chlorophenyl hydrazone; 826. \-{5-Amino-decyl-4,6-dihydro咄11 each [3,4-(:]carbazole

C:\2D-C0DE\91-01\90119473.ptd 第 83 頁 1327569 五、發明說明（81) _3_基}_4_氯苯甲酿胺； 8 27. N-{ 5 -胺基磺醯基-4, 6 -二氫吼咯并[3, 4-c]咄唑 -3 -基} - 1 -哌啶丙醯胺； 8 28. N-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3_基}_2_乙酿基苯曱酿胺； 829.1'1-{5-胺基續醯基-4,6-二氫吼17各并[3,4-〇:]°比°坐 -3-基}-4_乙酿基苯曱酿胺； 8 3 0 · N - { 5 -胺基續醯基-4，6 -二氫吼p各并[3，4 - c ] D比。坐 -3-基}-1-萘曱醯胺； _ 831. N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-2-萘曱醯胺； 832. N-{5 -胺基項醯基-4，6 -二氫吼B各并[3，4-c] D比。坐 -3-基}-3 -苯曱醯基丙醯胺； 833_ N-{5 -胺基續醯基-4，6 -二氫吼11 各并[3，4-c] D比0坐 -3_基}-4-乙醯胺基苯曱醯胺； 834· N-{5 -胺基續醯基- 4,6 -二氫B比11 各并[3，4-c] °比。坐 -3_基}-2，5_二曱氧苯曱酿胺； 835. N-{5 -胺基項醯基-4，6 -二氫吼11 各并[3，4-c] °比°坐 0-3-基}-2,6 -二曱氧苯曱醯胺； 836. N-{5 -胺基續醯基-4，6 -二氫吼17各并[3，4-c]"比。坐 _3 -基}-3，4_二曱氧苯曱酿胺； 8 37. N - { 5 -胺基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑 -3-基}-3，5_二曱氧苯曱酿胺； 8 38. N-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑C:\2D-C0DE\91-01\90119473.ptd Page 83 1327569 V. INSTRUCTIONS (81) _3_BASE}_4_ chlorobenzamide; 8 27. N-{5-Aminosulfonyl -4,6-dihydroindolo[3,4-c]oxazol-3-yl}-1 -piperidinepropanamine; 8 28. N-{5-aminosulfonyl-4,6 -dihydropyrrolo[3,4-c]carbazole-3-yl}_2_ethyl phenyl benzoate; 829.1'1-{5-amino sulfonyl-4,6-dihydroanthracene 17 Each [3,4-〇:]°°°-3-yl}-4_ethyl phenyl benzoate; 8 3 0 · N - { 5 -amino thiol-4,6 - two Hydroquinone p is each [3,4 - c ] D ratio. -3-yl}-1-naphthylamine; _ 831. N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl }-2-naphthylamine; 832. N-{5-amine-based mercapto-4,6-dihydroindole B each [3,4-c] D ratio. Sodium-3-yl}-3 -benzoylpropionamide; 833_ N-{5-amino sulfonyl-4,6-dihydroindole 11 each [3,4-c] D is 0-based -3 _} Acetyl phenyl hydrazide; 834 · N-{5-amino thiol- 4,6-dihydro-B ratio 11 and [3,4-c] ° ratio. Sitting -3_ base}- 2,5-dioxabenzoquinone; 835. N-{5-amine-based mercapto-4,6-dihydroindole 11 each [3,4-c] ° ratio 0-3- }}-2,6-dioxabenzoquinone; 836. N-{5-amino sulfonyl-4,6-dihydroindole 17 and [3,4-c]" _3 -yl}-3,4_dioxabenzoquinone; 8 37. N - { 5 -aminosulfonyl-4,6-dihydroindolo[3,4-c]pyrazole -3-yl}-3,5-dioxabenzoquinone; 8 38. N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

C:\2D-C0DE\91-01\90119473.ptd 第84頁 1327569 五、發明說明（82) -3-基}-3-(2-噻吩曱醯基）-丙醯胺； 839. N-{5 -胺基項醯基-4,6 -二氫吼17各并[3,4-c] n比。坐 -3_基}-2_蔡基乙酿胺； 840. N_{5_胺基續酿基_4，6_二氮°比p各并[3，4_c] n比〇坐 _3_基}-1_秦基乙酿胺； 841. N-{5 -胺基續醯基-4，6-二氫°比略并[3, 4-c] p比0坐 _3_基}-4_苯基苯甲酿胺； 842. N_{5-曱苯石黃酿基- 4,6 -二氫吼0各并[3，4-c] σ比。坐 _3_基}_乙酿胺； 843. Ν_{5_曱苯續酿基_4，6 -二氮0比洛弁[3，4-c] 0比。坐 -3_基}-環丙烧叛酿胺； 844. Ν-{5-曱苯石黃醯基- 4,6 -二氫吼17各并[3,4-c] 0比°坐 -3 -基}-異丁醯胺； 845. N-{5-甲苯石黃醯基-4, 6 -二氫〇比11 各并[3, 4-c] 0比唑 -3 -基}-環戍烧缓酿胺； 846. N-{5-曱苯石黃醢基- 4,6 -二氫吼17各并[3，4-c]nbn坐 _3_基}_苯甲酿胺； 847. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基}-曱基吡啶甲醯胺； 848. N-{5-甲苯續醯基- 4,6 -二氫D比11 各并[3,4-c] 0比0坐 -3-基卜菸鹼醯胺； 849. N-{5-曱苯石黃醯基-4，6 -二氫D比0各并[3,4-c] 0比。坐 _3_基}-異於驗酿胺； 850. N-{5-曱苯石黃醯基- 4,6 -二氫°比°各并[3，4-c] 〇比0坐C:\2D-C0DE\91-01\90119473.ptd Page 84 1327569 V. Description of the invention (82)-3-yl}-3-(2-thienyl)-propanamine; 839. N- {5-Amino-mercapto-4,6-dihydroindole 17 each [3,4-c] n ratio. Sit -3_base}-2_Caijiyi amine; 840. N_{5_Amine base _4,6_Dinitrogen ratio p and [3,4_c] n ratio _3_ base} -1_秦基乙乙胺; 841. N-{5-amino thiol-4,6-dihydrogen ratio slightly [3, 4-c] p ratio 0 _3_ ki}-4 _Phenylbenzamide; 842. N_{5-beanthine-branched- 4,6-dihydroindole 0 and [3,4-c] σ ratio. Sit _3_基}_Ethylamine; 843. Ν_{5_ 曱续酿 _ 4,6 - dinitrogen 0 than 弁 [ [3,4-c] 0 ratio. Sit -3_yl}-cyclopropanol retinol; 844. Ν-{5-bepholine xanthine- 4,6-dihydroindole 17 and [3,4-c] 0 than ° sit -3 Base}-isobutylamine; 845. N-{5-tolylxanthyl-4,6-dihydroindole ratio 11 and [3,4-c] 0-pyridin-3-yl}-cyclic oxime Amine; 846. N-{5-bepholine xanthine- 4,6-dihydroindole 17 and [3,4-c]nbn sit _3_yl}_benzamide; 847. N-{ 5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-mercaptopyridinecarboxamide; 848. N-{5-toluene fluorenyl - 4,6-dihydrogen D ratio 11 each [3,4-c] 0 to 0 -3- benzyl nicotinic amide; 849. N-{5-beanthine fluorenyl-4,6-two Hydrogen D is 0 and each is [3,4-c] 0 ratio. Sitting _3_base}-different from the amine; 850. N-{5-bepholine xanthine- 4,6-dihydrogen ratio Each [3,4-c] 〇 sits 0

C:\2D-C0DE\91-01\90119473.ptd 第85頁 1327569 五、發明說明（83) -3 -基}-3-曱基-2 -呋喃甲醯胺； 8 5 1. N - { 5 -曱苯石黃醯基-4，6 -二氫0比0各并[3，4 - c ] 0比0坐 -3-基}-嗔吩_2_缓酿胺； 852. ?^-{5-曱苯續酿基-4，6-二氫11比0各并[3,4-(：]〇比〇坐 -3_基}-噻吩-3-羧醯胺； 853. N-{ 5-甲苯磺醯基-4, 6 -二氫。比咯并[3, 4-c]吡唑 _3-基}_鄰-曱苯曱酿胺； 854. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑 _3_基}_間-曱苯曱酿胺； _ 8 55. N-{5-曱苯磺醯基-4,6-二氫咄咯并[3,4-c]吡唑 -3 -基}-對-甲苯曱醯胺； 856. N-{5-曱苯石黃醯基-4，6 -二氫吼11各并[3，4-c] π比0坐 _3_基}_水楊酿胺； 857· Ν-{5-曱苯石黃醯基- 4,6 -二氫D比ρ各并[3，4-c] °比°坐 _3-基}-2 -氟苯曱酿胺； 858. N-{5-曱苯石黃醢基- 4,6 -二氫D比0各并[3,4-c] D比。坐 -3-基}-3 -氟苯曱醯胺； 859. N-{5-甲苯石黃醯基- 4，6 -二氫°比°各并[3,4-c]吼〇坐 3_基}_4-氟苯曱酿胺； 860.1'1-{5-曱苯石黃醯基-4，6-二氫〇比〇各并[3，4-(：]〇比〇坐 -3-基}-噻吩-2-乙醯胺； 861_ N-{5-曱苯石黃酿基-4，6_二氫π比0各并[3，4-c] 0比〇坐 -3 -基}-噻吩-3-乙醯胺； 862· N-{ 5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]咄唑C:\2D-C0DE\91-01\90119473.ptd Page 85 1327569 V. INSTRUCTIONS (83) -3 -yl}-3-mercapto-2-furomylamine; 8 5 1. N - { 5-Phenylxanthine-4,6-dihydrogen 0 to 0 each [3,4 - c ] 0 to 0 -3-yl}- porphin_2_ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ ̄ 5-indene benzene-ternyl-4,6-dihydro 11-O-[3,4-(:] 〇〇 -3 -3_yl}-thiophene-3-carboxamide; 853. N-{ 5-toluenesulfonyl-4,6-dihydro.pyrolo[3,4-c]pyrazole-3-yl}-o-indolephthalene; 854. N-{5-nonylbenzenesulfonate Mercapto-4,6-dihydropyrrolo[3,4-indene]carbazole_3_yl}-m-indole benzoic acid; _ 8 55. N-{5-nonyl sulfonyl-4 , 6-dihydroindolo[3,4-c]pyrazol-3-yl}-p-toluidine; 856. N-{5-beanthine xanthyl-4,6-dihydroindole 11 Each [3,4-c] π is 0 _3_ yl} _ _ _ _ _ _ _ _ _ _ _ _ 5 { { { { { { { { { { { { { { { { { { { { { { { { { 3 3 3 3 3 3 4-c] ° ° ° _3-yl}-2 -fluorobenzoquinone; 858. N-{5-bepholine xanthine - 4,6-dihydro D ratio 0 each [3,4- c] D ratio. Sodium-3-yl}-3-fluorobenzoin; 859. N-{5-tolylxanthyl- 4,6-dihydrogen ratio °[3,4-c]吼Squat 3_base}_4-fluorine Brewing amine; 860.1'1-{5-bepholine xanthene-4,6-dihydroindole 〇[3,4-(:]〇〇 -3--3-yl}-thiophene-2-B醯 ; 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 861 Amine; 862· N-{ 5-nonylbenzenesulfonyl-4,6-dihydroindolo[3,4-c]carbazole

C:\2D-OODE\91-Ol\90119473.ptd 第86頁 1327569 五、發明說明（84) -3 -基卜苯基丙炔醯胺； 863. N-{5-曱苯磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑 -3_基}-3-氛基苯曱酿胺； 864. N-{5-曱苯項醯基-4,6 -二氫n比0各并[3,4-c] °比°坐 -3_基}-4-氰基苯曱酿胺； 865. N-{ 5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-反-桂皮醯胺； 866. N - {5-曱苯石黃醯基- 4,6 -二氫〇比0各并[3，4-c] 0比。坐 - 3 -基}-順-桂皮醯胺； 867. N-{5-曱苯石黃酿基_4，6 -二氫0比0各并[3，4-c] D比0坐 -3-基}_3_(3_11比。定基）丙稀酿胺； 868. N-{5-曱苯磺醯基-4,6-二氫吼咯并[3,4-(：]吡唑 -3_基}-3_(4_11比咬基）丙.稀酿胺； 869. N-{ 5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}_2_苯基丙酿胺； 870. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}-鄰-曱苯基乙酿胺； 871. N-{5-曱苯確醯基-4,6 -二氫0比0各并[3，4-c]°比0坐 -3_基}-間-甲苯基乙酿胺； 872. N-{5-甲苯石黃醯基- 4,6 -二氫D比略并[3,4-c] 0比0坐 _3_基}-對-曱苯基乙酿胺； 873. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基}-鄰-茴香醯胺； 874. N-{5_曱苯石黃酿基_4，6_二氫0比0各并[3，4_c] °比〇坐C:\2D-OODE\91-Ol\90119473.ptd Page 86 1327569 V. Description of the invention (84) -3 - phenyl phenylpropynylamine; 863. N-{5-nonyl sulfonyl sulfhydryl- 4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-3-ylphenylbenzoic acid; 864. N-{5-nonylphenylindolyl-4,6 - dihydrogen n is 0 and each [3,4-c] ° ratio -3 -yl}-4-cyanobenzoquinone; 865. N-{ 5-nonylbenzenesulfonyl-4, 6 - dihydroindolo[3,4-c]pyrazol-3-yl}-trans-cintoinamide; 866. N - {5-bepholine xanthine- 4,6-dihydroindole is 0 [3,4-c] 0 ratio. Sodium- 3 -yl}-cis-cinnamicin; 867. N-{5-beanthine yellow-based 4,6-dihydrogen 0 to 0 each [3 , 4-c] D is 0 -3-yl}_3_(3_11 ratio. base) acrylamide; 868. N-{5-nonylsulfonyl-4,6-dihydroindole[3 , 4-(:]pyrazole-3-yl}-3_(4_11 ratio), dilute amine; 869. N-{5-nonylbenzenesulfonyl-4,6-dihydroindole[ 3, 4-c]pyrazol-3-yl}_2-phenylpropanol; 870. N-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-(:] Pyrazole _3_yl}-o-indole phenylethylamine; 871. N-{5-nonylbenzene-4,6-dihydro 0 to 0 each [3,4-c]° ratio 0 sitting -3_yl}-m-tolyl Amine; 872. N-{5-tolylxanthyl- 4,6-dihydrogen D ratio slightly [3,4-c] 0 to 0 sitting _3_yl}-p-indole phenylethylamine; 873 N-{5-nonphenylsulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3-yl}-o-anisylamine; 874. N-{5_nonylbenzene Stone yellow wine base _4,6_ dihydrogen 0 to 0 each [3,4_c] ° than sitting

C:\2D-00DE\91-01\90119473.ptd 第87頁 1327569 五、發明說明（85) -3-基}-3-曱氧苯曱醯胺； 875_ N-{5-甲苯磺醯基-4,6-二氫咄咯并[3,4-〇]吡唑 -3 -基卜對-茴香醯胺； 876.1{5-甲苯石黃醯基-4,6-二氫0比11各并[3,4-(：]0比。坐 -3_基}_苯氣乙酿胺， 8 77. N-{5-甲苯磺醯基-4, 6 -二氫呲咯并[3, 4-c]吡唑笨基乙酿胺； 878. N-{5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_3_氣苯基乙酿胺； 879. N-{5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4 -c]吡唑 _3_基}_4_氟苯基乙酿胺； 880. N-{5-曱苯石黃醯基-4，6 -二氫11比17各并[3，4-c] D比0坐 -3-基}-3-(2-噻吩基）丙烯醯胺； 881.1'1-{5-甲苯石黃醯基-4，6-二氫〇比口各并[3，4-(：]11比。坐 -3-基}-3-(3-噻吩基）丙烯醯胺； 882. N-{5-曱苯石黃醢基- 4,6 -二氫0比3各并[3，4-c] °比"坐 -3-基}-3-(2 -噻吩基）丙醯胺； 883. N-{5-曱苯石黃醯基- 4,6 -二氫°比σ各并[3，4-c] 0比。坐 jjp 3_基}-2 -氣苯甲酿胺； 884· N_{5_甲苯石黃酿基_4，6_二氮0比17各并[3，4_c] n比0坐 _3_基}-3-氣苯甲酿胺； 885.1^1-{5-甲苯石黃醯基-4，6-二氫0比11各并[3，4-(：]0比〇坐 -3-基}-4_氯苯曱醯胺； 886.1^-{5-甲苯石黃醯基-4,6-二氫0比°各并[3,4-(；]〇比唑C:\2D-00DE\91-01\90119473.ptd Page 87 1327569 V. INSTRUCTIONS (85) -3-yl}-3-oxobenzoquinone; 875_ N-{5-toluenesulfonyl -4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl-p-anisylamine; 876.1{5-tolylxanthyl-4,6-dihydrogen 0 to 11 each [ 3,4-(:]0 ratio. Sit-3_yl}_benzene benzene, 6 77. N-{5-toluenesulfonyl-4,6-dihydroindole[3, 4- c] pyrazole stupidylamine; 878. N-{5-toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_3_qiphenyl Amine amine; 879. N-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_4_fluorophenylethylamine; 880. N -{5-beanthine xanthyl-4,6-dihydro 11 to 17 and [3,4-c] D to 0--3-yl}-3-(2-thienyl)propenylamine; 881.1 '1-{5-tolylxanthyl-4,6-dihydroindole is more than [3,4-(:]11 ratio. Sodium-3-yl}-3-(3-thienyl)propenylamine 882. N-{5-bepholine xanthine- 4,6-dihydrogen 0 to 3 each [3,4-c] ° ratio "sodium-3-yl}-3-(2-thienyl) Propylamine; 883. N-{5-beanthine xanthine- 4,6-dihydrogen ratio σ and [3,4-c] 0 ratio. Sitting jjp 3_based }-2 - gas benzoylamine; 884· N_{5_toluene yellow wine base _4,6_dia nitrogen 0 to 17 each [3,4_c] n ratio 0 sitting _3_ base}-3- Gas benzoic acid; 885.1^1-{5-tolylxanthyl-4,6-dihydrogen 0 to 11 each [3,4-(:]0 than 〇-3-yl}-4_chlorobenzene Indoleamine; 886.1^-{5-tolylxanthyl-4,6-dihydrogen 0 ratio °[3,4-(;]pyridazole

C:\2D-CODE\91-01\90119473.ptd 第88頁 1327569 五、發明說明（86) _3-基}-1-°底。定丙酿胺； 887. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_2_乙酿基苯甲酿胺； 8 88. N-{5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-乙醯基苯甲醯胺； 889. N-{5-曱苯磺醯基-4,6-二氫咣咯并[3,4-〇]吼唑 -3-基}-卜萘曱醯胺； 890. N-{5-曱苯續醯基-4，6 -二氫各并[3,4-c] 0比。坐 -3-基}-2-萘曱醯胺； 891. N-{5-曱苯石黃醯基-4, 6 -二氫〇比0各并[3,4-c] σ比。坐 -3-基}-3 -苯甲醯基丙醯胺； 892· Ν-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-4-乙醯胺基苯曱醯胺； 893. Ν-{5-甲苯石黃醢基- 4,6 -二氫°比°各并[3，4-c]d比哇 _3_基}_2，5_二甲氧苯甲酿胺； 894. N-{5-曱苯石黃醯基-4，6 -二氫各并[3, 4-c] 0比。坐 -3-基}-2,6 -二甲氧苯甲醯胺； 895. Ν-{5-甲苯續醯基-4, 6 -二氫0比ρ各并[3,4-c] π比0坐 -3-基}-3,4-二曱氧苯曱醯胺； 896. Ν-{5-曱苯石夤醢基-4，6 -二氫吼11 各并[3，4-c] π比0坐 - 3-基}-3，5 -二曱氧苯甲酿胺； 897. Ν-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-3-(2 -噻吩甲醯基）-丙醯胺； 898_ Ν_{5-曱苯續醯基- 4,6 -二氫〇比〇各并[3，4-(：]πΛ^C:\2D-CODE\91-01\90119473.ptd Page 88 1327569 V. Description of invention (86) _3-Base}-1-°. Acrylamine; 887. N-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazole-3-yl}_2_ethyl-brenylbenzamide; 8 88. N-{5-Toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-ethenylbenzamide; 889. N- {5-Indolylsulfonyl-4,6-dihydroindolo[3,4-indolyl]oxazol-3-yl}-b-naphthylamine; 890. N-{5-曱Benzene continued Base-4,6-dihydro each [3,4-c] 0 ratio. Sodium-3-yl}-2-naphthylamine; 891. N-{5-bepholine xanthine-4,6-dihydroindole ratio 0 and [3,4-c] σ ratio. -3-yl}-3-benzhydrylpropionamide; 892·Ν-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3 -yl}-4-acetamidobenzoin; 893. Ν-{5-tolylxanthyl- 4,6-dihydrogen ratio °[3,4-c]d than wow_3_ Base}_2,5-dimethoxybenzoic acid; 894. N-{5-bepholine xanthene-4,6-dihydro-[3,4-c] 0 ratio. sit-3-yl} -2,6-dimethoxybenzamide; 895. Ν-{5-toluene fluorenyl-4,6-dihydrogen 0 ratio ρ and [3,4-c] π ratio 0 sitting-3- }}-3,4-dioxabenzoquinone; 896. Ν-{5- fluorenyl-4,6-dihydroindole 11 each [3,4-c] π ratio 0 - 3-yl}-3,5-dioxaxybenzamide; 897. Ν-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3 -yl}-3-(2-thiophenemethyl)-propanamine; 898_ Ν_{5-nonylbenzene fluorenyl- 4,6-dihydroindole 〇[3,4-(:]πΛ ^

C:\2D-O0DE\91-Ol\9O119473.ptd 第89頁 1327569 五、發明說明（87) _3-基}_2_秦基乙酿胺； 8 99. N-{5-甲苯磺醯基-4, 6_二氫呲咯并[3, 4-c]吡唑 _3_基}_1_蔡基乙酿胺； 900_ N-{5-曱苯續醯基-4，6 -二氫口比口各并[3，4-c] D比。坐 -3-基}-4-苯基苯曱醯胺； 901. ^}-{5-芊基石黃酿基-4，6-二氫°比11各并[3，4-(：]'1比。坐 _3_基}_乙酿胺，； 902. N-{5-苄基續醯基- 4,6 -二氫吼17各并[3,4-c] °比°坐 _3_基}_環丙烧叛酿胺； _ 9 03. N-{ 5-亨基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑 -3 -基}-異丁酿胺； 904. N-{5-芊基石黃醯基-4，6 -二氫吼17各并[3，4-c] °比。坐 -3 -基卜環戊烷羧醯胺； 90 5. N-{5-芊基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_苯甲酿胺； 906. N-{5 -苄基石黃醯基-4，6 -二氫"比11各并[3，4-c] °比唾 -3 -基}-曱基吡啶甲醯胺； 907. N-{5 -辛基石黃醯基- 4,6 -二氫吼11各并[3，4-c] 0比0坐 3 -基}-於驗醯胺； 908.1^-{5-辛基績酿基-4，6-二氮11比17各并[3，4-〇]°比〇坐 -3-基}-異菸鹼醯胺； 909. N-{5-苄基石黃醯基-4，6 -二氫0比D各并[3，4-c] °比〇坐 -3-基}-3-甲基-2 -呋喃甲醯胺； 91 0· N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑C:\2D-O0DE\91-Ol\9O119473.ptd Page 89 1327569 V. Description of the Invention (87) _3-Base}_2_Qinyl Ethylamine; 8 99. N-{5-Toluenesulfonyl- 4,6_dihydroindolo[3,4-c]pyrazole_3_yl}_1_cacoylamine; 900_ N-{5-nonylbenzene thiol-4,6-dihydrogen port Each [3,4-c] D ratio. Sodium-3-yl}-4-phenylbenzamide; 901. ^}-{5-mercapto yellow wine-4,6-dihydrogen ratio 11 and [3,4-(:]' 1 ratio. Sit _3_基}_Ethylamine, 902. N-{5-Benzyl fluorenyl- 4,6-dihydroindole 17 and [3,4-c] ° ratio _ 3_基}_Cyclopropanol; _ 9 03. N-{ 5-Hhenylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl} - Isobutylamine; 904. N-{5-mercapto-stone xanthene-4,6-dihydroindole 17 each [3,4-c] °. Sodium-3-ylcyclopentane carboxamide; 90 5. N-{5-decylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_benzamide; 906. N-{5-benzyl Cornerstone xanthine-4,6-dihydro" ratio 11 and [3,4-c] ° than sal-3-yl}-mercaptopyridinecarboxamide; 907. N-{5 -octyl sulphate - 4 , 6-dihydroindole 11 each [3,4-c] 0 to 0 sitting 3 -yl}-in the test of decylamine; 908.1^-{5- octyl broth-4,6-diaza 11 to 17 each And [3,4-〇]° 〇基-3-yl}-isonicotin amide; 909. N-{5-benzyl sulfonyl-4,6-dihydro 0 to D each [3,4 -c] ° -3--3-yl}-3-methyl-2-furocarbamide; 91 0·N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3, 4 -c]pyrazole

C:\2D-OODE\91-Ol\90119473.ptd 第90頁 1327569 五、發明說明（88) -3-基}-奮吩-2-羧醯胺； 91 1. N-{ 5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吼唑 -3 -基}-噻吩-3 -羧醯胺； 912· N-{5-苄基石黃醯基-4, 6-二氫。比咯并[3, 4-c] °比唑 -3-基}-鄰-甲苯曱醯胺； 913. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基}-間-曱苯甲醯胺； 914. N-{ 5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基卜對-曱苯甲醯胺； 915. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}-苯基乙酿胺； 916. N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}-水揚酿胺； 917· N-{5-苄基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑 _3_基}-2-氟苯曱酿胺； 918. N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_3_氣苯曱酿胺； 919. N-{5-苄基石黃醯基- 4,6 -二氫D比p各并[3，4-c] 0比口坐 _3_基}-4-氟苯甲酿胺； 920· N-{5-苄基磺醯基-4,6-二氫咄咯并[3,4-〇]吡唑 -3 -基}-噻吩-2-乙醯胺； 921. N-{ 5-苄基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-噻吩-3-乙醯胺； 922. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑C:\2D-OODE\91-Ol\90119473.ptd Page 90 1327569 V. INSTRUCTIONS (88) -3-yl}-f-phen-2-carboxamide; 91 1. N-{ 5-benzyl Sulfonyl-4,6-dihydropyrrolo[3,4-c]indazol-3-yl}-thiophene-3-carboxycarboxamide; 912· N-{5-benzyl sulphate-4, 6- Dihydrogen. Bis-[3,4-c] °pyrazol-3-yl}-o-toluidine; 913. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3, 4-〇]pyrazol-3-yl}-m-nonylbenzamide; 914. N-{ 5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3 - kib-p-benzamide; 915. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazole-3-yl}-benzene Ethylamine; 916. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-hydrogen amine; 917· N- {5-Benzylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}-2-fluorobenzoquinone; 918. N-{5-benzyl Sulfomethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_3_ gas benzoquinone; 919. N-{5-benzyl fluorenyl- 4,6-di Hydrogen D ratio p and [3,4-c] 0 is more than _3_yl}-4-fluorobenzamide; 920· N-{5-benzylsulfonyl-4,6-dihydrogen咄[3,4-〇]pyrazol-3-yl}-thiophene-2-acetamide; 921. N-{ 5-benzylsulfonyl-4,6-dihydroindole[3 , 4-c]pyrazol-3-yl}-thiophene-3-acetamide; 922. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-anthracene] Azole

C:\2D-OODE\91-Ol\90119473.ptd 第91頁 1327569 五、發明說明（89) _3 -基卜苯基丙炔醯胺； 92 3. N-{ 5-苄基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑 -3-基}-3-氰基苯曱醯胺； 9 24. N-{5-苄基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 _3_基}_4_氛基苯曱酿胺； 925· N-{5-芊基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-反-桂皮醯胺； 926. N-{5-辛基磺醯基-4,6-二氫吡咯并[3,4-〇]»比唑 _ 3 -基}-順-桂皮醯胺；餐927. N-{ 5-辛基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吼唑 -3 -基} - 3 - ( 3 -吡啶基）丙烯醯胺； 928. N-{5-芊基石黃醯基- 4,6 -二氫°比°各并[3，4-c] °比〇坐 -3 -基} - 3 - ( 4 -吡啶基）丙烯醯胺； 929· N-{5-辛基石黃醯基-4，6 -二氫°比°各并[3, 4-c] °比°坐 _3_基}_2_苯基丙酿胺； 930.1^-{5-芊基石黃醯基-4，6-二氫〇比11各并[3,4-(：]°比°坐 _3_基}_間-曱苯基乙酿胺； 9 3 1. N - { 5 -苄基石黃醯基-4，6 -二氫0比p各并[3，4 - c ]吼0坐 #3 -基卜對-甲苯基乙醯胺； 932· N-{5-辛基磺醯基-4,6-二氫吡咯并[3,4-(；]吡唑 -3-基卜鄰-茴香醯胺； 933. N-{5-亨基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-3-甲氧苯曱醯胺； 934. N-{5-苄基磺醢基-4, 6 -二氫咁咯并[3, 4-c]吡唑C:\2D-OODE\91-Ol\90119473.ptd Page 91 1327569 V. INSTRUCTIONS (89) _3-KipPhenylpropynylamine; 92 3. N-{ 5-Benzylsulfonyl- 4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-3-cyanobenzoquinone; 9 24. N-{5-benzylsulfonyl-4, 6 -dihydroindolo[3,4-c]pyrazole-3-yl}_4_ylphenyl benzoate; 925·N-{5-nonylsulfonyl-4,6-dihydropyrrole [3,4-c]pyrazol-3-yl}-trans-cintoinamide; 926. N-{5-octylsulfonyl-4,6-dihydropyrrolo[3,4-〇]» Benzene _ 3 -yl}-cis-cinnamin; meal 927. N-{ 5-octylsulfonyl-4,6-dihydroindolo[3,4-c]carbazole-3-yl } - 3 - ( 3 -pyridyl) acrylamide; 928. N-{5-fluorenyl fluorenyl- 4,6-dihydrogen ratio °[3,4-c] ° 〇 sitting -3 }} - 3 - ( 4 -pyridyl) acrylamide; 929 · N-{5-octyl sulphate-4,6-dihydrogen ratio °[3, 4-c] ° ratio ° _3 _ base}_2_phenyl propylamine; 930.1^-{5-fluorenyl fluorenyl-4,6-dihydroindole ratio 11 and [3,4-(:]° ratio ° sitting_3_base}_间-曱phenylethylamine; 9 3 1. N - { 5 -benzylstone xanthene-4,6-dihydrogen 0 to p each [3,4 - c]吼0坐#3-kib-p-tolylacetamide; 932· N-{5-octylsulfonyl-4,6-dihydropyrrolo[3,4-(;]pyrazole- 3-carbo-anisoleamine; 933. N-{5-Henylsulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-methoxy Benzoylamine; 934. N-{5-benzylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazole

C:\2D-CODE\91-01\90119473.ptd 第92頁 1327569 五、發明說明（90) _3-基}-對-菌香酿胺； 935_ N-{5-芊基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 _3-基}-苯氧乙酿胺； 936. ^1-{5-苄基石黃酿基-4,6-二氫吼洛并[3,4-(：]'1比〇坐 _3_基}-2_氣苯基乙酿胺， 937. N-{5-苄基磺醯基-4,6-二氫吼咯并[3,4-(：]吡唑 _3-基}_3_氣苯基乙酿胺； 938_ N-{5 -苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3-基}-4_氣苯基乙酿胺； 939. N-{ 5 -苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3-(2 -噻吩基）丙烯醯胺； 940. N-{5-苄基石黃醯基- 4,6 -二氫吼11 各并[3,4-c] D比。坐 -3-基}-3-(3 -噻吩基）丙烯醯胺； 941. N-{5-苄基磺醯基-4, 6 -二氫咄咯并[3, 4-c]咄唑 -3-基}-3-(2-噻吩基）丙醯胺； 942. N-{5-辛基績醯基-4, 6 -二氫°比0各并[3,4-c] °比〇坐 _3_基}_2-氣苯曱酿胺； 943· N-{ 5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3-基}_3_氣苯甲酿胺； 944. N-{5-苄基石黃醯基- 4，6 -二氫吼17各并[3,4-c] 〇比0坐 _3-基}-4-氣苯曱醯胺； 945. N-{ 5-苄基磺醯基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-1-哌啶丙醯胺； 946. N-{5-苄基磺醯基-4,6-二氫吼咯并[3,4-〇]吼唑C:\2D-CODE\91-01\90119473.ptd Page 92 1327569 V. INSTRUCTIONS (90) _3-基}-pair-bacteria fragrant amine; 935_ N-{5-mercaptosulfonyl-4 ,6-dihydropyrrolo[3,4-indene]pyrazole-3-yl}-phenoxyethylamine; 936. ^1-{5-benzyl schisthol-4,6-dihydropyrrole And [3,4-(:]'1 is more than 〇3_yl}-2_ phenyl phenylethylamine, 937. N-{5-benzylsulfonyl-4,6-dihydrofluorene And [3,4-(:]pyrazole-3-yl}_3_ gas phenylethylamine; 938_ N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4- (:]pyrazole-3-yl}-4_henylphenylethylamine; 939. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3-yl}-3-(2-thienyl)propenylamine; 940. N-{5-benzyl fluorenyl- 4,6-dihydroindole 11 each [3,4-c] D ratio. -3-yl}-3-(3-thienyl)propenylamine; 941. N-{5-benzylsulfonyl-4,6-dihydroindolo[3,4-c]carbazole- 3-yl}-3-(2-thienyl)propanamide; 942. N-{5-octyl benzyl-4,6-dihydrogen ratio 0 and [3,4-c] ° _3_基}_2-gas benzoquinone; 943· N-{ 5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}_3_ Gas benzoic acid; 944. N-{ 5-Benzyl sulphate - 4,6-dihydroindole 17 each [3,4-c] 〇 is 0 _3-yl}-4-phenhydrin; 945. N-{ 5-benzyl Sulfhydryl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-1-piperidinepropanamine; 946. N-{5-benzylsulfonyl-4, 6-dihydroindolo[3,4-indole]carbazole

C:\2D-C0DE\91-01\90119473.ptd 第93頁 1327569 五、發明說明（91) _3_基}-2_乙酿基苯曱酿胺； 947. N-{5-辛基石黃醯基- 4,6 -二氫°比11 各并[3,4-c] °比〇坐 -3-基}-4-乙醯基苯曱醯胺； 948.1^-{5-苄基石黃酸基-4,6-二氫〇比11各并[3,4-0：]'1比〇坐 -3-基}-1_萘甲醯胺； 949. N-{5-苄基石黃醯基-4，6 -二氫吼11 各并[3, 4-c] °比。坐 -3-基}-2 -萘曱醯胺； 950. N-{5-辛基石黃醯基- 4,6 -二氫D比p各并[3，4-c] 坐 _3_基}_3_苯甲酿基丙酿胺； ® 951. Ν-{5-苄基石黃醯基-4，6-二氫11比洛并[3，4-(：]°比°坐 -3-基}-4-乙醯胺基苯曱醯胺； 952. N-{5 -苄基石黃趨基-4，6 -二氫吼17各并[3，4-c] °比〇坐 -3-基}_2，5_二甲氧苯曱酸胺； 953· N-{5-苄基石黃醯基- 4，6 -二氫吼11 各并[3，4-c] °比°坐 _3_基}_2，6_二甲氧苯甲酿胺； 954. N-{5-辛基石黃醯基-4,6 -二氫0比°各并[3，4-c] D比0坐 - :3-基}-3,4 -二曱氧苯曱醯胺； 955. N-{5 -苄基石黃醯基- 4,6 -二氫吼°各并[3，4-c] 0比0坐 3_基}_3，5 -二甲氧苯曱醢胺； 956. N-{5-罕基石黃醯基- 4,6 -二氫〇比p各并[3，4-c] D比0坐 _3_基}-3_(2_°塞吩曱酸基）-丙酿胺； 957· N-{5-辛基石黃醯基- 4，6 -二氫π比咯并[3，4-c] 0比0坐 ~3-基}-2 -蔡基乙酿胺； 958. N-{5- ¥基石黃醯基- 4,6 -二氫°比°各并[3,4-c] 0比0坐C:\2D-C0DE\91-01\90119473.ptd Page 93 1327569 V. INSTRUCTIONS (91) _3_BASE}-2_Ethyl benzoylamine; 947. N-{5-octyl sulphate - 4,6-dihydrogen ratio 11 and [3,4-c] ° ratio -3--3-yl}-4-ethylmercaptophenylamine; 948.1^-{5-benzyllithic acid -4,6-dihydroindole ratio 11 and [3,4-0:]'1 is more than 〇-3-yl}-1_naphthylcarbenamide; 949. N-{5-benzyl sulphate-4 , 6 - dihydroanthracene 11 each [3, 4-c] ° ratio. Sodium-3-yl}-2-naphthylamine; 950. N-{5-octyl sulphate - 4,6-dihydro D ratio p and [3,4-c] sit _3_yl}_3 _Benzene-based propylamine; ® 951. Ν-{5-benzyl fluorenyl-4,6-dihydro 11 piroxi[3,4-(:]°°°-3-yl}-4 - acetaminophen phenylamine; 952. N-{5-benzyl feldsparin-4,6-dihydroindole 17 and [3,4-c] ° 〇-3-yl}_2 ,5-dimethoxybenzoic acid amine; 953· N-{5-benzyl fluorenyl- 4,6-dihydroindole 11 each [3,4-c] ° ratio _3_ yl}_2, 6_Dimethoxybenzoic acid; 954. N-{5-octyl sulphate-4,6-dihydrogen 0 ratio °[3,4-c] D ratio 0 sitting - :3-yl}- 3,4-dioxabenzoguanamine; 955. N-{5-benzylphosphonium- 4,6-dihydroindole °[3,4-c] 0 to 0 sitting 3_yl}_3, 5- methoxybenzamine; 956. N-{5-Hanstone sulphate- 4,6-dihydroindole ratio p and [3,4-c] D ratio 0 _3_ yl}-3_ (2_°Cetyl decanoate)-propanolamine; 957· N-{5-octyl sulphate - 4,6-dihydro π-pyrolo[3,4-c] 0 to 0 sitting ~3-based }-2 -Cai Keyi Amine; 958. N-{5- ¥ Cornerstone Astragalus - 4,6-Dihydrogen °°[3,4-c] 0 to 0

C:\2D-C0DE\91-01\90119473.ptd 第94頁 1327569 五、發明說明（92) _3-基}_1-蔡基乙酿胺； 959. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}-4-苯基苯甲酿胺； 960. N-{5-乙醯基-4，6 -二氫 °比°各并[3,4-c] 0 比0坐- 3-基}，1^’-(4-氯罕基）脈； 961· N-{5-芊基-4, 6 -二氫吼咯并[3, 4-c]吼唑-3-基}，Ν’ -(4-氣芊基）脲； 962· Ν-{5 -苯基- 4,6 -二氫 °比°各并[3,4-c] ° 比。坐- 3- 基}，Ν’ -(4-氯苄基）脲； 963. N-{5 -胺基幾基_4，6 -二氫°比11 各并[3，4-c] °比°坐- 3-基}，1^’_(4_氣辛基）脈； 964· N-{5-乙基胺基羰基-4, 6 -二氫。比咯并[3, 4-c] >>比唑 965. N-{5-曱烧石黃醯基-4,6 -二氫0比略并[3, 4-c]0比0坐 _3_基}，1''1’_(4-氣：!^基）脈； 966. N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑 _3_基}，^-(4_氣爷基）脈； 967. N-{5-甲苯石黃醯基-4，6-二氫〇比17各并[3,4-0]〇比哇 _3_基}，1^’-（4-氣辛基）脈； 968· N-{5 -亨基胺基叛基_4，6_二氮0比π各弁[3，4-c] B比0坐 -3_基}，1'1’-(4-氯：:^基）脈； 969. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3-基}，1'1’-(4-氣：^基）脈； 970_ N-(5-(l -萘叛基）-4，5，6,7 -四氫 °比。定[4，3-c]° 比。坐C:\2D-C0DE\91-01\90119473.ptd Page 94 1327569 V. INSTRUCTIONS (92) _3-基}_1-Cai Keyi Amine; 959. N-{5-Benzylsulfonyl-4, 6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-phenylbenzamide; 960. N-{5-ethinyl-4,6-dihydrogen ratio °[3,4-c] 0 is 0 to 0 -3-yl}, 1^'-(4-chlorohanyl) vein; 961· N-{5-mercapto-4,6-dihydroanthracene [3,4-c]oxazol-3-yl}, Ν'-(4-carbazyl)urea; 962·Ν-{5-phenyl- 4,6-dihydrogen °° [3,4-c] ° ratio. Sit-3-yl}, Ν'-(4-chlorobenzyl)urea; 963. N-{5-amino-based _4,6-dihydrogen ratio 11 Each [3,4-c] ° ratio sits -3-yl}, 1^'_(4_gas octyl) vein; 964· N-{5-ethylaminocarbonyl-4, 6 - two Hydrogen. Bisino[3,4-c] >>Biazole 965. N-{5-曱烧石黄醯基-4,6-Dihydrogen 0 ratio slightly [3, 4-c]0 to 0 Sit _3_基}, 1''1'_(4-gas: !^ base) vein; 966. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3, 4- c] carbazole _3_yl}, ^-(4_ qi ji) pulse; 967. N-{5-toluene xanthine-4,6-dihydroindole ratio 17 and [3,4-0] 〇比哇_3_基},1^'-(4-gas octyl) pulse 968· N-{5 - Henrylamine-based rebel _4,6_dinitrogen 0 to π each 弁[3,4-c] B is 0 to 0-based, 1'1'-(4- Chlorine::^ base); 969. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl},1'1'-( 4- gas: ^ base) vein; 970_ N-(5-(l-naphthyl-rebase)-4,5,6,7-tetrahydrogen ratio. [4,3-c]° ratio.

C:\2D-C0DE\91-01\90119473.ptd 第95頁 1327569 五、發明說明（93) -3-基）-3-苯氧苯曱醯胺； 971. N-(5-(l -萘羰基）-4, 5, 6, 7 -四氫吡啶[4, 3-c]吡唑 -3 -基）-4 -第三丁基苯曱醯胺； 972. N-(5-(2-呋喃甲醯基）-4,5，6,7-四氫吡啶[4, 3-c] 。比唑-3-基）-(4 -苯基）苯基乙醯胺； 973.1^-(5-(2-呋喃曱醯基）-4,5,6,7-四氫吡啶[4,3-〇] °比唑-3-基）-2-(2-萘基）丙醯胺； 974. \-(5-(2-呋喃曱醯基）-4,5,6,7-四氫咄啶[4,3-〇] 吼唑-3-基）-2-(3-氟-4-苯基-苯基）丙醯胺； 975. N-(5-(2-曱氧苄基）-4,5,6,7-四氫吡啶[4,3-(：]吼唑-3-基）-(2 -萘）乙醯胺； 976. N-(5-(2-甲氧苄基）-4,5,6,7 -四氫吡啶[4,3-c]吡唑-3 -基）-[4-(1-咄咯啶-2 -酮）]苯基乙醯胺； 977. N-(5-(2-甲氧苯基）-4,5,6,7-四氫°比啶[4,3-〇]口比唑-3-基）-(4-苯基）苯基乙醯胺； 978. N-(5-(4-氟-苯甲醯基）-4,5,6,7 -四氫吡啶 [4,3-c]吡唑-3-基）-4-氟苯曱醯胺； 9 7 9. N-(5- 乙酿基-4，5，6，7-四氫-1H- 0 比0定[4，3-c] D 比0坐 3 -基）_3 -氟苯曱酿胺； 980. N-(5-乙醯基-4，5，6，7-四氫 0比咬[4，3-c] 〇比0坐- 3-基）_(2_萘）乙酿胺； 981. N-(5-乙醯基-4，5，6，7-四氫 °比。定[4，3-c] 〇比〇坐-3-基）乙醯胺； 982. N-(5-乙醯基-4, 5, 6, 7-四氫 D比咬[4, 3-c] D比。坐-3-C:\2D-C0DE\91-01\90119473.ptd Page 95 1327569 V. INSTRUCTIONS (93) -3-yl)-3-phenoxybenzamine; 971. N-(5-(l - Naphthylcarbonyl)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl)-4-tert-butylbenzamide; 972. N-(5-(2) -furomethylmercapto)-4,5,6,7-tetrahydropyridine [4,3-c].pyrazol-3-yl)-(4-phenyl)phenylacetamide; 973.1^-( 5-(2-furylfluorenyl)-4,5,6,7-tetrahydropyridine [4,3-〇] °pyrazol-3-yl)-2-(2-naphthyl)propanamine; 974. \-(5-(2-Furanyl)-4,5,6,7-tetrahydroacridine [4,3-indole]oxazol-3-yl)-2-(3-fluoro- 4-phenyl-phenyl)propanamine; 975. N-(5-(2-oximeoxybenzyl)-4,5,6,7-tetrahydropyridine [4,3-(:]carbazole- 3-yl)-(2-naphthyl)acetamide; 976. N-(5-(2-methoxybenzyl)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazole -3 -yl)-[4-(1-indolyl-2-one)]phenylacetamide; 977. N-(5-(2-methoxyphenyl)-4,5,6,7 - tetrahydropyridinium [4,3-indole]-b-pyrazol-3-yl)-(4-phenyl)phenylacetamide; 978. N-(5-(4-fluoro-benzhydryl) -4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-3-yl)-4-fluorophenylamine; 9 7 9. N-(5-B Base-4,5,6,7-tetrahydro-1H- 0 ratio 0 [4,3-c] D is 0 to 3 -yl)_3 -fluorobenzoquinone; 980. N-(5-B Mercapto-4,5,6,7-tetrahydro 0 ratio bite [4,3-c] 〇 than 0 sitting - 3-yl) _(2_naphthalene) ethylamine; 981. N-(5-B Mercapto-4,5,6,7-tetrahydrogen ratio. [4,3-c] 〇〇 -3-yl) acetamide; 982. N-(5-ethenyl-4, 5, 6, 7-tetrahydro D is more than bite [4, 3-c] D. Sitting -3-

C:\2D-CODE\91-01\90119473.ptd 第96頁 1327569 五、發明說明（94) 基）苯甲醯胺； 983. N-(5 -胺基羰基-4，5, 6, 7-四氫吼咬[4, 3-c] π比唑 _3_基）-苯基乙酿胺； 984. Ν-(5 -苯甲酿基-4，5，6，7-四氫口比口定[4，3-c] 0比0坐 _3_基）_(4_苯基）苯基乙酿胺； 985. Ν-(5 -苯甲醯基-4, 5，6, 7-四氫0比咬[4，3-c] 〇比唾 -3 -基）-3 -氟苯甲酿胺； 986. N-(5 -苯甲醯基-4，5，6，7 -四氫〇比口定[4，3-c] D比0坐 -3-基）-3-苯氧-苯曱醢胺； 987. N-(5 -苯甲醯基-4，5，6，7-四氫口比0定[4，3-c] D比0坐 _3 -基）-4-氣苯甲酿胺； 988. N-(5 -苯甲酿基-4，5，6，7-四氫°比0定[4，3-c] 0比唾 -3-基）-4-笨氧笨曱醯胺； 989· N-(5 -苯甲醯基-4, 5, 6, 7-四氫0比口定[4, 3-c] D比0坐 -3-基）-4-第三丁基苯甲醯胺； 990. N-(5 -苯曱酿基-4，5，6，7-四氫〇比。定[4，3-c] 0比0坐 -3 -基）乙醯胺； 991. N-(5-苯曱醢基-4, 5，6，7-四氫°比口定[4，3-c] D比0坐 -3-基）苯曱醯胺； 992.1^-(5-苯曱醢基-4，5，6,7-四氫〇比〇定[4,3-(：]0比〇坐 -3 -基）環丙烷羧醯胺； 993. N-(5 -苯甲醯基-4, 5，6, 7-四氫吼咬[4，3-c] 0比0坐 -3-基）苯基乙醯胺； 994. N-(5-苄基石黃醯基-4，5，6，7 -四氫π比咬[4，3-c] °比〇坐C:\2D-CODE\91-01\90119473.ptd Page 96 1327569 V. INSTRUCTIONS (94) Benzyl decylamine; 983. N-(5-Aminocarbonyl-4,5, 6, 7 - tetrahydrobite [4, 3-c] π-pyrazole_3_yl)-phenylethylamine; 984. Ν-(5-benzolic-4,5,6,7-tetrahydrogen Specific ratio [4,3-c] 0 to 0 sitting _3_yl)_(4_phenyl)phenylethylamine; 985. Ν-(5-benzylidene-4, 5,6, 7-tetrahydro 0 to bite [4,3-c] oxime saliva-3 -yl)-3-fluorobenzamide; 986. N-(5-benzylidene-4,5,6,7 - tetrahydroanthracene is determined by [4,3-c] D to 0--3-yl)-3-phenoxy-benzoguanamine; 987. N-(5-benzylidene-4,5, 6,7-tetrahydrogen port ratio 0 [4,3-c] D ratio 0 sitting _3 -yl)-4-gas benzoylamine; 988. N-(5-benzolic-4,5 , 6,7-tetrahydrogen ratio 0 [4,3-c] 0 than spani-3-yl)-4- oxo acesulfame; 989 · N-(5-benzylidene-4, 5, 6, 7-tetrahydro 0 is more than [4, 3-c] D is 0--3-yl)-4-t-butylbenzamide; 990. N-(5-benzoquinone -4,5,6,7-tetrahydroanthracene ratio. [4,3-c] 0 to 0-position -3 -yl)acetamide; 991. N-(5-benzoin-4, 5,6,7-tetrahydrogen ratio [4,3-c] D is 0 to -3-yl)benzamide; 992.1^-(5-benzoinyl-4,5,6,7-tetrahydropyrene is more stable [4,3-(:]0 than 〇 Sodium-3-yl)cyclopropanecarboxamide; 993. N-(5-benzylidene-4,5,6,7-tetrahydroindene [4,3-c] 0 to 0 sitting-3- Phenylacetamide; 994. N-(5-benzylglycosyl-4,5,6,7-tetrahydropyrene ratio bite [4,3-c] °

I C:\2D-C0DE\91-01\90119473.ptd 第97頁 1327569 五、發明說明（95) -3 -基）環丙烷羧醯胺； 995. N-(5 -苯基乙醯基）-4,5,6,7 -四氫0比。定[4，3-c]D比唑-3-基）-(2-萘）乙醯胺； 996. N-(5 -苯基乙醯基）-4,5,6,7-四氫吡啶[4,3-(：]吡唑-3-基）-苯基乙醯胺； 997. N，N -二甲基-N’-{3-(2 -苯基-嘍唑-4 -基）乙醯胺基 -4，5，6，7-四氫 °比°定[4，3-c] °比°坐-5-基}脲； 9 98. N，N-二曱基-Ν’ - {3-(苯并[1，3]二氧伍圜-5 -基）乙隨胺基-4，5，6，7 -四氫吼。定[4，3-c]吼°坐-5-基}脲；霉9 99· Ν，Ν-異丙基-Ν’-{3-(苯并[1，3]二氧伍圜-5-基）乙醯胺基-4, 5, 6, 7 -四氫吡啶[4, 3-c]吡唑-5-基}脲； 1000. N-[5-(1,3 -苯并二氧伍圜-5 -基羰基）-4, 5, 6,7-四氫吡啶[4，3 - c ]吡唑-3 -基]-3 -甲氧苯曱醯胺； 1001. N-[5-(l，3 -苯并二氧伍圜-5 -基羰基）-4,5,6,7-四氫咄啶[4，3 - c ]吡唑-3 -基]-3 -苯氧苯曱醯胺； 1002. N-[5-(1,3 -苯并二氧伍圜-5 -基羰基）-4,5, 6,7-四氫吡啶[4，3 - c ]吡唑-3 -基]-3 -苯氧苯曱醯胺； 1003. N-[5-(l，3-苯并二氧伍圜-5 -基羰基）-4,5,6,7-φ四氫咄啶[4, 3-c]吡唑-3-基]-4-第三丁基苯甲醯胺； 1004. N-[5-(2 -苯基乙醯基）-4,5, 6,7-四氫吡啶 [4, 3-c]吡唑-3 -基]乙醯胺； 1005. N-[5-(2 -苯基乙醯基）-4,5,6,7-四氫吡啶 [4, 3-c]吡唑-3 -基]苯甲醯胺； 1 00 6_ N-[5-(苄基磺醯基）-4, 5, 6, 7-四氫吼啶[4, 3-c]IC:\2D-C0DE\91-01\90119473.ptd Page 97 1327569 V. Description of the invention (95) -3 -yl)cyclopropanecarboxamide; 995. N-(5-phenylethenyl)- 4,5,6,7 - tetrahydrogen 0 ratio. [4,3-c]D-pyrazol-3-yl)-(2-naphthalene)acetamide; 996. N-(5-phenylethenyl)-4,5,6,7-tetrahydro Pyridine [4,3-(:]pyrazol-3-yl)-phenylacetamide; 997. N,N-dimethyl-N'-{3-(2-phenyl-carbazole-4 - Ethylamino-4,5,6,7-tetrahydrogen ratio [4,3-c] ° ratio °-5-yl}urea; 9 98. N,N-didecyl- Ν' - {3-(Benzo[1,3]dioxoindol-5-yl)ethane with amino-4,5,6,7-tetrahydroindole. [4,3-c]吼° sit-5-yl}urea; mold 9 99· Ν, Ν-isopropyl-Ν'-{3-(benzo[1,3]dioxos-5 -yl)acetamido-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-5-yl}urea; 1000. N-[5-(1,3-benzoic) Oxygen-5-ylcarbonyl)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl]-3-methoxybenzoquinone; 1001. N-[ 5-(l,3-benzodioxoindol-5-ylcarbonyl)-4,5,6,7-tetrahydroacridine [4,3 - c ]pyrazole-3-yl]-3-benzene Oxybenzophenone; 1002. N-[5-(1,3-benzodioxoindol-5-ylcarbonyl)-4,5,6,7-tetrahydropyridine [4,3 - c ]pyr N-[5-(l,3-benzodioxoindol-5-ylcarbonyl)-4,5,6,7-φ Tetrahydroacridine [4,3-c]pyrazol-3-yl]-4-t-butylbenzamide; 1004. N-[5-(2-phenylethenyl)-4,5 , 6,7-tetrahydropyridine [4, 3-c]pyrazol-3-yl]acetamide; 1005. N-[5-(2-phenylethenyl)-4,5,6,7 -tetrahydropyridine [4, 3-c]pyrazol-3-yl]benzamide; 1 00 6_ N-[5-(benzylsulfonyl)-4, 5, 6, 7-tetrahydroindole Pyridine [4, 3-c]

C:\2D-OODE\91-Ol\90119473.ptd 第98頁 1327569 五、發明說明（96) 吡唑-3-基]-3-溴苯甲醯胺； 1007. N-[5-(苄基磺醯基）-4,5,6,7 -四氫咄啶[4,3-c] 口比吐一 3 -基]-3-氟苯甲酿胺； 1008. N-[5-(苄基磺醯基）-4,5,6,7 -四氫吡啶[4,3-c] 吡唑-3 -基]乙醯胺； 1009. N-[5-(窄基磺醯基）-4,5,6,7 -四氫吡啶[4,3-c] 吡唑-3 -基]苯曱醯胺； 1010.1^-[5-(甲基磺醯基）-4,5,6,7-四氫吡啶[4,3-〇] 〇比0坐_3 —基]—3_氣_苯甲醯胺； 1011. N-[5-(曱基磺醯基）-4,5, 6,7 -四氫 °比啶[4,3-c] 吡唑-3-基]-3-曱氧-苯曱醯胺； 1012. N-[5-(甲基磺醯基）-4,5,6,7 -四氫吡啶[4,3-c] 吡唑-3 -基]-4 -氟苯曱醯胺； 1013.1^-[5-(曱基磺醯基）-4,5,6,7-四氫吡啶[4,3-〇] 吡唑-3-基]-4-苯氧苯甲醯胺； 1014.1^-[5-(甲基磺醯基）-4,5,6,7-四氫吼啶[4,3-〇] 0比°坐-3_基]-4-苯氧苯曱酿胺； 1015. N-[5-(甲基磺醯基）-4,5, 6,7-四氫口比啶[4,3-〇] 〇比°坐__3_基]-4—第三丁基—苯甲酸胺> 1016. N-[5-(甲基磺醯基）-4,5, 6,7-四氫口比啶[4,3-(：] 吡唑-3 -基]乙醯胺； 1017. N-[5-(甲基磺醯基）-4,5,6,7 -四氫吡啶[4,3-c] 吡唑-3 -基]苯曱醯胺； 1018.1^-[5-(甲基磺醯基）-4,5,6,7-四氫咄啶[4,3-(：]C:\2D-OODE\91-Ol\90119473.ptd Page 98 1327569 V. INSTRUCTIONS (96) Pyrazol-3-yl]-3-bromobenzamide; 1007. N-[5-(Benzyl) Benzene sulfhydryl)-4,5,6,7-tetrahydroacridine [4,3-c] 比一 -3 -yl]-3-fluorobenzamide; 1008. N-[5-( Benzylsulfonyl)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-3-yl]acetamidine; 1009. N-[5-(N-ylsulfonyl) -4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-3-yl]benzamide; 1010.1^-[5-(methylsulfonyl)-4,5,6 , 7-tetrahydropyridine [4,3-〇] 〇 is 0 _3 — base] — 3 _ _ benzoguanamine; 1011. N-[5-(nonylsulfonyl)-4,5 , 6,7-tetrahydropyridinium [4,3-c]pyrazol-3-yl]-3-indolyl-benzoguanamine; 1012. N-[5-(methylsulfonyl)- 4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-3-yl]-4-fluorobenzoguanamine; 1013.1^-[5-(indolylsulfonyl)-4, 5,6,7-tetrahydropyridine [4,3-indolyl]pyrazol-3-yl]-4-phenoxybenzamide; 1014.1^-[5-(methylsulfonyl)-4,5 ,6,7-tetrahydroacridine [4,3-〇] 0 to ° -3 -yl-4-phenoxybenzoquinone; 1015. N-[5-(methylsulfonyl)- 4,5, 6,7-tetrahydropyrazine [4,3-〇] 〇 ratio ° sitting __3_ base]-4-t-butyl-benzene Ammonium formate> 1016. N-[5-(methylsulfonyl)-4,5,6,7-tetrahydropyridinium [4,3-(:]pyrazol-3-yl]acetamide 1017. N-[5-(Methylsulfonyl)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-3-yl]benzamide; 1018.1^-[ 5-(methylsulfonyl)-4,5,6,7-tetrahydroacridine [4,3-(:]

C:\2D-G0DE\91-01\90119473.ptd 第99頁 1327569 五、發明說明（97) 吡唑-3 -基]環丙烷羧醯胺； 1019.1^1-[5-(曱基磺醯基）-4,5,6,7-四氫吡啶[4,3-〇] p比σ坐_ 3 _基]苯基乙酿胺； 1020. Ν-[5-(嗜琳-8-石黃醯基）-4, 5, 6, 7-四氫11比口定 [4, 3-c]吡唑-3-基]-4-苯氧苯曱醯胺； 1021. Ν-[5-(喳啉-8 -磺醯基）-4,5,6,7-四氫吡啶 [4, 3 — c]°比唑-3-基]乙醯胺； 1 022. N-[ 5-苯曱醯基-4, 5, 6, 7-四氫吡啶[4, 3-c]吼唑 -3 -基]-(2_蔡）乙酿胺；鲁 1023. N-[5 -異丁 SI 基-4，5，6，7-四氫°比°定[4，3-。]〇比〇坐 -3 -基]-敗苯曱酿胺； 1024.1^-[5-苯基乙醯基-4,5,6,7-四氫咄啶[4,31]吡唑-3-基]-3-氟苯甲醯胺； 1025. N-[5 -苯基乙醯基-4,5,6,7-四氫咄啶[4,3-〇]咄唑-3-基]-3-曱氧苯曱醯胺； 1026· N-[5 -苯基乙醯基-4,5,6,7-四氫吡啶[4,3-〇]吡唑-3-基]-3-苯氧苯甲醯胺； 1 027. N-[ 5 -苯基乙醯基-4, 5, 6, 7 -四氫咄啶[4, 3-c]咄 φ。坐-3-基]-4-氟苯曱醯胺； 1028.1[5-苯基乙醢基-4,5,6,7-四氫吡啶[4,3-〇]吡唑-3-基]-4-苯氧苯曱醯胺； 1029. N-[5-苯基乙醯基-4，5，6，7 -四氫吼咬[4，3-c] 口比唑-3-基]-4-第三丁基-苯甲醯胺； 1030. N-[5 -苯基乙醯基-4,5,6,7-四氫咄啶[4,3-〇]咄C:\2D-G0DE\91-01\90119473.ptd Page 99 1327569 V. INSTRUCTIONS (97) Pyrazol-3-yl-cyclopropanecarboxamide; 1019.1^1-[5-(indolylsulfonyl) )-[5-(嗜琳-8-石) Astragalus)-4, 5, 6, 7-tetrahydro 11 is more specific than [4, 3-c]pyrazol-3-yl]-4-phenoxybenzamine; 1021. Ν-[5-(喳啉-8-sulfonyl)-4,5,6,7-tetrahydropyridine [4, 3 — c]° oxazol-3-yl]acetamide; 1 022. N-[ 5-phenylhydrazine 4-, 5, 6, 7-tetrahydropyridine [4, 3-c]oxazol-3 -yl]-(2_cai) ethylamine; Lu 1023. N-[5-isobutyl SI- 4,5,6,7-tetrahydrogen ratio ° [4,3-. 〇〇 -3 -3 -3 - yl]- benzophenone amine; 1024.1^-[5-phenylethyl fluorenyl-4,5,6,7-tetrahydroacridine [4,31]pyrazole-3 -yl]-3-fluorobenzamide; 1025. N-[5-phenylethenyl-4,5,6,7-tetrahydroacridine[4,3-indolyl]oxazol-3-yl -3-oxophenhydrin; 1026· N-[5-phenylethyl fluorenyl-4,5,6,7-tetrahydropyridine [4,3-indolyl]pyrazol-3-yl]- 3-phenoxybenzamide; 1 027. N-[5-phenylethenyl-4,5,6,7-tetrahydroacridine [4,3-c]咄φ. -3-yl]-4-fluorobenzamine; 1028.1 [5-phenylethenyl-4,5,6,7-tetrahydropyridine[4,3-indolyl]pyrazol-3-yl] -4-phenoxybenzamine; 1029. N-[5-phenylethenyl-4,5,6,7-tetrahydroindole [4,3-c] orthazol-3-yl] -4-t-butyl-benzamide; 1030. N-[5-phenylethenyl-4,5,6,7-tetrahydroacridine [4,3-〇]咄

C:\2D-OODE\91-01\9O119473.ptd 第100頁 1327569 五、發明說明（98) 唑-3-基]環丙烷羧醯胺； 1031. N-{ 5-(2 -呋喃曱醯基）-4, 5, 6, 7 -四氫吡啶 [4,3-c]吡唑-3-基}-4_第三丁基-苯曱醯胺； 1 0 32. N-{5-(2 -萘磺醯基）-4, 5, 6, 7 -四氫吡啶[4, 3-c] 吡唑-3 -基} - 3 -溴苯曱醯胺； 1033. N-{5-(2-°塞0分基）乙醢基-4, 5, 6, 7-四氫吼口定 [4,3-c]吡唑-3-基}-3-曱氧苯曱醯胺； 1 0 34. N-{ 5-(2 -噻吩基）乙醯基-4, 5, 6, 7-四氫吡啶 [4,3-c]咄唑-3-基卜3-苯氧苯甲醯胺； 1035.1{5-(2-噻吩基）乙醯基-4,5,6,7-四氫吡啶 [4,3-c]吡唑-3-基}-4-氟苯曱醯胺； 1036.1^-{5-(2-噻吩基）乙醯基-4,5,6,7-四氫吡啶 [4,3-c]吡唑-3-基}-4-苯氧苯甲醯胺； 1 0 37. N-{ 5-(2 -噻吩基）乙醯基-4, 5, 6, 7 -四氫吡啶 [4,3-c]吡唑-3-基}-4_第三丁基-苯曱醯胺； 1 03 8. N-{ 5-(2 -噻吩基）乙醯基-4, 5, 6, 7 -四氫吡啶 [4,3-c]吡唑-3-基}乙醯胺； 1039. N-{5-(2-°塞吩基）乙醯基-4,5，6，7-四氫吼口定 [4，3 - c ]吡唑-3 -基卜環丙烷羧醯胺； 1040. N-{5-(3 -三氟曱基苯）磺醯基_4,5,6,7-四氫吼啶 [4，3-c] 0比〇坐-3_基}_3 - 臭苯曱酿胺； 1041.1^-{5-(4-氣苯）磺醯基-4,5,6,7-四氫吡啶 [4,3-c]吡唑-3-基}-3-溴苯曱醯胺； 1042.1^-{5-(4-氟苯）磺醯基-4,5,6,7-四氫咄啶C:\2D-OODE\91-01\9O119473.ptd Page 100 1327569 V. INSTRUCTIONS (98) Zin-3-yl]cyclopropanecarboxamide; 1031. N-{ 5-(2-furan Base)-4, 5, 6, 7-tetrahydropyridine [4,3-c]pyrazol-3-yl}-4_t-butyl-benzoguanamine; 1 0 32. N-{5- (2-naphthosulfonyl)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-3-bromophenylamine; 1033. N-{5- (2-° plug 0 base) acetamyl-4, 5, 6, 7-tetrahydrofuran [4,3-c]pyrazol-3-yl}-3-oxobenzoquinone; 1 0 34. N-{ 5-(2-Thienyl)ethenyl-4,5,6,7-tetrahydropyridine[4,3-c]oxazol-3-yl-3-benzophenone Indoleamine; 1035.1{5-(2-thienyl)ethenyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-4-fluorobenzamide 1036.1^-{5-(2-Thienyl)ethinyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-4-phenoxybenzidine Amine; 1 0 37. N-{ 5-(2-thiophenyl)ethinyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-4_ Tributyl-benzoguanamine; 1 03 8. N-{ 5-(2-thiophenyl)ethenyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-3 -yl}acetamide; 1039. N-{5-(2-°secenyl)ethinyl-4,5 6,7-tetrahydroindolizine [4,3 - c ]pyrazol-3-ylcyclopropanecarboxamide; 1040. N-{5-(3-trifluorodecylbenzene)sulfonyl _4 ,5,6,7-tetrahydroacridine [4,3-c] 0 is more than -3 -yl}_3 - odorous benzoquinone; 1041.1^-{5-(4-gasbenzene)sulfonyl -4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-3-yl}-3-bromobenzoguanamine; 1042.1^-{5-(4-fluorophenyl)sulfonyl -4,5,6,7-tetrahydroacridine

C:\2D-C0DE\91-01\90119473.ptd 第101頁 1327569 五、發明說明（99) [4,3-c]吡唑-3-基}-3_溴苯甲醯胺； 1043.1{5-(4-甲氧苯）磺醯基-4,5,6,7-四氫吼啶 [4,3-c]吡唑-3-基}-3-溴苯甲醯胺； 1044. N-{5-(4-第三丁基苯）磺醯基-4, 5, 6, 7-四氫吼啶 [4,3-c]吡唑-3-基}-3-溴苯曱醯胺； 1045. N-{5-(4-曱苯磺醯基）-4,5,6,7-四氫吼啶 [4,3-c]吡唑-3-基}-3-溴苯甲醯胺； 1046. N-{5-( 17奎琳-8-石黃醯基）-4，5，6，四氫口比口定 [4,3-c]吼唑-3-基}-3-氟苯甲醯胺； • 1047. N-{5-(喳啉-8 -磺醯基）-4,5,6,7 -四氫吡啶 [4,3-c]呲唑-3 -基}-3_甲氧-苯曱醯胺； 1048. N-{5-(嗜啉-8-石黃醯基）-4，5, 6, 7 -四氫D比0定 [4,3-c]吡唑-3-基}-4-氟-苯曱醯胺； 1049. N-{5-(喳啉-8 -磺醯基）-4,5,6,7-四氫吼啶 [4,3-c]吡唑-3-基}-4 -苯氧-苯甲醯胺； 1050. N-{5-(喳啉-8 -磺醯基）-4,5,6,7 -四氫吡啶 [4,3-c]吡唑-3-基}-4-第、三丁基-苯曱醯胺； 1051. N-{5-(喳啉-8 -磺醯基）-4, 5, 6, 7 -四氫吡啶 • 4,3-c]吡唑-3-基}-苯曱醯胺； 1052. N-{5-(喳啉-8 -磺醯基）-4,5,6,7-四氫吡啶 [4, 3-c]吡唑-3-基卜環丙烷羧醯胺； 1 0 53. N-{5-(喳'^ 啉-2 -羰基）-4, 5, 6, 7-四氫吼啶 [4,3-c]吡唑-3-基}-3-苯氧苯甲醯胺； 1054. N-{5-(喳 g 啉-2 -羰基）-4,5,6,7-四氫咄啶 illC:\2D-C0DE\91-01\90119473.ptd Page 101 1327569 V. INSTRUCTIONS (99) [4,3-c]pyrazol-3-yl}-3_bromobenzamide; 1043.1{ 5-(4-methoxyphenyl)sulfonyl-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-3-yl}-3-bromobenzamide; 1044. N-{5-(4-Tertibutylbenzene)sulfonyl-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-3-yl}-3-bromophenylhydrazine醯amine; 1045. N-{5-(4-indolylsulfonyl)-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-3-yl}-3-bromo Benzalamine; 1046. N-{5-(17-Quinol-8-Astrachinin)-4,5,6, tetrahydrol-portion [4,3-c]oxazol-3-yl}- 3-fluorobenzamide; • 1047. N-{5-(porphyrin-8-sulfonyl)-4,5,6,7-tetrahydropyridine [4,3-c]carbazole-3 }}-3_methoxy-benzoguanamine; 1048. N-{5-(Phenyl-8- sulphate)-4,5, 6, 7-tetrahydro D ratio 0 [4,3-c Pyrazol-3-yl}-4-fluoro-benzoguanamine; 1049. N-{5-(porphyrin-8-sulfonyl)-4,5,6,7-tetrahydroacridine [4] , 3-c]pyrazol-3-yl}-4-phenoxy-benzamide; 1050. N-{5-(porphyrin-8-sulfonyl)-4,5,6,7-four Hydropyridine [4,3-c]pyrazol-3-yl}-4-, tert-butyl-benzoguanamine; 1051. N-{5-(porphyrin-8-sulfonyl)-4, 5, 6, 7-tetrahydropyridine • 4,3-c]pyrazol-3-yl}-benzoguanamine; 1052. N-{5-(porphyrin-8-sulfonyl)-4,5,6 , 7-tetrahydropyridine [4, 3-c]pyrazol-3-ylcyclopropanecarboxamide; 1 0 53. N-{5-(喳'^ oxalin-2-carbonyl)-4, 5, 6, 7-tetrahydroacridine [4,3-c]pyrazol-3-yl}-3-phenoxybenzamide; 1054. N-{5-(喳g porphyrin-2-carbonyl)-4 ,5,6,7-tetrahydroacridine ill

mm I! C:\2D-OODE\91-Ol\90119473.ptd 第102頁 1327569 五、發明說明（100) [4,3-c]吡唑-3-基}-4_第三丁基-苯曱醯胺； 1055.1{5-[2-(2-噻吩基）乙醯基]-4,5,6,7-四氫吡啶 [4,3-c]吡唑-3 -基}苯甲醯胺； 1056. N-{5-苯續醯基-4，5，6，7-四氫°比°定[4，3-c] °比〇坐 - 3 -基} _ 3 _ >臭苯曱酿胺； 1057. N-{5 -苯石黃醯基-4，5,6，7-四氫D比咬[4，3-c] °比〇坐 _3 -基}_3-敗苯曱酿胺； 1058.1^-{5-苯石黃酿基-4，5，6，7-四氫°比°定[4，3-(：]11比〇坐 -3_基}_3_苯氧苯甲酿胺； 1059.1'1-{5-苯確蕴基-4，5，6，7-四氫11比°定[4，3-(：]11比〇坐 -3 -基}-4-氟苯甲醯胺； 1060. N-{5-苯石黃醯基-4，5，6，7-四氫°比。定[4，3-c] π比。坐 _3_基}_4_苯氧苯曱酿胺； 1061. Ν-{5-苯石黃醯基-4，5,6,7-四氫°比。定[4，3-c] °比唾 -3-基}-4-第三丁基-苯曱醯胺； 1062. N-{5-苯績醯基-4，5，6，7-四氫吼。定[4，3-c] n比0坐 -3 -基}乙醯胺； 1063.1'}-{5-苯石黃醯基-4，5，6，7-四氫'3比°定[4，3-(：]11比〇坐 -3-基}苯曱醯胺； 1064. N-{5 -苯石黃贐基-4，5，6，7-四氫n比0定[4，3-c] D比0坐 _3_基}_環丙炫叛酿胺； 1065. N-{5-苄基磺醯基-4,5,6,7-四氫咄啶[4,3-〇]吡。坐-3_基}_3_甲氧苯甲酿胺； 1066. N-{5-爷基磺醯基-4,5,6,7-四氫吡啶[4,3-(：]吡Mm I! C:\2D-OODE\91-Ol\90119473.ptd Page 102 1327569 V. INSTRUCTIONS (100) [4,3-c]pyrazol-3-yl}-4_t-butyl- Benzoylamine; 1055.1{5-[2-(2-thienyl)ethenyl]-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-3-yl}benzene醯amine; 1056. N-{5-Benzene fluorenyl-4,5,6,7-tetrahydrogen ratio °[4,3-c] ° ratio 〇 sitting - 3 -yl} _ 3 _ > Odor benzoquinone amine; 1057. N-{5 - benzoate xanthyl-4,5,6,7-tetrahydro D ratio bite [4,3-c] ° 〇 sitting _3 -基}_3-benzene Brewing amine; 1058.1^-{5-Phenyl yellow-branched-4,5,6,7-tetrahydrogen ratio °[4,3-(:]11 than squat-3_yl}_3_benzene Oxybenzamide; 1059.1'1-{5-Benzene-4,5,6,7-tetrahydro 11 ratio [4,3-(:]11 than 〇-3-yl}- 4-fluorobenzamide; 1060. N-{5-Phenylxanthyl-4,5,6,7-tetrahydrogen ratio. [4,3-c] π ratio. Sit_3_基}_4 _phenoxybenzoquinone amine; 1061. Ν-{5-phenylxanthyl-4,5,6,7-tetrahydrogen ratio. [4,3-c] ° than sal-3-yl}-4 - tert-butyl-benzoguanamine; 1062. N-{5-phenylindole-4,5,6,7-tetrahydroindole. [4,3-c] n ratio 0 sitting -3 Acetamine; 1063.1'}-{5- Phenylxanthyl-4,5,6,7-tetrahydro'3 ratio [4,3-(:]11 is more than 〇-3-yl}phenyl hydrazide; 1064. N-{5 - phenylene Astragalo-4,5,6,7-tetrahydron is 0 to [4,3-c] D is 0 to sit _3_yl}_cyclopropane retinol; 1065. N-{5-benzyl sulfonate Mercapto-4,5,6,7-tetrahydroacridine [4,3-indolyl]pyridinium-sodium-3_yl}_3_methoxybenzoic acid; 1066. N-{5-arylsulfonate 4-,5,6,7-tetrahydropyridine [4,3-(:]pyridyl

C:\2D-C0DE\91-01\90119473.ptd 第103頁 1327569 五、發明說明（101) 唑-3-基}-3-苯氧苯甲醯胺； 1067. N-{5-窄基磺醯基-4,5,6,7-四氫吡啶[4,3-〇]吡 β坐_3_基}_4_氣苯甲蕴胺； 1068. Ν-{5-辛基磺醯基-4,5,6,7-四氫吡啶[4,3-(：]吡唑-3-基}-4-苯氧苯甲醯胺； 1 0 6 9. Ν-{ 5-辛基磺醯基-4, 5, 6, 7-四氫吡啶[4, 3-c]吡。坐-3-基}_4-第三丁基-苯曱酿胺； 1 070. Ν-苄基-Ν’ - {3-(2-(2 -萘）丙醯胺基）-4,5,6,7 -四氫°比D各并[4，3 - c ] °比°坐-5 -基}脲； 1071. N-辛基-Ν’ - (3-(2-(6-曱氧-2-萘）丙醯胺基） -4，5，6,7-四氫0比11各并[4,3-(：]°比〇坐-5-基}脲； 1072. N-芊基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7-四氫吡口各并[4，3 - c ] n比σ坐-5 -基}脲； 1073. Ν-苄基-Ν’-{3-(3-甲氧-苯曱醯胺基）-4,5,6,7-四氫°比D各并[4，3 - c ]"比°坐-5 -基}脲； 1074. N-苄基-N’-{3-(3-甲基-丁醯胺基）-4,5,6,7-四氫吼p各并[4，3 - c ] °比°坐-5 -基}脲； 1 075. N-苄基-Ν’ - {3-(4-苯基）苯乙醯胺基-4, 5, 6, 7 -四 .氫°比ρ各并[4，3 - c ]"比°坐-5 -基}脲； 1076. Ν -丁基-Ν’-{3-(2-(2 -萘）丙醢胺基）-4,5,6,7-四氫D比D各并[4，3 _ c ] °比嗤-5 -基}脲； 1077. N - 丁基-N’-{3-(2-(6-曱氧-2-萘）丙醯胺基） -4, 5, 6, 7-四氫吼11 各并[4, 3-c] °比°坐-5-基}脲； 1078. N-丁基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7-四氫吡C:\2D-C0DE\91-01\90119473.ptd Page 103 1327569 V. INSTRUCTIONS (101) Zyrazin-3-yl}-3-phenoxybenzamide; 1067. N-{5-Narrow base Sulfo-yl-4,5,6,7-tetrahydropyridine [4,3-indolyl]pyridinyl-1 _3_yl}_4_gas benzylamine; 1068. Ν-{5-octylsulfonyl -4,5,6,7-tetrahydropyridine [4,3-(:]pyrazol-3-yl}-4-phenoxybenzamide; 1 0 6 9. Ν-{ 5-octylsulfonate Mercapto-4,5,6,7-tetrahydropyridine [4,3-c]pyr.,sodium-3-yl}_4-tert-butyl-benzoquinone; 1 070. Ν-benzyl-Ν '-{3-(2-(2-naphthalene)propanylamino)-4,5,6,7-tetrahydrogen ratio D and [4,3 - c ] ° ratio ° sitting -5 -yl} Urea; 1071. N-octyl-Ν'-(3-(2-(6-oxime-2-naphthalene)propanylamino)-4,5,6,7-tetrahydro 0 to 11 each [ 4,3-(:]°〇〇-5-yl}urea; 1072. N-mercapto-Ν' - {3-(2-naphthyl)acetamido-4, 5, 6, 7-four Hydropyrryl groups each [4,3 - c ] n ratio σ--5-yl}urea; 1073. Ν-benzyl-Ν'-{3-(3-methoxy-benzoguanamine)-4 , 5,6,7-tetrahydrogen ratio D and [4,3 - c ]" ratio ° sit-5-yl}urea; 1074. N-benzyl-N'-{3-(3-A -butyrylamino)-4,5,6,7-tetrahydroindole p each [4,3 - c ] ° ratio ° sitting - 5-amino}urea; 1 075. N-benzyl-Ν'-{3-(4-phenyl)phenylethylamino-4, 5, 6, 7-tetra. Hydrogen ratio ρ and [4 ,3 - c ]"比°-5-yl}urea; 1076. Ν-butyl-Ν'-{3-(2-(2-naphthyl)propylamino)-4,5,6, 7-tetrahydrogen D ratio D and [4,3 _ c ] ° than 嗤-5 -yl} urea; 1077. N - butyl-N'-{3-(2-(6-oxime-2- Naphthalene) propylamino) -4, 5, 6, 7-tetrahydroindole 11 each [4, 3-c] ° ratio -5-yl}urea; 1078. N-butyl-Ν' - {3-(2-naphthyl)acetamido-4, 5, 6, 7-tetrahydropyridyl

C:\2D-C0DE\91-01\90119473.ptd 第104頁 1327569 五、發明說明（102) 口各并[4，3 - c ] °比°坐-5 -基丨脲； 1079. N- 丁基-N’-{3-(3-曱氧-丁醯胺基）-4,5,6,7-四氫0比11各并[4，3 - c ]吼°坐-5 -基}脲； 1080. N- 丁基-N’-{3-[2-(4-苯基-3-氟-苯基）丙醯胺基]-4，5，6，7-四氫11比11各并[4，3-〇]'1比°坐-5-基}脲； 1081. N- 丁基-Ν’ - {3-苯曱醯胺基-4, 5, 6, 7-四氫吡咯并 1082. Ν- 丁基-Ν’ - {3 -苯乙醯胺基-4, 5,6,7-四氫咄咯并 [4，3 - c ] °比 °坐-5 -基}脲； 1083. Ν-乙基-Ν’ - (3-(2-(2 -萘）丙醯胺基）-4, 5, 6, 7 -四氫D比洛并[4, 3 - c ] °比°坐-5 -基}脲； 1084. N-乙基-N’-{3-(2-(6-曱氧-2 -萘）丙醯胺基） -4,5，6，7-四氫°比11各并[4,3-(：]'1比°坐-5-基}脲； 1085. N-乙基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7 -四氫吼 0各并[4，3 - c ] °比°坐-5 -基}脲； 1086. Ν-乙基-Ν’ - {3-(3-曱氧-丁醯胺基）-4,5,6，7-四氫0比D各并[4，3 - c ] °比°坐-5 -基}脲； 1087. N-乙基-N’-{3-(4-氟苯曱醯胺基）-4,5,6,7 -四氫 °比p各并[4，3 - c ]吼°坐-5 -基}脲； 1088. N-乙基-Ν’ - {3-(4 -苯基）苯乙醯胺基-4, 5, 6, 7-四氫11比略并[4，3 - c ] °比°坐-5 -基}脲； 1089. Ν-乙基- Ν’ _{3-[2-(4_苯基_3_ it -苯基）丙酿胺基]-4，5，6, 7-四氫°比略并[4，3-c] °比。坐-5-基}脲； 1090. N-乙基-Ν’ - {3-苯曱醯胺基-4, 5, 6, 7-四氫咄咯并 m C:\2D-00DEWl-01\90119473.ptd 第105頁 1327569 五、發明說明（103) [4，3 - c ] °比 °坐-5 -基}脲； 1091. N-乙基-Ν’ - {3 -苯乙醯胺基-4, 5, 6, 7-四氫吡咯并 [4，3 - c ] °比 °坐-5 -基}脲； 1092. Ν-異丙基-Ν’ - {3-U -曱基-吲哚-3 -基）乙醯胺基 -4，5，6, 7 -四氫D比ρ各并[4,3-c] °比°坐-5-基}脲； 1093. N-異丙基-N’-{3-(2-(2 -萘）丙醯胺基）-4,5,6,7-四氫°比p各并[4, 3 - c ]吼°坐-5 -基}脲； 1094. N -異丙基-N’-{3-(2-(6-甲氧-2 -萘）丙醯胺基） -4，5，6，7 -四氫0比p各并[4,3-c] 0比。坐-5-基}脲；馨1095. N -異丙基-Ν’ - {3-(2 -苯基-1,3 -噻唑-4 -基）乙醯胺基-4, 5，6，7 -四氫吼11各并[4，3-c] °比°坐-5-基}脲； 1096. Ν -異丙基-Ν’-{3-(3 -氟苯曱醯胺基）-4,5,6,7 -四氫°比ρ各并[4，3 - c ] °比°坐-5 -基}脲； 1097. Ν -異丙基-Ν’ - {3-(3-曱氧-苯曱醯胺基） -4，5，6，7-四氫D比略并[4,3-c] °比。坐-5-基}脲； 1098. N-異丙基-N’-{3-(4-氟-苯曱醯胺基）-4,5,6,7-四氫n比p各并[4，3 - c ] °比°坐-5 -基}脲； 1099. N -異丙基-Ν’ - {3-(4-苯基）苯乙醯胺基-4, 5, 6, 7- 氫°比11各并[4，3 - c ] °比β坐-5 -基}脲； 1 100. Ν -異丙基-Ν’ - {3-(4-第三丁基-苯曱醯胺基） -4，5，6，7-四氫吼°各并[4,3-c] D比0坐-5-基}脲； 1101. N -異丙基-Ν’ _{3_[2_(4_苯基氣-苯基）丙酿胺基]-4, 5, 6,7 -四氫 Β比 ρ各并[4, 坐-5-基}脲； 1102. N-異丙基-Ν’-{3-[4-(1-咄咯啶-2 -酮）]苯乙醯胺C:\2D-C0DE\91-01\90119473.ptd Page 104 1327569 V. INSTRUCTIONS (102) Mouth [4,3 - c ] ° ratio ° sitting -5-carbazide; 1079. N- Butyl-N'-{3-(3-oxo-butylammonium)-4,5,6,7-tetrahydro 0 to 11 each [4,3 - c ]吼°-5-yl Urea; 1080. N-butyl-N'-{3-[2-(4-phenyl-3-fluoro-phenyl)propanylamino]-4,5,6,7-tetrahydro 11 ratio 11 each [4,3-〇]'1°°°-5-yl}urea; 1081. N-butyl-Ν' - {3-benzoguanamine-4, 5, 6, 7-four Hydropyrrolidone 1082. Ν-butyl-Ν' - {3-phenylethylamino-4,5,6,7-tetrahydroindole[4,3 - c] °°°-5-yl Urea; 1083. Ν-ethyl-Ν' - (3-(2-(2-naphthyl)propanylamino)-4, 5, 6, 7-tetrahydro D-bi-l[4, 3 - c ° °°°-5-yl}urea; 1084. N-ethyl-N'-{3-(2-(6-oxime-2-naphthalene)propanylamino)-4,5,6, 7-tetrahydrogen ratio 11 and [4,3-(:]'1 ratio °-5-yl}urea; 1085. N-ethyl-Ν' - {3-(2-naphthyl)acetamide Base-4, 5, 6, 7-tetrahydroindole 0 and [4,3 - c ] ° ratio ° sit-5-yl}urea; 1086. Ν-ethyl-Ν' - {3-(3- Oxygen-butylamino)-4,5,6,7-tetrahydro 0 to D and [4 3 - c ] °°°-5-yl}urea; 1087. N-ethyl-N'-{3-(4-fluorophenylguanidino)-4,5,6,7-tetrahydrogen More than p and [4,3 - c ]吼° sit-5-yl}urea; 1088. N-ethyl-Ν' - {3-(4-phenyl)phenethylamino-4, 5, 6, 7-tetrahydrogen 11 ratio slightly [4,3 - c ] ° ratio ° sitting -5 -yl} urea; 1089. Ν-ethyl- Ν' _{3-[2-(4_phenyl_ 3_ it-phenyl) propylamino]-4,5,6,7-tetrahydrogen ratio slightly [4,3-c] °. Sodium-5-yl}urea; 1090. N-ethyl -Ν' - {3-benzoguanamine-4, 5, 6, 7-tetrahydroindole m C:\2D-00DEWl-01\90119473.ptd Page 105 1327569 V. Description of invention (103) [4,3 - c ] °°°-5-yl}urea; 1091. N-ethyl-Ν' - {3-phenethylamino-4, 5, 6, 7-tetrahydropyrrolo[ 4,3 - c ] °°°-5-yl}urea; 1092. Ν-isopropyl-Ν' - {3-U-mercapto-indol-3-yl)acetamido-4, 5,6,7-tetrahydrogen D ratio ρ and [4,3-c] ° ratio °-5-yl}urea; 1093. N-isopropyl-N'-{3-(2-(2 -naphthalene)propanolamine)-4,5,6,7-tetrahydrogen ratio p and [4, 3 - c ]吼° sit-5-yl}urea; 1094. N-isopropyl-N '-{3-(2-(6-methoxy-2-naphthalene)propanoid Amino) -4,5,6,7-tetrahydro 0 is a ratio of p to [4,3-c] 0. Sodium-5-yl urea; succinyl 1095. N-isopropyl-indole-{3-(2-phenyl-1,3-thiazol-4-yl)acetamido-4, 5,6, 7-tetrahydroanthracene 11 each [4,3-c] ° ratio °-5-yl}urea; 1096. Ν-isopropyl-Ν'-{3-(3-fluorophenylguanidino) -4,5,6,7 -tetrahydrogen ratio ρ and [4,3 - c ] ° ratio ° sit-5 -yl}urea; 1097. Ν-isopropyl-Ν' - {3-(3 - oxime-benzoguanamine) -4,5,6,7-tetrahydro D ratio slightly [4,3-c] ° ratio. Sodium-5-yl urea; 1098. N-isopropyl-N'-{3-(4-fluoro-benzoguanamine)-4,5,6,7-tetrahydron ratio p and [ 4,3 - c ] °°°-5-yl}urea; 1099. N-isopropyl-Ν' - {3-(4-phenyl)phenethylamino-4, 5, 6, 7 - Hydrogen ° ratio of 11 and [4,3 - c ] ° ratio β sit-5-yl}urea; 1 100. Ν-isopropyl-Ν' - {3-(4-t-butyl-benzoquinone Amidino) -4,5,6,7-tetrahydroindole °[4,3-c] D is 0--5-yl}urea; 1101. N-isopropyl-Ν' _{3_ [2_(4_Phenyl-phenyl)propylamino]-4, 5, 6,7-tetrahydroindole ratio ρ[4, sit-5-yl}urea; 1102. N-isopropyl Base-Ν'-{3-[4-(1-咄rrolidine-2-one)]phenethylamine

C:\2D-OODE\91-Ol\90119473.ptd 第106頁 1327569 五、發明說明（104) 基-4, 5, 6, 7 -四氫吼17各并[4, 3-c] p比。坐-5-基}脲； 1103. N-異丙基-Ν’ - {3-乙醯胺基-4, 5, 6, 7-四氫咄咯并 [4,3-〇]吼°坐-5-基}脲； 1104. Ν-異丙基-Ν’ - {3 -苯甲醯胺基-4, 5, 6, 7-四氫吡咯并[4，3-c]D比。坐-5-基}脲； 1105. N-異丙基-Ν’ - {3 -環丙烷羧醯胺基-4, 5, 6, 7 -四氫 "比ρ各并[4，3 - c ] D比°坐-5 -基}脲； 1106. N-異丙基-Ν’ - {3 -苯乙醯胺基-4, 5, 6,7 -四氫吡咯并[4，3-c]°比吐-5-基}脲； 1107· N-苯基-Ν’ - {3-(2_萘）乙醯胺基-4, 5, 6, 7-四氫吡 0各并[4，3 - c ] °比。坐-5 -基}脲； 1108. Ν-苯基-Ν’-{3-(3-氟苯曱醯胺基）-4,5,6,7 -四氫 0比°各并[4，3 - c ]吼°坐-5 -基}脲； 1109. Ν-苯基-Ν’ - {3-(3_ 甲基-苯甲醯胺基）-4, 5, 6,7-四氫D比洛并[4，3 - c ] π比。坐-5 -基}脲； 1110. Ν-苯基-Ν’-{3-(3-苯氧-苯曱醯胺基）-4,5,6,7-四氩°比ρ各并[4，3 - c ] °比。坐-5 -基}脲； 1111. Ν-苯基-Ν’-{3-(4 -苯氧-苯甲醯胺基）-4,5,6,7-四氫吼°各并[4，3 - c ]吼°坐-5 -基}脲； 1112. Ν-苯基-Ν’ - {3-(4_第三丁基-苯曱醯胺基） -4,5，6, 7—四氫〇比口各并[4, 3_c] 0比口坐_5_基}脲； 1113. Ν-苯基-Ν’ - {3-乙醯胺基-4, 5, 6, 7-四氫吼咯并 [4,3-(：]吼。坐-5-基}脲； 1114. Ν-笨基-Ν’ - {3 -苯曱醯胺基-4, 5,6,7 -四氫咄咯并C:\2D-OODE\91-Ol\90119473.ptd Page 106 1327569 V. INSTRUCTIONS (104) BASE-4, 5, 6, 7-tetrahydroindole 17 and [4, 3-c] p ratio . Sodium-5-yl urea; 1103. N-isopropyl-Ν' - {3-acetamido-4, 5, 6, 7-tetrahydroindole[4,3-〇]吼 sitting -5-yl}urea; 1104. Ν-isopropyl-Ν' - {3-benzamide-5,5,6,7-tetrahydropyrrolo[4,3-c]D ratio. Sodium-5-yl}urea; 1105. N-isopropyl-Ν'-{3-cyclopropanecarbamoylamino-4, 5, 6, 7-tetrahydro" ratio ρ和[4,3 - c ] D ratio ° sitting -5 -yl}urea; 1106. N-isopropyl-Ν' - {3 - phenethylamino-4, 5, 6,7-tetrahydropyrrolo[4,3- c]° 吐-5-yl}urea; 1107· N-phenyl-Ν' - {3-(2_naphthalene)acetamido-4, 5, 6, 7-tetrahydropyridinium each [ 4,3 - c ] ° ratio. Sodium-5-yl}urea; 1108. Ν-phenyl-Ν'-{3-(3-fluorophenylguanidino)-4,5,6,7-tetrahydro- 0 ratio °[4, 3 - c ]吼° sit-5-yl}urea; 1109. Ν-phenyl-Ν' - {3-(3_methyl-benzamide)-4, 5, 6,7-tetrahydro D Bilo and [4,3 - c ] π ratio. Sodium-5-yl}urea; 1110. Ν-phenyl-Ν'-{3-(3-phenoxy-phenylguanidino)-4,5,6,7-tetra-argon ratio ρ 4,3 - c ] ° ratio. Sodium-5-yl}urea; 1111. Ν-phenyl-Ν'-{3-(4-phenoxy-benzamide)-4,5,6,7-tetrahydroindole °[4 ,3 - c ]吼° sit-5-yl}urea; 1112. Ν-phenyl-Ν' - {3-(4_t-butyl-benzoguanamine)-4,5,6,7 - tetrahydroanthracene is more than [4, 3_c] 0 than the mouth _5_yl} urea; 1113. Ν-phenyl-Ν' - {3-acetamido-4, 5, 6, 7- Tetrahydroindolo[4,3-(:]吼.sodium-5-yl}urea; 1114. Ν-stupyl-Ν' - {3-benzoguanamine-4, 5,6,7 - Tetrahydropyrrole

C:\2D-00DE\91-01\90119473.ptd 第107頁 1327569 五、發明說明（105) [斗^-^吼唾-云-基丨脲； 1115. N-苯基-Ν’ - {3-環丙烷羧醯胺基-4, 5, 6, 7-四氫吡 0各并[4，3 - c ] °比°坐-5 -基}脲； 1116. Ν-苯基-Ν’ - {3-苯乙醯胺基-4, 5, 6, 7-四氫吡咯并 [4，3 - c ]咄唑-5 -基}脲； 1117. Ν-丙基-Ν’ - {3-(4 -苯基）苯乙醯胺基-4, 5, 6, 7-四氫0比D各并[4，3 - c ] °比°坐-5 -基}脲； 1118. N- 丁基-Ν’ - {3-(2 -萘）乙醯胺基-6, 6 -二甲基 -4，6 -二氫吼11各并[3,4-c] D比。坐- l-基}脲； 1119. N- 丁基-Ν’ - {3-(3 -溴）苯曱醯胺基-6,6 -二曱基 _4，6_二氮吼11各弁[3，4-c] °比°坐_1_基}脈； 1120. N- 丁基-Ν’ - {3-(4-氟）苯甲醯胺基-6, 6 -二甲基 _4，6_二氮D比Β各弁[3，4_c] π比β坐-1_基}脈； 1121. Ν -丁基-Ν’ - {3-(4-第三丁基）苯甲醯胺基-6, 6 -二曱基-4，6_二氮0比略并[3，4_c] 0比0坐_1_基}脈； 1122. N- 丁基-Ν’ - {3 -環丙烷羧醯胺基-6, 6-二甲基 -4，6 -二氫。比ρ各并[3，4 - c ] °比。坐-1 -基}脲；曱基-4, 6 1123. Ν- 丁基-Ν’ - {3 -苯乙醯胺基-6,6-0比口各并[3，4 - c ] 0比°坐-5 -基}脲；甲基 1124. N-乙基-Ν’- {3-(2 -萘）乙醯胺基-6, 6 -4，6 -二氫吼Β各并[3，4 - c ] °比°坐-1 -基}脲； 1125. Ν_乙基_Ν’ _{3_(3_漠.）苯曱酿胺基_6，6_二曱基 -4，6 -二氫吼°各并[3，4 - c ] °比。坐-1 -基}脲； 1126. Ν-乙基-Ν’- {3_(4-氟）苯曱醯胺基-6, 6 -二甲基C:\2D-00DE\91-01\90119473.ptd Page 107 1327569 V. Description of invention (105) [斗^-^吼吼-cloud-giving urea; 1115. N-phenyl-Ν' - { 3-cyclopropanecarboxyguanamine-4,5,6,7-tetrahydropyridinium each [4,3 - c ] ° ratio ° sit-5-yl}urea; 1116. Ν-phenyl-Ν' - {3-Phenylethylamino-4,5,6,7-tetrahydropyrrolo[4,3-c]indazol-5-yl}urea; 1117. Ν-propyl-Ν' - {3 -(4-phenyl)phenethylamino-4,5,6,7-tetrahydrogen 0 to D each [4,3 - c ] ° ratio ° sit-5-yl}urea; 1118. N- Butyl-Ν'-{3-(2-naphthalene)acetamido-6,6-dimethyl-4,6-dihydroindole 11 each [3,4-c] D ratio. Sodium-l-yl}urea; 1119. N-butyl-indole-{3-(3-bromo)benzoguanamine-6,6-dimercapto-4,6-diazepine 11 [3,4-c] °°°_1_1 base}; 1120. N-butyl-Ν' - {3-(4-fluoro)benzimidamide-6,6-dimethyl_ 4,6_Dinitrogen D is more than 弁[3,4_c] π is β-1_基}; 1121. Ν-butyl-Ν' - {3-(4-t-butyl)benzate Amidino-6,6-dimercapto-4,6-diaza 0 is slightly more than [3,4_c] 0 to 0 sitting on the _1_yl} vein; 1122. N-butyl-Ν' - {3 - cyclopropanecarboxyguanamine-6,6-dimethyl-4,6-dihydrogen. The ratio ρ is [3,4 - c ] ° ratio. Sodium-1 -yl urea; thiol-4, 6 1123. Ν-butyl-Ν' - {3 - phenethylamino-6,6-0 than each [3,4 - c ] 0 Sodium-5-yl urea; methyl 1124. N-ethyl-Ν'- {3-(2-naphthalene)acetamido-6,6-4,6-dihydroindole 3,4 - c ] ° ratio °-1 -yl}urea; 1125. Ν_ethyl_Ν' _{3_(3_ desert.) benzoquinone amine _6,6_dimercapto-4 , 6-dihydroindole ° and [3,4 - c ] ° ratio. Sodium-1 -yl}urea; 1126. Ν-ethyl-Ν'- {3_(4-fluoro)benzoguanamine-6,6-dimethyl

C:\2D-CODE\9卜01\90119473.ptd 第108頁 1327569 五 '發明說明（106) -4，6 -二氫吼p各并[3，4 - c ] °比。坐-1 -基}脲； 1127. N-乙基-Ν’ - {3-(4-第三丁基）苯曱醯胺基-6, 6 -二曱基-4,6-二氫吡咯并[3,4-(：]0比唑-1-基}脲； 1128. Ν-乙基-Ν’- {3 -環丙烷羧醯胺基-6, 6 -二曱基 -4，6-二氫°比洛并[3，4-〇]17比。坐-1-基}脲； 1129. Ν-乙基-Ν’ - {3 -苯乙醯胺基-6, 6 -二甲基-4, 6 -二氫°比各并[3，4 - c ] °比°坐-5 -基}脲； 1130.1{5-(2-噻吩基-乙醯基）-6,6-二甲基-4,6-二氫吡啶[3, 4-c]咄唑-1-基}-(3 -溴）苯甲醯胺； 1131.^{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶[3, 4-c]吡唑-3 -基}-(2 -萘）乙醯胺； 1132.1{5-(2-噻吩基-乙醯基）-6,6-二甲基-4,6-二氫吼啶[3，4 - c ]吡唑-3 -基} - (4 -氟）苯曱醯胺； 1133.1^-{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶[3,4-c]吡唑-3-基}-(4-第三丁基）苯曱醯胺； 1134.1^-{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶[3，4 - c ]吡唑-3 -基}環丙烷羧醢胺； 1135.1^-{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶[3,4-c]吡唑-3-基}苯乙醯胺； 1136.1^-{5-(4-氟苯曱醯基）-6,6-二曱基-4,6-二氫 »比啶[3,4-c]吡唑-1-基}-(3-溴）苯甲醯胺； 1137. ^{5-(4-氟苯曱醯基）-6,6-二曱基-4,6-二氫吼啶[3,4-c]吡唑-1-基}-(4-氟）苯曱醯胺； 1138. [{5-(4-氟苯曱醯基）-6,6-二甲基-4,6-二氫C:\2D-CODE\9 Bu 01\90119473.ptd Page 108 1327569 Five 'Inventions (106) -4,6-Dihydroindole p each [3,4 - c ] ° ratio. Sodium-1 -yl}urea; 1127. N-ethyl-Ν'-{3-(4-t-butyl)benzoguanamine-6,6-dimercapto-4,6-dihydropyrrole And [3,4-(:]0-pyrazol-1-yl}urea; 1128. Ν-ethyl-Ν'- {3-cyclopropanecarboxamido-6,6-dimercapto-4,6 - dihydro-pyrylene and [3,4-〇]17 ratio. sit-1-yl}urea; 1129. Ν-ethyl-Ν' - {3 - phenethylamino-6,6-dimethyl The base-4,6-dihydrogen ratio is [3,4 - c] °°°-5-yl}urea; 1130.1{5-(2-thienyl-ethenyl)-6,6-di Methyl-4,6-dihydropyridine [3,4-c]oxazol-1-yl}-(3-bromo)benzamide; 1131.^{5-(2-thienyl-ethenyl) -6,6-diamidino-4,6-dihydropyridine [3,4-c]pyrazol-3-yl}-(2-naphthyl)acetamide; 1132.1{5-(2-thienyl) -Ethyl)-6,6-dimethyl-4,6-dihydroacridine [3,4 - c ]pyrazol-3-yl}-(4-fluoro)benzoguanamine; 1133.1^- {5-(2-Thienyl-ethenyl)-6,6-dimercapto-4,6-dihydropyridine [3,4-c]pyrazol-3-yl}-(4-third Benzoamine; 1134.1^-{5-(2-thienyl-ethenyl)-6,6-diamidino-4,6-dihydropyridine [3,4-c]pyrazole-3 -yl}cyclopropanecarboxamide; 1135.1^-{5-(2-thiophene -ethylamino)-6,6-diamidino-4,6-dihydropyridine [3,4-c]pyrazol-3-yl}phenethylamine; 1136.1^-{5-(4-fluoro Benzoyl)-6,6-diamidino-4,6-dihydro»bipyridine [3,4-c]pyrazol-1-yl}-(3-bromo)benzamide; 1137. ^{5-(4-Fluorobenzoyl)-6,6-dimercapto-4,6-dihydroacridine [3,4-c]pyrazol-1-yl}-(4-fluoro) Phenylamine; 1138. [{5-(4-Fluorophenyl)-6,6-dimethyl-4,6-dihydro

C:\2D-00DE\91-01\90119473.ptd 第109頁 1327569 五、發明說明（107) 吼啶[3, 4-c]吡唑-3 -基卜（2 -萘）乙醯胺； 1139. N-{5-(4-氟苯甲醯基）-6, 6 -二曱基-4, 6 -二氫。比啶[3,4-c]0比唑-3-基}-(4-第三丁基）苯曱醯胺； 1140.1^-{5-(4-氟苯曱醯基）-6,6-二甲基-4,6-二氫吡啶[3, 4-c]咄唑-3 -基}環丙烷羧醯胺； 1141.1^-{5-(4-氟苯甲醯基）-6,6-二曱基-4,6-二氫吡啶[3，4 - c ]吡唑-3 -基}苯乙醯胺； 1142. N-{5- 乙醯基-6, 6 一二曱基-4, 6- 二氫〇比啶[3, 4- -c ] 吼0坐_ 3 - 基}-(2 -萘）乙臨胺 > 鲁 1143. N-{5- 乙醯基-6, 6 —二曱基-4, 6- 二氫口比啶[3, 4- -C] °比口坐-1 - 基} - ( 3 _漠）苯甲醯胺 9 1144. N-{5- 乙醯基-6, 6 -二曱基-4, 6- 二氮〇比啶[3, 4- -C ] 〇比0坐-3- 基}-(4 氟）苯曱醯胺 > 1145. N-{5- 乙醯基-6, 6 -二曱基-4, 6- 二氮〇比啶[3, 4- -C ] 〇比0坐-3 - 基}-(4 -第三丁基）苯. 曱醯胺； 1146. N-{ 5- 乙醯基-6, 6 —.二曱基-4, 6 - 二氫〇比啶[3, 4- -c ] 〇比唾-3 - 基}環丙烷羧醯胺 1147. N-{5- 乙醯基-6, 6 一曱基-4, 6 - 二氫口比啶[3, 4- -C] p比唑-3 -基}苯乙醯胺； 1148. N-{5 -苯乙醯基-6, 6 -二甲基-4, 6 -二氫吡啶 [3,4-c]吼唑-3-基}-(2 -萘）乙醯胺； 1149. N-{5 -苯乙醯基-6, 6 -二甲基-4,6 -二氫吡啶 [3,4-c]"比唑-1-基}-(3-溴）苯甲醯胺； 1150. N-{5 -苯乙醯基-6, 6 -二甲基-4, 6 -二氫吡啶C:\2D-00DE\91-01\90119473.ptd Page 109 1327569 V. Description of the Invention (107) Acridine [3, 4-c]pyrazole-3-yl (2-naphthyl)acetamide; 1139. N-{5-(4-Fluorobenzylidene)-6,6-dimercapto-4,6-dihydrogen. Bis-[3,4-c]0-pyrazol-3-yl}-(4-t-butyl)benzoguanamine; 1140.1^-{5-(4-fluorophenylindenyl)-6,6 -Dimethyl-4,6-dihydropyridine [3,4-c]oxazol-3-yl}cyclopropanecarboxamide; 1141.1^-{5-(4-fluorobenzhydryl)-6, 6-dimercapto-4,6-dihydropyridine [3,4 - c ]pyrazole-3-yl}phenethylamine; 1142. N-{5-ethenyl-6,6-diyl -4, 6-dihydroindolepyridinium [3, 4- -c ] 吼0 sitting _ 3 - yl}-(2 -naphthalene) ethionamine > Lu 1143. N-{5-Ethyl -6 , 6 —Dimercapto-4,6-dihydropyrazine [3, 4- -C] ° than the mouth -1 - yl} - ( 3 _ desert) benzamide 9 1144. N-{5 - Ethyl-6,6-dimercapto-4,6-diazepinei[3,4- -C] 〇 to 0 -3-yl}-(4 fluoro)benzamine> 1145. N-{5-Ethyl-6,6-dimercapto-4,6-diazolidine [3, 4- -C ] 〇 ratio 0 sitting -3 - yl}-(4 - Tributyl) benzene. decylamine; 1146. N-{ 5-ethenyl-6,6-.dimercapto-4,6-dihydroindolepyridinium [3, 4- -c ] -3 -yl}cyclopropanecarboxamide 1147. N-{5-Ethyl-6,6-mercapto-4,6- Dihydropyridinium [3, 4- -C] p-pyrazol-3-yl}phenethylamine; 1148. N-{5-phenethyl fluorenyl-6,6-dimethyl-4,6- Dihydropyridine [3,4-c]oxazol-3-yl}-(2-naphthyl)acetamide; 1149. N-{5-phenethylamino-6,6-dimethyl-4,6 -dihydropyridine [3,4-c]"pyrazol-1-yl}-(3-bromo)benzamide; 1150. N-{5-phenethyl -6,6-dimethyl -4,6-dihydropyridine

C:\2D-CODE\91-01\90119473.ptd 第110頁 1327569 五、發明說明（108) [3,4-c]吡唑-3 -基}-(4-氟）苯曱醯胺； 1151. N-{5 -苯乙醯基-6,6 -二曱基-4, 6 -二氫咄啶 [3,4-c]°比唑-3-基}-(4-第三丁基）苯曱醯胺； 1152. N-{5 -苯乙醯基-6, 6 -二甲基-4, 6_二氫吡啶 [3,4-c]吡唑-3-基}環丙烷羧醯胺； 1153. N-異丙基-Ν’ - {3-(4-第三丁基-苯甲醯胺基）-4，5，6，7 -四氫°比。定[3，4-c] °比°坐-6-基}脲； 1154. Ν-{6-(2-°塞吩基）乙醯基-4, 5，6，7 -四氫°比口定 [3,4-c]吡唑-3-基}-4-第三丁基-苯曱醯胺； 1155. N-{6-乙醯基-4，5，6，7-四氫0比〇定[3，4-c] 0比0坐- 3-基}-4 -第三丁基-苯甲醯胺； 1156. N-{6-曱烷磺醯基-4,5,6,7-四氫吡啶[3,4-〇] 〇比°坐-3_基}_4-第三丁基-苯曱酿胺； 1157. N-乙基-Ν’ - {3-(4-第三丁基-苯甲醯胺基） -4, 5，6, 7 -四氫0比。定[3, 4-c]0比唾-6-基}脲； 1158.1^-{6-(3-曱基）丁醯基-4,5,6,7-四氫咄啶 [3,4-c]吡唑-3-基}-4-第三丁基-苯甲醯胺； 1159.1^-{6-(2-〇夫0南曱醯基）-4，5,6,7-四氫〇比咬 [3,4-c]吡唑-3-基}-4-第三丁基-苯曱醯胺； 1160. N_{6_苯乙酿基-4，5，6，7-四氮〇比°定[3，4_c] 0比口坐 -3-基}-4-第三丁基-苯曱醯胺； 1161. N-{6 -苯基磺醯基-4,5,6,7-四氫吡啶[3,4-〇]吡唑-3-基}-4_第三丁基-苯曱醯胺； 1162. N-{6-(喳啉-8 -磺醯基）-4,5,6,7_四氫吡啶C:\2D-CODE\91-01\90119473.ptd Page 110 1327569 V. INSTRUCTIONS (108) [3,4-c]pyrazol-3-yl}-(4-fluoro)benzoguanamine; 1151. N-{5-phenethyl fluorenyl-6,6-dimercapto-4,6-dihydroacridine [3,4-c]°bazol-3-yl}-(4-third Benzoamine; 1152. N-{5-phenethyl fluorenyl-6,6-dimethyl-4,6-dihydropyridine [3,4-c]pyrazol-3-yl}cyclopropane Carboxylamidine; 1153. N-isopropyl-hydrazide - {3-(4-t-butyl-benzylamino)-4,5,6,7-tetrahydrogen ratio. [[3,4-c] ° ratio °-6-yl}urea; 1154. Ν-{6-(2-°secenyl)ethinyl-4, 5,6,7-tetrahydrogen ratio Oral [3,4-c]pyrazol-3-yl}-4-t-butyl-benzoguanamine; 1155. N-{6-ethenyl-4,5,6,7-tetrahydro 0 is determined by [3,4-c] 0 to 0 sitting - 3-yl}-4 -t-butyl-benzamide; 1156. N-{6-decanesulfonyl-4,5, 6,7-tetrahydropyridine [3,4-〇] 〇 ratio ° sitting -3 _}_4-tert-butyl-benzoquinone; 1157. N-ethyl-Ν' - {3-(4 - tert-butyl-benzamide amino group - 4, 5, 6, 7 - tetrahydrogen 0 ratio. [3, 4-c]0 is more than spani-6-yl}urea; 1158.1^-{6-(3-indolyl)butanyl-4,5,6,7-tetrahydroacridine [3,4-c Pyrazol-3-yl}-4-t-butyl-benzamide; 1159.1^-{6-(2-〇夫0南曱醯基)-4,5,6,7-tetrahydroanthracene Specific [3,4-c]pyrazol-3-yl}-4-t-butyl-benzoguanamine; 1160. N_{6_phenylethyl-4,5,6,7-tetrazide 〇 ratio ° [3,4_c] 0 is more than -3-yl}-4-t-butyl-benzoguanamine; 1161. N-{6-phenylsulfonyl-4,5,6, 7-tetrahydropyridine [3,4-〇]pyrazol-3-yl}-4_t-butyl-benzoguanamine; 1162. N-{6-(porphyrin-8-sulfonyl)- 4,5,6,7_tetrahydropyridine

C:\2D-C0DE\91-01\90119473.ptd 第111頁 1327569 五、發明說明（109) [3, 4-c] °比0坐-3-基}_4-第三丁基-苯曱酿胺； 1163. N-{5 -異戊基- 4,6 -二氫 π 比 11 各并[3, 4-c]吼。坐- 3- 基} - 4 -第基-苯曱醯胺 1164. Ν-{5 -苯乙基- 4，6 -二氫 °比口各并[3，4-c]"比〇坐-3_ 基} -4-第三丁基-苯曱醯胺； 1165. N-[5_(2_°塞吩_2_基乙基）_4，6_二氮σ比p各弁 [3,4-c]吡唑-3-基]-4-第三丁基-苯曱醯胺； 1166. N，N-二曱基-N’-{3-(2 -萘-2 -基-丙醯胺基）-4,6-二氫"比D各并[3，4 - c ]吼。坐-5 -基]脲； 1167.1'1-{5-(哌啶-1-基）二基曱醯基-4,6-二氫吡咯并 [3,4-c]吡唑-3-基卜3-(2-萘-2-基）-丙醯胺基；以及 1168. N，N -二曱基-N’-{3-(2-苯基-噻唑-4 -基）乙醯胺基-4，5，6，7-四氫°比咬[3,4-(：]11比°坐-5-基]脲。如前文指示，（I)化合物之製備方法表示本發明之又一目的。 )化合物及其醫藥可接受性鹽係根據一種方法製包含： I I )化合物C:\2D-C0DE\91-01\90119473.ptd Page 111 1327569 V. Description of invention (109) [3, 4-c] ° ratio -3-yl}_4-tert-butyl-benzoquinone Amine amine; 1163. N-{5-isopentyl-4,6-dihydroπ ratio 11 and [3, 4-c]吼. Sit-3-yl}-4-diyl-benzoguanamine 1164. Ν-{5-phenethyl- 4,6-dihydro-°°[3,4-c]" -3_ base} -4-t-butyl-benzoguanamine; 1165. N-[5_(2_°cephen-2-ylethyl)_4,6-diazo σ ratio p 弁[3,4 -c]pyrazol-3-yl]-4-t-butyl-benzoguanamine; 1166. N,N-dimercapto-N'-{3-(2-naphthalen-2-yl-propionium) Amino)-4,6-dihydro" is more than D[3,4 - c ]吼. Sodium-5-yl]urea; 1167.1'1-{5-(piperidin-1-yl)diylindenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl 3-(2-naphthalen-2-yl)-propaninamine; and 1168. N,N-dimercapto-N'-{3-(2-phenyl-thiazol-4-yl)acetamide Base-4,5,6,7-tetrahydrogen ratio [3,4-(:]11 to °-5-yl]urea. As indicated above, the preparation of the compound of (I) represents a further A purpose. The compound and its pharmaceutically acceptable salt are prepared according to one method: II) a compound

NC OH 式（I 備，其 a)式（ m (CH2)m (CH2)n (ΙΟNC OH formula (I, a) of the formula ( m (CH2)m (CH2)n (ΙΟ

RdRd

,c R, c R

Rb 前如義定中其Rb is as defined before

氫為 tr TTVHydrogen is tr TTV

a RRa及1以 NIRa RRa and 1 to NIR

b Rb R

c Rc R

d R 定 π及 md R π and m

C:\2D-OODE\91-Ol\90119473.ptd 第112頁五、發明說明（110) 義如前，與肼或肼鹽反應，因而C:\2D-OODE\91-Ol\90119473.ptd Page 112 5. Inventions (110) As before, react with strontium or barium salts, thus

為氫以及R〗定義如前且非為氫，化合物，其中R b)將如此所得式⑴化合物飞轉= f ’ "定義如前且非為氫，以及m種式⑴化合物’其如前文式⑴，及/或若有所需b、Hd、Wn定義藥可接受性鹽。將式（1)化合物轉成其醫前述方法為可根據眾所周熟諳技藝人士顯缺易知#ί t 類似方法。物方係呈異構物混合物獲得， ^化。單一n里堪札Μ & s 貞〗其根據s知技術分離成為早式（I)異構物仍然屬於本發明之範圍。巧」穴、，根據業界取所周知之技術將對應鹽轉成自由態化 s物（I )仍然屬於本發明之範圍。 ’ '、肼鹽為例如肼二鹽酸鹽、硫酸鹽或乙酸鹽。 ==:驟心’式⑴）化合物與肼或肼鹽間之反應可於，化罝之馱如鹽酸'乙酸或硫酸存在下，於適當溶劑如四氫呋喃、1，4 -二今烷、乙腈、甲醇或乙醇，於約室溫至回流溫度範圍反應一段約3 〇分鐘至約8小時時間。式(_/)雙環°比唑類，其中R為氫，係根據方法步驟a)獲得，該雙環吼唑可轉成多種具有R非氫的式（丨）衍生物及/ 或轉成其鹽*> 如後文說明’此等轉化係根據習知技術經由胺基衍生物與烧化、醯化、磺化劑等適當反應進行。就此方面而言值得注意者為，可獲得視需要產生的副產物’例如經由前述反應也發生於氮吡唑原子產生的副產For hydrogen and R, as defined above and not hydrogen, the compound, wherein R b) will fly the compound of formula (1) thus obtained = f ' " as defined above and not hydrogen, and m compounds of formula (1) Formula (1), and/or if desired b, Hd, Wn define a pharmaceutically acceptable salt. The compound of the formula (1) is converted into a medical treatment. The foregoing method is known to those skilled in the art. The object system is obtained as a mixture of isomers. It is still within the scope of the invention to separate into an early (I) isomer according to the s knowing technique. It is still within the scope of the invention to convert the corresponding salt into a free state s (I) according to well-known techniques in the industry. '', 肼 salt is, for example, hydrazine dihydrochloride, sulfate or acetate. ==: The reaction between the compound of the formula (1) and the ruthenium or osmium salt can be carried out in the presence of a hydrazine, such as hydrochloric acid, acetic acid or sulfuric acid, in a suitable solvent such as tetrahydrofuran, 1,4-dioxane, acetonitrile, Methanol or ethanol is reacted at a temperature ranging from about room temperature to reflux for a period of from about 3 minutes to about 8 hours. Formula (_/) bicyclic bis-azoles, wherein R is hydrogen, obtained according to method step a), the bicyclic oxazole can be converted into a plurality of formula (丨) derivatives having R non-hydrogen and/or converted into salts thereof *> As will be described later, 'these transformations are carried out by an appropriate reaction of an amine derivative with a burn-in, a hydrazine, a sulfonating agent or the like according to a conventional technique. In this respect, it is worth noting that by-products which are produced as needed may be produced, for example, by the aforementioned reaction, by the production of nitrogen pyrazole atoms.

C:\2D-00DE\91-01\90119473.ptd 第113頁 1327569 五、發明說明（111) 物。如此，接著需要分離期望式（I )化合物之步驟。根據本發明方法之較佳過程方面，其可避免前述副產物的生成，根據前述步驟a )所得式（I )化合物首先支撐於適當樹脂上，然後遵照前述步驟b )反應。因此本發明之又一目的係一種式（I )化合物之製備方法，其中R 'R!、Ra、Rb、Rc、Rd、m及η定義如前，該方法包含： a )式（I I )化合物C:\2D-00DE\91-01\90119473.ptd Page 113 1327569 V. INSTRUCTIONS (111). Thus, the step of isolating the desired compound of formula (I) is then required. According to a preferred process aspect of the process of the present invention, the formation of the aforementioned by-products can be avoided, and the compound of the formula (I) obtained according to the aforementioned step a) is first supported on a suitable resin and then reacted in accordance with the aforementioned step b). A further object of the invention is therefore a process for the preparation of a compound of formula (I) wherein R 'R!, Ra, Rb, Rc, Rd, m and η are as defined above, the process comprising: a) a compound of formula (I I )

NC 0HNC 0H

(ii) Rc I Ra Ri 其中心定義如前且非為氫以及Ra、Rb、Rc、Rd、m及η定義如前，與肼或肼鹽反應，因而獲得式（I)化合物，其中R為氫以及R,定義如前且非為氫； a’）如此所得式（I)化合物與式（I I I)異氰酸酯聚苯乙烯系樹脂反應(ii) Rc I Ra Ri having a central definition as before and not hydrogen and Ra, Rb, Rc, Rd, m and η as defined above, reacting with a ruthenium or osmium salt, thereby obtaining a compound of formula (I) wherein R is Hydrogen and R, as defined above and not hydrogen; a') The compound of formula (I) thus obtained is reacted with an isocyanate polystyrene resin of formula (III)

(III) 獲得式（I V)聚苯乙烯曱基脲(III) Obtaining (I V) polystyrene-based urea

C:\2D-G0DE\9l-01\901l9473.ptd 第114頁 1327569 五、發明說明（112)C:\2D-G0DE\9l-01\901l9473.ptd Page 114 1327569 V. Description of invention (112)

其中Ra 、 Rb 且非為氫；Wherein Ra, Rb and not hydrogen;

Rc ' Rd、πι及η定義如前以及R!定義如前 b)將如此所得式（I V)化合物轉成式（ν )化合物 /Rc ' Rd, πι and η are defined as before and R! is defined as before b) The compound of the formula (IV) thus obtained is converted into a compound of the formula (ν) /

HNHN

Kb X 其中R具有前文報告之定義但非為氫以及Ri、Ra Rc、Rd、m及η定義如前；以及 C)於強驗條件下割裂式（V)化合物而去除樹脂且獲得期 ;:(=或〜及，將式⑴化合物轉成任-注意雖然前文報告方、醫藥可接受性鹽。唑衍生物之轉化方法無法，於具有R等於氫的式（I)胺基吡吼唑環的反應性氮，但如f別β比吐環位置3的胺基部分與本反應顯示對環氮的醯。別文指示’根據前述步驟a，）之作用具有出乎意料的高度選擇Kb X wherein R has the definition previously stated but is not hydrogen and Ri, Ra Rc, Rd, m and η are as defined above; and C) the compound is removed by cracking the compound of formula (V) under strong conditions and the period of acquisition is obtained; (= or ~ and, the compound of the formula (1) is converted to any - note that although the above-mentioned report, the pharmaceutically acceptable salt. The conversion method of the azole derivative is not possible, and the aminopyrazole ring of the formula (I) having R equal to hydrogen Reactive nitrogen, but such as the amino group portion of the beta group 3 than the spitting ring position and the reaction showed a enthalpy of the ring nitrogen. The effect of the indication 'according to the aforementioned step a,' has an unexpectedly high degree of choice.

C:\2D-C0DE\91-01\90119473.ptd 第115頁 1327569 五、發明說明（113) 性’因而允許於隨後步驟b)獲得單獨轉化吡唑環位置3之胺基，結果獲得期望之式（V)化合物。於步驟a’），式（I I I )異氰酸根甲基聚苯乙烯系樹脂與前文疋義式（I)化合物之反應可於適當溶劑如N，n-二甲基曱醯胺、二。氣曱烷、氣仿、乙腈、甲苯或其混合物，於約5 C至約3 5 C範圍之溫度進行一段約3 〇分鐘至約7 2小時時間。如後文說明，已經進行式（IV)化合物之轉成式（v)化合 ^勿後，隨後於步驟c)割裂樹脂係根據習知技術之後述處理於強鹼條件下進行。 ^例s之，可採用水性鈉或鉀氫氣化物於適當助溶劑如 J醇、乙醇、二甲基曱醯胺、烷或乙腈共存進 Ί7 ° 和條件下於約至約㈣溫度進行至約7日時間又式（I )化合物視需要進杆夕臨由態化合⑯、以及將異構物Λγ% Λ 鹽轉成自藉習知方法進行。構物-合物分離成單-異構物皆可至於方法步驟]3)，式, 等於氫之式(Iv)化合物轉：對：轉，或更佳具 (V)衍生物其根據業界已知 ' ϋ t虱的式（I)或技術進行。化醯化或鲼化胺基之習知特別式（I)或（V)化合物I中设在、强ώ北法 OR，、w,、_c“， '中以糸選自非為氫的R，、其中R’C:\2D-C0DE\91-01\90119473.ptd Page 115 1327569 V. INSTRUCTIONS (113) Sex 'and thus allow for the subsequent conversion of the amine group at position 3 of the pyrazole ring separately in step b), resulting in the desired a compound of formula (V). In the step a'), the reaction of the isocyanatomethylpolystyrene resin of the formula (I I I) with the compound of the above formula (I) may be carried out in a suitable solvent such as N, n-dimethyl decylamine. The gas, the gas, the acetonitrile, the toluene or a mixture thereof is subjected to a temperature in the range of from about 5 C to about 35 C for a period of from about 3 minutes to about 72 hours. As will be described later, the conversion of the compound of the formula (IV) to the formula (v) has not been carried out, and then the resin is cleaved in the step c), which is carried out under the conditions of a strong base, as described later in the art. For example, the aqueous sodium or potassium hydrogenate can be used in a suitable co-solvent such as J alcohol, ethanol, dimethyl decylamine, alkane or acetonitrile at a temperature of about 7 ° and at about to about (iv) to about 7 The compound of the formula (I) is converted into a self-borrowing method by the method of converting the isomer Λγ% Λ salt as needed. The separation of the structure-complex into a mono-isomer can be carried out as a method step]3), a formula equivalent to hydrogen (Iv) compound trans: pair: trans, or better (V) derivative according to the industry Knowing the formula (I) or technique of 'ϋ t虱. The conventional formula (I) or (V) of the compound of the formula (I) or (V) is located in the strong north method OR, w,, _c ", ' is selected from the group consisting of non-hydrogen R , where R'

1^27569 五、發明說明（114) 及R"由前文報告定義；r 及η定義如前可經由式（j) 等於氫’與式（VI)化合物 R-X 其中R定義如前，氫除外 >臭〇非為氫以及Ra、Rb、Rc、R(i、ιη 化合物或式（IV)化合物其具有R 反應製備 (VI) 以及X為適當離去基較佳為氯或前述反應可根據章界y ^ 呆介承所周知之醯化、磺化哎煊仆脸A 之習知程序進行，習知妒卜 κ化4沉化胺基脸N N -異兩且 &序例如係於第三級鹼如三乙基 fe、N，M - —吳丙基乙某脍+ #、_ f甲Θs a 或咄啶存在下，於適當溶劑如甲一、凡、方、***、四氫呋喃、乙腈或NN -二曱基甲醯胺’於約-lot:至回流範圍之溫度進行約3〇分鐘至約9 6小時時間。由前文说明對業界人士顯然易知具有尺等於_s〇2NR，r"之式（I)或（V)化合物之製備實質上可如前述進行，或另外經由具有R等於-SC^NHR’之式（I)或（v)化合物於任何適當烷化部分，根據眾所周知之二取代磺醯胺基之製備方法適當反應製備。式（I)或（V)化合物’其中R為-C0NHR，基，R，具有氫以外之前文報告之疋義’Ri非為氣以及Ra、Rb、Rc、Rd、m及η 定義如前’式（I)或（V)化合物可經由具有R等於氫之式（I) 或（IV)化合物與式（VII)化合物反應製備。 R’NCO (VII) 其中R’定義如前但非為氫’ 因而獲得對應式（I)或（v)化合物其可視需要地進一步與1^27569 V. Inventive Note (114) and R" are defined by the previous report; r and η are as defined above by formula (j) equal to hydrogen 'and compound of formula (VI) RX where R is as defined above, except for hydrogen > The skunk is not hydrogen and Ra, Rb, Rc, R (i, iπ or compound of formula (IV) which has R reaction to prepare (VI) and X is a suitable leaving group, preferably chlorine or the aforementioned reaction may be according to the boundary y ^ 留介介所所、、、、、、、、、、、、、、、、、、、、、、、、、 , , , , , , , , , , , , , , , , , , , , a base such as triethyl fe, N, M - wupropyl ethane # + #, _ f 甲 Θ s a or acridine in the presence of a suitable solvent such as A, Fan, Fang, Ethyl, Tetrahydrofuran, Acetonitrile or NN - II The mercaptocarbamide is subjected to a temperature of from about 3 minutes to about 96 hours at a temperature of about -lot: from the foregoing description, it is apparent to those skilled in the art that it has a rule equal to _s〇2NR, r" The preparation of the I) or (V) compound can be carried out substantially as described above, or additionally via a compound of formula (I) or (v) having R equal to -SC^NHR' When the alkylation moiety is prepared by a suitable reaction according to the well-known preparation method of the disubstituted sulfonamide group, the compound of the formula (I) or (V) wherein R is -C0NHR, a group, and R, has a meaning other than hydrogen. 'Ri is not a gas and Ra, Rb, Rc, Rd, m and η are as defined above. The compound of formula (I) or (V) may be via a compound of formula (I) or (IV) having R equal to hydrogen and formula (VII). Compound reaction preparation. R'NCO (VII) wherein R' is as defined above but not hydrogen' thus obtaining a corresponding compound of formula (I) or (v) which may optionally further

111 m 画· 丨_ 111 11H C:\2D-00DE\91-0lW01l9473.ptd 第 117 頁 1327569 五、發明說明（115) 式（V I I I )化合物反應 R"-x (VIII) 其中R"定義如前但非為氫’以及X為適當離去基較佳為氣或溴，因而獲得式（I)或（V)化合物’其中R為-CONR’ R1·，其中R’及R"非為氫。前述化合物（I)或（IV)與式（VII)化合物之反應可於第三級鹼如三乙基胺、N，N -二異丙基乙基胺或吡啶存在下，於適當溶劑如甲苯、二氯曱炫、氣仿、乙喊、四氫p夫p南、乙腈或N，N -二曱基曱醯胺，於約-1 0 °C至回流溫度反應經歷 •約3 0分鐘至約7 2小時時間。具有R等於- CONHR’之式（I)或（V)化合物視情況需要接著轉成具有K等於-CONR’ R"之對應衍生物，係根據習知用於製備二取代脲基衍生物之方法進行。式（I)或（V)化合物其中R為-C〇NR，R"基，R，及R"具有氫以外之前文報告之定義，R1非為氫以及Ra、Rb、Rc、Rd、 m及n定義如前’該式（I)或（v)化合物可經由式（I)或（IV) 化合物具有R等於氫與氯曱酸4 -硝基苯酯反應以及隨後與式（IX )化合物反應製備。 • R’R__NH (IX) 其中R’及R"定義如前但非為氫。反應係根據習知用於製備二取代之脈基竹生物之方法進行。另外’式（I )或（I V )化合物具有R等於氫可於還原條件下與式（X)化合物反應。 R’-CHO (X)111 m painting · 丨 _ 111 11H C:\2D-00DE\91-0lW01l9473.ptd Page 117 1327569 V. Description of invention (115) Compound of formula (VIII) reacts R"-x (VIII) where R" However, if it is not hydrogen and X is a suitable leaving group, it is preferably gas or bromine, thereby obtaining a compound of formula (I) or (V) wherein R is -CONR' R1., wherein R' and R" are not hydrogen. The reaction of the aforementioned compound (I) or (IV) with the compound of the formula (VII) can be carried out in a suitable solvent such as toluene in the presence of a tertiary base such as triethylamine, N,N-diisopropylethylamine or pyridine. , dichloropurine, gas, yoke, tetrahydrop-p, acetonitrile or N,N-dimercaptoamine, reacted at about -10 ° C to reflux temperature • about 30 minutes to About 7 2 hours. A compound of formula (I) or (V) having R equal to -CONHR', which is optionally converted to a corresponding derivative having K equal to -CONR' R", according to conventional methods for preparing disubstituted ureido derivatives get on. A compound of formula (I) or (V) wherein R is -C〇NR, R" group, R, and R" have hydrogen as defined in the previous report, R1 is not hydrogen and Ra, Rb, Rc, Rd, m and n is defined as before 'the compound of formula (I) or (v) may have a reaction of a compound of formula (I) or (IV) having R equal to hydrogen with 4-nitrophenyl chloroantimonate and subsequent reaction with a compound of formula (IX) preparation. • R'R__NH (IX) where R' and R" are as defined above but not hydrogen. The reaction is carried out according to a conventional method for preparing a disubstituted vein-based bamboo organism. Further, the compound of the formula (I) or (IV) having R equal to hydrogen can be reacted with the compound of the formula (X) under reducing conditions. R’-CHO (X)

第118頁 C:\2D-C0DE\91-01\90119473.ptd 1327569 發明說明（116) 其中R’定義如前但非為氫因而獲得對應式（1)或（v)化合物，其中R為R CH2-基以R’定義如前但非為氣。反應係於適當溶劑例如N，N-二甲基曱醯胺、N，N_二甲基乙醯胺、氯仿、二氯甲烧、四氫咬喃或乙腈，視需要於作為助溶劑的乙酸、乙醇或曱醇存在下於約Μ 〇 CC至回流溫度反應經歷約3 0分鐘至約4日時間。習知於反應介質之還原劑為例如爛氫化納、三乙酿氧侧氫化納等。Page 118 C:\2D-C0DE\91-01\90119473.ptd 1327569 DESCRIPTION OF THE INVENTION (116) wherein R' is as defined above but not hydrogen and thus obtains a corresponding compound of formula (1) or (v) wherein R is R The CH2- group is defined by R' as before but not by gas. The reaction is carried out in a suitable solvent such as N,N-dimethyldecylamine, N,N-dimethylacetamide, chloroform, methylene chloride, tetrahydrocyanate or acetonitrile, if necessary as acetic acid as a cosolvent The reaction is carried out at about ΜCC to reflux temperature in the presence of ethanol or decyl alcohol for a period of from about 30 minutes to about 4 days. The reducing agent conventionally used in the reaction medium is, for example, sodium hydride or triethyl ethoxyhydride.

由前文說明’業界人士顯然易知前述式（I)、（IV)及（v) 化合物也可經由R基以外的官能基（如前文徹底說明），以實質類似方式且根據習知合成有機方法反應而方便地轉成其他衍生物（I)、（IV)或（V)。舉例言之，其中R!為-COOtBu之式（I)、（IV)或（V)化合物可經由使用適當酸如三氟乙酸或鹽酸處理而被水解成其中 1^為11之式（\〇化合物。至目前為止，前述式（1)、（IV)或（V)化合物，其中心為氫原子，容易經由實質如前文對R基所述處理而轉成對應烧化、酿化或確化衍生物。From the foregoing, it is apparent to those skilled in the art that the compounds of the above formulae (I), (IV) and (v) can also be synthesized in a substantially similar manner and according to conventional organic methods via functional groups other than the R group (as fully explained above). The reaction is conveniently converted to other derivatives (I), (IV) or (V). For example, a compound of formula (I), (IV) or (V) wherein R! is -COOtBu can be hydrolyzed to a formula wherein 1^ is 11 by treatment with a suitable acid such as trifluoroacetic acid or hydrochloric acid (\〇 The compound of the above formula (1), (IV) or (V) has a hydrogen atom at the center, and is easily converted into a corresponding calcination, brewing or derivatization derivative by substantially treating the R group as described above. .

又一實例中，前述任一種化合物，其中Ra、Rb、及Rd 中之一或多者為-CH2〇H，可方便地經由屬於帶有Ra、Rb、 Rc 及 Rd 中之一或多者為 _(^2_〇_以（|^)21：611或-(：112-〇_1^之對應經保護的衍生物方便地製備。反應係根據習知技術進行，例如於適當溶劑如N，N -二甲基甲醯胺、氯仿、二氯甲烧、四氫呋喃、甲醇、乙醇或乙In still another example, any one of the foregoing compounds, wherein one or more of Ra, Rb, and Rd is -CH2〇H, conveniently via one or more of those having Ra, Rb, Rc, and Rd _(^2_〇_ is conveniently prepared as the corresponding protected derivative of (|^) 21:611 or -(:112-〇_1^. The reaction is carried out according to a conventional technique, for example, in a suitable solvent such as N , N-dimethylformamide, chloroform, methylene chloride, tetrahydrofuran, methanol, ethanol or

C: \2D.OODE\91 ·01 \90119473 .ptd 第119頁 1327569 五、發明說明（117) 腈，於約-1 0 °C至回流溫度反應經歷約3 0分鐘至約7 2小時時間與適當氟陰離子來源如氫化四丁基録反應進行。同理’前述具有一或多個Ra、Rb、Rc及Rd等於-CH2OH之化合物（I)、（IV)或（V)可與式（VI)化合物反應 R-X (VI) 其中R為R’ ，R’定義如前但非為氫，以及X為適當離去基，因而獲得對應化合物帶有一或多個Ra、Rb、Rc及Rd為 -CH20R，，R’ 非為氫。後述反應可於鹼如氫化鈉、Ν，Ν-二異丙基乙基胺或„比D定 _存在下，為適當溶劑如曱苯、二氣甲烷、氣仿、***、四氫呋喃、乙腈或N，N-二曱基曱醯胺於約-1 〇艽至回流溫度進行。業界人士顯然易知當製備本發明目的之式（丨）化合物時，於起始物料或其中間物内部可能造成非期望的副反應之非必要的官能基須根據習知技術適當保護。同理，後者總成自由態脫保護化合物可根據已知程序進行。根據本發明之方法目的，全部式（丨j（丨丨丨）、（v丨）、 (VII)、（VIII)、（IX)及（X)化合物為已知且可根據已知方 0去獲得。特別，式（VI)至（X)化合物為市面可購得或方便根據習知方法製備，式（I I )化合物可根據前述程序製備參考 Gadekar，Sheekrishna M.等人，醫藥化學期刊.1968 11(3), 616-618; Hong, C. Y. ； Kim> γ. κ. . Chang !C: \2D.OODE\91 ·01 \90119473 .ptd Page 119 1327569 V. INSTRUCTIONS (117) The nitrile reacts at about -10 ° C to reflux temperature for about 30 minutes to about 72 hours. A suitable source of fluoride anion such as a tetrabutyl hydride reaction is carried out. Similarly, the aforementioned compound (I), (IV) or (V) having one or more of Ra, Rb, Rc and Rd equal to -CH2OH can be reacted with a compound of the formula (VI) wherein R is R', R' is as defined above but not hydrogen, and X is a suitable leaving group, thus obtaining the corresponding compound with one or more of Ra, Rb, Rc and Rd as -CH20R, and R' is not hydrogen. The reaction described later can be in the presence of a base such as sodium hydride, hydrazine, hydrazine-diisopropylethylamine or „比定定, as a suitable solvent such as toluene, dioxane, methane, diethyl ether, tetrahydrofuran, acetonitrile or N. , N-dimercaptodecylamine is carried out at a temperature of about -1 Torr to reflux temperature. It is apparent to those skilled in the art that when preparing a compound of the formula (丨) for the purpose of the present invention, it may cause non-initiation in the starting material or its intermediate. The non-essential functional groups of the desired side reactions are suitably protected according to conventional techniques. Similarly, the latter free-state deprotecting compounds can be carried out according to known procedures. According to the method of the present invention, all formulas (丨j(丨) The compounds of 丨丨), (v丨), (VII), (VIII), (IX) and (X) are known and can be obtained according to the known formula. In particular, the compounds of the formulae (VI) to (X) are The product is commercially available or conveniently prepared according to conventional methods. The compound of formula (II) can be prepared according to the aforementioned procedure. Reference Gadekar, Sheekrishna M. et al., Med. Chem. 1968 11(3), 616-618; Hong, CY; Kim&gt γ. κ. . Chang !

J. Η. , Kim, S. H. ； Choi, H. ； Nam, D. H. ； Kim, YJ. Η. , Kim, S. H. ; Choi, H. ; Nam, D. H. ; Kim, Y

1327569 五、發明說明（118) Z. ; Kwak， J. H.，醫藥化學期刊；1997， 40(22) 3584 3593， Pedersen， H_ ; Brauner~Obsborne， Η ;1327569 V. INSTRUCTIONS (118) Z.; Kwak, J. H., Journal of Medicinal Chemistry; 1997, 40(22) 3584 3593, Pedersen, H_; Brauner~Obsborne, Η;

Ball, J. R. ; Frydenvang, K. ； Meier, E. ; Bogeso, K. P. ; Krogsgaard-Larsen，生物有機醫藥化學丨99 9，7， 795-809 。 * 明式（I)化合物較佳係以最後，業界人士顯然易知本發組合方式進行前述反應製備。舉例言之，如前述製備的立合物可與式（VI)至（X)之多種I於樹脂粒子上的式（IV)化獲得數以千計的不同種式（v)合物根據組合化學法反應方便地轉成本發明式（I )衍生物合物。此等衍生物隨後可因此本發明之又一目的為— (V)成員： ’’’、—種組合化學存庫包含多個式Ball, J. R.; Frydenvang, K.; Meier, E.; Bogeso, K. P.; Krogsgaard-Larsen, Bioorganic Pharmacology, 丨99 9,7, 795-809. * The compound of the formula (I) is preferably in the final form, and it is apparent to those skilled in the art that the present invention can be carried out by the above-mentioned reaction. For example, a complex prepared as described above can be obtained by formula (IV) of a plurality of I of formula (VI) to (X) on a resin particle to obtain thousands of different species (v) compounds according to combinatorial chemistry. The reaction is conveniently transferred to the derivative of the formula (I) of the invention. These derivatives may then be further objects of the invention - (V) members: ''', a combination chemical library containing a plurality of formulas

R及R]為相同或相異且分別為氣、、選自R，、-C0R，、-C00R，，、子或視需要經取代基團 -NH-C(=NH)NHR，、-C(=NH)Mhr， R 、_CQNr’r"、、-S〇2R，、-so2nhr，或R and R are the same or different and are respectively a gas, selected from R, -C0R, -C00R, ,, or optionally substituted groups -NH-C(=NH)NHR, -C (=NH)Mhr, R , _CQNr'r", , -S〇2R,, -so2nhr, or

l327569 五、發明說明（119) ' 〜S〇2NR’ R";其中R’及R”為相同或相異且分別係選自氫或 ^需要經，一步取代之直鏈或分支Ci_C6烷基、芳基、C3-C6 %烷基及芳基q-C6烷基或R，及R"共同形成q q伸烷基鏈；L327569 V. Inventive Note (119) '~S〇2NR' R"; where R' and R" are the same or different and are respectively selected from hydrogen or ^, a straight-chain or branched Ci_C6 alkyl group which is substituted in one step, An aryl group, a C3-C6 % alkyl group, and an aryl q-C6 alkyl group or R, and R" together form a qq alkylene chain;

Ra、Rb、Rc及Rd為相同或相異且分別係選自氫、視需要進 :步經取代之直鏈或分支鏈燒基、芳基 '芳基C「C6炫 :,CH2〇R f，其中R，定義如前，或Ra及Rb及/或Rc及Rd 與其鍵結之碳原子共同形成 . 基自^成一視需要經取代之C3-C6環烷 &，m及η各自刀別表不〇或丨 ^ l或等於2(m + nS2)。疋正數，但規疋m + ri係小於較佳前述樹脂為聚笨乙燒备笨乙稀樹脂。 ~糸树月曰，特別甲基異氰酸酷聚 I理學式（I )化合物具有作為蛋白質數如可用於限制腫瘤細胞未經調節的=卩制劑活性，因此例於治療上可用於治療多種腫瘤例3 ^。膀胱癌、結腸癌、卵巢癌及子宮内*頰瘤如乳癌、肺癌、骨肉瘤，及血液惡性病如白血病。骐癌，肉瘤如軟組織及此外，式（I)化合物也可用於治 >乾癬、動脈粥狀硬化關聯的血管平^、他細胞増生病症如後狹窄、以及血管再度狹窄， β肌細胞増生、及手術推定蛋白質激酶抑制劑之抑制活' /σ療阿茲海默氏病。係經由基於使用多重篩檢_ΡΗ 96孔|生之選定化合物之強度 (Mi Hi pore))之檢定分析方法測定平板C米里孔公司置於各孔底’經洗滌/過濾步驟&’其中磷酸纖維素濾紙可結合帶正電基質。Ra, Rb, Rc and Rd are the same or different and are respectively selected from hydrogen, if necessary: a linear or branched alkyl group substituted by a step, an aryl 'aryl C" C6 Hyun:, CH2〇R f , wherein R, as defined above, or Ra and Rb and/or Rc and Rd are formed together with the carbon atom to which they are bonded. The C3-C6 naphthenes & Not 〇 or 丨 ^ l or equal to 2 (m + nS2). 疋 positive number, but the standard + m + ri is less than the preferred resin is a polystyrene bromide resin. ~ eucalyptus, special methyl Isocyanate is a compound of formula (I) having a protein number, such as can be used to limit the unregulated activity of sputum cells in tumor cells, and thus can be used therapeutically for treating various tumors. 3 ^ Bladder cancer, colon cancer , ovarian cancer and intrauterine x-carcinoma such as breast cancer, lung cancer, osteosarcoma, and hematological malignancies such as leukemia. Carcinoma, sarcoma such as soft tissue and, in addition, the compound of formula (I) can also be used for treatment > dry, atherosclerosis Associated blood vessels, his cell-proliferative conditions such as posterior stenosis, and vascular stenosis, β-muscle growth, and Surgical Presumptive Protein Kinase Inhibitor Inhibition of Live A/Hyper Therapy Alzheimer's Disease is determined by assay analysis based on the use of multiple screenings ΡΗ 96 pores | Mi Hi pores C. Miricon is placed at the bottom of each well 'washing/filtering step &' where the phosphocellulose filter paper can be combined with a positively charged matrix.

C:\2D-00DE\9l-01\90119473.ptd 第122頁 1327569 五、發明說明（120) --- 當放射性標記的磷酸根部分藉絲/蘇激崦轉移給與濾紙結合的組織腺時，於閃爍計數器測量發射的光。 cdk2/環素A活性之抑制檢定分析C:\2D-00DE\9l-01\90119473.ptd Page 122 1327569 V. INSTRUCTIONS (120) --- When the radiolabeled phosphate moiety is transferred to the tissue gland bound to the filter paper by silk/sumer The emitted light is measured in a scintillation counter. Inhibition assay analysis of cdk2/cyclin A activity

激酶反應：1.5 /zM組織腺H1基質，25 matpuz # CM Ρ33 ATP)，30毫微克桿病毒共同表現的cdk2/環素a , 10/zM抑制劑於終容積100微升緩衝液（TRIS HC1 1{) _ pH 7·5，MgC12 10 mM，7·5 mM DTT)添加至9“LU 字形孔底平板的各孔。於37°C培育10分鐘後藉加入2〇微升EDTA 12〇 mM中止反應。捕捉：1 00微升由各孔移至多重篩檢板，讓基質結合至磷酸纖維素濾紙。然後平板以150微升/孔不含Ca++/Mg++之pBs 洗3次及藉多重篩檢過濾系統過濾。檢測：讓過濾器於37 °C乾燥，然後加入丨00微升/孔閃燦劑，於頂計數儀器藉放射性計數偵測up標記組織腺Ηι。” 結果：資料經分析，以相對於每種活性（〗〇〇%)之抑制百分比表示。全部顯示抑制作用2 50%之化合物進一步經分析俾研究與定義強度（IC50)，以及經由Ki計算得知抑制劑之動力""學 ^^^/定：使用之測定方案同前文說明，此處抑制劑係於0.0045至10从Μ範圍之不同濃度試驗。實竣〜腦程式GraphPad Prizm使用四參數邏輯算式分析：y=底 + (頂-底）/(1 + 10-((1 oglC50-x)* 斜率）） ' 此處X為抑制劑濃度之對數值，y為反應；y始於底而以sKinase reaction: 1.5/zM tissue gland H1 matrix, 25 matpuz # CM Ρ33 ATP), 30 ng of rod virus co-expressed cdk2/cycline a, 10/zM inhibitor in final volume 100 μl buffer (TRIS HC1 1 {) _ pH 7·5, MgC12 10 mM, 7·5 mM DTT) was added to each well of a 9" LU-shaped bottom plate. After incubation for 10 minutes at 37 ° C, 2 〇 microliters of EDTA 12 〇 mM was aborted. Reaction: Capture: 100 μl from each well to multiple screening plates, allowing the matrix to bind to the phosphocellulose filter paper. The plate is then washed three times with 150 μl/well of Ca++/Mg++ without pBs and multiple screenings Filtration system filtration. Detection: Let the filter dry at 37 °C, then add 丨00 μl/well of flashing agent, and use the radioactive counting to detect the up-labeled tissue gland in the top counting instrument.” Result: The data was analyzed to Percent inhibition relative to each activity (〗〖%). All showed inhibition 2 50% of the compound was further analyzed, 俾 research and defined intensity (IC50), and the power of the inhibitor was calculated by Ki calculation "" learning ^^^: The assay used was the same as explained above. Here the inhibitor is tested at different concentrations ranging from 0.0045 to 10 from the hydrazine range. Real ~ Brain program GraphPad Prizm uses a four-parameter logistic analysis: y = bottom + (top-bottom) / (1 + 10-((1 oglC50-x) * slope)) ' where X is the concentration of inhibitor concentration Value, y is the reaction; y starts at the bottom and s

C: \2D-00DE\91-01\90119473.ptd 第】23頁 1327569 五、發明說明（121) 字形走至頂。 1^計算：變更八丁？及組織腺111基質濃度：4,8，12,24,48 //»1 用於ATP(含成比例稀釋的p337-ATP)及0.4，0.8， 1.2, 2. 4, 4. 8//M用於組織腺，為無及有兩種不同經適當選擇的抑制劑濃度存在下使用。實驗資料係使用隨機雙反應劑系統公式藉電腦程式 n S i g m a P 1 〇 t11做K i測定分析：C: \2D-00DE\91-01\90119473.ptd Page 23 of 1327569 V. Description of invention (121) The glyph goes to the top. 1^ Calculation: Change eight Ding? And tissue gland 111 matrix concentration: 4,8,12,24,48 //»1 for ATP (containing proportional dilution of p337-ATP) and 0.4, 0.8, 1.2, 2. 4, 4. 8//M For use in tissue glands, for use in the absence and presence of two different appropriately selected inhibitor concentrations. The experimental data was analyzed by the computer program using the stochastic double-reactant system formula n S i g m a P 1 〇 t11:

Vmax (A) (B)Vmax (A) (B)

aKAKBaKAKB

(A) + _(B)_ + (A) (B) KA KB aKAKB ' 此處A = A T P及B =組織腺H1。此外選定之化合物係於嚴格與細胞週期相關的絲/蘇激評審決定特徵（cdk2/環素E、cdkl/環素B1、cdk4/環素 D1)也決定對MAPK、PKA、EGFR、IGF1-R、Cdc7/dbf4 及阿羅拉-2之特異性。 c d k 2 /環素E活性之抑制檢定分析 _ 激酶反應：1 · 5 // Μ組織腺Η1 (西革瑪公司# η - 5 5 0 5 )美質 ’ 25 μΜ ATP(0. 2 //Ci P33 r -ΑΤΡ)，15 毫微克桿病毒共同表現c d k 2 / G S T -環素E，適當濃度抑制劑於終容積1 〇〇微升緩衝液（TRIS HC1 10 mM pH 7.5，MgCl2 10 mM，？ j mM DTT + 0. 2毫克/毫升BSA)加至96孔U字形孔底平板之各孔。於37 °C培育1 〇分鐘後，藉加入20微升EDTA 1 20 _中(A) + _(B)_ + (A) (B) KA KB aKAKB ' where A = A T P and B = tissue gland H1. In addition, the selected compounds are characterized by stringent cell cycle-related silk/suffering assays (cdk2/cyclin E, cdkl/cyclin B1, cdk4/cyclin D1) and also for MAPK, PKA, EGFR, IGF1-R , Cdc7/dbf4 and Arora-2 specificity. Inhibition assay for cdk 2 /cyclin E activity _ Kinase reaction: 1 · 5 // Μ tissue adenine 1 (Sigma 2 η - 5 5 0 5 ) 美 ' ' 25 μΜ ATP (0. 2 //Ci P33 r -ΑΤΡ), 15 ng of rod virus together to express cdk 2 / GST - cyclin E, appropriate concentration inhibitor in final volume 1 〇〇 microliter buffer (TRIS HC1 10 mM pH 7.5, MgCl2 10 mM, ? j mM DTT + 0.2 mg/ml BSA) was added to each well of a 96-well U-shaped bottom plate. After incubating at 37 °C for 1 〇, borrow 20 μl of EDTA 1 20 _

C:\2D-OODE\91-Ol\90119473.ptd I327569 1 ~**" ______________ 五、發明說明（122) " —— 止反應。捕捉：1 0 0微升由各孔移至多重篩檢平板，讓基質結合至碟酸纖維素濾紙。然後平板以丨50微升/孔不含Ca++/Mg++之 pBS洗3次’以及藉多重篩檢過濾系統過濾。檢測：讓過濾器於37。〇乾燥，然後加入丨〇〇微升/孔閃爍劑’由頂計數儀器藉放射性計數而檢測經up標記的组織腺C:\2D-OODE\91-Ol\90119473.ptd I327569 1 ~**" ______________ V. Invention Description (122) " —— Stop the reaction. Capture: One hundred microliters was transferred from each well to a multi-screening plate to allow the matrix to bind to the sour cellulose filter paper. The plates were then washed 3 times with 50 μl/well of p++ without Ca++/Mg++ and filtered by a multi-screen filtration system. Detection: Let the filter be at 37. 〇 dry, then add 丨〇〇 microliter/well scintillator' to detect up-tagged tissue glands by radioactivity counting by top counting instrument

Hi。 cdk 1 /環素B1活性之抑制檢定分析激酶反應：1.5 組織腺H1(西革瑪公司# H-5 5 0 5 )基貝 ’ 25 " Μ ATP( 〇. 2 /z Ci P33 r - ATP)，30 毫微克桿病毒共同表現cdk 1 /環素B1，適當濃度抑制劑於終容積1 〇〇微升Hi. Inhibition assay for cdk 1 /cyclin B1 activity assay Kinase reaction: 1.5 Tissue gland H1 (Sigma company # H-5 5 0 5 ) Kibe ' 25 " Μ ATP ( 〇. 2 /z Ci P33 r - ATP ), 30 ng of rod virus together to express cdk 1 /cycline B1, the appropriate concentration of inhibitor in the final volume of 1 〇〇 microliter

緩衝液（TRIS HC1 10 mM pH 7.5，MgCl2 10 mM，7·5 mM DTT + 0.2^克/毫升BSA)加至96孔U字形孔底平板之各孔。於37。(：培育10分鐘後，藉加入20微升EDTA 120 mM中止反應。捕捉：1 0 0微升由各孔移至多重篩檢平板，讓基質結合至碟酸纖維素濾紙。然後平板以1 50微升/孔不含Ca++ /Mg++之 PBS洗3次’以及藉多重篩檢過濾系統過濾。檢測：讓過濾器於3 7 °C乾燥，然後加入1 〇〇微升/孔閃爍劑’由頂計數儀器藉放射性計數而檢測經33 p標記的組織腺 H1 〇 cdk4/環素D1活性之抑制檢定分析激酶反應：0. 4 小鼠GST-Rb( 7 69-921 )(#sc-4112#| 聖塔克魯茲公司）基質，10 μ M ATP(0. 5 "Ci P33 rBuffer (TRIS HC1 10 mM pH 7.5, MgCl2 10 mM, 7·5 mM DTT + 0.2^g/ml BSA) was added to each well of a 96-well U-shaped bottom plate. At 37. (: After 10 minutes of incubation, the reaction was stopped by the addition of 20 μl of EDTA 120 mM. Capture: 100 μl of each well was transferred from each well to a multi-screening plate, and the matrix was allowed to bind to the sour cellulose filter paper. Then the plate was 1 50 Microliters/wells were washed 3 times without Ca++/Mg++ in PBS' and filtered by multiple screening filtration system. Detection: Let the filter dry at 37 °C, then add 1 〇〇 microliter/well scintillator' from top The counting instrument detects the inhibition of the 33 p-labeled tissue gland H1 〇cdk4/cyclin D1 activity by radioactivity counting. Kinase reaction: 0.4 mouse GST-Rb ( 7 69-921 ) (#sc-4112#| Santa Cruz Corporation) Matrix, 10 μM ATP (0. 5 "Ci P33 r

C:\2D-OODE\91-01\90l19473.ptd 第125頁 1327569 五、發明說明（123) -ATP) ’ 1〇〇笔微克桿病毒共同表現wGST_cdk4/GST_環素 D1，適當浪度抑制劑於終容積5〇微升緩衝液（TRIS HC1 1〇 niM pH 7. 5，MgCl2 10 mM，7. 5 mM DTT + 〇 2 毫克/ 毫升 BSA)加至96孔U字形孔底平板之各孔。於37乞培育4〇分鐘後’藉加入20微升EDTA 120 中止反應。捕捉：60微升由各孔移至多重筛檢平^，讓基質結合至磷酸纖維素濾紙。然後平板以15〇微升/孔不含Ca++/Mg++之 PBS洗3次，以及藉多重篩檢過濾系統過濾。檢測：讓過濾器於37。(：乾燥，然後加入i〇〇微升/孔閃爍 I劑，由頂計數儀器藉放射性計數而檢測經33P標記的组織腺H1 。 ΜAPK活性之抑制檢定分析激酶反應：10 ΜΒΡ(西革瑪公司# μ-1891)基質，25 ΑΤΡ(0· 2 //Ci Ρ33 γ-ΑΤΡ)，25 毫微克細菌表現之 GST-ΜΑΡΚ(上態（Upstate)生技公司#14-173)，適當濃度抑制劑於終容積100微升緩衝液（TRIS HC1 10 mM pH 7.5，C:\2D-OODE\91-01\90l19473.ptd Page 125 1327569 V. Description of the invention (123) -ATP) ' 1 〇〇微 micro-cluster virus common performance wGST_cdk4/GST_cycline D1, appropriate wave suppression Add to the final volume of 5 μL of buffer (TRIS HC1 1〇niM pH 7.5, MgCl 2 10 mM, 7.5 mM DTT + 〇 2 mg / ml BSA) to each well of a 96-well U-shaped bottom plate . After incubation for 4 minutes at 37 ’, the reaction was stopped by adding 20 μl of EDTA 120. Capture: 60 microliters were moved from each well to multiple screenings to allow the matrix to bind to the phosphocellulose filter paper. The plates were then washed 3 times with 15 μL/well of Ca++/Mg++ free PBS and filtered through a multi-screen filtration system. Detection: Let the filter be at 37. (: Dry, then add i〇〇 microliter/well scintillation I agent, and detect the 33P-labeled tissue gland H1 by radioactivity counting by top counting instrument. Inhibition assay of ΜAPK activity analysis Kinase reaction: 10 ΜΒΡ (Sigma) Company # μ-1891) matrix, 25 ΑΤΡ (0· 2 //Ci Ρ33 γ-ΑΤΡ), 25 ng of bacterial expression of GST-ΜΑΡΚ (Upstate (Technology #14-173), appropriate concentration inhibition In a final volume of 100 μl buffer (TRIS HC1 10 mM pH 7.5,

MgCl2 10 mM ’ 7. 5 mM DTT + 0. 1 毫克/ 毫升BSA)加至96 孔U 字形孔底平板之各孔。於37〇C培育15分鐘後’藉加入20微 •升EDTA 120 mM中止反應。捕捉：1 0 0微升由各孔移至多重篩檢平板’讓基質結合至磷酸纖維素濾紙。然後平板以丨5 〇微升/孔不含Ca++ /Mg++之 PBS洗3次，以及藉多重篩檢過濾系統過濾。檢測：讓過濾器於3 7 °C乾燥，然後加入1 0 0微升/孔閃燦劑，由頂計數儀器藉放射性計數而檢測經33P標記的組織腺MgCl2 10 mM ' 7. 5 mM DTT + 0.1 mg/ml BSA) was added to each well of a 96-well U-shaped bottom plate. After incubation for 15 minutes at 37 ° C, the reaction was stopped by adding 20 μl of EDTA 120 mM. Capture: 100 microliters from each well to multiple screening plates' to allow the matrix to bind to the phosphocellulose filter paper. The plates were then washed 3 times with 丨5 〇 microliters/well of Ca++/Mg++ free PBS and filtered through a multi-screen filtration system. Detection: The filter was dried at 37 ° C, then 1000 μl/well of flashing agent was added, and the 33P-labeled tissue gland was detected by the top counting instrument by radioactivity counting.

C:\2D-OODE\91-Ol\90ll9473.ptd 第126頁 1327569 五、發明說明（124) 一-— H1 〇 PKA活性之抑制檢定分析激酶反應：10 組織腺H1.(西革瑪公司# h_55〇5)基質，10 ATP(0_2 #Ci P33r〜ATp) ^單位牛心ρκ"Α(西革瑪公司# 2 6 4 5 ),適當濃度抑制劑於終容積丨〇〇微升緩衝C:\2D-OODE\91-Ol\90ll9473.ptd Page 126 1327569 V. INSTRUCTIONS (124) I--H1 〇PKA activity inhibition assay Analytical kinase reaction: 10 Tissue gland H1. (西格玛公司# H_55〇5) Matrix, 10 ATP(0_2 #Ci P33r~ATp) ^Unit Niu Xinρκ"Α(西格玛#2 6 4 5 ), appropriate concentration inhibitor in final volume 丨〇〇 microliter buffer

液（TRIS HC1 10 mM pH 7.5 ’MgCl2 1〇 mM，7.5 mM DTT + 0· 2毫克/毫升BSA)加至96孔U字形孔底平板之各孔。於37 t：培育5分鐘後，藉加入20微升EDTA 120 mM中止反應。捕捉：1 0 0微升由各孔移·至多重篩檢平板，讓基質結合至碟酸纖維素濾紙。然後平板以1 50微升/孔不含Ca++/Mg++之 PBS洗3次，以及藉多重篩檢過濾系統過濾。仏測：讓過遽器於3 7 C乾燥’然後加入1 〇〇微升/孔閃爍劑，由頂計數儀器藉放射性計數而檢測經33 p標記的组織跦 H1。 ’ E G F R活性之抑制檢定分析激酶反應：25 nM居家生物素化Po lyGluTyr (西革瑪公司# 02 75 )基質 ’25 ATP(0.3 #Ci P33r-ATP)，80 毫微克桿病毒共同表現G S T - E G F R，適當濃度抑制劑於終容積1 〇〇微升緩衝液（Hepes 50 mM pH 7. 5，MnCl2-MgCl2 3 mM，1 mM DTT + 3 NaV03 ’ 〇_ l毫克/毫升BSA)加至96孔U字形孔底平板之各孔《於37 °C培育5分鐘後’藉加入20微升EDTA 120 mM中止反應。捕捉：1 0 0微升由各孔移至鏈絲菌抗生物素新鮮平板，讓The solution (TRIS HC1 10 mM pH 7.5 'MgCl2 1 mM mM, 7.5 mM DTT + 0.2 mg/ml BSA) was added to each well of a 96-well U-shaped bottom plate. After 37 minutes of incubation, the reaction was stopped by the addition of 20 μl of EDTA 120 mM. Capture: 100 μl of each well was transferred to a multi-screening plate to allow the matrix to bind to the sour cellulose filter paper. The plates were then washed 3 times with 150 liters/well of Ca++/Mg++ free PBS and filtered through a multi-screen filtration system. Speculation: Let the filter dry at 3 7 C. Then add 1 〇〇 microliter/well scintillator, and the 33 p labeled tissue 跦 H1 is detected by the top counting instrument by radioactivity counting. 'Inhibition assay for EGFR activity assay Kinase reaction: 25 nM home biotinylated Po lyGluTyr (Sigma 5 # 75 75 ) Matrix '25 ATP (0.3 #Ci P33r-ATP), 80 ng of rod virus together to express GST - EGFR , the appropriate concentration of inhibitor in a final volume of 1 〇〇 microliter buffer (Hepes 50 mM pH 7.5, MnCl2-MgCl2 3 mM, 1 mM DTT + 3 NaV03 ' 〇 _ l mg / ml BSA) was added to 96-well U The wells of the bottom plate of the glyphs were "incubated at 37 ° C for 5 minutes" to stop the reaction by adding 20 μl of EDTA 120 mM. Capture: 1 0 0 μl moved from each well to a fresh plate of Streptomyces avidin, let

c：\2D-C0DE\91-01\90119473.ptd 第127頁 1327569 五、發明說明（125) 生物素化基質結合至平板.然後平板以15〇微升/孔不含c:\2D-C0DE\91-01\90119473.ptd Page 127 1327569 V. INSTRUCTIONS (125) The biotinylated matrix is bound to the plate. The plate is then contained at 15 μL/well.

Ca++/Mg++ 之PBS 洗3 次。檢測：於頂計數儀器做放射性計數。 I GF 1 -R活性之抑制檢定分析 I G F 1 R活|·生之抑制檢定分析係根據如下方案進行。，酶反應.1 0以Μ生物素化MBP(西革瑪公司型號m-ι 891 ) 土貝〇 //Μ 抑制劑冷ATP，2 ηΜ 33Ρ-ΑΤΡ，及 22.5毫微克1〇卩11(與6〇/^冷^13於室溫前培育3〇分鐘）於終容積30微升緩衝液（5〇 mM HEpES ρΗ 79，3心 1 "Cl2 1 mM DTTNaV03)加至96孔U字形孔底平板之 J1"於至'皿培育35分鐘後，藉加入100微升含32 mM 厂、50 0 &ATP 、〇. 1% 崔頓（Triton) X100 及 1〇毫克 Z升^糸菌抗生物素塗層SPA珠之PBS緩衝液内中止反二c; HI :月1 5刀在里後，取出1 1 0微升懸浮液，移轉至含1 0 0微升 5M CsCl 之 96 1^^14·=,,. 私L九子千板。4小時後平板於派克公司頂計數放射性讀取器讀取2分鐘。。果貝驗資料係使用電腦程式G r aphPad P r i zm分析。 j外 > 推疋蛋白質激酶抑制劑抑制活性及選定化合物之 ^二ί係里由基於使用S P A (閃爍近似值檢定分析）9 6孔平析方法測定。檢定分析係基於鏈絲菌抗生物素塗層朱捕捉由組織腺磷酸化位置衍生而得的生物素化肽〇 m標記磷酸鹽#分藉絲激酶轉移至生物素化 ”且4腺時’ &閃爍計數器測量發射的光。Wash 3 times with Ca++/Mg++ PBS. Detection: Radioactivity counting is performed on the top counting instrument. Inhibition assay analysis of I GF 1 -R activity I G F 1 R live | The inhibition assay was performed according to the following protocol. , Enzyme reaction. 10 Μ biotinylated MBP (Sigma Sigma model m-ι 891) Tube 〇 / / Μ inhibitor cold ATP, 2 ηΜ 33Ρ-ΑΤΡ, and 22.5 ng 1〇卩11 (with 6 〇 / ^ cold ^ 13 incubation at room temperature for 3 〇 minutes) in a final volume of 30 μl buffer (5 mM HEpES ρΗ 79, 3 heart 1 " Cl2 1 mM DTTNaV03) was added to the 96-well U-shaped bottom Tablet J1" After 35 minutes of incubation, add 100 μl of 32 mM plant, 50 0 & ATP, 〇. 1% Triton X100 and 1 〇 mg Z 糸Sustained anti-two c in the PBS buffer of the coated SPA beads; HI: After the knives in the month of 15 knives, remove 110 μl of the suspension and transfer to 96 1^^ containing 1000 μl of 5M CsCl 14·=,,. Private L nine sons. After 4 hours, the plate was read for 2 minutes at the Parker top count radioactive reader. . The fruit test data was analyzed using a computer program G r aphPad P r i zm. j outside > The protein kinase inhibitor inhibitory activity and the selected compound were determined based on the 96-well analytical method based on the use of S P A (flicker approximation assay). The assay consists of a biotinylated peptide 〇m-labeled phosphate derived from the site of adenosine phosphorylation based on Streptococcus avidin-coated Zhu. The transfer of silk kinase to biotinylation and 4 glandular & The scintillation counter measures the emitted light.

1327569 五、發明說明（126) c d k 5 / P 2 5活性之抑制檢定分析 c d k 5 / p 2 5活性之抑制檢定分析係根據下述方案進行。激酶反應：1.0 //M生物素化組織腺肽基質，0.25 yCi P33g-ATP ’ 4 nM cdk5/p25 複體 ’ 〇-10〇 “Μ 抑制劑於終容積 100 微升緩衝液（Hepes 20 mM pH 7.5，MgCl2 15mM，1 mM DTT)添加至96孔U字形孔底平板之各孔。於3了。〇培育2〇分鐘後’藉加入500微克SPA珠於含〇· 1%崔頓χι〇〇、5〇 "μ ATP及5 mM EDTA之磷酸鹽緩衝鹽水而中止反應。讓珠粒沉降’結果於33 P -標記肽的放射性係由頂計數閃燦計數器檢測。結果：資料經分析且使用下式以％抑制表示： 10 0Χ(1-(未知液-背景值）/(酶對照組-背景值D IC 5 0值係使用四參數邏輯算式變化計算. Y=100/[l + 10-（（LogEC50-X)* 斜率）] 此處X = Log( /z M)以及Y = %抑制。 cdc7/dbf 4活性之抑制檢定分析 cdc7/dbf 4活性之抑制檢定分析係根據如不方案進行。生物素MCM2基g #cdc7/dbf4複體於ατρ存在下使用 r33-ATP追蹤進行轉移磷酸化反應。然後經磷酸化的生物素-MCM2基質藉鏈絲菌抗生物素塗層SPA珠粒捕捉，磷酸化程度藉沒計數評估。 cdc7/dbf 4活性之抑制係於96孔平板根據如下方案進行。於平板之各孔内加入：1327569 V. INSTRUCTION DESCRIPTION (126) inhibition assay for c d k 5 / P 2 5 activity The inhibition assay for c d k 5 / p 2 5 activity was carried out according to the following protocol. Kinase reaction: 1.0 //M biotinylated tissue gland peptide matrix, 0.25 yCi P33g-ATP ' 4 nM cdk5/p25 complex ' 〇-10〇 Μ 抑制剂 inhibitor in final volume 100 μl buffer (Hepes 20 mM pH 7.5, MgCl2 15 mM, 1 mM DTT) was added to each well of a 96-well U-shaped bottom plate. After 3 〇 incubation for 2 minutes, 'By adding 500 μg SPA beads to 〇·1% 崔顿χι〇〇 , 5 〇 " μ ATP and 5 mM EDTA phosphate buffered saline to stop the reaction. Let the beads settle. 'Results The radioactivity of the 33 P -labeled peptide was detected by the top counting flash counter. Results: The data was analyzed and used The following formula is expressed as % inhibition: 10 0 Χ (1 - (unknown liquid - background value) / (enzyme control - background value D IC 5 0 value is calculated using a four-parameter logistic formula change. Y = 100 / [l + 10- ((LogEC50-X)* slope)] where X = Log( /z M) and Y = % inhibition. cdc7/dbf 4 activity inhibition assay analysis cdc7/dbf 4 activity inhibition assay analysis is based on no protocol The biotin MCM2 group g #cdc7/dbf4 complex is used in the presence of ατρ to track the phosphorylation reaction using r33-ATP. The prime-MCM2 matrix was captured by streptavidin-resistant biotin-coated SPA beads, and the degree of phosphorylation was evaluated by counting. The inhibition of cdc7/dbf 4 activity was performed on 96-well plates according to the following protocol. :

1327569 五、發明說明（127) -10微升基質（生物素化MCM2，6 終濃度） -10 微升酶（Cdc7/Dbf4，12. 5 nM 終濃度） -1 0微升試驗化合物（1 2種遞增濃度於nM至以Μ之範圍而產生劑量-反應曲線） -10微升冷ΑΤΡ(10 "Μ終濃度）與放射性ΑΤΡ(與冷ΑΤΡ為 1/2500莫耳比）之混合物隨後用於起始反應，讓反應於37 °C進行。基質、酶及ATP 於50 mM 含15 mM MgC12，2 mM DTT > 3 μ, M NaV03，2 mM甘油磷酸酯及0.2毫克/毫升BSA之HEPES pH #7. 9稀釋。試驗化合物溶劑也含有1 0% DMSO。培育20分鐘後，經由於各孔内加入100微升PBS pH 7. 4 中止反應，該PBS含有50 mM EDTA、1 mM冷ATP 、〇. 1%崔頓X 100及10毫克/毫升鏈絲菌抗生物素塗層SPA珠粒。於室溫培育1 5分鐘後，讓生物素化MCM2 -鏈絲菌抗生物素S P A珠粒交互作用，珠粒使用派克公司細胞收穫機（過濾對（Fi 1 termate))捕捉於96孔過濾平板（單一過濾 (U n i f i 11 e r ) G F / BTM)，以蒸德水洗然後使用頂計數器（派克公司）計數。 _ 計數扣除空白組，然後使用非線性迴歸分析（西革瑪圖）測定IC50做分析。阿羅拉-2活性之抑制檢定分析選定的化合物之抑制活性及強度係經由一種檢定分析方法測定，該方法使用鏈絲菌抗生物素閃爍近似值檢定分析珠粒（安莫森醫藥生技公司）於96孔平板進行。反應結束 1 m 1 η _ C: \2D-00DE\91 -01 \90119473. ptd 第 130 頁 1327569 五、發明說明（128) 時，生物素化肽基質於珠粒捕捉，隨後使用CsC 12形成成層。當放射性標記磷酸根部分藉激酶移轉至與珠粒結合的肽時，有閃爍計數器測量發射的光。阿羅拉-2活性之抑制檢定分析係於96孔平板根據如下方案進行。激酶反應：8 // Μ生物素化肽（重複4次L R R W S L G )，1 〇〆μ ATP ( 〇· 5 μ Ci P33g-ATP ) ’ 1 Ο ηΜ 阿羅拉2，1 〇 ν Μ 抑制劑於終容積60微升緩衝液（HEPES 50 mM pH 7.0，MgCl2 lOmM，1 mM DTT，0· 125 毫克 / 毫升BSA， 3 βΜ 正飢酸鹽 )添加至9 6孔U字形孔底平板之各孔。於室溫培育3 〇分鐘後中·止反應，生物素化狀藉加入1 〇〇微升珠粒懸浮液捕捉。成層：100微升CsCl2，7. 5 Μ添加至各孔，讓其放置丨小時，隨後於頂計數儀器計數放射性。結果：資料經分析且參照酶總活性（=1 〇〇%；)以抑制百分比表示。全部顯示抑制2 60%之化合物進一步分析俾經由丨C5〇計算研究抑制劑強度。 ° 使用方案同前述’但使用抑制劑之一系列稀釋。實驗資料使用如下公式藉非線性迴歸匹配：1327569 V. INSTRUCTIONS (127) -10 microliters of matrix (biotinylated MCM2, 6 final concentration) - 10 microliters of enzyme (Cdc7/Dbf4, 12. 5 nM final concentration) - 10 microliters of test compound (1 2 Increasing concentrations from nM to Μ to produce a dose-response curve) - 10 μl of cold mash (10 "final concentration) and radioactive cesium (with chiller enthalpy of 1/2500 mole ratio) At the initial reaction, the reaction was allowed to proceed at 37 °C. The matrix, enzyme and ATP were diluted in 50 mM HEPES pH #7.9 with 15 mM MgC12, 2 mM DTT > 3 μ, M NaV03, 2 mM glycerophosphate and 0.2 mg/ml BSA. The test compound solvent also contained 10% DMSO. After incubation for 20 minutes, the reaction was stopped by adding 100 μl of PBS pH 7.4 in each well containing 50 mM EDTA, 1 mM cold ATP, 〇. 1% Triton X 100 and 10 mg/ml Streptomyces. Avidin coated SPA beads. After incubation for 15 minutes at room temperature, the biotinylated MCM2-streptavidin SPA beads were interacted and the beads were captured on a 96-well filter plate using a Parker cell harvester (Fi 1 termate). (Single filtration (U nifi 11 er) GF / BTM), washed with steamed water and then counted using a top counter (Pike). _ Count the blank group and then use the nonlinear regression analysis (Sigma) to determine the IC50 for analysis. Inhibition assay for Arolah-2 activity The inhibitory activity and intensity of selected compounds were determined by a assay using a Streptococcus avidin scintillation approximation assay to analyze the beads (Amersen Medical Biotech) 96 well plates were used. End of reaction 1 m 1 η _ C: \2D-00DE\91 -01 \90119473. ptd Page 130 1327569 V. Inventive Note (128), biotinylated peptide matrix is captured in beads, followed by formation of layers using CsC 12 . When the radiolabeled phosphate moiety is transferred to the peptide bound to the beads by a kinase, a scintillation counter measures the emitted light. Inhibition assay analysis of Arola-2 activity was performed on 96-well plates according to the following protocol. Kinase reaction: 8 // Μ biotinylated peptide (repeated 4 times LRRWSLG), 1 〇〆μ ATP (〇· 5 μ Ci P33g-ATP ) ' 1 Ο η Μ Arora 2,1 〇ν Μ Inhibitor in final volume 60 μl of buffer (HEPES 50 mM pH 7.0, MgCl 2 10 mM, 1 mM DTT, 0·125 mg/ml BSA, 3 βΜ gestation) was added to each well of a 96-well U-shaped bottom plate. After incubation for 3 minutes at room temperature, the reaction was stopped and the biotinylated material was captured by adding 1 〇〇 microliter bead suspension. Layering: 100 μl of CsCl2, 7.5 Μ was added to each well, allowed to stand for 丨 hours, and then radioactivity was counted on a top counting instrument. RESULTS: Data were analyzed and expressed as percent inhibition by reference to total enzyme activity (=1 〇〇%;). All showed inhibition of 2 60% of the compounds for further analysis. The inhibitor intensity was studied via 丨C5〇. ° Use the protocol in the same way as the previous 'but use one of the inhibitors. The experimental data was matched by nonlinear regression using the following formula:

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度’"為觀察得之反應速度，V。為於無抑制劑存在下之速度，以；, 4 及L 1」為抑制劑濃度。 a5 3 ί⑴ '合物適合投予哺乳類例如人類’可藉尋 :J:投樂’劑量係依據病人年齡、•重投徑決定。处克至==合：=r的適當劑量為每劑本發明化合物可以多種劑型投藥，例如經口投藥呈錠 ::膠囊劑二糖衣或膜衣錠、液體溶液劑或懸浮液劑劑，，直腸技藥呈栓劑劑型；腸外投藥如肌肉注射或藉靜及/或鞘内及/或脊椎内注射或輸入投藥。脈 —此外本發明化合物可呈單劑或另外於組合治療方法投樂’組合治療包含額外化學治療如放射性治療或化學计劃組合細胞抑制劑或細胞毒劑、抗生素類型藥劑、浐= 劑、抗代謝劑、激素劑、免疫劑、干擾素類型劑、環=人酶抑制劑（例如C0X-2抑制劑，特別西里夸克司。 (celecoxib)、若非夸克司（r〇fec〇xib)、帕拉夸克司參parecoxib)及凡戴夸克司（valdec〇xib))、金屬基質酶抑制劑、端粒酶抑制劑、酪胺酸激酶抑制劑、抗生子受體劑、抗-HER劑、抗-EGFR劑、抗血管新生劑 '法尼基轉移酶抑制劑、ras-raf信號轉導路徑抑制劑、細胞^ 期抑制劑、其他cdks抑制劑、微管素結合劑、拓樸異° Ϊ抑制劑 '拓樸異構酶丨丨抑制劑等^ '、晦Degree '" for the observed reaction rate, V. For the speed in the absence of the inhibitor, 4, and L 1" are the inhibitor concentrations. A5 3 ί(1) 'Complex suitable for administration to mammals such as humans' can be borrowed: J: The amount of dose is determined by the age of the patient and the weight of the cast. The appropriate dosage of gram to == combination: = r is that the compound of the present invention can be administered in various dosage forms, for example, orally in the form of a capsule: a capsule disaccharide or a film coating, a liquid solution or a suspension preparation, The rectal bolus is in the form of a suppository; parenteral administration such as intramuscular or by intravenous and/or intrathecal and/or intrathecal or enteral administration. Pulses - furthermore, the compounds of the invention may be administered in a single dose or in combination with a combination of therapeutic methods. The combination therapy comprises additional chemotherapy such as radiotherapy or chemical planning combined with a cytostatic or cytotoxic agent, an antibiotic type agent, a sputum agent, an anti-metabolite Agents, hormonal agents, immunizing agents, interferon type agents, ring = human enzyme inhibitors (such as C0X-2 inhibitors, especially celecoxib, celecoxib, r〇fec〇xib, paraqueque Parecoxib) and valdec〇xib, metalloproteinase inhibitors, telomerase inhibitors, tyrosine kinase inhibitors, antibiotic receptors, anti-HER agents, anti-EGFR agents , anti-angiogenesis agent 'farnesyltransferase inhibitors, ras-raf signal transduction pathway inhibitors, cell inhibitors, other cdks inhibitors, tubulin binding agents, topological inhibitors Park isomerase inhibitors, etc. ^ ', 晦

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1327569 五、發明說明（130) 舉例言之，本發明化合物可組合一或多種化學治療劑投藥例如伊絲梅斯丁（ e X e m e s t a n e )、福姆梅斯丁 (f ormestane)、阿那思翠左（anas t r ozo 1 e )、里翠左 (letrozole)、法翠左（fadrozole)、紫杉烧（taxane)、紫杉烧衍生物、包囊紫杉烧類、C P T -11、喜樹驗衍生物、蔥環素（a n t h r a c y c 1 i n e )糖苷例如朵松盧比辛 (doxorubicin)、伊達盧t匕辛（idarubicin)、伊皮盧比辛 (epirubicin)、伊妥普賽德（etoposide) ' 那福賓 (navelbine)、芬布萊斯丁（vinblastine) ' 卡布派萊丁 (carboplatin)、西司派萊丁（cisplatin)、伊司達慕斯丁 (est ramus t i ne )' 西里夸克司、塔慕西芬（tamoxifen)、拉隆西芬（raloxifen)、蘇庚（Sugen)SU-5416、蘇庚 SU-6668、贺西普丁（Herceptin)等’視需要於微脂粒調配劑投藥。若調配成固定劑量，則此種組合產物採用於前述劑量範圍之本發明化合物以及於核准劑量範圍之其他醫藥活性劑。當不適合組合配方時，式（丨）化合物可與已知抗癌劑循序使用® 本發明也包括醫藥組成物包含式（1)化合物或其醫藥可接受性鹽組合醫藥可接受性賦形劑（可為載劑或稀釋劑）。含本發明化合物之醫藥組成物通常係遵循習知方法製備，可以醫藥適當劑型投藥。例如固體口服劑型連同活性化合物含有稀釋劑如乳糖、1327569 V. INSTRUCTIONS (130) For example, a compound of the invention may be administered in combination with one or more chemotherapeutic agents such as e X emestane, normestane, anasicui Left (anas tr ozo 1 e ), letrozole, fadrozole, taxane, yew derivative, cystic yew, CPT -11, hi tree test Derivatives, anthracyclines (inhracyc 1 ine) glycosides such as doxorubicin, idarubicin, epirubicin, etoposide 'nafbin (navelbine), vinblastine 'carboplatin, cisplatin, est ramus ti ne' Siriquak, Tamu Tamoxifen, raloxifen, Sugen SU-5416, Su Geng SU-6668, Herceptin, etc. are administered as needed in the liposome formulation. If formulated as a fixed dose, such combination products employ a compound of the invention in the aforementioned dosage range and other pharmaceutically active agents in the approved dosage range. When not suitable for combination, the formula (丨) compound can be used sequentially with known anticancer agents. The present invention also includes a pharmaceutical composition comprising a compound of formula (1) or a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable excipient ( Can be a carrier or a diluent). The pharmaceutical composition containing the compound of the present invention is usually prepared according to a conventional method, and can be administered in a suitable pharmaceutical form. For example, a solid oral dosage form together with the active compound contains a diluent such as lactose,

C:\2D-OODE\91-Ol\90119473.ptd 第133頁 1327569 五、發明說明（131)-- 葡萄糖、薦糖、蔬糖、纖維素、玉米殿粉或馬铃著殿粉；巧滑劑如氧化石夕、滑石、硬脂酸' 鎂或與硬脂酸，及/或聚乙二醇類；黏結劑如澱粉、***膠、明膠、甲基纖維厂a 、甲土，維素或聚乙稀基°比略· °定酿I ;崩散劑如殿粉、褐藻I、褐藻酸鹽或乙醇酸澱粉鈉；發泡混合物丨染料；甜味劑；濕潤劑如卵磷脂、波里索貝（p〇lys〇rbates)、月桂基硫酸鹽；以及—般用於醫藥調配劑之無毒藥理無活性物質。該醫藥製劑可以已知方式製造，例如混纟、造粒、 /丁錠、包糖衣、或包膜衣過程。口服投藥用液體分散液可為糖漿劑、乳液劑及懸浮液劑。 1 Ϊ m含有蔗糖或蔗糖含甘油及/或甘露糖醇及/ 或山梨糖醇作為載劑。果;劑含有例如天然膠、填脂、痛納、肌肉内注射用懸浮= 聚乙烯醇作為載劑。種醫藥可接受性載劑例如以劑醇類如丙二醇以及若有二欖油 '油酸乙酯、甘㉟鹽。靜脈注射或C 朵卡因（lidc)caine)鹽劑，或較佳靜脈注射或装:液劑含有例如無菌水作為載水溶液或含有丙二醇作&用）谷液劑可呈無菌水性等張鹽栓劑連同活性化合物 =W ^ 可可脂、聚乙二醇、聚3有一種醫藥可接受性載劑例如活性劑或卵填脂。A 伸乙基♦山梨糖醇脂肪酸酯界面C:\2D-OODE\91-Ol\90119473.ptd Page 133 1327569 V. Description of invention (131) -- Glucose, recommended sugar, vegetable sugar, cellulose, corn temple powder or horse bell powder; Such as oxidized stone, talc, stearic acid 'magnesium or with stearic acid, and / or polyethylene glycol; adhesives such as starch, gum arabic, gelatin, methyl fiber plant a, clay, vitamins or Polyethylene base ° ratio · ° 定定 I; disintegration agent such as temple powder, brown algae I, alginate or sodium starch glycolate; foaming mixture anthraquinone dye; sweetener; wetting agent such as lecithin, Boriso P〇lys〇rbates, lauryl sulfate; and non-toxic pharmacologically inactive substances commonly used in pharmaceutical formulations. The pharmaceutical preparation can be manufactured in a known manner, such as a mash, granulation, /butment, sugar coating, or coating process. The liquid dispersion for oral administration can be a syrup, an emulsion, and a suspension. 1 Ϊ m contains sucrose or sucrose containing glycerin and/or mannitol and/or sorbitol as carrier. The agent contains, for example, natural gum, fat-filling, pain, and suspension for intramuscular injection = polyvinyl alcohol as a carrier. A pharmaceutically acceptable carrier is, for example, a pharmaceutically acceptable alcohol such as propylene glycol and, if any, oleic oil, ethyl oleate, gansyl salt. Intravenous or C. docaine (caine) salt, or preferably intravenous or liquid: a solution containing, for example, sterile water as a carrier solution or a solution containing propylene glycol as & The suppository together with the active compound = W ^ cocoa butter, polyethylene glycol, poly 3 has a pharmaceutically acceptable carrier such as an active agent or an egg fat. A stretch ethyl ♦ sorbitol fatty acid ester interface

C:\2D-00DE\91-01\90119473.ptd 第134頁 1327569 五、發明說明（132) --—- 本發明也提供式（I )化合物或其醫藥可接受性鹽用以製造藥物用於正在接受同時、分開或循序抗癌治療的病人治療經由蛋白質激_活性變更引起的及/或關聯的疾病。下列實施例意圖舉例說明本發明但非限制性。 f施例1 N-(3-氰基丙基），n-芊基甘胺酸乙酯之製備 N-苄基甘胺酸乙酯（〇17莫耳，32.8克）及無水碳酸鉀 (0. 187莫耳’ 25. 8克）懸浮於300毫升乙腈，逐滴加入4一;臭C:\2D-00DE\91-01\90119473.ptd Page 134 1327569 V. INSTRUCTION DESCRIPTION (132) --- The present invention also provides a compound of formula (I) or a pharmaceutically acceptable salt thereof for use in the manufacture of a medicament Patients undergoing simultaneous, separate or sequential anti-cancer therapy are treated for diseases caused by changes in protein activation activity and/or associated. The following examples are intended to illustrate the invention but are not limiting. f Example 1 Preparation of N-(3-cyanopropyl), n-decylglycine ethyl ester N-benzylglycine ethyl ester (〇17 mol, 32.8 g) and anhydrous potassium carbonate (0 187 Moer ' 25. 8 g) suspended in 300 ml of acetonitrile, added dropwise to 4;

丁腈，（0 . 1 8 7莫耳，2 7 · 7克）。所得混合物回流攪拌1 6小時然後過濾。濾液經蒸發至乾獲得淡黃色油，油使用己坑 /乙酸乙酯（2 : 1 )作為洗提劑於矽膠藉急速層析術純化，獲得標題化合物呈無色油（5 5 . 3克，8 3%)。實施例2 N-(3 -氰基丙基），N-(第三丁酯基）甘胺酸乙酯之製備 N-(3 -氰基丙基），N-苄基甘胺酸乙酯（0.13莫耳，33.8 克）’二碳酸二第三丁酯（0.26莫耳，56.7克）及鈀/碳 (10如/卩’3.4克）懸浮於400宅升無水乙醇及於巴爾裝置於 4 0 PS I氫化6小時。所得混合物經過慮及濾液蒸發至乾獲Nitrile, (0.18 7 m, 2 7 · 7 g). The resulting mixture was stirred at reflux for 16 hours and then filtered. The filtrate was evaporated to dryness to give a pale yellow oil, which was purified eluting with EtOAc (EtOAc) 3%). Example 2 Preparation of N-(3-cyanopropyl), N-(t-butyl ester)glycolic acid ethyl ester N-(3-cyanopropyl), ethyl N-benzylglycine (0.13 mol, 33.8 g) 'Dibutyl dicarbonate (0.26 mol, 56.7 g) and palladium/carbon (10 such as / 卩 '3.4 g) suspended in 400 liters of absolute ethanol and in the Barr device at 4 0 PS I was hydrogenated for 6 hours. The resulting mixture was subjected to evaporation of the filtrate to dryness.

得淡黃色油。粗料使用己烷/乙酸乙酯（7 : 3 )作為洗提劑於石夕膠It急速層析術純化’獲得標題化合物呈無色油（2 5 3 克，72%)。 ' 名 · 實施例3 氰基-3-氧基-1-。底》定敌酸第三丁酯之製備 N-(3-氰基丙基），N-(第三丁酯基）甘胺酸乙酯（〇〇9莫Light yellow oil. The crude material was purified using hexane/EtOAc (EtOAc:EtOAc) 'Name · Example 3 Cyano-3-oxy-1-. Preparation of Dicesterate D-Butyl Ester N-(3-Cyanopropyl), N-(T-Butyl Ethyl) Glycolate (〇〇9 Mo

C： \2D.〇〇DE\91-01\90119473.ptd 第135頁 1327569 五、發明說明（133) 耳，24. 3克）溶解於350毫升曱苯及溶液於〇冷卻。逐份加入第二丁氧化鉀（0· 1莫耳，Η. 2克）同時攪拌。經3〇分鐘後加入500毫升飽和氣化銨溶液及⑽以㈣鹽酸調整至6 〇分離有機相且水層以DCM洗兩次。收集的有機層以硫酸鈉脫水，過濾及蒸發。所得黃色油（19 8克，98%)未經進一步醇化即用於次一步驟。 f施例4 氫吡咯并[3，4 - c ]吼唑 3 -胺基- 5- (第三丁酷基）_4,6-之製備 3-氰基-4-氧基-1-吡咯啶羧酸第三丁酯（〇〇856莫耳， 18.0克）及肼二鹽酸鹽（0.1 027莫耳，1〇 8克）於45〇毫升乙醇之混合物於6(TC授拌4小時。冷卻所得混合物至K後，緩慢逐滴加人飽和錢氫鋼；容液（1〇〇毫升）。溶劑經真空蒸發’殘餘水以乙酸乙酯萃取，古k ' „ •—十丨一找s社如卞取有機相以無水硫酸鈉脫 ^ 寸U 產物，使用二氯曱烷：曱醇 (4 6 : 4 )作為洗k劑於石夕勝雜各；丰既 9 ^ m 胗稭急速層析術純化，獲得標題化合物呈白色固體（5. 91克，31%)。C: \2D.〇〇DE\91-01\90119473.ptd Page 135 1327569 V. Description of invention (133) Ear, 24. 3 g) Dissolved in 350 ml of hydrazine and solution in 〇 to cool. A second potassium pentoxide (0.1 mole, Η. 2 g) was added portionwise while stirring. After 3 minutes, 500 ml of saturated ammonium hydride solution was added and (10) adjusted to 6 以 with (iv) hydrochloric acid. The organic phase was separated and the aqueous layer was washed twice with DCM. The collected organic layer was dried over sodium sulfate, filtered and evaporated. The resulting yellow oil (19 g, 98%) was used in the next step without further alcohol. f Example 4 Preparation of hydrogen pyrrolo[3,4 - c ]carbazole 3 -amino- 5- (t-butanyl)_4,6- 3-cyano-4-oxy-1-pyrrolidine A mixture of tributyl carboxylic acid (〇〇856 mol, 18.0 g) and hydrazine dihydrochloride (0.1 027 mol, 1 〇 8 g) in 45 ml of ethanol was stirred at 6 (TC for 4 hours). After the obtained mixture is brought to K, the saturated hydrogen hydrogen steel is slowly added dropwise; the liquid solution (1 〇〇 ml). The solvent is evaporated in vacuo. The residual water is extracted with ethyl acetate. The ancient k ' „ • For example, the organic phase is extracted with anhydrous sodium sulfate to remove the U product, and the dichlorosilane: decyl alcohol (4 6 : 4 ) is used as a washing agent in Shi Xisheng; each of the 9 ^ m stalks rapid chromatography The title compound was obtained as a white solid (5. 91 g, 31%).

熔點 1 9 5 - 1 9 7 °C (M + H)+ = 224 以類似方式始於適當3-氰美_4, 制供丁几人从亂基氧基-1 -吡咯啶羧酸酯可製備下列化合物： 3 -胺基-5-乙醯基-4 β-- 办、，Melting point 1 9 5 - 1 9 7 ° C (M + H) + = 224 In a similar manner, starting from the appropriate 3-cyanoacetin _4, the system can be used for several people from cyclyloxy-1 -pyrrolidine carboxylate. The following compounds were prepared: 3-amino-5-ethinyl-4β--,

4, b —虱0比咯并[3 4-c]吡唑熔點259-260 °C } J (M + H)+ = l 664, b —虱0 is more than [3 4-c]pyrazole melting point 259-260 °C } J (M + H)+ = l 66

1327569 五、發明說明（134) 3 -胺基- 5- (第三丁 S旨基）-6,6 -二曱基-4，6 -二氫D比11 各并 [3，4 - c ] °比 °坐1327569 V. INSTRUCTIONS (134) 3-Amino- 5-(Tertiary S-)-6,6-dimercapto-4,6-dihydro-D ratio 11 and [3,4 - c ] ° than ° sitting

熔點 1 0 0 - 1 0 2 °C (M + H)+ = 252 3 -胺基- 5- (第三丁 S旨基）-6-窄氧甲基-4，6_二氫吼13各并 [3，4 - c ] °比 D坐 (M + H)+ = 345 以類似方式，始於適當4_氛基_3_氧基-1_°底°定缓酸第三丁酯，製備下列化合物： 3 -胺基-6-(第三丁酯基）-4, 5, 6, 7 -四氫吡啶[3, 4-c] 0比唑第三丁酯Melting point 1 0 0 - 1 0 2 °C (M + H)+ = 252 3 -Amino- 5- (Third-butylene)-6-Narrow-oxymethyl-4,6-dihydroindole 13 And [3,4 - c ] ° is more than D sitting (M + H) + = 345 in a similar manner, starting from the appropriate 4_yl group _3_oxy-1_° bottom to determine the acidity of the third butyl ester, prepared The following compounds: 3-amino-6-(t-butyl ester)-4, 5, 6, 7-tetrahydropyridine [3, 4-c] 0-pyrazole tert-butyl ester

熔點 1 5 3 -1 5 5 °C (M + H)+ = 238 以類似方式，始於適當3-氰基_4_氧基瓜°定敌酸第三丁酯，製備下列化合物： 3 -胺基-5-(第三丁酯基）-4,5,6，7 -四氫吡啶[4, 3-c] 口比唑第三丁酯Melting point 1 5 3 -1 5 5 ° C (M + H) + = 238 In a similar manner, starting from the appropriate 3-cyano-4-imoxy guar-tert-butyl ester, the following compounds were prepared: 3 - Amino-5-(t-butylester)-4,5,6,7-tetrahydropyridine[4,3-c] orthoazole tert-butyl ester

熔點 1 5 1 -1 5 5 °C (M + H)+ = 238 實施例5 N-{3 -胺基-5-(第三丁酯基）-4, 6 -二氫η比咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲之製備 3 -胺基-5-(第三丁酯基）-4, 6 -二氫咄咯并[3,4-c]吡唑 (10. 7毫莫耳，2.4克）溶解於20毫升二氯甲烷無水物於氮Melting point 1 5 1 -1 5 5 ° C (M + H) + = 238 Example 5 N-{3 -amino-5-(t-butyl ester)-4,6-dihydro-n-pyrano[ Preparation of 3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene urea 3-amino-5-(t-butylester)-4,6-dihydroindole[ 3,4-c]pyrazole (10.7 mmol, 2.4 g) dissolved in 20 ml of dichloromethane anhydrate in nitrogen

C:\2D-00DE\91-01\90119473.ptd 第137頁 1327569 五、發明說明（135) 氣氣氛下添加至先前於200毫升無水二氯曱烧溶脹的異氰酸曱酯聚苯乙烯樹脂（20 0-40 0篩目，2% DVB，負載1. 49毫莫耳/克，1 0克）。結果所得懸浮液於22 °C溫和攪拌1 8小時至溶液中不再偵測得微量3 -胺基-5 -(第三丁酯基）-4，6 -二氫吡咯并[3, 4-c ]咄唑為止。樹脂經過濾，以二氯曱烷及曱醇洗滌及真空脫水。以類似方式可製備下列化合物： N-{3 -胺基-5-乙醯基- 4,6 -二氫吼11 各并[3,4-c] °比°坐-1-基}，Ν’ -曱基聚苯乙烯脲 • 1^-{3-胺基-5-(第三丁酯基）-6,6-二曱基-4,6-二氫吡咯并[3,4-(：]吡唑-1-基}，1^’-甲基聚苯乙烯脲 Ν-{3 -胺基-5-(第三丁酯基）-6-苄氧曱基-4, 6 -二氫吡咯并[3, 4-c] °比唑-l-基}，！^’ -甲基聚苯乙烯脲 N-{3 -胺基- 6- (第三丁醋基）-4,5,6,7-四氫°比。定[3,4-c] 吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 !^-{3-胺基-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4,3-(：] 吡唑-1 -基}，Ν ’ -曱基聚苯乙烯脲實施例6 φ Ν-{3 -苯乙醯胺基-5-(第三丁酯基）-4,6 -二氫°比咯并 [3,4-c]咄唑-1-基},Ν’-曱基聚苯乙烯脲之製備苯乙醯氣（24. 08毫莫耳，3. 18毫升）於10毫升無水二氯曱烷之溶液逐滴添加至N-{3 -胺基-5-(第三丁酯基）-4, 6-二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲（3. 01 毫莫耳，3.5克），該脲事先於90毫升無水二氯曱烷及16. 5C:\2D-00DE\91-01\90119473.ptd Page 137 1327569 V. INSTRUCTIONS (135) Addition to a polystyrene resin isocyanate which was previously swollen in 200 ml of anhydrous dichlorohydrazine. (20 0-40 0 mesh, 2% DVB, load 1. 49 mmol/g, 10 g). As a result, the obtained suspension was gently stirred at 22 ° C for 18 hours until no trace of 3-amino-5-(t-butyl ester)-4,6-dihydropyrrolo[3, 4- was detected in the solution. c] carbazole. The resin was filtered, washed with dichloromethane and decyl alcohol and vacuum dried. The following compounds can be prepared in a similar manner: N-{3-amino-5-ethenyl- 4,6-dihydroindole 11 each [3,4-c] °°--1-yl}, Ν '-mercaptopolystyrene urea•1^-{3-amino-5-(t-butylester)-6,6-dimercapto-4,6-dihydropyrrolo[3,4-( :]pyrazol-1-yl},1^'-methylpolystyrene-indole-{3-amino-5-(t-butylester)-6-benzyloxyindolyl-4,6-di Hydropyrrolo[3,4-c] ° azole-l-yl}, !^'-methylpolystyrene urea N-{3-amino-6-(tributyl vine)-4,5 ,6,7-tetrahydrogen ratio. [3,4-c]pyrazol-1-yl}, Ν'-methyl polystyrene urea!^-{3-amino-5-(third butyl Esteryl)-4,5,6,7-tetrahydropyridine [4,3-(:]pyrazol-1-yl}, Ν '-mercaptopolystyrene urea Example 6 φ Ν-{3 - benzene Ethylamino-5-(t-butylester)-4,6-dihydropyrolo[3,4-c]oxazol-1-yl}, Ν'-mercaptopolystyrene Preparation of phenelethane gas (24. 08 mmol, 3.18 ml) in 10 ml of anhydrous dichloromethane was added dropwise to N-{3-amino-5-(t-butyl ester)- 4,6-Dihydropyrrolo[3,4-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene (3.11 mmol) , 3.5 g), the urea in 90 ml dry dichloromethane previously alkoxy and 16.5 Yue

C:\2D-C0DE\91-01\90119473.ptd 第138頁 1327569 五、發明說明（136) 毫升DIEA( 9 6. 32毫莫耳）溶脹。結果所得懸浮液於22 °C溫和攪拌1 8小時。然後樹脂經過濾，以二氣甲烷、甲醇洗滌及真空脫水。以類似方式，經由使用適當醯氣可製備下列化合物： N_{3_乙酿胺基- 5- (第三丁 S旨基）-4，6_二氫吼11 各并 [3,4-c]吡唑-1-基}，1^’-曱基聚苯乙烯脲 N-{3 -環丙烷羧醯胺基-5-(第三丁酯基）-4,6 -二氫咄咯并[3,4-c]吡唑-1-基},1\1’-甲基聚苯乙烯脲 N-{3 -異丁醯胺基-5-(第三丁酯基）-4,6 -二氫吡咯并[3, 4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3 -環戊院缓酿胺基-5-(第三丁自旨基）-4，6 -二氫n比0各并[3,4-c]DitD坐-1_S}，N’_甲基聚苯乙稀脈 N_{3_苯甲酿胺基-5-(第三丁醋基）-4，6 -二氫0比ρ各并[3， 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-甲基吡啶甲醯胺基-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3 -於驗酿胺基- 5- (第三丁 _基）-*4，6 -二氫n比p各并[3, 4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3 -異菸鹼醢胺基- 5- (第三丁酯基）-4, 6 -二氫吡咯并 [3,4-〇]吡唑-1-基}，1^’-甲基聚苯乙烯脲 N-{3-(3-甲基-2 -呋喃）-醯胺基-5-(第三丁酯基）-4,6-二氫0比p各并[3,4-c] 0比°坐-1-基},^1’ -曱基聚苯乙稀脲 N_{3_(嗔吩_2_缓酿胺基）_5_(第三丁自旨基）-4，6_二氮〇比咯并[3,4-c] °比唑-1-*}，N’-曱基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 138 1327569 V. INSTRUCTIONS (136) Swelling in milliliters of DIEA (9 6. 32 millimoles). As a result, the resulting suspension was gently stirred at 22 ° C for 18 hours. The resin was then filtered, washed with di-methane, methanol and vacuum dehydrated. In a similar manner, the following compounds can be prepared via the use of appropriate helium: N_{3_ethinylamino-5-(t-butyryl)-4,6-dihydroindole 11 each [3,4-c Pyrazol-1-yl}, 1^'-mercaptopolystyrene urea N-{3-cyclopropanecarboxyguanidino-5-(t-butyl ester)-4,6-dihydroindole [3,4-c]pyrazol-1-yl},1\1'-methylpolystyrene urea N-{3-isobutylammonium-5-(t-butyl ester)-4,6 -dihydropyrrolo[3,4-c]pyrazol-1-yl},N'-mercaptopolystyrene urea N-{3 -cyclopentanyl slow-lating amine-5- Base)-4,6-dihydron n is 0 and each [3,4-c]DitD sits -1_S}, N'_methyl polystyrene ring N_{3_benzamide-5-( Third butyrate)-4,6-dihydrogen 0 to ρ-[3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene-ruthenium-{3-methylpyridine Methionamine-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-mercaptopolystyrene urea N-{ 3 - in the presence of amine-5-(T-butyryl)-*4,6-dihydro-n-p-[3,4-c]pyrazol-1-yl}, N'-fluorenyl Polystyrene urea N-{3 -isonicotinium amide- 5- (t-butyl ester)-4,6-dihydropyrrolo[3,4-anthracene Pyrazol-1-yl}, 1^'-methyl polystyrene urea N-{3-(3-methyl-2-furan)-nonylamino-5-(t-butyl ester)-4 ,6-dihydrogen 0 to p each and [3,4-c] 0 to ° sitting-1-yl}, ^1'-mercaptopolyphenylene urea N_{3_(嗔 _2_2_ 酿酿Base)_5_(third butyl from the base)-4,6-diazepinepyrolo[3,4-c] °pyrazole-1-*}, N'-mercaptopolystyrene

C:\2D-OODE\91-Ol\90119473.ptd 第139頁 1327569 五、發明說明（137) N-{3-(噻吩-3 -羧醯胺基）-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 N-{3-(鄰曱苯甲醯胺基）-5-(第三丁酯基）-4,6 -二氫吼咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(間曱苯甲醯胺基）-5-(第三丁酯基）-4,6 -二氫吡咯并[3, 4-c]吡唑-1-基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3-(對曱苯甲醯胺基）-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3 -水楊酿胺基- 5- (第三丁 S旨基）-4, 6 -二氮π比洛弁[3, ίϊ-c]吡唑-1-基}，Ν’-甲基聚苯乙烯脲 N-{3-(2- it苯曱酿胺基）-5-(第三丁 S旨基）-4，6 -二氫口比咯并[3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(3_氟苯甲酿胺基）-5-(第三丁西旨基）-4，6 -二氫σ比咯并[3,4-c]咄唑曱基聚苯乙烯脲 N-{3-(4- it苯甲酿胺基）-5-(第三丁 S旨基）-4，6 -二氫0比咯并[3,4-c]吡唑-1-基}，『_曱基聚苯乙烯脲 N-{3-(°塞吩-2-乙酿胺基）-5-(第三丁 S旨基）-4，6_二氫0比咯并[3,4-c]咄唑-1-基}，Ν’ -曱基聚苯乙烯脲 N-{3-(°塞吩-3-乙酿胺基）-5-(第三丁自旨基）-4,6 -二氫π比咯并[3,4-c]吡唑曱基聚苯乙烯脲 Ν-{3 -苯基丙炔醯胺基-5-(第三丁酯基）-4, 6 -二氫咄咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(3 -氰基苯甲醯胺基）-5-(第三丁酉旨基）- 4，6 -二氫咄咯并[3, 4-c]吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲C:\2D-OODE\91-Ol\90119473.ptd Page 139 1327569 V. INSTRUCTIONS (137) N-{3-(thiophene-3-carboxycarboxamide)-5-(t-butyl ester) -4,6-dihydropyrrolo[3,4-c]pyrazole-1-*}, N'-mercaptopolystyrene urea N-{3-(o-phthalylamino)-5- (t-butyl ester)-4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene uranium-{3-(m-phenylene) Methionido)-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-ylindole, Ν'-mercaptopolystyrene uranium- {3-(p-Minylamino)-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-A Polystyrene urea N-{3 - salicylamino- 5- (Third-butyl group)-4,6-diaza π piroxime [3, ίϊ-c]pyrazol-1-yl },Ν'-methyl polystyrene urea N-{3-(2- it benzoguanamine)-5-(t-butylene)-4,6-dihydro-portion ,4-c]pyrazol-1-yl},N'-mercaptopolystyrene urea N-{3-(3-fluorobenzamide)-5-(t-butylidene)-4 ,6-dihydroσ-pyrolo[3,4-c]oxazolyl polystyrene urea N-{3-(4- it phenylamino)-5-(Third -4,6-dihydro- 0-pyrolo[3,4-c]pyrazol-1-yl}, "_mercaptopolystyrene urea N-{3-(°Cet-2-Erytamine -5-(Third-butyl group)-4,6-dihydro- 0-pyrrolo[3,4-c]oxazol-1-yl}, Ν'-mercaptopolystyrene urea N- {3-(°Cet-6-3-ethylamino)-5-(Third-butyl)-4,6-Dihydropyr-pyrolo[3,4-c]pyrazolylpolyphenylene Ethylene urea-p-{3-phenylpropynyl decylamino-5-(t-butyl ester)-4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, hydrazine '-Methylpolystyrene-indole-{3-(3-cyanobenzamide)-5-(t-butylindole)- 4,6-dihydroindole[3, 4-c Pyrazol-1-ylindole, Ν'-methyl polystyrene urea

C:\2D-00DE\91-0l\90119473.ptd 第140頁 1327569 五、發明說明（138) N-{3-(4-氰基苯甲醯胺基）-5-(第三丁酯基）-4,6_二氮吼咯并[3,4-c]吡唑-1_基}，^_曱基聚苯乙烯脲 N-{ 3-反桂皮醯胺基_5-(第三丁酯基）-4, 6 -二氫咣洛并 [3,4-(：]吡唑_1-基}，^-甲基聚苯乙烯脲 N-{3 -順桂皮醯胺基-5_(第三丁酯基）-4, 6 -二氫咄嘻并 [3,4-c]吡唑-1-基丨，N’_曱基聚苯乙烯脲 N-{3-[3-(3 -吡啶基）丙烯醯胺基]-5-(第三丁酯基） -4, 6 -二氫吡咯并[3, 4_c]吼。坐-1-基}，N，-曱基聚笨乙稀脲 N - {3-[3-(4-0比咬基）丙烯醯胺基]_5-(第三丁酷美） -4,6-二氫吡咯并[3,4_(：]11比0坐-1''基}，1'1’-甲基聚笨乙稀服 N-{3-(2-苯基丙醯胺基）_5_(第三丁酯基）-4,6 -二氣口比 0各并[3,4-c]p比0坐-1_基丨，N -曱基聚苯乙稀脲 N-{3-鄰甲苯基乙醯胺基-5_(第三丁酯基）-4 6---咯并[3, 4_c]吼唑-1-基丨，Ν’ -甲基聚苯乙烯脲. Ν-{3-間甲苯基乙醯胺基_5_(第三丁酯基）-4,6 -二礼η 咯并[3,4-c]0比唑-1-基}，Ν’_曱基聚苯乙烯脲里 °比咯并 Ν-{3 -對甲苯基乙醯胺基_5_(第三丁酯基）-4,6 -二洛并[3,4-c]吡唑-1_基}，1 _曱基聚笨乙烯脲 N-{3-鄰茴香醯胺基-5-(第三丁酯基）-4,6 -二氣 [3,4-c] 0比唾-1-基}，『-甲基聚笨乙稀脲 N-{3_(3-曱氧苯曱醯胺基）_5-(第三丁能基）—4 6 _ Λ 吡咯并[3, 4-c]吡唑-1-基丨，Ν’_曱基聚笨乙烯服氣氫0比嘻并 Ν_{3_對菌香酿胺基_5_(第二丁 S旨基）~4 β_ [3，4-c]吼0坐-1_基丨，^ _甲基聚笨乙稀服C:\2D-00DE\91-0l\90119473.ptd Page 140 1327569 V. INSTRUCTIONS (138) N-{3-(4-Cyanobenzamide)-5-(T-butyl ester group -4,6-diazapyrrolo[3,4-c]pyrazole-1_yl},^_mercaptopolystyrene urea N-{ 3-anti-guinea amide-5-(third Butyl ester)-4,6-dihydroindolo[3,4-(:]pyrazol-1-yl},^-methylpolystyrene urea N-{3-cis cinnamyl-5- (t-butyl ester)-4,6-dihydroindeno[3,4-c]pyrazol-1-ylindole, N'-mercaptopolystyrene urea N-{3-[3-( 3-pyridyl)propenylamino]-5-(t-butylester)-4,6-dihydropyrrolo[3,4_c]indole. sitting-1-yl},N,-fluorenyl poly Ethylurea N - {3-[3-(4-0 than butyl) acrylamido]]_5-(Third Cum) -4,6-dihydropyrrolo[3,4_(:]11 Sitting on -1'' base than 0, 1'1'-methyl polystyrene N-{3-(2-phenylpropionamido)_5_(t-butyl ester)-4,6 - The ratio of the two ports is 0 and the ratio of [3,4-c]p is 0 to 1_base, N-mercaptopolyphenylene urea N-{3-o-tolylethylamino-5-(third Esteryl)-4 6---pyrido[3,4_c]oxazol-1-ylindole, Ν'-methylpolystyrene. Ν-{3-m-tolyl oximeamino group _5 _(t-butyl ester)-4,6-two η 咯[3,4-c]0-pyrazol-1-yl}, Ν'_曱-based polystyrene urea ratio {3-p-Tolylethylammonium _5_(t-butylester)-4,6-dioxa[3,4-c]pyrazole-1-yl},1 _fluorenylpolystyrene N-{3-o-anisylamino-5-(t-butylester)-4,6-diox[3,4-c] 0-sal-1-yl}, "-methyl poly stupid Dilute urea N-{3_(3-oxabenzoquinone)_5-(third butenyl)-4 6 _ 吡pyrrolo[3,4-c]pyrazole-1-ylindole, Ν' _ 曱聚聚聚乙乙乙乙乙乙 _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ , ^ _ methyl poly stupid clothing

C:\2D-O0DE\91-Ol\9O119473.ptd 第141頁 1327569 五、發明說明（139) N-{3 -苯氧乙醯胺基-5-(第三丁酯基）-4, 6 -二氫。比咯并 [3,4-(：]吡唑-1-基}，1^’-甲基聚苯乙烯脲 N-{3-(2-氟苯基乙酿胺基）-5-(第三丁自旨基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}, Ν’ -甲基聚苯乙烯脲 Ν_{3-(3_氟苯基乙龜胺基）-5-(第三丁 S旨基）-4，6_二氮咄咯并[3, 4 - c ]咄唑-1 -基}, Ν ’ -甲基聚苯乙烯脲 Ν_{3-(4_氟苯基乙酿胺基）_5-(第三丁 S旨基）-4，6 -二說 °比咯并[3,4-c]吡唑-1-基}，Ν’-曱基聚苯乙烯脲 Ν-{3-[3-(2 -噻吩基）丙烯醯胺基]-5-(第三丁酯基）-•t，6-二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-[3-(3 -噻吩基）丙烯醯胺基]-5-(第三丁酯基）-4，6-二氫°比|1各并[3,4-〇:]11比〇坐-1-基}，1'1’-曱基聚苯乙稀脲 Ν-{3-[3-(2 -噻吩基）丙醯胺基]-5-(第三丁酯基）-4,6-二氫°比D各并[3，4 - c ] 0比0坐-1 -基}，N ’ -曱基聚苯乙稀脲 N-{3-[2 -氣苯曱醯胺基]-5-(第三丁酯基）-4, 6 -二氫吼咯并[3,4-c]吡唑-1-*}，N’ -曱基聚苯乙烯脲 N-{3-[3_氯苯曱酿胺基]-5_(第三丁酷基）-4,6 -二氮0比咯并[3,4-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 φ N-{3-(4 -氣苯曱醯胺基）-5-(第三丁酯基）-4,6 -二氫口比 11 各并[3,4-c] °比°坐-1-基}，^1’ -曱基聚苯乙烯脲 Ν-{3-(1-哌啶丙醯胺基）-5-(第三丁酯基）-4, 6 -二氫吡咯并[3,4-c]吡唑-1-基}，1^’-甲基聚苯乙烯脲 N_{3_(2_乙酿基苯曱酿胺基）_5_(第三丁自旨基）- 4，6_二氫吡咯并[3, 4-c]吡唑-1-基}, Ν’ -甲基聚苯乙烯脲C:\2D-O0DE\91-Ol\9O119473.ptd Page 141 1327569 V. INSTRUCTIONS (139) N-{3-phenoxyethylamino-5-(t-butyl ester)-4, 6 - Dihydrogen. Bis-[3,4-(:]pyrazol-1-yl}, 1^'-methylpolystyrene urea N-{3-(2-fluorophenylethylamino)-5-( ,3,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-methylpolystyrene-hydrazide_{3-(3_fluorophenyl Tortosyl)-5-(t-butylene)-4,6-diazapyrrolo[3,4-c]carbazole-1 -yl}, Ν '-methylpolystyrene hydrazine _ {3-(4-fluorophenylethylamino)_5-(t-butyryl)-4,6-di-r-r-[3,4-c]pyrazol-1-yl}, Ν'-Mercapto-polystyrene-ruthenium-{3-[3-(2-thiophenyl)propenylamino]-5-(t-butylester)-•t,6-dihydropyrrolo[3 , 4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-[3-(3-thiophenyl)propenylamino]-5-(t-butyl ester group -4,6-dihydrogen ratio|1 each [3,4-〇:]11 is more than 〇-yl}, 1'1'-mercaptopolystyrene-ruthenium-{3-[ 3-(2-Thienyl)propanylamino]-5-(t-butylester)-4,6-dihydrogen ratio D and [3,4 - c ] 0 to 0 sit-1 -yl },N '-mercaptopolyphenylene urea N-{3-[2- benzoquinone]-5-(t-butyl ester)-4,6-dihydroindole[3, 4-c]pyrazole-1-*}, N' - mercapto polystyrene urea N-{3-[3_chlorophenylhydrazone]-5_(t-butanyl)-4,6-diaza 0-pyrolo[3,4-c]pyridyl Imidazole-1-*}, N'-mercaptopolystyrene urea φ N-{3-(4-quinophenylamino)-5-(t-butyl ester)-4,6-dihydrogen port Ratio of 11 to [3,4-c] ° ratio -1 -yl}, ^1'-mercaptopolystyrene-indole-{3-(1-piperidinepropanylamino)-5-( Tert-butyl ester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl},1^'-methylpolystyrene urea N_{3_(2_ethyl-branched benzene Brewed amine)_5_(Third-butyl)- 4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-methyl polystyrene

C:\2D-CODE\91-01\90119473_ptd 第142頁 1327569 五、發明說明（140) N-{3-(4-乙酿基苯甲醯胺基）-5-(第：r 丁布一丁酯基）-4 氫吼咯并[3, 4-c]毗唑-1-基}，N’ -甲基聚苯乙歸服’— Ν-{3-(1-萘曱醯胺基）-5-(第三丁酯基）_4 _ 并[3, 4-c]吡唑-卜基}，Ν’ -曱基聚笨乙烯脲各 Ν-{3-(2 -萘甲醯胺基）-5_(第三丁酯基）_4,6_二并[3, 4-c]吡唑-1-基丨，Ν’ -甲基聚笨乙烯氫°比。各脲 Ν-{3-(3-苯甲醯基丙醯胺基）-5-(第三丁 g旨基）一4 6 _ 氫吡咯并[3,4-c]吡唑-1-基}，1^’-甲基聚苯乙烯脲 — N-{3-(4-乙醯胺基笨甲醯胺基）一 5-(第三丁 s旨基）6 二氩吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚笨乙稀服’ Ν-{3-(2,5 -二甲氧苯曱醯胺基）-5-(第三丁酿基）6 二氩咄咯并[3,4-c]吡唑-1-基}，^’-曱基聚笨乙&服’ ~ N-{3-(2,6 -二甲氧苯曱醢胺基）-5-(第三丁 g旨基）_4 二氩咄咯并[3,4-c]e比唑-1-基}，『-曱基聚笨乙稀服’ N-{3-(3,4-二甲氧苯甲醯胺基）-5-(第三丁龜基）_4 二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -甲基聚笨乙歸服’ Ν-{3-(3,5 -二曱氧笨曱醯胺基）-5-(第三丁 a旨基）_4 二氫吡咯并[3, 4-c] 11比唑-1-基}，Ν’ -甲基聚笨乙婦服’ 6 Ν-{3-3-(2 -噻吩醯）-丙醯胺基-5-(第三丁 g旨基）__4 氫吡咯并[3,4-c]吡唑-1-基}，N’-曱基聚笨乙稀^服 * 6' ~ N-{3-(2-萘基乙醯胺基）-5-(第三丁酯基）_4 洛并[3,4-c] 〇比0坐-1_基},『-甲基聚苯乙稀服 N-{3-(1-萘基乙醯胺基）-5-(第三丁酯基）_4,6_ _ 0各并[3, 4-c] 0比0坐-I-基丨，Ν’ -甲基聚苯乙歸服C:\2D-CODE\91-01\90119473_ptd Page 142 1327569 V. INSTRUCTIONS (140) N-{3-(4-Ethylbenzamide)-5-(: r: Butyl ester)-4 hydroquino[3,4-c]pyrazole-1-yl}, N'-methyl polyphenylene tributary '- Ν-{3-(1-naphthylamino group )-5-(t-butyl ester group)_4 _ and [3, 4-c]pyrazole-buyl}, Ν'-fluorenyl polystyrene ethylene urea Ν-{3-(2-naphthylcarboxamide Base)-5_(t-butylester)_4,6-bis[3,4-c]pyrazol-1-ylindole, Ν'-methyl polystyrene hydrogen ratio. Each urea-{3-(3-benzylmercaptopropylamino)-5-(t-butylg-yl)- 4 6 _hydropyrrolo[3,4-c]pyrazol-1-yl }, 1^'-methyl polystyrene urea - N-{3-(4-ethylammonium benzylamino) 5-(t-butyl s-yl) 6 diar-pyrrolo[3, 4-c]pyrazol-1-yl}, Ν'-fluorenyl polystyrene' 服-{3-(2,5-dimethoxybenzoguanidino)-5- (third butyl) (6) diar-argonium [3,4-c]pyrazol-1-yl}, ^'-fluorenyl polyphenylene & 'N-{3-(2,6-dimethoxybenzene)曱醢Amino)-5-(Third butyl group)_4 Diargonium [3,4-c]e than oxazol-1-yl}, 『-曱基聚笨乙服' N- {3-(3,4-Dimethoxybenzamide)-5-(Third Butyryl)_4 Dihydropyrrolo[3,4-c]pyrazole-l-yl},Ν' - Methyl poly bromide belongs to 'Ν-{3-(3,5-dioxooxabenzamine)-5-(tactinyl)_4 dihydropyrrolo[3, 4-c] 11-Bizozol-1-yl}, Ν'-methyl poly phenyl women's clothing '6 Ν-{3-3-(2-thiophene 醯)-propanylamino-5-(third butyl group) __4 Hydropyrrolo[3,4-c]pyrazol-1-yl}, N'-fluorenyl polystyrene^6* ~ N-{3-(2-naphthylethylamino)- 5- (third Esteryl)_4 lorata[3,4-c] 〇 is 0-1_ base}, "-methylpolystyrene N-{3-(1-naphthylethylamino)-5- (T-butyl ester group)_4,6_ _ 0 each [3, 4-c] 0 to 0 sit-I-based Ν, Ν '-methyl polyphenyl benzene

II

C: \2D-CDDE\91 -01 \901 )9473. ptd 第143頁 1327569 五、發明說明（141) N-{3-(4 -苯基苯曱醯胺基）_5-(第三丁酉旨基）-4，6 -二氫咄咯并[3, 4-c]咄唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(2 -呋喃醯胺基）-5-(第三丁酯基）-4,6 -二氫吼咯并[3,4-c]吡唑-l-基}，！^’ -甲基聚苯乙烯脲 N-{3-(4_苯氧苯甲酿胺基）-5-(第三丁醋基）-4，6 -二氫吡咯并[3, 4-c] °比唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(3 -苯氧苯甲醯胺基）-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑曱基聚苯乙烯脲 N-{3-(4_第三丁基-苯曱酿胺基）-5-(第三丁自旨基）-4，6-•二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν_{3_胡椒基叛醒胺基-5-(第三丁醋基）-4，6 -二氫D比17各并[3,4-c]吡唑-1-基}，1\1’-甲基聚苯乙烯脲 N-{3-(2 -萘）丙醯胺基-5-(第三丁酯基）-4,6 -二氫°比咯并[3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3-(6-甲氧-2 -萘）丙醯胺基-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]咄唑-1-基}，『-曱基聚苯乙烯脲 N - {3-(2-乙基丁醯胺基）-5-(第三丁酯基）-4, 6 -二氫吼咯并[3,4-c]咄唑-1-基}，N’-曱基聚苯乙烯脲 Ν-{3-(4_π比基-苯基）丙酿胺基- 5- (第三丁 S旨基） -4,6-二氫吡咯并[3,4-<:]吡唑-1-基}，^-甲基聚苯乙烯脲 N-{3-(2 -氧基-吼洛°定-1-基）苯基}丙醯胺基- 5- (第三丁酯基）-4, 6 -二氫吡咯并[3, 4-c]咄唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(雙環[4. 2. 0]辛-1, 3, 5-三烯-7-羧醯胺基）-5-(第C: \2D-CDDE\91 -01 \901 ) 9473. ptd Page 143 1327569 V. Description of Invention (141) N-{3-(4-Phenylphenylguanidino)_5-(Third -4,6-dihydroindolo[3,4-c]oxazol-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-(2-furanylamino)- 5-(T-butyl ester)-4,6-dihydroindolo[3,4-c]pyrazole-l-yl},! ^'-Methylpolystyrene urea N-{3-(4-phenoxybenzoylamino)-5-(tributylacetate)-4,6-dihydropyrrolo[3, 4-c ° ° oxazol-1-yl}, Ν'-mercaptopolystyrene urea-{3-(3-phenoxybenzamide)-5-(t-butyl ester)-4,6- Dihydropyrrolo[3,4-c]pyrazolyl polystyrene urea N-{3-(4_t-butyl-benzoindolyl)-5-(Third-butyl) 4,6-•Dihydropyrrolo[3,4-c]pyrazole-l-yl},Ν'-mercaptopolystyrene uranium Ν{3_Pepper-based Rescuing Amino-5-(Third Acetyl)-4,6-dihydro D ratio 17 and [3,4-c]pyrazol-1-yl},1\1'-methylpolystyrene urea N-{3-(2-naphthalene Amidino-5-(t-butyl ester)-4,6-dihydropyrolo[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N -{3-(6-methoxy-2-naphthalene)propanylamino-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]oxazol-1-yl },『-曱-based polystyrene urea N - {3-(2-ethylbutylamido)-5-(t-butyl ester)-4,6-dihydroindole[3,4- c] carbazol-1-yl}, N'-mercaptopolystyrene uranyl-{3-(4_π-base-phenyl) propylamino- 5- (Third-butyl)- 4, 6-dihydrogen [3,4-<:]pyrazol-1-yl},^-methylpolystyrene urea N-{3-(2-oxy-indolyl-1-yl)phenyl} Propylamino-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]oxazol-1-yl}, Ν'-methylpolystyrene-ruthenium-{ 3-(bicyclo[4. 2. 0]octyl-1,3,5-triene-7-carboxyguanidino)-5-(

C:\2D-C0DE\91-01\90119473.ptd 第144頁 1327569 五、發明說明（142) 三丁 S旨基）-4，6 -二氫p比p各并[3，4-c] °比〇坐-1_基}，Ν’ _曱基聚苯乙烯脲 Ν-{3-(2 -氧基-吡咯啶-1-基）苯乙醯胺基-5-(第三丁酯基）-4,6 -二氫0比0各并[3,4-c] 0比0坐-1-基}，1^’-甲基聚苯乙稀脈 N-{3-(4 -咄咯啶-1-基）苯乙醯胺基-5-(第三丁酯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-l-基}, Ν’ -甲基聚苯乙烯脲 Ν-{3-(4_三氟i曱基）苯乙酿胺基_5_(第三丁自旨基）-4,6-二氮吼*1 各弁[3，4_c] 0比0坐_1_基}，1^’ -曱基聚苯乙稀脈 N_{3_(2-漠）苯乙酿胺基-5-(第三丁自旨基）_4, 6_二氫0比咯并[3,4-c]吡唑-1-基},『-曱基聚苯乙烯脲 N-{3-[4-(吡咯啶-1-基-羰基曱氧基）]苯乙醯胺基-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3-[3-(胺基幾基甲氧）苯乙酿胺基]-5-(第三丁 S旨基） -4,6-二氫〇比11各并[3,4-(：]0比〇坐-1-基}，1^’-曱基聚苯乙烯脲 N-{3-[4-(2 -氧基唑啶-3 -基）苯乙醯胺基]-5-(第三丁酯基）-4, 6 -二氫0比0各并[3,4-c] 0比。坐-l-基}，！^’ -甲基聚苯乙烯脲 N-{3-[4-(4-甲基哌啡基）苯乙醯胺基]-5-(第三丁酯基） -4,6-二氫"比咯并[3,4-〇]吡唑-1-基}^’-曱基聚苯乙烯脲 N-{3_(苯并[1，3]二氧伍圜_5_基）乙酿胺基-5-（第三丁酯基）-4,6 -二氫吡咯并[3, 4-c]咄唑-l-基}，Ν’ -曱基聚苯乙稀脈C:\2D-C0DE\91-01\90119473.ptd Page 144 1327569 V. Description of the invention (142) Tributyl S-based)-4,6-dihydro-p ratio p and [3,4-c] °〇〇-1_基},Ν' _曱-based polystyrene urea-{3-(2-oxy-pyrrolidin-1-yl)phenylethylamino-5-(t-butyl ester Base)-4,6-dihydrogen 0 to 0 each [3,4-c] 0 to 0-spin-1-yl}, 1^'-methylpolyphenylene oxide N-{3-(4 - Ethrolidin-1-yl)phenethylamino-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazole-l-yl}, Ν' - Methyl polystyrene uranyl-{3-(4-trifluoroifluorenyl)phenylethylamine _5_(Third butyl)-4,6-diazepine*1 弁[3, 4_c] 0 to 0 sitting _1_ base}, 1^' - fluorenyl polystyrene ring N_{3_(2- desert) phenylethylamino-5-(third butyl from the base)_4, 6 _Dihydro 0-pyrolo[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-[4-(pyrrolidin-1-yl-carbonyldecyloxy) )] phenethylamino-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-methyl polystyrene N-{3-[3-(Aminomethylmethoxy) phenylethylamino]-5-(Third-butyl)- 4,6-dihydroindole ratio 11 and [3,4- (:]0 ratio Sodium-1-yl}, 1^'-mercaptopolystyrene urea N-{3-[4-(2-oxoxazolidin-3-yl)phenylethylamino]-5-(third Esteryl)-4,6-dihydrogen 0 to 0 each [3,4-c] 0 ratio. Sit-l-yl}, !^'-methyl polystyrene urea N-{3-[4- (4-methylpiperidinyl) phenethylamino]-5-(t-butyl ester)-4,6-dihydro "pyrolo[3,4-indole]pyrazol-1-yl }^'-Mercapto-polystyrene urea N-{3_(benzo[1,3]dioxosulfanyl-5-yl)ethanoyl-5-(t-butylester)-4,6- Dihydropyrrolo[3,4-c]carbazole-l-yl}, Ν'-mercaptopolystyrene

C:\2D-C0DE\91-01\90119473.ptd 第145頁 1327569 五、發明說明（143) N-{3-[4-(2 -氧基-vg唑啶-3 -基）苯乙醯胺基]-5-(第三丁酯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(2 -苯基-1，3 -噻唑-4 -基）乙醯胺基-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑-1-*}，N’-曱基聚苯乙稀脲 Ν-{3-[4-(1-吡咯啶-2 -酮）苯曱醯胺基]-5-(第三丁酯基）-4,6 -二氫吡咯并[3,4-c]吡唑-1- *}，N’ -曱基聚苯乙稀脈 _ N-{3-[2-(3 -氧基-3,4,4&，83-四氫-2}1-苯并[1，4]嚿畊 -6 -基）乙醯胺基]-5-(第三丁酯基）-4, 6 -二氫。比口各并 [3,4-c] °比0坐-1-&}，N，-曱基聚苯乙烯脲 N-{3-(1-曱基-吲哚-3 -基）乙醯胺基-5-(第三丁酯基） -4, 6 -二氫°比咯并[3,4-c]咄唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(6-氧基-611-。荅°井-1-基）乙酿胺基-5-(第三丁酉旨基）-4,6 -二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙稀脈 Ν-{3_(4-(嗎嚇>-1_基）-苯基）乙酿胺基-5-(第三丁自旨基） 0"4,6-二氫°比咯并[3,4-(：]吡唑-1-基}，1^’-曱基聚苯乙烯脲 Ν-{3_(4 - 13比π定基乙酿胺基）-5_(第三丁醋基）-4, 6 -二氫咄咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯氧乙醢胺基-5-(第三丁酯基）-4, 6 -二氫吡咯并 [3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(3 -吡啶基乙醯胺基）-5-(第三丁酯基）-4,6 -二氫C:\2D-C0DE\91-01\90119473.ptd Page 145 1327569 V. INSTRUCTIONS (143) N-{3-[4-(2-Oxo-vgoxazolidine-3-yl)phenidinium Amino]-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene uranium-{3 -(2-phenyl-1,3-thiazol-4-yl)acetamido-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazole- 1-*}, N'-mercaptopolystyrene-indole-{3-[4-(1-pyrrolidin-2-one)phenylindolyl]-5-(t-butyl ester)- 4,6-dihydropyrrolo[3,4-c]pyrazole-1-*}, N'-mercaptopolystyrene _ N-{3-[2-(3-oxy-3, 4,4&,83-tetrahydro-2}1-benzo[1,4]indole-6-yl)acetamido]-5-(t-butylester)-4,6-dihydrogen . Comparing with the mouth [3,4-c] ° than 0 sitting -1-&}, N,-mercaptopolystyrene urea N-{3-(1-mercapto-indol-3-yl) Amidino-5-(t-butyl ester)-4,6-dihydropyrolo[3,4-c]oxazol-1-yl}, N'-mercaptopolystyrene urea N- {3-(6-oxy-611-.荅 well-1-yl)ethanoyl-5-(t-butylindole)-4,6-dihydropyrrolo[3,4-c] Pyrazole-l-yl}, Ν'-mercaptopolystyrene-{3_(4-(TM)>-1_yl)-phenyl)ethinyl-5-(third butyl Since the purpose of the base) 0" 4,6-dihydro-pyrano[3,4-(:]pyrazol-1-yl},1^'-mercaptopolystyrene uranium-{3_(4 - 13 π定基乙胺基)-5_(Third butyl acetate)-4,6-dihydroindolo[3,4-c]pyrazol-1-yl},Ν'-mercaptopolystyrene Urea-{3-phenoxyethylamino-5-(t-butylester)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-曱Polystyrene urea N-{3-(3-pyridylethylamino)-5-(t-butyl ester)-4,6-dihydrogen

C:\2D-OODE\91-Ol\90119473.ptd 第146頁 1327569 五、發明說明（144) 吡咯并[3,4-c],比唑一卜基}，N，_曱基聚苯乙烯脲 N~{3-[5-(4 -氣苯基）呋喃_2_羧醯胺基]_5_(第三丁铲㊁)服4,6-二氫〇比洛并[3,41]0比0坐_1_基}，『_曱基聚苯曰乙 NM3-[喳啉-6-羧醯胺基]_5_(第三丁酯基）_4,6_二咯并[3, 4-c]呲唑-；!_基}，N，_甲基聚苯乙烯脲 N-{3-[2-甲基-5 -苯基-呋喃_3_羧醯胺基]_5_(第=t 二)-4, 6-二氫吼，各并[3, 4_c] 0比。坐_ i _基}，N，-曱基聚-苯乙曰师服 # N-{3-[苯并呋喃_2_羧醯胺基卜（第三丁酯基4 6_二虱吡咯并[3, 4-c]吡唑―卜基丨，N’ „曱基聚苯乙烯脲 N-{3-[6 -氣於鹼醯胺基]_5_(第三丁酯基）一4 -笱咯并[3’4-c]咄唑-^基}，N’_甲基聚苯乙烯脲父发N-{3- [5-氣噻吩_2_羧醯胺基]_5_(第三丁酯基6—二，吡咯开[3, 4-c]吡唑基丨，N，_甲基聚笨乙烯脲，實施例7 ，N-{3-苯乙醯胺基_4, 6_二氫吡咯并[3, 4_c]咄唑— I—基 N -曱基聚苯乙稀服之製備 N/3-苯乙醯胺基—5_(第三丁酯基）_4,卜二氫咄咯并[3, -c]吡唑-1-基}，N’_甲基聚苯乙烯脲（3〇1毫莫耳）使用 =FA 50%於無水二氣曱烷溶液處理。結果所得懸浮液於22 C溫和攪拌2小時，然後以TFA 1 0%於無水二氣甲烷、二氣甲院、曱醇洗滌及真空脫水。以類似方式’經由使用適當N-{ 3·醯胺基-5-(第三丁酯C:\2D-OODE\91-Ol\90119473.ptd Page 146 1327569 V. INSTRUCTIONS (144) Pyrrolo[3,4-c],biazole-diyl},N,_mercaptopolystyrene Urea N~{3-[5-(4-Phenylphenyl)furan_2_carboxyguanidino]_5_(Third Shovel II) is served with 4,6-dihydroindolebi[3,41]0 __基基_, _ 曱聚聚 N N N N , , , , , , 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 c]carbazole-;!_yl}, N,_methyl polystyrene urea N-{3-[2-methyl-5-phenyl-furan_3_carboxyguanidino]_5_(第=t b)-4,6-Dihydroindole, each [3, 4_c] 0 ratio. _ _ _ _ base}, N, - 曱基聚-苯乙曰师服# N-{3-[benzofuran_2_carboxyguanamine-based (t-butyl ester 4 6_ dipyridamole [3, 4-c]pyrazole-bryzine, N' „mercaptopolystyrene urea N-{3-[6-gas to alkali amidino]_5_(t-butyl ester)-4-笱咯[3'4-c]carbazole-yl}, N'-methyl polystyrene urea parent N-{3- [5-athiophene-2-carboxylate] _5_ (third Ester 6-di, pyrrole[3,4-c]pyrazolylindole, N,-methyl polystyrene urea, Example 7, N-{3-phenethylamino group _4, 6_2 Preparation of hydrogen pyrrolo[3,4_c]carbazole-I-based N-fluorenyl polystyrene N/3-phenylethylamino--5-(t-butyl ester)-4, dihydropyrrole And [3, -c]pyrazol-1-yl}, N'-methyl polystyrene urea (3 〇 1 mmol) was treated with =FA 50% in anhydrous dioxane solution. Stir gently at 22 C for 2 hours, then wash with TFA 10% in anhydrous di-methane, dioxin, decyl alcohol and vacuum dehydration. In a similar manner 'via the use of appropriate N-{3-amido-5- (third butyl ester

C:\2D-OODE\91-Ol\90ll9473.ptd 第147頁 1327569 五、發明說明（145) 基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲可製備下列化合物： Ν_{3-乙酿胺基_4，6_二氫各并[3，4-c] ρ比0坐_1_基} ，Ν’ -曱基聚苯乙烯脲 Ν-{3 -環丙烧缓醯胺基- 4,6 -二氫°比洛并[3,4-c]n比唾-1-基}，Ν’ -曱基聚苯乙烯脲 1{3-異丁醯胺基-4,6-二氫咄咯并[3,4-(：]吡唑-1-基}， Ν’ -甲基聚苯乙烯脲 Ν-{3 -環戊烧鼓醯胺基- 4,6 -二氫°比°各并[3,4-<:]πώ^-1-•基丨，Ν’ -曱基聚苯乙烯脲 1^-{3-苯甲醯胺基-4,6-二氫吡咯并[3,4-〇:]吡唑-1-基}, Ν’ -甲基聚苯乙烯脲 Ν - { 3 -曱基°比σ定曱醯胺基-4，6 -二氫°比0各并[3，4 - c ] 0比0坐 -卜基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -终驗醯胺基-4, 6 -二氫D比洛并[3, 4-c] °比°坐-1-基}， Ν’ -曱基聚苯乙烯脲 Ν-{3 -異於驗醯胺基-4，6 -二氫吼17各并[3, 4-c] D比。坐-1-基}，Ν’ -曱基聚苯乙烯脲 _1^-{3-(3-曱基-2-呋喃）-醯胺基-4,6-二氫吡咯并 [3,4-(：]吼唑-1-基}，1^-甲基聚苯乙烯脲 N-{3-( Β塞吩-2-叛醯胺基）-4, 6 -二氫11比Β各并[3, 4-c]吨〇坐 -l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(嗔吩-3-緩醯胺基）-4, 6 -二氫°比略并[3, 4-c]吼0坐 -卜基}，Ν’ -曱基聚苯乙烯脲C:\2D-OODE\91-Ol\90ll9473.ptd Page 147 1327569 V. INSTRUCTIONS (145) BASE)-4,6-Dihydropyrrolo[3,4-c]pyrazol-1-yl} , Ν'-methyl polystyrene urea can prepare the following compounds: Ν_{3-ethylamino group _4,6-dihydro each [3,4-c] ρ ratio 0 sitting_1_ base}, Ν '-Mercapto-polystyrene-hydrazide-{3-cyclopropanol- hydrazino- 4,6-dihydro-pyrolo[3,4-c]n than sul-1-yl}, Ν' - Mercapto-polystyrene urea 1{3-isobutylguanidino-4,6-dihydroindolo[3,4-(:]pyrazol-1-yl}, Ν'-methyl polystyrene Ν-{3-cyclopentanthene oxime- 4,6-dihydrogen ratio °[3,4-<:]πώ^-1-• 丨,Ν'-曱-based polystyrene Urea 1^-{3-benzylaminoamido-4,6-dihydropyrrolo[3,4-indolyl]pyrazol-1-yl}, Ν'-methylpolystyrene uranium - { 3 - 曱 ° ° σ 曱醯曱醯 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 {3 - Final test for amidino-4,6-dihydro D than lopand [3, 4-c] ° ratio -1-yl}, Ν'-mercaptopolystyrene uranyl-{3 - Different from the test of amidino-4,6-dihydroindole 17 and [3, 4-c] D ratio. Sit-1-yl}, Ν - mercapto polystyrene urea_1^-{3-(3-mercapto-2-furan)-nonylamino-4,6-dihydropyrrolo[3,4-(:]carbazole-1- },1^-methyl polystyrene urea N-{3-( cenet-2-pyramine)-4,6-dihydro 11 Β 并 [3, 4-c] ton 〇 Sodium-l-yl}, Ν'-methyl polystyrene-ruthenium-{3-(嗔--3- 醯醯 ))-4,6-dihydrogen ratio is slightly [3, 4-c]吼0 sitting-buki}, Ν'-mercaptopolystyrene

C:\2D-C0DE\9I-01\90119473.ptd 第148頁 1327569C:\2D-C0DE\9I-01\90119473.ptd Page 148 1327569

C:\2D.O0DE\91-01\90119473.ptd 第149頁 1327569 五、發明說明（147) N - { 3 -反桂皮醯胺基-4, 6 -二氫吡咯并[3，4 - c ]吡唑-1 -基丨，Ν’ -甲基聚苯乙烯脲 Ν - { 3 -順桂皮醯胺基-4, 6 -二氫D比略并[3，4 - c ]"比°坐-1 -基丨，Ν’ -曱基聚苯乙烯脲 1'1-{3-[3-(3-吼啶基）丙烯醯胺基]-4,6-二氫《比咯并 [3,4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 ^}-{3-[3-(4-咄啶基）丙烯醯胺基]-4,6-二氫吡咯并 [3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3-(2 -苯基丙醢胺基）-4, 6 -二氫吼11 各并[3, 4-c] B比0坐 •卜基}，Ν’ -曱基聚苯乙烯脲 1\1-丨3-鄰甲苯基乙醯胺基-4,6-二氫吼咯并[3,4-(：]°比唑 _1_基}，1^ _甲基聚苯乙稀脈 Ν_{ 3-間甲苯基乙醯胺基-4, 6-二氫咄咯并[3, 4-c]吼唑 -l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -對曱苯基乙醯胺基-4,6 -二氫°比咯并[3,4_c]吡唑曱基聚苯乙稀服 N-{3-鄰茴香醯胺基-4,6 -二氫吡咯并[3,4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 φΝ-{3-(3-曱氧苯甲醯胺基）-4,6 -二氫吡咯并[3,4-c]吡唑- l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -對茴香醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3_苯氧乙酿胺基_4，6_二氮D比ρ各并[3,4-c] °比〇坐_1_ 基}，Ν’ -曱基聚苯乙烯脲C:\2D.O0DE\91-01\90119473.ptd Page 149 1327569 V. INSTRUCTIONS (147) N - { 3 -Anti-Cassia Amidino-4,6-dihydropyrrolo[3,4 - c Pyrazol-1 -ylindole, Ν'-methylpolystyrene uranium - { 3 -cis cinnamino-amine 4,6-dihydrogen D ratio slightly [3,4 - c ]" ratio ° Sodium-1 -yl hydrazide, Ν'-mercaptopolystyrene 1'1-{3-[3-(3-acridinyl)propenylamino]-4,6-dihydro 3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene urea}-{3-[3-(4-acridinyl)propenylamino]-4,6-di Hydropyrrolo[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-(2-phenylpropionamido)-4,6-dihydroindole 11 Each [3, 4-c] B is 0 to sit on the base, and the Ν'-mercaptopolystyrene urea 1\1-丨3-o-tolylacetamido-4,6-dihydroanthracene And [3,4-(:]°Biazole_1_yl}, 1^ _Methylpolystyrene Ν_{ 3-m-tolylethylamino-4,6-dihydroindole[ 3, 4-c]carbazole-l-yl}, Ν'-mercaptopolystyrene-ruthenium-{3-p-phenyl phenylacetamido-4,6-dihydrogen ratio [3, 4_c]pyrazolyl polystyrene N-{3-o-anisylamino-4,6-dihydropyrrolo[3,4-c] Zin-1-yl}, Ν'-mercaptopolystyrene urea φΝ-{3-(3-曱-oxybenzoguanamine)-4,6-dihydropyrrolo[3,4-c]pyrazole - l-yl}, Ν'-mercaptopolystyrene uranyl-{3-p-anisylamino-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν '-Methylpolystyrene urea-{3_phenoxyethylamino} 4,6-diaza D ratio ρ and [3,4-c] ° ratio _1_1_ base}, Ν' - Mercapto polystyrene

C:\2D-00DE\91-01\90119473.ptd 第150頁 1327569 五、發明說明（148) N_{3-(2-氟苯基乙酿胺基）_4，6_二氮吼11各并[3，4-c] π比唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(3-氟苯基乙醯胺基）-4, 6 -二氫"比咯并[3, 4-c]吼唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(4-氟苯基乙醯胺基）-4,6 -二氫咄咯并[3,4-c]吡唑-1-基}，1^’_曱基聚苯乙烯脲 Ν-{3-[3-(2-α塞吩基）丙烯醢胺基]-4，6 -二氫吼11 各并 [3,4-c] °比唑曱基聚苯乙烯脲 1^-{3-[3-(3-噻吩基）丙烯醯胺基]-4,6-二氫吡咯并 [3,4-〇]吡唑-1-基}^’-甲基聚苯乙烯脲 Ν-{3-[3-(2-°塞吩基）丙醯胺基]-4,6-二氫11比11各并 [3,4-c]吡唑-1-基}^’ -曱基聚苯乙烯脲 N-{3-[2 -氣苯甲醯胺基]-4, 6 -二氫吼咯并[3, 4-c]吡唑 -1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-[3_氯苯曱酿胺基]-4,6 -二氫°比0各并[3，4-c] Β比0坐 -1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3_(4_氯苯甲酿胺基）_4，6_二氫°比17各并[3，4_c] 11比0坐 -1-基}, Ν’ -曱基聚苯乙烯脲 Ν-{3-(1_°底°定丙酿胺基）-4,6 -二氫吼11各并[3,4-c] °比〇坐 -l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(2-乙醯基苯甲醯胺基）-4, 6 -二氫吡咯并[3,4-c] 吡唑- l-基},Ν’ -甲基聚苯乙烯脲 Ν-{3-(4-乙醯基苯甲醯胺基）-4, 6 -二氫咄咯并[3,4-c] 吡唑-l-基}，Ν’ -曱基聚苯乙烯脲C:\2D-00DE\91-01\90119473.ptd Page 150 1327569 V. INSTRUCTIONS (148) N_{3-(2-Fluorophenylethylamino)_4,6-diazepine 11 [3,4-c] π-biazole-l-yl}, Ν'-mercaptopolystyrene urea-{3-(3-fluorophenylethylamino)-4,6-dihydro" Bis-[3,4-c]oxazol-1-yl}, N'-mercaptopolystyrene urea N-{3-(4-fluorophenylacetamido)-4,6-dihydrogen咄[3,4-c]pyrazol-1-yl},1^'_mercaptopolystyrene-indole-{3-[3-(2-α-sepeptyl)propenylamino]- 4,6-dihydroindole 11 each [3,4-c] ° oxazolyl polystyrene urea 1^-{3-[3-(3-thienyl)propenylamino]-4,6 -dihydropyrrolo[3,4-indolepyrazol-1-yl}^'-methylpolystyrene-indole-{3-[3-(2-°Septyl)propanylamino]- 4,6-dihydrogen 11 to 11 and [3,4-c]pyrazol-1-yl}^'-mercaptopolystyrene urea N-{3-[2- gasbenzamide]- 4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene-ruthenium-{3-[3_chlorobenzoinyl]-4 ,6-dihydrogen ratio 0 each and [3,4-c] Β is 0 -1-yl}, Ν'-methyl polystyrene uranium-{3_(4_chlorobenzamide) _4,6_ dihydrogen ratio 17 Each [3,4_c] 11 to 0 is sitting on a -1-yl}, Ν'-mercaptopolystyrene-ruthenium-{3-(1_°°°-propylamino)-4,6-dihydroanthracene 11 each [3,4-c] ° 〇 - -l- base}, Ν '-methyl polystyrene urea-{3-(2-ethylmercaptobenzamide)-4, 6 -dihydropyrrolo[3,4-c]pyrazole-l-yl}, Ν'-methyl polystyrene-indole-{3-(4-ethylmercaptobenzamide)-4, 6 -dihydroindolo[3,4-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene

C:\2D-C0DE\91-01\90119473.ptd 第151頁 1327569 五、發明說明（149) Ν-{3-(1-萘曱醯胺基）-4,6 -二氫咄咯并[3,4-c]吡唑-1-基}, Ν’ -甲基聚苯乙烯脲 Ν-{3-(2 -萘甲醯胺基）-4,6 -二氫吼咯并[3,4-c]吡唑-卜基}, Ν’ -曱基聚苯乙烯脲 Ν-{3-(3 -苯曱醯基丙醯胺基）-4, 6 -二氫吡咯并[3,4-c] 吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-乙醯胺基苯甲醯胺基）-4,6 -二氫咄咯并 [3,4-c]°比唑-1-基}，Ν’-曱基聚苯乙烯脲 Ν-{3-(2,5 -二曱氧苯曱醯胺基）-4,6 -二氫吼咯并 • 3,4-c]吡唑-1-基}，『_曱基聚苯乙烯脲 N-{3-(2,6 -二甲氧苯曱醯胺基）-4,6 -二氫°比°各并 [3,4-〇:]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3-(3,4 -二曱氧苯曱醯胺基）-4,6 -二氫吡咯并 [3,4-c]咄唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(3,5 -二曱氧苯甲醯胺基）-4,6 -二氫咄咯并 [3,4-c]咄唑-1-基}，N’-曱基聚苯乙烯脲 Ν-{3-[3-(2-σ塞吩醯）-丙醯胺基]-4, 6 -二氫D比11 各并 [3,4-c]咄唑-1-基}，N’ -曱基聚苯乙烯脲 • N- {3-(2 -萘基乙醢胺基）-4, 6 -二氫D比p各并[3, 4-c] 0比唾 -1-基}, Ν’ -曱基聚苯乙烯脲 Ν-{3-(1-萘基乙醯胺基）-4,6 -二氫咄咯并[3,4-c]吡唑 -1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4 -苯基苯曱醯胺基）-4,6-二氫吡咯并[3,4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 151 1327569 V. INSTRUCTIONS (149) Ν-{3-(1-Naphthylamino)-4,6-dihydroindole[ 3,4-c]pyrazol-1-yl}, Ν'-methylpolystyrene-indole-{3-(2-naphthylamino)-4,6-dihydroindole[3, 4-c]pyrazole-buji}, Ν'-mercaptopolystyrene-indole-{3-(3-phenylhydrazinopropylamino)-4,6-dihydropyrrolo[3,4 -c] pyrazol-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-(4-acetamidobenzylidinium)-4,6-dihydroindole[3 , 4-c]°bizozol-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-(2,5-dioxabenzoquinone)-4,6-dihydroanthracene咯•• 3,4-c]pyrazol-1-yl}, _曱-based polystyrene urea N-{3-(2,6-dimethoxybenzoguanamine)-4,6-di The ratio of hydrogen to °[3,4-〇:]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-(3,4-dioxabenzoquinone)- 4,6-dihydropyrrolo[3,4-c]oxazol-1-yl}, N'-mercaptopolystyrene urea N-{3-(3,5-dioxabenzoguanamine) -4,6-dihydroindolo[3,4-c]oxazol-1-yl}, N'-mercaptopolystyrene-ruthenium-{3-[3-(2-σ-septene) )-propylamino]-4, 6 - two Hydrogen D ratio 11 and [3,4-c]oxazol-1-yl}, N'-mercaptopolystyrene urea • N- {3-(2-naphthylethylamino)-4, 6 - Dihydrogen D is more than p and [3, 4-c] 0 is more than sul-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-(1-naphthylacetamido)-4 ,6-dihydroindolo[3,4-c]pyrazol-1-yl},Ν'-mercaptopolystyrene-indole-{3-(4-phenylphenylguanidino)-4 ,6-dihydropyrrolo[3,4-c]pyrazole-l-yl},Ν'-mercaptopolystyrene

C:\2D-CODE\91-01\90119473.ptd 第 152 頁 1327569 五、發明說明（150) Ν-{3-(2-σ夫喃醯胺基）-4, 6 -二氫咄略并[3, 4-c] D比唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(4-苯氧苯曱醯胺基）-4,6 -二氫吡咯并[3,4-c]呲唑-l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(3 -苯氧苯曱醯胺基）-4,6 -二氫吡咯并[3,4-c]吼唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-第三丁基-苯曱醯胺基）-4,6 -二氫吡咯并 [3,4-c]咄唑-1-基}^’-甲基聚苯乙烯脲 N-{3-胡椒基羧醯胺基-4, 6 -二氫吼咯并[3,4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(2 -蔡）丙酿胺基-4，6 -二氫。比ρ各并[3，4-c] °比°坐-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(6-曱氧-2 -萘）丙醯胺基-4,6-二氫吡咯并[3,4-(：] 口比唑-1-基}，1^，一曱基聚苯乙烯脲 Ν-{3-(2-乙基丁醯胺基）-4, 6 -二氫°比°各并[3, 4-c]吡。坐 _1_基}，1^,_曱基聚苯乙..稀脈 Ν-{3-(4-0比洛咬-1-基-苯基）丙醯胺基-彳^-二氫吼洛并 [3,4-c]吡唑-1-*},Ν’ -甲基聚苯乙烯脲 Ν-{3-(2 -氧基-吡咯啶-1-基）苯基}丙醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-1-基}, Ν’ -曱基聚苯乙烯脲 Ν-{3-(雙環[4. 2. 0]辛-1，3, 5 -三稀-7-叛醯胺基）-4，6-二氫吡咯并[3,4-c]吡唑-1_基},1^’-曱基聚苯乙烯脲 N-{3-(2 -氧基-吡咯啶-1-基）苯乙醯胺基-4,6 -二氫吡咯并[3,4-c]吡唑-1-基}，N’-甲基聚苯乙烯脲C:\2D-CODE\91-01\90119473.ptd Page 152 1327569 V. INSTRUCTIONS (150) Ν-{3-(2-σ-fusinoguanidino)-4,6-dihydroanthracene [3, 4-c] D-pyrazol-1-yl}, Ν'-methyl polystyrene-indole-{3-(4-phenoxyphenylguanidino)-4,6-dihydropyrrole [3,4-c]carbazole-l-yl}, Ν'-methyl polystyrene-indole-{3-(3-phenoxybenzoguanamine)-4,6-dihydropyrrolo[ 3,4-c]oxazol-1-yl}, Ν'-mercaptopolystyrene-indole-{3-(4-t-butyl-benzoguanamine)-4,6-dihydropyrrole And [3,4-c]oxazol-1-yl}^'-methylpolystyrene urea N-{3-piperidinylcarboxamide-4,6-dihydroindole[3,4- c]pyrazol-1-yl}, Ν'-methyl polystyrene uranium-{3-(2-Cai) propylamino-4,6-dihydrogen. Ratio ρ and [3,4-c] ° ratio sits-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-(6-oxime-2-naphthalene) propylamine- 4,6-dihydropyrrolo[3,4-(:] orthoazole-1-yl}, 1^, monodecyl polystyrene uranyl-{3-(2-ethylbutylideneamino) -4,6-Dihydrogen °° each [3, 4-c]pyr. sit _1_ base}, 1^, _ 曱聚 polyphenyl benzene.. dilute pulse Ν-{3-(4-0 Bilo-1-yl-phenyl)propanylamino-彳^-dihydroindolo[3,4-c]pyrazole-1-*}, Ν'-methyl polystyrene uranium- {3-(2-Oxo-pyrrolidin-1-yl)phenyl}propanylamino-4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, Ν' - mercapto polystyrene urea-{3-(bicyclo[4. 2. 0]oct-1,3,5-tris-7-treazone)-4,6-dihydropyrrolo[3 ,4-c]pyrazole-1_yl},1^'-mercaptopolystyrene urea N-{3-(2-oxy-pyrrolidin-1-yl)phenylethylamino-4,6 -dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-methyl polystyrene urea

C:\2D-CODE\91-01\90119473.ptd 第153頁 1327569 五、發明說明（151) N-{3-(4 -咄咯啶-1-基）苯乙醯胺基-4, 6 -二氫咄咯并[3, 4_c]吡唑—卜基丨，Ν’ —曱基聚苯乙烯脲 1^-{3-(4-三氟曱基）苯乙醯胺基-4,6-二氫吼咯并 [3,4-c]咄唑曱基聚苯乙烯脲 Ν-{3-(2 -溴）苯乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _1_基}，1^’_甲基聚苯乙稀脈 Ν-{3-[4-(吡咯啶-1-基-羰基曱氧基）]苯乙醯胺基-4,6-二氫0比π各并[3, 4 - c ] 0比。坐-1 -基}，Ν ’ -甲基聚苯乙稀脲 Ν-{3-[3-(胺基幾基曱氧）苯乙酿胺基]-4，6 -二氫Β比ρ各并 _3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3-[4-(2 -氧基-坐。定-3-基）苯乙酿胺基]-4, 6 -二氫吡咯并[3，4 - c ]吡唑-1 -基}，Ν ’ -曱基聚苯乙烯脲 Ν-{3-[4-(4-甲基派°井基）苯乙酿胺基]-4，6 -二氫°比0各并 [3,4-c]吡唑-1-基}，Ν’-曱基聚苯乙烯脲 ^{3-(苯并[1，3]二氧伍圜-5-基）乙醯胺基-4,6-二氫吡咯并[3,4-c]吡唑甲基聚苯乙烯脲 Ν-{3-[4-(2 -氧基坐°定-3-基）苯乙醯胺基]-4，6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3_(2_苯基_1，3_ °塞°坐-4 -基）乙酿胺基-4，6 -二氮°比ρ各胃并[3, 4-c]吡唑-1-*}，Ν’ -曱基聚苯乙烯脲 N-{3-[4-(1-吡咯啶-2 -酮）苯甲醯胺基]-4,6 -二氫吡咯弁[3，4_c] °比〇坐-1-基}，1^’_曱基聚苯乙稀脈 N-{3-[2-(3-氧基-3, 4, 4a，8a-四氫-2H-苯并[1，4] $ 畊 -6 -基）乙醯胺基]-4, 6 -二氫吼洛并[3,4-c] 0比。坐-1-基}C:\2D-CODE\91-01\90119473.ptd Page 153 1327569 V. INSTRUCTIONS (151) N-{3-(4-Pyrrolidin-1-yl)phenylethylamino-4,6 -dihydroindolo[3,4_c]pyrazole-bylindole, Ν'-mercaptopolystyrene urea 1^-{3-(4-trifluoromethyl)phenylethylamino-4,6 -dihydroindolo[3,4-c]oxazolyl polystyrene urea-{3-(2-bromo)phenylethylamino-4,6-dihydropyrrolo[3, 4- c]pyrazole_1_yl}, 1^'_methylpolystyrene oxime-{3-[4-(pyrrolidin-1-yl-carbonyloximeoxy)]phenethylamino-4 , 6-dihydrogen 0 is more than π and [3, 4 - c ] 0 ratio. Sodium-1 -yl}, Ν '-methyl polystyrene uranium-{3-[3-(amino aryloxy) phenylethylamino]-4,6-dihydroindole ratio ρ And _3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-[4-(2-oxy-sodium-but-3-yl)phenylethylamine 4-[6,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν '-mercaptopolystyrene uranium-{3-[4-(4-methylpy Well base) phenylethylamino]-4,6-dihydrogen ratio 0 and [3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene urea {3-( Benzo[1,3]dioxoindol-5-yl)acetamido-4,6-dihydropyrrolo[3,4-c]pyrazolemethylpolystyrene-ruthenium-{3-[ 4-(2-oxyl-n-but-3-yl)phenethylamino]-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-fluorenyl Polystyrene uranyl-{3_(2_phenyl_1,3_ °°°-s-4-yl)ethanoamine-4,6-diaza ratio ρ stomach and [3, 4-c] Pyrazole-1-*}, Ν'-mercaptopolystyrene urea N-{3-[4-(1-pyrrolidin-2-one)benzimidamide]-4,6-dihydropyrrole [3,4_c] ° 〇 -1--1-yl}, 1^'_ 曱聚 polyphenylene hydride N-{3-[3-(3-oxy-3, 4, 4a, 8a-tetrahydrogen) -2H-benzo[1,4] $ 耕-6 -基Acetylglucosamine] -4, 6 - dihydro roar and Luo [3,4-c] 0 ratio. Sitting -1-base}

C:\2D-CODE\91-01\90119473.ptd 第154頁 1327569 五、發明說明（152) ,Ν’ -曱基聚苯乙烯脲 1^-{3-(1-甲基-吲哚-3-基）乙醯胺基-4,6-二氫吡咯并 [3,4-c]吼唑-1-基}，1^’-曱基聚苯乙烯脲 ^{3-(6-氧基-611-嗒啡-1-基）乙醯胺基-4,6-二氫呲咯弁[3，4-c] °比。坐_1_基}，1^1’_曱基聚苯乙稀服 ?^-{3-(4-(嗎啉-1-基）-苯基）乙醯胺基-4,6-二氳吼咯并 [3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(4_ D比咬基乙酿胺基）_4，6_二氮吼17各并[3，4-c] 0比唑-1-基}，『-曱基聚苯乙烯脲 N-{3 -苯氧乙酿胺基-4，6_二氮0比11 各并[3,4_c] D比°坐-1 -基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(3- °比。定基乙醯胺基）-4，6 -二氫D比ρ各并[3，4-c] 0比唑-l-基},Ν’ -甲基聚苯乙烯脲 Ν-{3-[5-(4-氣苯基）β夫喃-2-緩醯胺基]-4, 6 -二氫吡°各并[3，4-c] 0比0坐-1_S}，N’ _曱基聚苯乙稀脈 N-{3-[喑琳-6-缓醯胺基]-4，6 -二氫D比°各并[3,4-c] D比。坐 -1-基}，Ν’ -曱基聚苯乙烯脲 ^{3-[2-甲基-5-苯基-呋喃-3-羧醯胺基]-4,6-二氫吡咯并[3,4-c]吼唑-1-基}^’-甲基聚苯乙烯脲 N-{3-[苯并B夫喃-2-叛醯胺基]-4，6 -二氫吼^各并[3，4-c] 口比唑-1-；&}，N，-曱基聚苯乙烯脲 N_{3_[6_氯於驗酿胺基]_4,6~二氮吼0各并[3,4-c] p比0坐 -1-基}，Ν’ -甲基聚笨乙烯脲 Ν-{3-[5 -氯°塞吩-2-叛醯胺基]-4, 6 -二氫D比洛并[3,4-c]C:\2D-CODE\91-01\90119473.ptd Page 154 1327569 V. INSTRUCTIONS (152), Ν'-mercaptopolystyrene urea 1^-{3-(1-methyl-吲哚- 3-yl)acetamido-4,6-dihydropyrrolo[3,4-c]oxazol-1-yl}, 1^'-mercaptopolystyrene urea^{3-(6-oxygen Base-611-indol-1-yl)acetamido-4,6-dihydropurine [3,4-c] ° ratio. Sit _1_基}, 1^1'_曱-based polystyrene service?^-{3-(4-(morpholin-1-yl)-phenyl)acetamido-4,6-di氲吼[3,4-c]pyrazol-1-yl}, N'-mercaptopolystyrene urea N-{3-(4_D ratio acetylamino)_4,6-diaza吼17 each [3,4-c] 0-pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-phenoxyethylamino-4,6-diaza 0 to 11 each And [3,4_c] D is more than -1 -yl}, Ν'-mercaptopolystyrene-ruthenium-{3-(3- ° ratio. acetylamino)-4,6-dihydrogen D ρ 各 [3,4-c] 0 azole-l-yl}, Ν'-methyl polystyrene-ruthenium-{3-[5-(4-phenylphenyl)β-pentan-2-醯醯 ] ] ] -4 -4 -4 -4 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 , , , , , , , , - - - - 6-reactive oxime]-4,6-dihydrogen D ratios each [3,4-c] D ratio. -1--1-yl}, Ν'-mercaptopolystyrene^{3-[2-methyl-5-phenyl-furan-3-carboxyguanidino]-4,6-dihydropyrrolo[ 3,4-c]oxazol-1-yl}^'-methylpolystyrene urea N-{3-[benzo-Baffran-2-retinylamino]-4,6-dihydroanthracene^ Each [3,4-c] portazole-1-(&}, N,-mercaptopolystyrene urea N_{3_[6_chlorine in the amine-based]_4,6-diazepine0 Each [3,4-c] p is 0-position-1-yl}, Ν'-methyl polystyrene-urea-ruthenium-{3-[5-chloro-ceto-2-pyrutylamino]-4 , 6-dihydro D, biluo[3,4-c]

C:\2D-CODE\91-01\90119473.ptd 第155頁 1327569 五、發明說明（153) D比唑-1-基}，Ν’ -甲基聚苯乙烯脲實施例8 Ν-{ 3-苯乙醯胺基-5 -苯乙醯基-4, 6 -二氫„比Β各、，咄唑-1-基丨，Ν，-曱基聚苯乙烯脲之製備〇开[3,4-c] 苯乙酸（0.43毫莫耳’58.5毫克），圓沾（〇.43臺 47. 3微升）及PyBop(0. 43毫莫耳，2 23. 8毫券、> 莫耳’ 毛兄）添加至笨乙酿胺基-4，6 -二氫吼略并[3，4-c] °比"坐n，聚苯乙稀脲（0.086毫莫耳’100毫克），該服事先於4毫升無水N，N-二甲基曱醯胺溶脹。結果所得懸浮液於22溫和 ►搜拌24小時。然後樹脂經過濾，以N，N_二曱基曱醯胺'一氣甲烷 '甲醇洗滌及真空脫水。一以類似方式經由使用適當羧酸可製備下列化合物： N-{3 -苯乙醯胺基-5-乙醯基-4, 6 -二氫吼咯并[3, 4_ci 唑-l-基}，Ν’ -曱基聚苯乙烯脲 ΝΜ3-苯乙醯胺基-5-苯甲醯基-4, 6_二氫吡咯并[3, 4一吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲 ’ ^{3-苯乙醯胺基-5-(2,6-二曱氧苯曱醯基）一4,6_ 氫吼嘻并[3,4-c] 〇比吐-1-基}，Ν’_曱基聚苯乙烯脲『Ν-{ 3-苯乙醯胺基-5-( 2, 6-二甲氧苯曱醯基卜4,6-二口比哈并[3,4-c] 口比唑-1-*}，N，-甲基聚苯乙烯脲’ 里 N-{3-苯乙醯胺基-5-(2一氯苯曱醯基）_4, 6_二氫呲咯 [3, 4-c]吼唑-1-基}，N，-甲基聚苯乙烯脲 N-{3-苯乙醯胺基-5-(2-氯苯基乙醯基）_4, 6_二氫咣并[3,4-c]吡唑-1-基}，『-曱基聚笨乙烯脲C:\2D-CODE\91-01\90119473.ptd Page 155 1327569 V. INSTRUCTIONS (153) D-Bizozol-1-yl}, Ν'-methyl polystyrene urea Example 8 Ν-{ 3 -Phenylacetamido-5-phenethyl fluorenyl-4,6-dihydro hydrazine, carbazole-1-yl hydrazine, hydrazine, hydrazine-polystyrene urea preparation [3, 4-c] phenylacetic acid (0.43 mM '58.5 mg), round dip (〇.43 units 47. 3 μl) and PyBop (0. 43 mAh, 2 23. 8 vouchers, > Mohr '毛兄' added to the stupid amine-4,6-dihydroindole and [3,4-c] ° ratio " sit n, polystyrene (0.086 millimoles '100 mg), The solution was swollen in advance with 4 ml of anhydrous N,N-dimethylguanamine. The resulting suspension was stirred at 22 ° for 24 hours. The resin was then filtered to give N,N-didecylamine. Methane 'methanol washing and vacuum dehydration. The following compounds can be prepared in a similar manner via the use of the appropriate carboxylic acid: N-{3-phenethylamino-5-ethenyl-4,6-dihydroindole[3 , 4_ci azole-l-yl}, Ν'-mercaptopolystyrene uranyl 3-phenylethylamino-5-benzhydryl-4,6-dihydropyrrolo[3, 4-pyridyl -1-ylindole, Ν'-methyl polystyrene urea ' ^{3-phenethylamino-5-(2,6-dioxaphenyl)- 4,6-hydroindolo[ 3,4-c] 〇比吐-1-基},Ν'_曱-polystyrene urea Ν-{ 3- phenylethylamino-5-( 2, 6-dimethoxybenzoyl Bu 4,6-dibi Biha and [3,4-c] portazole-1-*}, N,-methyl polystyrene urea 'N-{3-phenethylamino-5- (2-chlorophenylindenyl)_4,6-dihydroindole [3,4-c]oxazol-1-yl}, N,-methyl polystyrene urea N-{3-phenylethylamine 5-(2-chlorophenylethyl)- 4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, "-mercapto polystyrene

1327569 五、發明說明（154) N-{3 -苯乙醯胺基-5-(2-氟苯甲醯基）-4, 6 -二氫吡咯并 [3，4-c]咄唑-1-基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(4-氟苯甲醯基）-4,6 -二氫吼咯并 [3,4-c] D比唑-1-基},N’ -曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(2 -呋喃醯基）-4,6 -二氫咄咯并[3, 4-c]°比唑-1-基丨，Ν’-甲基聚苯乙烯脲 Ν-{3 -苯乙酿胺基_5-(. 3_σ夫喃酿基）_4, 6_二氫D比ρ各并[3, 4-c]吼唑曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(2-甲氧苯曱醯基）-4, 6 -二氫吡咯并[3,4-c] u比唑-1-基},『-曱基聚苯乙烯脲 N-{3 -苯乙酿胺基-5-（2_甲氧苯乙酿基）-4，6_二氮0比洛并[3,4-c]吡唑-1-基}，『-甲基聚苯乙烯脲 N-{3 -苯乙酿胺基_5-(2_曱基苯乙酿基）_4，6_二氮11比洛并[3,4 - c] D比。坐-1_基}，『_曱基聚苯乙稀脈 N-{3 -苯乙醯胺基-5-(2 -喳唁醯基）-4,6 -二氫吡咯并[3, 4-c]吡唑-1-基},『-曱基聚苯乙烯脲 N-{3 -苯乙酿胺基- 5- (2-°塞吩乙酿基）-4，6 -二氫吼°各并 [3,4-c]吡唑-1-*}，N’ -曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(2-曱苯曱醯基）-4, 6 -二氫吡咯并 [3,4-c]吡唑-1-*}，N’ -曱基聚苯乙烯服 N-{3 -苯乙醯胺基-5-(5-氟-2-曱苯甲醯基）-4, 6 -二氫吡咯并[3,4-c]吡唑-1-S},N’ -曱基聚苯乙烯脲 N-{3_苯乙酿胺基_5-(3_苯曱酿基）_4, 6_二氮0比0各并[3, 4-c]吡唑-1-基},『_曱基聚苯乙烯脲1327569 V. INSTRUCTIONS (154) N-{3-Phenylethylamino-5-(2-fluorobenzhydryl)-4,6-dihydropyrrolo[3,4-c]carbazole-1 -based, Ν'-mercaptopolystyrene-ruthenium-{3-phenylethylamino-5-(4-fluorobenzhydryl)-4,6-dihydroindole[3,4- c] D-pyrazol-1-yl}, N'-mercaptopolystyrene urea N-{3-phenylethylamino-5-(2-furanyl)-4,6-dihydroindole [3, 4-c]°Bizozol-1-ylindole, Ν'-methyl polystyrene uranium-{3-phenylethylamino}5-(.3_σ夫喃牛)_4, 6_ Dihydrogen D ratio ρ and [3, 4-c]oxazolyl polystyrene urea-{3-phenylethylamino-5-(2-methoxybenzoinyl)-4, 6 - Dihydropyrrolo[3,4-c]u-pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-phenylethylamino-5-(2-methoxyphenyl) -4,6-dinitro- 0-pyrazino[3,4-c]pyrazol-1-yl}, "-methyl polystyrene urea N-{3-phenylethylamino]_5-(2 _Mercaptophenethyl phenyl) _4,6_dinitrogen 11 is more than [3,4 - c] D ratio. Sit -1_base}, _ 曱聚聚聚 N N-{3 - phenethylamino-5-(2-indolyl)-4,6-dihydropyrrolo[3, 4 -c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-phenylethylamino- 5-(2-°cetophenidyl)-4,6-dihydroanthracene °[3,4-c]pyrazole-1-*}, N'-mercaptopolystyrene urea N-{3-phenylethylamino-5-(2-indolyl)- 4,6-dihydropyrrolo[3,4-c]pyrazole-1-*}, N'-mercaptopolystyrene N-{3-phenethylamino-5-(5-fluoro- 2-曱benzylidene)-4,6-dihydropyrrolo[3,4-c]pyrazole-1-S}, N'-mercaptopolystyrene urea N-{3_phenylethylamine Base_5-(3_benzoquinone)_4,6-diaza 0 to 0 each [3,4-c]pyrazol-1-yl}, _曱-based polystyrene

C:\2D-C0DE\91-01\90119473.ptd 第157頁 1327569 五 '發明說明（155) N-{3_苯乙醯胺基-5-(3-氣苯乙醯基）-4, 6 -二氫吡咯并 [3,4-〇]吡唑-1-基}，1^’-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(3-環戊基丙醯基）-4, 6 -二氫吡咯并[3,4-c]吡唑-1-*}，N’-甲基聚苯乙烯脲 N-{3 -苯乙酿胺基_5-(3-氟苯曱酿基）-4，6 -二氯n比11 各弁 [3,4-c]咄唑-1-*}，N’-曱基聚苯乙烯脲 N-{3_苯乙酿胺基_5_(3_甲氧苯乙酿基）-4，6_二氮0比洛并[3,4-c]吡唑-1-基}，N’_曱基聚苯乙烯脲 N - {3-笨乙醢胺基-5-(3-曱基苯乙醯基）-4,6 -二氫吡咯馨并[3, 4-c]吡唑-1-基}，N’_曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(3-甲苯曱醯基）-4,6 -二氫吡咯并 [3,4-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(4-溴苯乙醯基）-4, 6-二氫吡咯并 [3,4-c]吡唑曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(4-氯苯甲醯基）-4, 6 -二氫吼咯并 [3,4-c]吡唑曱基聚苯乙烯脲 N-{3 -苯乙酸胺基_5_(4_氣苯乙酿基）_4，6·_二氮吼p各并[3, 4-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3 -苯乙.酿胺基_5_(4_二甲基胺基苯甲酿基）_4，6_二氫°比略并[3,4-c] 曱基聚苯乙浠脲 Ν-{3-苯乙醯胺基-5-(4-氟苯曱醯基）-4, 6 -二氫吼咯并 [3,4-c]咄唑-1-基},N’-甲基聚苯乙烯脲 N-{3_苯乙酿胺基- 5- (4-曱氧苯乙酿基）-4,6 -二氫吼口各并[3,4-c] °比唑-1-*}，N’-曱基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 157 1327569 V'Inventive Description (155) N-{3_Phenylamino-5-(3-phenylphenidinyl)-4, 6-dihydropyrrolo[3,4-indolepyrazol-1-yl},1^'-mercaptopolystyrene urea N-{3-phenylethylamino-5-(3-cyclopentyl) Propionyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-1-*}, N'-methylpolystyrene urea N-{3-phenylethylamino}5- (3-fluorophenylhydrazine)-4,6-dichloron ratio 11 弁[3,4-c]carbazole-1-*}, N'-mercaptopolystyrene urea N-{3_ Phenylethylamine _5_(3-methoxyphenylethyl)-4,6-diaza 0bilobo[3,4-c]pyrazol-1-yl}, N'-mercaptopolybenzene Ethylene urea N - {3- oxaethylamino-5-(3-mercaptophenylethyl)-4,6-dihydropyrrolidin[3,4-c]pyrazol-1-yl}, N'_mercaptopolystyrene urea N-{3-phenylethylamino-5-(3-tolylthio)-4,6-dihydropyrrolo[3,4-c]pyrazole-1 -yl}, N'-methyl polystyrene urea N-{3-phenylethylamino-5-(4-bromophenethyl)-4,6-dihydropyrrolo[3,4-c Pyrazolyl-based polystyrene urea N-{3-phenethylamino-5-(4-chlorobenzylidene)-4,6-dihydroindolo[3,4-c]pyrazole Mercapto polystyrene N-{3-phenylacetic acid amine _5_(4_ phenethylphenyl)_4,6·_diazepine p-[3,4-c]pyrazol-1-yl}, N'-A Polystyrene urea N-{3-phenylethyl arylamino _5_(4-dimethylaminobenzyl yl) _4,6-dihydrogen ratio slightly [3,4-c] fluorenyl Polystyrene uranyl-{3-phenethylamino-5-(4-fluorophenylindenyl)-4,6-dihydroindolo[3,4-c]oxazol-1-yl }, N'-methyl polystyrene urea N-{3_phenylethylamino- 5-(4-indoleoxyphenyl)-4,6-dihydropurine each [3,4- c] °biazole-1-*}, N'-mercaptopolystyrene

C:\2D-OODE\91-Ol\90119473.ptd 第158頁 1327569 五、發明說明（156) N-{3 -苯乙醯胺基-5-(4-曱基苯乙醯基）-4,6 -二氫吡咯并[3,4-c]咄唑曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(4-甲苯曱醯基）-4,6 -二氫吡咯并 [3,4-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 N-{3_苯乙酿胺基_5-( σ塞吩_2_截基）-4，6 -二氫吼13各并 [3,4-c]吡唑-1-基}，『_甲基聚苯乙烯脲 N-{3-笨乙酿胺基-5-(反_2_苯基-1_環丙烧幾基）-4，6-二氫吡咯并[3, 4-c]咄唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5 - 丁醯基-4, 6 -二氫吡咯并[3,4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3_苯乙酿胺基_5_環丙烧鑛基-4，6 -二氫吼17各弁 [3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3_苯乙酿胺基_5_(1_甲基環丙烧）叛基_4，6_二氣°比咯并[3,4-c]吡唑-1-基}^’_甲基聚苯乙烯脲 N-{3-苯乙醜胺基_5_(2，2，3，3_甲基環丙烧）幾基_4, 6-二氫0比咯并[3, 4-c]吡唑-1-基}, Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5 -異戊醯基-4, 6 -二氫咄咯并[3, 4-c] 吼唑-1-基}，Ν，-曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5 -異噶唑-5-羰基-4, 6 -二氫吼咯并 [3,4-c]吡唑-1-基丨，Ν’-曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-間-茴香醯基-4, 6 -二氫吡咯并 [3,4-〇]吡唑-1-基丨，1'1’-甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-於驗醯基-4, 6 -二氫吼洛并[3,4-<:] 吡唑-1-基}，Ν’ -甲基聚苯乙烯脲C:\2D-OODE\91-Ol\90119473.ptd Page 158 1327569 V. INSTRUCTIONS (156) N-{3-Phenylethylamino-5-(4-mercaptophenylethyl)-4 ,6-dihydropyrrolo[3,4-c]oxazolyl polystyrene urea N-{3-phenylethylamino-5-(4-methylphenyl)-4,6-dihydrogen Pyrrolo[3,4-c]pyrazole-1-*}, N'-mercaptopolystyrene urea N-{3_phenylethylamino-5-( σ septene_2_cyl)- 4,6-dihydroindole 13 each [3,4-c]pyrazol-1-yl}, "_methyl polystyrene urea N-{3-stupylamino-5-(reverse_2 _Phenyl-1_cyclopropanol)-4,6-dihydropyrrolo[3,4-c]oxazol-1-yl}, Ν'-methyl polystyrene uranium-{3 - Phenylamino-5-butanyl-4,6-dihydropyrrolo[3,4-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene uranium-{3_phenylene Amine _5_cyclopropanol-based-4,6-dihydroindole 17 弁[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3_benzene乙胺胺基_5_(1_Methylcyclopropane) 叛基_4,6_二气°比[[,4-c]pyrazol-1-yl}^'_methylpolystyrene Urea N-{3-phenylethyl acetamido_5_(2,2,3,3-methylcyclopropane) benzyl, 4-dihydro- 0-pyrrolo[3,4-c]pyrazole -1-base}, Ν'-Methylpolystyrene-ruthenium-{3-phenethylamino-5-isopentamyl-4,6-dihydroindolo[3,4-c]oxazol-1-yl} , hydrazine, - mercapto polystyrene urea-{3-phenylethylamino-5-isoxazol-5-carbonyl-4,6-dihydroindolo[3,4-c]pyrazole- 1-ylindole, Ν'-mercaptopolystyrene uranyl-{3-phenethylamino-5-m-anisyl-4,6-dihydropyrrolo[3,4-indole]pyrazole -1-ylindole, 1'1'-methyl polystyrene uranyl-{3-phenethylamino-5-in the test of fluorenyl-4,6-dihydroindolo[3,4-<;:]pyrazol-1-yl},Ν'-methylpolystyrene

C:\2D-C0DE\91-01\90119473.ptd 第159頁 1327569 五'發明說明（157) [^-{3-苯乙醯胺基-5-對-@香醯基-4,6-二氫吡咯并 [3,4-c]吡唑-1-基}，N’ -曱基聚苯乙烯脲 N-{3_苯乙酿胺基_5_苯氧乙酿基_4，6_二氮π比洛并 [3,4-c]吡唑-曱基聚苯乙烯脲 Ν_{3 -苯乙酿胺基_5_窄氧乙酿基_4，6_二氮ρ比11 各弁 [3,4-〇]"比唑-1-基}^’-甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(1-萘甲醯基）-4, 6 -二氫吼咯并[3, 4-c]咄唑-1-*}，N’-甲基聚苯乙烯脲 N_{3_苯乙酿胺基_5_ 丁 _2_快酿基_4,6_二氮°比^各弁 _3,4-c]吡唑-1-基},『-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-丙酮醯基-4, 6 -二氫吡咯并[3,4-c] 口比。坐_1—基h N，—曱基聚苯乙稀脲 N_{3 -苯乙酿胺基_5_(1，3_苯并二氧伍圜_5_基幾基） -4，6-二氫0比11各并[3,4-(：]°比〇坐-1-基}，1'1’-曱基聚苯乙稀脲 N_{3_苯乙酿胺基_5_(2, 2_二甲基丙酿基）_4，6 -二氮〇比咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 ^{3-苯乙醯胺基-5-(2,4-二氣-5-氟苯曱醯基）-4,6-二氫〇比〇各并[3,4-c] °比°坐-1-基}，^1’-曱基聚苯乙稀脲 _ N-{3 -苯乙醯胺基-5-(2-曱基戊-4 -烯醯基）-4,6 -二氫咄咯并[3,4-c]咄唑_1-基}^’-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(3 -碘-4-曱基苯曱醯基）-4, 6 -二氫吡咯并[3，4 - c ]吡唑-1 -基}，N ’ -曱基聚苯乙烯脲 N-{3 -苯乙酿胺基_5_(4_氯_2，5_二氣苯甲酿基）-4，6 -二氫°比°各并[3，4 - c ] 0比0坐-1 -基}，N ’ -甲基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 159 1327569 Five 'Inventions (157) [^-{3-Phenylethylamino-5-p-@香醯基-4,6- Dihydropyrrolo[3,4-c]pyrazol-1-yl},N'-mercaptopolystyrene urea N-{3_phenylethylamine _5_phenoxyethyl ketone_4,6 _Dinitro-π pyrrolo[3,4-c]pyrazole-fluorenyl polystyrene uranium Ν{3 - phenylethylamino}_5_narrow oxyethylene _4,6_diazo ρ ratio 11弁[3,4-〇]"Bizozol-1-yl}^'-methylpolystyrene-indole-{3-phenylethylamino-5-(1-naphthomethyl)-4 , 6-dihydroindolo[3,4-c]carbazole-1-*}, N'-methyl polystyrene urea N_{3_phenylethylamine _5_丁_2_ fast brewing _4,6_Dinitrogen ° ratio 弁3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-phenylethylamino-5-acetone oxime Base-4,6-dihydropyrrolo[3,4-c] ratio. Sitting _1-based h N,-decyl polystyrene urea N_{3 - phenylethylamine _5_(1,3_benzodioxanthene _5_yl) -4,6- Dihydrogen 0 to 11 each [3,4-(:]° is more than -1-yl}, 1'1'-mercaptopolyphenylene urea N_{3_phenylethylamine _5_(2 , 2_dimethylpropanyl)_4,6-diazepine-pyrolo[3,4-c]pyrazol-1-yl},Ν'-methylpolystyrene urea^{3-phenylethyl Amidino-5-(2,4-dioxa-5-fluorobenzoinyl)-4,6-dihydroindole is more than [3,4-c] °°-1-yl} ,^1'-fluorenyl polystyrene _ N-{3 - phenylethylamino-5-(2-mercapto-4-indolyl)-4,6-dihydroindole[ 3,4-c]carbazole_1-yl}^'-mercaptopolystyrene urea N-{3-phenethylamino-5-(3-iodo-4-mercaptophenyl)- 4,6-dihydropyrrolo[3,4 - c ]pyrazole-1-yl},N '-mercaptopolystyrene urea N-{3 -phenylethylamino}5_(4_chloro_2 , 5_2 gas benzoyl)-4,6-dihydrogen ratio °[3,4 - c ] 0 to 0 sitting -1 -yl}, N '-methyl polystyrene

C:\2D-C0DE\91-01\90119473.ptd 第160頁 1327569 五、發明說明（158) N-{3 -苯乙酿胺基_5-(環丁基魏基）-4，6 -二氫D比σ各并[3, 4-c]咄唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙酸胺基- 5- ( 11比咬-3 -基幾基）-4，6 -二氫η比ρ各并 [3,4-c]吡唑-1-*}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-異丁醯基-4,6-二氫°比咯并[3,4-c] 吡唑-1 -基}，N ’ -曱基聚苯乙烯脲 N-{3-苯乙醢胺基- 5- (1-Η-苯并三0坐-5-幾基）-4，6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(1-曱基-吲哚-3 -基）乙醯基-4,6-二氫°比11各并[3，4 - c ] 0比0坐-1 -基}, N ’ -甲基聚苯乙烯脲 1^{3-苯乙醯胺基-5-(2-甲基-°比。定-3-幾基）-4，6-二氫咄咯并[3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-苯乙醯胺基-5-(2-甲基磺醯胺基吼唑-4 -羰基）-4, 6-二氫吼咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(2-嗎啉曱基-5-呋喃曱醯基）-4,6-二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3_苯乙酿胺基_5-(2_苯基_°塞唾_4_基）乙酿基_4，6-二氫咄咯并[3, 4-c] »比唑-1-基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3-苯乙醯胺基-5-(2 -硫曱基比啶-3 -羰基）-4,6 -二氫吡咯并[3, 4-c]吼唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基- 5- (3-°夫喃甲醯基）-4，g -二氫吡咯并 [3,4-c]吡唑-1-基}，『-甲基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(3-0比σ定基-乙醯基）-4, 6 -二氫吼17各并[3,4-c]吡唑-1-基}^’-甲基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 160 1327569 V. INSTRUCTIONS (158) N-{3-Phenylethenyl-5-(cyclobutylweiyl)-4,6- Dihydrogen D ratio σ and [3, 4-c]oxazol-1-yl}, Ν'-methyl polystyrene urea-{3-phenylacetic acid amine- 5- (11 than bite-3 -基))-4,6-dihydro-n-ratio ρ-[3,4-c]pyrazole-1-*}, Ν'-mercaptopolystyrene-ruthenium-{3-phenylethylamino group -5-isobutyl indolyl-4,6-dihydropyrolo[3,4-c]pyrazol-1-yl},N '-mercaptopolystyrene urea N-{3-phenylethylamino group - 5-(1-indole-benzo-3-oxo-5-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl},Ν'-mercaptopolybenzene Ethylene urea N-{3-phenethylamino-5-(1-indolyl-indol-3-yl)ethenyl-4,6-dihydrogen ratio 11 and [3,4 - c ] 0 to 0 sitting -1 -yl}, N '-methyl polystyrene urea 1^{3-phenethylamino-5-(2-methyl-° ratio: -3-amino)-4 ,6-dihydroindolo[3,4-c]pyrazol-1-yl},N'-mercaptopolystyrene urea N-{3-phenethylamino-5-(2-methyl Sulfhydryl oxazole-4 -carbonyl)-4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, Ν'-methylpolystyrene uranium-{3 - Phenylacetam 5-(2-morpholinino-5-furanthyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-methyl polyphenyl Ethylene uranium-{3_phenylethylamino}5-(2-phenylene-pyrene-4-yl)ethenyl-4,6-dihydroindolo[3,4-c] » Bizolium-1-ylindole, Ν'-mercaptopolystyrene-indole-{3-phenethylamino-5-(2-thioindolinyl-3-carbonyl)-4,6-dihydrogen Pyrrolo[3,4-c]oxazol-1-ylindole, Ν'-methylpolystyrene-indole-{3-phenethylamino- 5-(3-°-folyl)- 4,g-dihydropyrrolo[3,4-c]pyrazol-1-yl}, "-methyl polystyrene urea N-{3-phenylethylamino-5-(3-0 ratio σ Stationary-ethenyl)-4,6-dihydroindole 17 and [3,4-c]pyrazol-1-yl}^'-methylpolystyrene

C:\2D-C0DE\91-01\90119473.ptd 第161頁 1327569 五、發明說明（159) N-{3 -苯乙醯胺基-5-(3 -噻吩曱醯基）-4, 6 -二氫吡咯并 [3,4-〇]吡唑-1-基}，！'1’-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(4-甲基-哌。井-1-基）乙醯基-4, 6-二氫吡咯并[3, 4-c]吼唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(5-乙醯胺基-2 -呋喃甲醯基）-4,6-二氫。比咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基- 5- (7-曱氧-苯并0夫喃-2-幾基）-4，6-二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基_5-(8 -唆琳）幾基-4，'6 -二氫D比ρ各并[3， _4-c] 比唑-1-基}，Ν，-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(苯并呋喃-2 -羰基）-4,6 -二氫吡咯并[3,4-c]吡唑曱基聚苯乙烯脲 N-{3-苯乙醯胺基-5-(吲哚-2 -基）羰基-4, 6 -二氫咄咯并 [3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(哌啶-1-基）乙醯基-4, 6 -二氫咄咯并[3,4-c]吼唑甲基聚苯乙烯脲 N-{3 -苯乙酿胺基_5_( 各_3_幾基）_4，6_二氮吼^各并 [3,4-〇]吡唑-1-基}^’-甲基聚苯乙烯脲 • Ν-{3 -苯乙酿胺基-5_( π比0各咬-1-基獄基）曱基_4，6_二氮吡咯并[3,4-c]吡唑-1-基}，1^’-甲基聚苯乙烯脲 N-{3_苯乙酿胺基_5-( °比°井_2_幾基）-4, 6_二氫吼0各并 [3,4-(：]吡唑-1-基}，1^’-曱基聚苯乙烯脲 N-{3 -苯乙酿胺基_5-( D比咬_3_截基）-4，6 -二氫吼。各并 [3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 161 1327569 V. INSTRUCTIONS (159) N-{3-Phenylethylamino-5-(3-thiophenanthryl)-4, 6 -Dihydropyrrolo[3,4-indolylpyrazole-1-yl},! '1'-mercaptopolystyrene urea N-{3-phenethylamino-5-(4-methyl-piperidin-1-yl)ethenyl-4,6-dihydropyrrolo[ 3, 4-c]oxazol-1-yl}, Ν'-methyl polystyrene uranyl-{3-phenethylamino-5-(5-acetamido-2-furancarbenyl )-4,6-dihydrogen. Bis-[3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-phenylethylamino- 5-(7-oxime-benzo- 0喃-2-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-phenylethylamino group _5-(8-唆琳), ketone-4, '6-dihydrogen D ratio ρ and [3, _4-c] bisazol-1-yl}, fluorene, fluorenyl polystyrene urea N- {3-Phenylethylamino-5-(benzofuran-2-carbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazolyl polystyrene urea N-{3-benzene Acetylamino-5-(indol-2-yl)carbonyl-4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N -{3-Phenylethylamino-5-(piperidin-1-yl)ethenyl-4,6-dihydroindolo[3,4-c]carbazolemethylpolystyreneurea N- {3 -Phenylethylamine_5_(each _3_yl)_4,6-diazepine^[3,4-〇]pyrazole-1-yl}^'-methylpolystyrene Urea • Ν-{3 - phenylethylamino-5-( π ratio 0 each bit -1- phenyl group) fluorenyl _4,6-diazapyrrolo[3,4-c]pyrazole-1- Base}, 1^'-methyl polystyrene urea N-{3_phenylethylamino}5-(° ratio ° well_2_base)-4,6-dihydroindole 0 each [3 ,4-(:]pyrazole-1- },1^'-Mercapto-polystyrene urea N-{3-phenylethylamino-5-(D-biting_3_trindyl)-4,6-dihydroindole. Each [3,4 -c]pyrazol-1-yl}, N'-mercaptopolystyrene

C:\2D-C0DE\91-01\90119473.ptd 第162頁 1327569 五、發明說明（160) N-{3-苯乙醯胺基- 5- (吡啶-4-羰基）-4, 6-二氫吡咯并 [3,4-c]吡唑甲基聚苯乙烯脲 N-{3-苯乙醯胺基_5-( σ比0各-3 -基獄基）乙醯基-4，6 -二氫吡咯并[3, 4-c]咄唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(喳啉-4 -羰基）-4,6-二氫吡咯并 [3,4-c]吡唑-1-*}，N’ -曱基聚苯乙烯脲 N-{3-苯乙醯胺基-5-(喳啉-6 -羰基）-4, 6 -二氫吡咯并 [3,4-c]吼唑-1-基}，1^’-甲基聚苯乙烯脲 N-{3-苯乙醯胺基-5-(3-曱氧環己基）羰基-4, 6 -二氫咄咯并[3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3 -苯乙酿胺基_5_(8 -氧基_5，6，7，8_四氮秦_2_基）叛基乙醯基- 4，.6-二氫σ比0各并[3，4-c] °比°坐-1-*}，N’-曱基聚苯乙烯脲 N-{3_苯乙酿胺基_5_[2_(6_氧基_1(611)_。荅°丼基）乙酿基 -4,6 -二氫吡咯并[3, 4-c]吡唑-l-基}, Ν’ -甲基聚苯乙烯脲 Ν-{3-苯乙酿胺基_5-[2-氟- 5- (三氣曱基）苯曱酿基] -4, 6 -二氫吼咯并[3,4-c]咄唑-l-基},Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-[4-(1Η-咪唑-1-基）苯甲醯基] -4, 6-二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{ 3 -苯乙醯胺基-5-[4-(1-咪唑基曱基）苯甲醯基] -4,6 -二氫吡咯并[3,4-c]吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-[4-(1-吡咯啶-2 -酮）苯曱醯基]-4, 6 -二氫吡咯并[3, 4-c]吼唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-苯乙醯胺基-5-[4-(胺基磺醯基）丁醯基]-4, 6 -二C:\2D-C0DE\91-01\90119473.ptd Page 162 1327569 V. INSTRUCTIONS (160) N-{3-Phenylethylamino- 5-(pyridine-4-carbonyl)-4, 6- Dihydropyrrolo[3,4-c]pyrazolemethylpolystyreneurea N-{3-phenethylamino- 5-( σ ratio 0--3-phenyl)-indolyl-4, 6-dihydropyrrolo[3,4-c]oxazol-1-yl}, Ν'-mercaptopolystyrene urea-{3-phenylethylamino-5-(porphyrin-4-carbonyl) -4,6-dihydropyrrolo[3,4-c]pyrazole-1-*}, N'-mercaptopolystyrene urea N-{3-phenethylamino-5-(porphyrin -6-carbonyl)-4,6-dihydropyrrolo[3,4-c]oxazol-1-yl}, 1^'-methyl polystyrene urea N-{3-phenylethylamino group- 5-(3-oxocyclohexyl)carbonyl-4,6-dihydroindolo[3,4-c]pyrazol-1-yl}, N'-mercaptopolystyrene urea N-{3 - Phenylethylamine _5_(8-oxy-5,6,7,8-tetrazin-2-yl) ridylamino- 4,.6-dihydro σ is 0 [3, 4-c] °°°-1-*}, N'-mercaptopolystyrene urea N-{3_phenylethylamine_5_[2_(6_oxy_1(611)_.荅丼 ) ) -4 -4 4,6-dihydropyrrolo[3,4-c]pyrazole-1-yl}, Ν'-methyl polystyrene uranyl-{3-phenylethylamino _5-[ 2-fluoro-5-(trimethylsulfonyl)benzoquinone]-4,6-dihydroindolo[3,4-c]carbazole-l-yl}, fluorene-fluorenyl polystyrene Urea-{3-phenylethylamino-5-[4-(1Η-imidazol-1-yl)benzylidene]-4,6-dihydropyrrolo[3,4-c]pyrazole- 1-yl},Ν'-mercaptopolystyrene-indole-{3-phenylethylamino-5-[4-(1-imidazolylhydrazyl)benzylidene]-4,6-dihydrogen Pyrrolo[3,4-c]pyrazole-1-ylindole, Ν'-methylpolystyrene-indole-{3-phenethylamino-5-[4-(1-pyrrolidine-2- Keto)phenyl phenyl]-4,6-dihydropyrrolo[3,4-c]carbazole-l-yl}, Ν'-mercaptopolystyrene uranyl-{3-phenylethylamino group -5-[4-(Aminosulfonyl)butanyl]-4, 6-di

C:\2D-C0DE\91-01\90119473.ptd 第163頁 1327569 五、發明說明（161) 氫0比σ各并[3，4 - c ] π比。坐-1 -基}，N ’ -曱基聚苯乙稀脲 Ν-{3 -苯乙醯胺基-5-[5-(1-嗎啉基甲基）呋喃-2 -羰基] -4, 6 -二氫吡咯并[3, 4-c]吡唑-l-基},Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5 -胺基曱醯氧乙醯基-4, 6 -二氫咄咯并[3，4-c]0比。坐_1_基}，1^’_曱基聚苯乙稀脈 N-{3 -苯乙醯胺基-5 -乙氧乙醯基-4,6 -二氫吡咯并 [3，4-c]吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν-{3-苯乙醯胺基-5-曱基吼啶醯基-4, 6-二氫咄咯并[3, 4-c]吡唑-1-基}，Ν’-甲基聚苯乙烯脲 _實施例9 Ν-{3 -苯乙醯胺基-5 -對曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基丨，Ν’ -曱基聚苯乙烯脲之製備對甲苯磺醯氯（0.43毫莫耳，82.0毫克）及DIEA (2.58¾ 莫耳，441. 7微升）添加至N-{3_苯乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吼唑-卜基}，Ν’ -曱基聚苯乙烯脲（0. 086毫莫耳，100毫克），該脲事先於4毫升無水二氯甲烷溶脹。結果所得懸浮液於22 °C溫和攪拌24小時。然後樹脂經過濾，以二氯甲烷及甲醇洗滌，及真空脫水。 g 以類似方式經由使用適當磺醯胺可製備下列化合物： N-{3-苯乙醯胺基-5-甲烷磺醯基-4,6 -二氫σ比咯并 [3,4-c]吡唑甲基聚苯乙烯脲 Ν - {3_苯乙酿胺基-5-窄基石黃酿基_4，6_二氮σ比洛弁 [3，4_c] 17比0坐-1-基}，1^’-甲基聚苯乙稀服 N-{3-苯乙酿胺基**5 -苯項酿基-4，6 -二氮σ比13各弁[3，4-c]C:\2D-C0DE\91-01\90119473.ptd Page 163 1327569 V. INSTRUCTIONS (161) Hydrogen 0 is greater than σ and [3,4 - c ] π ratio. -1 -yl},N '-mercaptopolystyrene-indole-{3-phenethylamino-5-[5-(1-morpholinylmethyl)furan-2-carbonyl] -4 , 6-dihydropyrrolo[3,4-c]pyrazole-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-phenethylamino-5-amino oxime Mercapto-4,6-dihydroindolo[3,4-c]0 ratio. Sit _1_基},1^'_曱-based polystyrene-chloride N-{3-phenethylamino-5-ethoxyethyl hydrazino-4,6-dihydropyrrolo[3,4- c]pyrazol-1-ylindole, Ν'-methylpolystyrene-indole-{3-phenethylamino-5-indenylpyridinyl-4,6-dihydroindole[3 , 4-c]pyrazol-1-yl}, Ν'-methyl polystyrene urea - Example 9 Ν-{3 - phenethylamino-5-p-phenylenesulfonyl-4,6- Preparation of dihydropyrrolo[3,4-c]pyrazole-1-ylindole, Ν'-mercaptopolystyrene urea p-toluenesulfonyl chloride (0.43 mmol, 82.0 mg) and DIEA (2.583⁄4 Mo Ear, 441. 7 μl) was added to N-{3_phenethylamino-4,6-dihydropyrrolo[3,4-c]carbazole-byl}, Ν'-mercaptopolybenzene Ethylene urea (0.086 mmol, 100 mg), which was previously swollen in 4 ml of anhydrous dichloromethane. As a result, the resulting suspension was gently stirred at 22 ° C for 24 hours. The resin was then filtered, washed with dichloromethane and methanol, and dried in vacuo. g The following compounds can be prepared in a similar manner via the use of the appropriate sulfonamide: N-{3-phenethylamino-5-methanesulfonyl-4,6-dihydroσpyrrolo[3,4-c] Pyrazole methyl polystyrene urea Ν - {3_ phenylethylamino-5-narrow keel yellow broth _4,6_diazo σ pyrrole [3,4_c] 17 to 0 sitting -1- group },1^'-Methylpolystyrene service N-{3-phenylethylamine **5-benzene-branched-4,6-diaza σ ratio 13 弁[3,4-c]

C:\2D-C0DE\91-01\90119473.ptd 第164頁 1327569 五、發明說明（162) 口比唑-1 -基}，N，一曱基聚苯乙烯脲 N_{3 -苯乙酿胺基_5_異丁烧續酿:基_4，6_二氮吼0各弁[3, 4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(喳啉-8 -磺醯基）-4,6 -二氫吡咯并 [3,4-c]。比唑-1-基}，N’-甲基聚苯乙烯脲 N-{3 -苯乙醯胺基-5-(萘-1-磺醯基）-4, 6 -二氫吼咯并 [3，4_c] D比。坐_1_基},1^’_甲基聚苯乙稀脈 N-{3 -苯乙醯胺基-5-(4-氟苯磺醯基）-4,6 -二氫吼咯并[3, 4-c]吡唑-1—基丨，ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-(4-甲氧苯磺醯基）-4, 6 -二氫吼咯并[3,4-c]吡唑-1-基}，『-甲基聚苯乙烯脲 N_{3_苯乙酿胺基-5 -（4 -三氟曱基苯石黃酷基）-4，6 -二氮比σ各并[3，4-c] D比。坐-1-基}，『-曱基聚苯乙浠脲 Ν-{3 -苯乙酿胺基_5_(3_三氟曱基苯石黃酿基）-4，6_二氮 0比ρ各并[3 , 4 - c ] 0比。坐-1 -基}，Ν ’ -曱基聚苯乙稀脲 Ν-{3_苯乙酿胺基-5-(2 -三說甲基苯石黃酿基）-4，6_二氯吡咯并[3 , 4 - c ]吡唑-1 -基}，Ν ’ -甲基聚苯乙烯脲 Ν_{3_苯乙酿胺基_5_(4_氣苯石黃酿基）_4，6_二氯°比略并 [3,4-c]吡唑-1-*}，Ν’-甲基聚苯乙烯脲 Ν_{3_苯乙酿胺基- 5- (4-第三丁基苯石黃酿基）-4，6_二氫 0比17各并[3, 4 - c ] 0比0坐-1 -基}，N ’ -曱基聚苯乙烯脲 N_{3 -苯乙酿胺基_5_(2_氛基苯石黃酿基）-4,6_二氯B比0各并[3,4_c] °比。坐_1_基},1^’_曱基聚苯乙稀脈實施例1 0C:\2D-C0DE\91-01\90119473.ptd Page 164 1327569 V. INSTRUCTIONS (162) Oryzazol-1 -yl}, N, monodecyl polystyrene urea N_{3 - phenylethyl Amino _5_isobutyl sinter sinter: base _4,6_diazepine 0 弁[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3 - phenethylamino-5-(porphyrin-8-sulfonyl)-4,6-dihydropyrrolo[3,4-c]. Bizozol-1-yl}, N'-methyl polystyrene urea N-{3-phenylethylamino-5-(naphthalene-1-sulfonyl)-4,6-dihydroindole[ 3,4_c] D ratio. Sit on _1_base}, 1^'_methyl polystyrene ring N-{3-phenethylamino-5-(4-fluorophenylsulfonyl)-4,6-dihydroindole [3, 4-c]pyrazole-1 -ylindole, ν'-mercaptopolystyrene-indole-{3-phenylethylamino-5-(4-methoxyphenylsulfonyl)-4, 6-dihydroindolo[3,4-c]pyrazol-1-yl}, "-methyl polystyrene urea N_{3_phenylethylamino-5-(4-trifluorodecylbenzene) Shihuangkuji)-4,6-diaza ratio σ and [3,4-c] D ratio.坐-1-基}, 『-mercaptopolyphenyl hydrazide {-{3 - phenylethylamine _5_(3_trifluorodecyl phenyl fluorite)-4,6_dinitrogen 0 ratio ρ is each [3, 4 - c ] 0 ratio. Sit-1 -yl}, Ν '-mercaptopolystyrene uranyl-{3_phenylethylamino-5-(2-tris-methylphenyl sulphate)-4,6-dichloro Pyrrolo[3 , 4 - c ]pyrazole-1-yl}, Ν '-methyl polystyrene urea Ν{{_phenylethylamino}_5_(4_phenyl yellow wine)_4,6 _Dichloro ° ratio slightly [3,4-c]pyrazole-1-*}, Ν'-methyl polystyrene urea Ν{{_phenylethylamino- 5- (4-tert-butyl Phenyl yellow base)-4,6_dihydrogen 0 to 17 each [3, 4 - c ] 0 to 0 sitting -1 -yl}, N ' -mercaptopolystyrene urea N_{3 - phenyl The amine-based _5_(2_yl benzophenone)-, 4,6-dichloroB ratio is 0 and [3,4_c] °. Sitting on _1_base}, 1^'_曱-based polystyrene pulse Example 1

C:\2D-GODE\91-01\90119473.ptd 第165頁 1327569 五、發明說明（163) N_{3_苯乙酿胺基_5_乙基胺基幾基_4，6 -二氣°比D各并[3， 4-c]吡唑曱基聚苯乙烯脲之製備異氰酸乙酯（0.43毫莫耳，33. 8微升）添加至N-{3 -苯乙醯胺基-4，6 -二氫0比洛并[3,4-c] D比0坐-1-基},1^’ -甲基聚苯乙烯脲（0.086毫莫耳，100毫克），該脲事先於4毫升無水二氯曱烷溶脹。結果所得懸浮液於22 °C溫和攪拌24小時。然後樹脂經過濾，以二氯甲烷、曱醇洗滌及真空脫水。以類似方式經由使用適當異氰酸酯可製備下列化合物： N-{3 -苯乙醯胺基- 5- (1-蔡基）胺基叛基- 4,6 -二氫0比0各 •并[3, 4-c]吡唑-1-基}，N’ -甲基聚苯乙烯脲 N-{3-苯乙醯胺基- 5- (1-萘基）胺基幾基-4，6 -二氫0比p各弁[3，4-c] D比。坐_1_基}，^_曱基聚苯乙稀脈 !'}-{3_苯乙酿胺基-5-(2，4_二氣苯基）胺基幾基-4，6_二氫吡咯并[3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3 -苯乙醯胺基- 5- (2,5-二曱氧苯基）胺基獄基-4，6-二氫°比咯并[3,4-c] °比唑-1-*}，N’ -曱基聚苯乙烯脲 N-{3 -苯乙酿胺基-5_(2，6_二氟苯曱酿基）胺基幾基 -4, 6 -二氫吡咯并[3, 4-c]咄唑-l-基}，Ν’ -曱基聚苯乙烯脲 0 Ν-{3-苯乙酿胺基- 5- (2，6 -二甲基苯基）胺基幾基-4, 6-二氫咄咯并[3, 4 - c ]吡唑-1 -基}，N ’ -甲基聚苯乙烯脲 N-{3-苯乙酿胺基- 5- (2-氣苯基）胺基幾基-4, 6 -二氫11比咯并[3,4-c]咄唑-1-*},N’ -曱基聚苯乙烯脲 N-{3 -苯乙酿胺基-5-(2-乙氧苯基）胺基幾基-4,6 -二氫比咯并[3, 4-c]°比唑-1-基}，Ν’ -曱基聚笨乙烯脲C:\2D-GODE\91-01\90119473.ptd Page 165 1327569 V. INSTRUCTIONS (163) N_{3_phenylethylamino-5-ethylamino-based _4,6-dioxin Preparation of ethyl isocyanate (0.43 mmol, 33.8 μL) added to N-{3-phenylacetamide at a ratio of D to each [3, 4-c]pyrazolyl polystyrene urea Base-4,6-dihydro- 0-bi-[3,4-c] D is 0-position-1-yl}, 1^'-methylpolystyrene (0.086 mmol, 100 mg), The urea was previously swollen in 4 ml of anhydrous dichloromethane. As a result, the resulting suspension was gently stirred at 22 ° C for 24 hours. The resin was then filtered, washed with dichloromethane, methanol and vacuum dried. The following compounds can be prepared in a similar manner via the use of the appropriate isocyanate: N-{3-phenethylamino- 5-(1-caiyl)amino-based derivatyl- 4,6-dihydrogen 0 to 0 each and [3 , 4-c]pyrazol-1-yl}, N'-methyl polystyrene urea N-{3-phenethylamino- 5-(1-naphthyl)amino-yl-4,6- Dihydrogen 0 is more than p [3,4-c] D ratio. Sit _1_基}, ^_曱基聚苯乙脉脉!'}-{3_phenylethylamino-5-(2,4_diphenyl)amino group-4,6_ Dihydropyrrolo[3,4-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-phenylethylamino- 5-(2,5-dioxanylphenyl) Amine base, 4,6-dihydro-pyrano[3,4-c] °, azole-1-*}, N'-mercaptopolystyrene urea N-{3-phenylethylamine -5-(2,6-difluorophenyl fluorenyl)aminoamino-4,6-dihydropyrrolo[3,4-c]carbazole-l-yl}, fluorene-fluorenyl polyphenylene Ethylene urea 0 Ν-{3-phenylethylamino-5-(2,6-dimethylphenyl)amino-based-4,6-dihydroindolo[3,4-c]pyrazole -1 -yl},N '-methyl polystyrene urea N-{3-phenylethylamino- 5-(2-phenylphenyl)amino-based benzyl-4,6-dihydro-11 [3,4-c]carbazole-1-*}, N'-mercaptopolystyrene urea N-{3-phenylethylamino-5-(2-ethoxyphenyl)amino group- 4,6-dihydropyrolo[3,4-c]°bazol-1-yl}, Ν'-fluorenyl polystyrene

C:\2D-C0DE\91-01\90119473.ptd 第166頁 1327569 五、發明說明（164) N-{3 -苯乙酿胺基_5-(2-氟-3-(三氟曱基）苯基）胺基叛基-4, 6 -二氫吡咯并[3, 4-c]吼唑-l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3_苯乙酿胺基- 5- (2 -異丙基苯基）胺基数基_4，6_二氫吡咯并[3,4-c]吡唑曱基聚苯乙烯脲 N-{3_苯乙酿胺基-（2-甲氧苯基）胺基幾基-4，6_二氫吡咯并[3, 4-c] 比唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν_{3_苯乙酿胺基_5_(2-甲基窄基）胺基獄基_4，6_二氫 0比咯并[3,4-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3_苯乙酿胺基-5-(2 -秦基）胺基獄基_4，6 -二氮π比0各并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -苯乙酿胺基_5_(3, 4 -二氣苯基）胺基幾基-4，6-二氫°比π各并[3，4 - c ] °比°坐-1 -基}，Ν ’ -甲基聚苯乙烯脲 Ν-{3_苯乙酿胺基- 5- (3 -氣苯基）胺基獄基-4，6_二氮°比 0各并[3，4-c] D比0坐_1_基}，1^’_甲基聚苯乙稀脈 N-{3 -苯乙酿胺基- 5- (3-氣苯基）胺基幾基-4，6_二氫D比咯并[3,4-c]咄唑-1-*}，N’-曱基聚苯乙烯脲 N-{3_苯乙酿胺基- 5- (3-曱氧苯基）胺基獄基-4，6 -二氫吡咯并[3,4-c]吡唑-1-基}，1^’ -曱基聚苯乙烯脲 N-{3_苯乙酿胺基- 5- (4 -聯苯基）胺基叛基-4, 6 -二氮0比咯并[3,4-c]吡唑-1-基}，N’ -甲基聚苯乙烯脲 N-{3_苯乙酿胺基_5_(4_氣苯基）胺基獄基-4，6_二氮π比咯并[3, 4-c]咄唑-1-基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3_苯乙酿胺基_5_(4_私苯甲酿基）胺基幾基_4，6_二C:\2D-C0DE\91-01\90119473.ptd Page 166 1327569 V. INSTRUCTIONS (164) N-{3-Phenylamino-7-(2-fluoro-3-(trifluoromethyl) Phenyl)amino-based tetamine-4,6-dihydropyrrolo[3,4-c]carbazole-l-yl}, Ν'-methylpolystyrene-indole-{3_phenylethylamine 5-(2-isopropylphenyl)amino group _4,6-dihydropyrrolo[3,4-c]pyrazolyl polystyrene urea N-{3_phenylethylamine -(2-methoxyphenyl)amino-based-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl},Ν'-methylpolystyrene Ν_{3_ Phenylethylamine _5_(2-methyln-yl)amine-based prison group _4,6-dihydro- 0-pyrrolo[3,4-c]pyrazol-1-yl}, 曱-mercapto group Styrene urea N-{3_phenylethylamino-5-(2-methyl)amine-based prison base_4,6-diaza π ratio 0 and [3, 4-c]pyrazole-1- } Ν 曱曱曱曱曱曱 { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { [3,4 - c ] °°°-1 -base}, Ν '-methyl polystyrene uranium-{3_phenylethylamino- 5-(3-phenylene)amine -4,6_Dinitrogen ° ratio 0 and [3,4-c] D ratio 0 sitting_1_1 base}, 1^'_methyl polyphenylene Ethyl sulfide N-{3-phenylethylamino- 5-(3-phenylphenyl)amino-based 4-,6-dihydro D-pyrolo[3,4-c]carbazole-1- *}, N'-mercaptopolystyrene urea N-{3_phenylethylamino- 5-(3-indolylphenyl)amine-based prison base-4,6-dihydropyrrolo[3,4 -c]pyrazol-1-yl},1^'-mercaptopolystyrene urea N-{3_phenylethylamino- 5-(4-diphenyl)amino-based t-group-4, 6- Diazo 0-pyrolo[3,4-c]pyrazol-1-yl}, N'-methylpolystyrene urea N-{3_phenylethylamino-5_(4-hydrophenyl)amine Kiba base-4,6_diazoπ-pyrolo[3,4-c]carbazol-1-ylindole, Ν'-mercaptopolystyrene uranium-{3_phenylethylamine _5_ (4_ private benzoyl) amino group _4,6_ two

C:\2D-C0DE\91-01\90119473.ptd 第167頁 1327569 五、發明說明（165) 氫吡咯并[3,4-c]吡唑-1-*}，N’-曱基.聚苯乙烯脲 N-{3-苯乙醯胺基-5-(4-氟苯基）胺基羰基-4, 6 -二氫吼咯并[3,4-c]吡唑-1-基}，N’_曱基聚苯乙烯脲 N-{3 -苯乙醯胺基- 5- (4-曱氧节基）胺基叛基-4,6 -二氫吡咯并[3,4-c]吡唑-1-S}，N’-曱基聚苯乙烯脲 N-{3-苯乙酿胺基-5- (4_曱氧苯基）胺基数基_4，6 -二氮吡咯并[3, 4-c]吡唑-1-基}, Ν’ -曱基聚苯乙烯脲 Ν_{3_苯乙酿胺基-5_(反_2_苯基環丙基）胺基幾基_4, 6_ 二氫0比°各并[3,4-c] °比°坐-1-*},Ν’ -曱基聚苯乙嫦脲 _ Ν-{3 -苯乙酿胺基- 5- [(R)-( + )_l_苯乙基]胺基幾基 -4，6-二氫°比°各并[3，4-(：]°比°坐-1-基}^’-甲基聚苯乙稀脲 N-{3_苯乙酿胺基- 5_[(S)-(-)-l -苯乙基]胺基叛基 -4,6-二氫0比0各并[3,4-<:]11比〇坐-1-基}，^-曱基聚苯乙稀脲 N-{3 -苯乙醯胺基- 5- [3-(三It甲基）苯基]胺基徵基 -4,6 -二氫吼0各并[3,4-c]°比。坐-1-基}，^’-甲基聚苯乙稀脲 N-{3-苯乙醯胺基-5-[4-(三氟甲氧）苯基]胺基羰基 -4,6-二氫°比11各并[3,4-(：]'1比唑-1-基},『-甲基聚苯乙稀脲 N-{ 3-苯乙醯胺基-5-苯曱醯胺基羰基-4, 6-二氫吡咯并 _3,4-c]。比。坐-1-基}，N，-甲基聚苯乙稀脲 N-{3-苯乙醯胺基-5-環己基胺基羰基-4,6 -二氫吡咯并 [3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-苯乙酿胺基-5_異丙基胺基幾基-4，6_二氫11比p各并 [3,4-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 N-{3 -苯乙酿胺基-5-正丁基胺基叛基-4，6_二氫°比。各并C:\2D-C0DE\91-01\90119473.ptd Page 167 1327569 V. INSTRUCTIONS (165) Hydropyrrolo[3,4-c]pyrazole-1-*}, N'-fluorenyl. Styrene urea N-{3-phenethylamino-5-(4-fluorophenyl)aminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-1-yl} , N'_decyl polystyrene urea N-{3- phenylethylamino- 5-(4-oxaoxy)amino-based tetamine-4,6-dihydropyrrolo[3,4-c Pyrazole-1-S}, N'-mercaptopolystyrene urea N-{3-phenylethylamino-5-(4-oxaphenyl)amino group _4,6-diazapyrrole And [3, 4-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene urea Ν{{_phenylethylamino-5-(trans-2-phenylcyclopropyl)amino group Base _4, 6_ dihydrogen 0 ratio °[3,4-c] ° ratio -1-*}, Ν'-mercaptopolyphenyl hydrazine _ Ν-{3 - phenylethylamine - 5- [(R)-( + ) _l_phenethyl]amino group - 4,6-dihydrogen ratio ° and [3,4-(:] ° ratio °-1-yl} ^'-Methyl polystyrene urea N-{3_phenylethylamino- 5_[(S)-(-)-l-phenethyl]amino-based tetamine-4,6-dihydro- 0 ratio 0 each [3,4-<:]11 is more than -1-yl}, ^-mercaptopolyphenylene urea N-{3-phenylethylamino- 5- [3-(three It Methyl)phenyl]amino group -4,6-dihydroindole 0 each [3,4-c]° ratio. sit-1-yl},^'-methyl polystyrene urea N-{3-phenylethylamino-5 -[4-(Trifluoromethoxy)phenyl]aminocarbonyl-4,6-dihydrogen ratio 11 and [3,4-(:]'1-pyrazol-1-yl}, "-methyl Polystyrene urea N-{ 3-phenethylamino-5-benzoguanidinocarbonyl-4,6-dihydropyrrolo-3,4-c]. Ratio -1-yl}, N,-methyl polystyrene urea N-{3-phenethylamino-5-cyclohexylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl }, N'-mercaptopolystyrene urea N-{3-phenylethylamino-5-isopropylaminomethyl-4,6-dihydrogen 11 ratio p and [3,4-c] Pyrazol-1-yl}, N'-mercaptopolystyrene urea N-{3-phenylethylamino-5-n-butylamino-based 4-,6-dihydrogen ratio

C:\2D-CODE\91-01\90119473.ptd 第168頁 1327569 五、發明說明（166) [3,4-c]呲唑-1-S}，N’-曱基聚笨乙烯脲 N-{3_苯乙酿胺基-5_苯基胺基数基_4，6-二氫吼11各并[3, 4-c]吡唑-1-基}，1^’-甲基聚苯乙烯脲 N-{3 -苯乙醯胺基-5 -對甲苯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吡唑-1 -基}，Ν’ -曱基聚苯乙烯脲 Ν_{3 -苯乙醒胺基-5-三氣乙酿基胺基幾基_4，6_二氫0比咯并[3,4-c]吡唑-1-*}，Ν’-曱基聚苯乙烯脲 1^-{3_苯乙酿胺基_5-苯乙基胺基幾基_4，6-二氮°比11各并 [3,4-c]咄唑-1-基}^’ -甲基聚苯乙烯脲 N-{3 -苯乙酿胺基- 5- [3，5 -武（三it甲基）苯基]胺基幾基 -4,6-二氫0比'?各并[3,4-〇];1比〇坐-1-基},1'1’-曱基聚苯乙烯脲 N - {3_苯乙酿胺基~5-第三丁基胺基数基-4，6_二氮13比D各并[3,4-c]咄唑-1-*}，N’-甲基聚苯乙烯脲 N_{3_苯乙酿胺基_5_[2，6_二異丙基苯基]胺基数基 -4,6-二氫〇比p各并[3,4-c] 〇比0坐-1-*}，N’-甲基聚苯乙烯脲 N-{3_苯乙酿胺基-5_[2，6_二乙基苯基]胺基幾基- 4,6-二氫D比B各并[3，4 - c ] °比。坐-1 -基}, N ’ - +甲基聚苯乙稀脲 N-{3_苯乙酿胺基-5-辛基胺基截基_4, 6_二氮D比p各并[3， 4-c]吡唑-l-基},Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯乙醯胺基-5-[(r)-(-)-l-(l -萘基）乙基]胺基羰基_4，6_二氫0比11 各并[3,4-c] D比11 坐-1_S}，N’_曱基聚苯乙稀脲實施例1 Γ' N-{5_苯基乙酿基_4，6_二氫0比p各并[3，4-c] π比。坐_3-基}C:\2D-CODE\91-01\90119473.ptd Page 168 1327569 V. INSTRUCTIONS (166) [3,4-c]carbazole-1-S}, N'-fluorenyl polystyrene -{3_phenylethylamino-5-phenylamino-based group 4,6-dihydroindole 11-[3,4-c]pyrazol-1-yl}, 1^'-methyl poly Styrene urea N-{3-phenethylamino-5-p-tolylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazole-1-yl}, Ν' - Mercapto-polystyrene-urea Ν{{-Phenylethylamino-5-tris-ethyl arylamino group _4,6-dihydro- 0-pyrrolo[3,4-c]pyrazole-1- *}, Ν'-mercaptopolystyrene urea 1^-{3_phenylethylamino-5-phenethylamino group _4,6-diaza ratio 11 and [3,4- c] oxazol-1-yl}^'-methyl polystyrene urea N-{3-phenylethylamino- 5-[3,5-wu(tritylmethyl)phenyl]amino group -4,6-dihydrogen 0 ratio '? each [3,4-〇]; 1 than 〇 -1-yl}, 1'1'-mercaptopolystyrene urea N - {3_phenylethyl Amino-5-t-butylamino group--4,6-diaza 13 to D-[3,4-c]carbazole-1-*}, N'-methylpolystyrene urea N_{ 3_phenylethylamino-_5_[2,6-diisopropylphenyl]amino group-4,6-dihydroindole ratio p and [3,4-c] 〇 is 0 -1- *},N '-Methyl polystyrene urea N-{3_phenylethylamino-5-[2,6-diethylphenyl]amino-yl- 4,6-dihydro D is more than B [3, 4 - c ] ° ratio. Sitting -1 -yl}, N ' - + methyl polystyrene urea N-{3_phenylethylamino-5-octylamino group _4, 6_dia nitrogen D ratio p and [ 3, 4-c]pyrazole-1-yl}, Ν'-methyl polystyrene uranium-{3-phenethylamino-5-[(r)-(-)-l-(l- Naphthyl)ethyl]aminocarbonyl_4,6-dihydrogen 0 to 11 each [3,4-c] D ratio 11 sits -1_S}, N'-decyl polystyrene urea Example 1 'N-{5_phenylethyl ketone_4,6_dihydrogen 0 is more than p and [3,4-c] π ratio. Sitting _3-base}

C:\2D-OODE\91-Ol\90119473.ptd 第169頁 1327569C:\2D-OODE\91-Ol\90119473.ptd Page 169 1327569

苯基乙醯胺之製備水性氫氧化鈉35%(1· 72毫莫耳，ία料斗、、* -Γ 城升）添力〇至享弈於 4毫升甲醇溶脹的N-{3 -苯乙醯胺基_5_苯乙醢基_4,6_二氮口比洛并[3, 4-c]。比唾-1-基}，N，-甲基聚苯乙烯脲（〇·’ 〇86毫莫耳）。結果所得懸浮液於4〇。(：溫和攪拌72小時。然後樹脂經過濾’濾液以2 5 %鹽酸中和及蒸發至乾。殘餘物分溶於氣仿（4毫升）及飽和碳酸氫鈉溶液（2 〇〇微升）^有機層以硫酸鈉脫水及蒸發獲得標題化合物呈黃色固體（2 1 · 〇毫克，65%) 〇 • ]H-NMR (DMSO-de) ^ ρρπι; 7. 3-7. 1 (m) ； 4.6-4.4(m)； 3. 67(s) ; 3. 6(s)。 (M + H)+ = 360 類似地，經由使用適當實施例6及7所述曱基聚笨乙烯獲得： 1^-{5-乙醯基-4,6-二氫吡咯并[3,44]吡唑_3_基}苯基乙醯胺】H-NMR (DMS0-d6) 5 ppm :12. 23(s);7.3~7.2(m);4.6-4. 3(m);3,59(s)；K97(s) (M + H)+ = 284 N_辛基-N’_{3_笨基乙醯胺基_4, 6—>氫吡咯并[3,4-c] °比唾-5 -基}脈 iH_NMR (DMS0-d6) 5ppm:1〇.6(s);7. 3一7. l(m);6.85(t 寬）；4.37(s 寬）；4.23(d);3.6(s)。Preparation of phenylacetamide Aqueous sodium hydroxide 35% (1·72 mmol, ία hopper, * -Γ 城升) Add 〇 to enjoy the 4 ml of methanol swelled N-{3 - phenyl Amidino _5_phenidinyl _4,6-diazabibiloxime [3, 4-c]. More than sal-1-yl}, N,-methyl polystyrene (〇·' 〇86 mmol). The resulting suspension was at 4 Torr. (: Stir gently for 72 hours. Then the resin was filtered. The filtrate was neutralized with 25% hydrochloric acid and evaporated to dryness. The residue was dissolved in EtOAc (4 mL) and sat. NaH. The title compound was obtained as a yellow solid (2 1 ·································· - 4.4 (m); 3. 67 (s); 3. 6 (s). (M + H) + = 360 Similarly, obtained by using the fluorenyl polystyrene described in Appropriate Examples 6 and 7: 1^ -{5-Ethyl-4,6-dihydropyrrolo[3,44]pyrazole-3-yl}phenylacetamide]H-NMR (DMS0-d6) 5 ppm :12.23(s );7.3~7.2(m);4.6-4. 3(m);3,59(s);K97(s) (M + H)+ = 284 N_octyl-N'_{3_ stupid Acetylamino-4,6->hydropyrrolo[3,4-c] ° than salin-5-yl} pulse iH_NMR (DMS0-d6) 5ppm: 1〇.6(s); 7. 3 7. l(m); 6.85 (t wide); 4.37 (s wide); 4.23 (d); 3.6 (s).

C:\2D-C0DE\91-01\90119473.ptd 第170頁 1327569 五、發明說明（168) (M + H)+ = 375 1^-{5-曱苯石黃醯基-4，6-二氫0比0各并[3,4-(：]11比。坐-3-基} 苯基乙醯胺 Ή-NMR (DMS〇-d6) (5ppm: 7.7(d); 7.39(d); 7.3-7.2(m); 4.4-4.2(m);3.56(s);2.34(s)。 (M + H)+ = 396 N-乙基-Ν’ - {3 -苯基乙醯胺基-4, 6 -二氫吡咯并[3, 4-c] 。比唆-5 -基}脲 ]H-NMR (DMS0_d6)(5ppm:7.3-7.1(m);6.2(t 寬）；4.3(s 寬）；3. 59(s) ; 3. 03(m) ; 1⑴。 (M + H)+ = 31 3 N-{5-乙醯基-4，6 -二氫口比0各并[3，4-c] °比》坐-3-基}-4-(苯基）苯基乙醯胺 Ή-NMR (DMSO-d6) (5 ppm : 7. 6 - 7. 3 ( m ) ; 4. 6 - 4. 3 ( m ); 3.64(s);1.98(s)。 (M + H)+ = 360 N-{5-乙醯基-4，6 -二氫°比°各并[3，4-c] °比°坐-3-基}-2 -萘基乙醯胺 UMR (DMSO-d6) dppm:7.9-7.5(m);4.6-4.3(m) ;3.78(s);l.97(s)。 (M + H)+ = 334 實施例1 2 4, 6 -二氫D比洛并[3, 4-c]吡唑-3-基衍生物存庫之製備步驟a :C:\2D-C0DE\91-01\90119473.ptd Page 170 1327569 V. INSTRUCTIONS (168) (M + H)+ = 375 1^-{5-Indanthylxanthyl-4,6-dihydrogen 0 to 0 each [3,4-(:]11 ratio. -3-yl} phenylacetamide Ή-NMR (DMS〇-d6) (5ppm: 7.7(d); 7.39(d); 7.3 -7.2(m); 4.4-4.2(m); 3.56(s); 2.34(s). (M + H)+ = 396 N-ethyl-Ν' - {3-phenylethylamino-4 , 6-dihydropyrrolo[3,4-c]. 唆-5-yl}urea]H-NMR (DMS0_d6) (5ppm: 7.3-7.1(m); 6.2(t wide); 4.3(s wide ); 3. 59(s) ; 3. 03(m) ; 1(1). (M + H)+ = 31 3 N-{5-Ethyl-4,6-dihydrogen port is 0 and [3, 4-c] ° ratio 坐-3-yl}-4-(phenyl)phenylacetamide Ή-NMR (DMSO-d6) (5 ppm : 7. 6 - 7. 3 ( m ) ; 6 - 4. 3 ( m ); 3.64(s); 1.98(s). (M + H)+ = 360 N-{5-ethenyl-4,6-dihydrogen °°[3, 4-c] ° ratio -3-yl}-2-naphthylacetamide UMR (DMSO-d6) dppm: 7.9-7.5 (m); 4.6-4.3 (m); 3.78 (s); 97(s). (M + H)+ = 334 Example 1 Preparation of a 4,6-dihydro-D-Bisto[3,4-c]pyrazol-3-yl derivative library Procedure a:

C:\2D-OODE\91-01\90119473.ptd 第171頁 1327569 五、發明說明（169) ' 一 540克3 -胺基~5-(第三丁酯基）_4 6_二氫吡咯并[3,4_ 。比唑係根據實施例4報告之程序製備。步驟b : ·、結果所得3-胺基-5-(第三丁酯基）_4, 6_二氫咄咯并 [3, 4-c]吡唑根據實施例5報告之程序支撐於甲基異氰酸酯聚苯乙烯樹脂（ 200-400篩目，2%DVB，負載1. 49毫莫耳/ 克，900克）。步驟c: 結果所得N-{3 -胺基- 5- (第三丁酯基）_4, 6 -二氫呲咯并 _ 3, 4-c]吼嗅-1-基丨，Ν’ -曱基聚笨乙烯脲分成96個不同批次（各批1 5克）。各批次根據實施例6所述程序與適當醯基氣反應獲得實施例6列舉之產物。步驟d : 96批次之N-{3 -醯基醯胺基-5-(第三丁酯基）-4,6 -二氫 °比咯并[3,4-c]咄唑-1—基}，N’_曱基聚苯乙烯脲根據實施例7所述程序各別使用TFA 50%於無水二氯曱烷溶液處理，獲得實施例7列舉之產物。步驟e : 鲁步驟d所得9 6批次中之一批次分成1 4 9批次（各5 〇毫克）。 1 4 9批次各別與實施例8使用的9 5種羧酸、實施例9使用的 1 5種續酿氯及實施例1 〇使用的1 5種異氰酸酯反應。步驟f : 步驟e所得各1 4 9批次根據實施例11報告程序水解獲得 149種單一4,6 -二氫吡哈并[3, 4-c]吼峻-3-基衍生物（各C:\2D-OODE\91-01\90119473.ptd Page 171 1327569 V. INSTRUCTIONS (169) 'A 540 g of 3-amino-5~(3-tert-butyl)- 4 6-dihydropyrrole [3,4_. The bisazole was prepared according to the procedure reported in Example 4. Step b: The resulting 3-amino-5-(t-butylester)-4,6-dihydroindolo[3,4-c]pyrazole was supported on methyl according to the procedure reported in Example 5. Isocyanate polystyrene resin (200-400 mesh, 2% DVB, load 1.49 mmol/g, 900 g). Step c: The resulting N-{3-amino-5-(t-butylester)-4,6-dihydroindolo- 3,4-c]oxime-1-ylindole, Ν'-曱The base polystyrene urea was divided into 96 different batches (15 g each). Each batch was reacted with an appropriate hydrazine base according to the procedure described in Example 6 to obtain the product recited in Example 6. Step d: 96 batches of N-{3-mercaptoamino-5-(t-butylester)-4,6-dihydropyr-[3,4-c]carbazole-1- The base, N'-decyl polystyrene urea was treated with TFA 50% in anhydrous dichloromethane solution according to the procedure described in Example 7 to give the product of Example 7. Step e: One of the batches of 96 batches obtained in step d is divided into 149 batches (5 各 each). The batches of 1 4 9 were each reacted with 9 5 kinds of carboxylic acids used in Example 8, 15 kinds of continuously brewed chlorine used in Example 9, and 15 kinds of isocyanates used in Example 1. Step f: Each of the 149 batches obtained in step e was hydrolyzed according to the procedure of Example 11 to obtain 149 single 4,6-dihydropyhaha[3,4-c]indole-3-yl derivatives (each

C:\2D-C0DE\9l-0l\90H9473.ptd 第172頁 1327569 五、發明說明（170) 7-14毫克）。步驟g : 步驟d之其餘95批次各別進行步驟e及f。整個綜合化學製備方法獲得96X1 49 = 1 4304種各別4, 6-二氫D比ρ各并[3, 4 - c ]吼。坐-3 -基衍生物存庫。前述綜合存庫之代表性化合物為： Ν-{5-乙酿基- 4,6 -二氫D比σ各并[3，4-c] D比。坐-3-基} - 0夫°南 -2 -叛醢胺；1H-NMR (DMSO-d6) d ppm:7.9(ni);7.4(m); 6. 7(m);4, 6-4. 4(m);2. 02(s)。 N-{5-乙醯基-4, 6 -二氫0比D各并[3, 4-c] n比。坐-3-基}-5-氯 0 塞 B分-2-缓醯胺；1H-NMR (DMS0-d6) d ppm:8.0-7.9(m) ;7.2(m);4. 6-4.4(m) ; 2. 03(s)。 1'1-{5-乙醯基-4,6-二氫0比17各并[3,4-(：]〇比°坐-3-基}-6-氯於臉醯胺；1H-NMR (DMSO-d6) d ppm:8.95(s);8.4(m) ;7.6(m) ;4· 7-4.4(m);2· 03(s)。 N-{5-乙醢基一 4，6 —二氫°比口各并[3，4_c] 0比0垒一3—基}-苯弁 0夫喃-2-叛醯胺；1H-NMR (DMS〇-d6) d ppm:7.8-7.3(m) ;4.7-4·4(m);2. 03(s)。 N-{5_乙酿基~4，6_二氮n比p各并[3，4_c] 0比0坐-3_基}_4_苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.5-7.2(m); 4· 7-4. 4(m);2. 0(s)。 N-{5_乙酿基**4，6 -二氮n比D各并[3，4_c] 0比0坐-3_基}_4_第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.9-7.8(m) ;7.5-7.4(m);4.7-4.4(m);2.03(s);1.30(s)。C:\2D-C0DE\9l-0l\90H9473.ptd Page 172 1327569 V. Description of invention (170) 7-14 mg). Step g: The remaining 95 batches of step d are subjected to steps e and f, respectively. The entire comprehensive chemical preparation method obtained 96X1 49 = 1 4304 kinds of 4, 6-dihydrogen D ratio ρ and [3, 4 - c ] 吼. Take a 3-base derivative library. Representative compounds of the aforementioned comprehensive storage are: Ν-{5-ethyl-branched- 4,6-dihydrogen D ratio σ and [3,4-c] D ratio. -3--3-基} - 0 Fu nan-2 - ruthenium; 1H-NMR (DMSO-d6) d ppm: 7.9 (ni); 7.4 (m); 6. 7 (m); 4, 6- 4. 4(m); 2. 02(s). N-{5-ethinyl-4,6-dihydrogen 0 is a ratio of D to [3, 4-c] n. -3--3-yl}-5-chloro 0 ose B -2- decylamine; 1H-NMR (DMS0-d6) d ppm: 8.0-7.9 (m); 7.2 (m); 4. 6-4.4 ( m) ; 2. 03(s). 1'1-{5-Ethyl-4,6-dihydrogen 0 to 17 each [3,4-(:]〇 ratio ° sitting-3-yl}-6-chloro to acetophenone; 1H- NMR (DMSO-d6) d ppm: 8.95 (s); 8.4 (m); 7.6 (m); 4·7-4.4 (m); 2· 03 (s). N-{5-ethylhydrazine- 4 , 6 - dihydrogen ° ratio each [3,4_c] 0 to 0 base -3 - base} - benzoquinone 0 fumon-2-rebelamine; 1H-NMR (DMS〇-d6) d ppm: 7.8 -7.3(m); 4.7-4·4(m); 2. 03(s). N-{5_乙酿基~4,6_Dinitrogen n ratio p and [3,4_c] 0 to 0 Sitting on -3_yl}_4_phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm: 7.5-7.2 (m); 4· 7-4. 4 (m); 2. 0 (s) N-{5_乙牛基**4,6-diaza n ratio D and [3,4_c] 0 to 0 sitting -3_yl}_4_t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 4.7-4.4 (m); 2.03 (s); 1.30 (s).

C:\2D-00DE\91-01\90119473.ptd 第173頁 1327569 五、發明說明（171) N-{5-乙酿基-4，6 -二氫0比σ各并[3，4-c] 0比0坐-3_基}-胡椒基醯胺； Ν-{5-乙酿基-4，6 -二氫°比°各并[3, 4-c] °比°坐-3_基}_[2-曱基-5-苯基-呋喃-3-羧醯胺];1H-NMR (DMS0-d6) d ppm:7. 6-7. 3(m);4. 7-4_ 4(m);2· 62(s);2. 03(s)。 N - { 5 -乙酿基-4，6 -二氫B比0各并[3，4-c] D比0坐-3-基}_(嗜啉-6-羧醯胺）；1H-NMR (DMS0-d6) d ppm:9.0(m);8.7-8. 5(m);8.3-7.9(m);7.6(m);4.7-4.2(m);2.05(s)。 ^{5-乙醯基-4，6-二氫0比口各并[3,4-〇]0比〇坐-3-基}-鲁L5-(4-氯苯基）呋喃-2-羧醯胺];1H-NMR (DMS0-d6) d ppm:8.0-7. 2(m);4·7-4·4(m);2.03(s)。 N-{5-曱烧石黃醯基- 4,6 -二氫D比p各并[3,4-c] 0比〇坐-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm: 7.9-7.8(m);7.5-7.4(m);4.5-4.4(m);2.96(s);1.28(s)。 N-{5 -苯石黃醢基-4, 6 -二氫°比σ各并[3, 4-c] °比。坐-3-基}-4_ 第三丁基苯曱醯胺；111-題尺（0肘80-(16)(1??111:7.9-7.8(m);7.7-7.6(m);7.5-7.4(m);4.5-4.3(m);1.28(s)。 N-{5 -苯曱醯基- 4,6 -二氫〇比0各并[3,4-c] 0比唾-3-基}-4-•第三丁基苯甲醯胺；1H-NMR (DMSO-d6) d ppm: 7. 9-7. 8 (m);7.6-7.4(m);4.7-4·5(m);l.26(s) 〇 N-{5-(l -蔡）項醯基-4, 6 -二氫°比°各并[3, 4-c]吼°坐-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:8.3-8.2(m);8.1-8.0(m);7.9-7.8(m);7.8-7.6(m); 7. 5-7.4(m);4. 6-4. 5(m);l. 27(s)。C:\2D-00DE\91-01\90119473.ptd Page 173 1327569 V. INSTRUCTIONS (171) N-{5-Ethyl-4,6-dihydrogen 0 to σ each [3,4- c] 0 to 0 sitting -3_yl}-piperidinylamine; Ν-{5-ethyl-branched-4,6-dihydrogen ratio °[3, 4-c] °°°-3 _[}][[2-indolyl-5-phenyl-furan-3-carboxamide]; 1H-NMR (DMS0-d6) d ppm: 7. 6-7. 3(m); 4. 7- 4_ 4(m); 2· 62(s); 2. 03(s). N - { 5 -Ethyl-4,6-dihydro B is 0 and each [3,4-c] D is 0--3-yl}_(porphyrin-6-carboxyguanamine); 1H- NMR (DMS0-d6) d ppm: 9.0 (m); 8.7-8. 5 (m); 8.3-7.9 (m); 7.6 (m); 4.7-4.2 (m); 2.05 (s). ^{5-Ethyl-4,6-dihydrogen 0 is a ratio of [3,4-〇]0 to -3--3-yl}-Lu L5-(4-chlorophenyl)furan-2- Carboxylamidine]; 1H-NMR (DMS0-d6) d ppm: 8.0-7. 2 (m); 4·7-4·4 (m); 2.03 (s). N-{5-曱烧石黄醯基- 4,6-Dihydro D ratio p and [3,4-c] 0 is more than 〇-3-yl}-4-t-butylbenzamide; 1H - NMR (DMSO-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 4.5-4.4 (m); 2.96 (s); 1.28 (s). N-{5 - benzoate xanthyl-4,6-dihydrogen ratio σ and [3, 4-c] ° ratio. Sodium-3-yl}-4_t-butylbenzamide; 111-foot ruler (0 angling 80-(16) (1??111:7.9-7.8(m); 7.7-7.6(m); 7.5 -7.4 (m); 4.5-4.3 (m); 1.28 (s). N-{5-benzoinyl- 4,6-dihydroindole is 0 to each [3,4-c] 0 than saliva- 3-yl}-4-•t-butylbenzamide; 1H-NMR (DMSO-d6) d ppm: 7. 9-7. 8 (m); 7.6-7.4 (m); 4.7-4· 5(m);l.26(s) 〇N-{5-(l-Cai) 醯-yl-4,6-dihydrogen ratio °[3, 4-c]吼° sitting-3- } _ _ butyl benzyl hydrazide; 1H-NMR (DMS0-d6) d ppm: 8.3-8.2 (m); 8.1-8.0 (m); 7.9-7.8 (m); 7.8-7.6 ( m); 7. 5-7.4(m); 4. 6-4. 5(m); l. 27(s).

C:\2D-00DE\91-01\90119473.ptd 第174頁 1327569 五、發明說明（172) N_{5_(1-蔡甲酿基）_4，6_二氮0比p各弁[3，4_c]D比0坐- 3_ 基卜4 -第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:8.0-7. 9(m);7.9-7.7(m);7.6-7.4(m);4.8-4.2(m); 1. 23(s)。 N-{5-苯乙醯基- 4,6 -二氫吼11 各并[3,4-c] n比。坐-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm·· 7. 9-7· 8 (m);7.5-7.4(m);7.3-7.2(m);4.7-4.4(m);3.7-3.6(m); 1.29(s)。 N-苯基-Ν’ - {3-(4-第三丁基-苯甲醯胺基）-4,6 -二氫吡〇各并[3，4-。]°比哇-5-基}脲；111-題1^(0肘30-(16)(1??111:7. 9-7.8(m);7.5-7.4(m);7.3-7.2(m);6.9-6.8(m); 4. 6-4. 5(m) ; 1. 27(s)。 N-異丙基_N’ - {3-(4_第三丁基-苯曱酿胺基）-4，6 -二氫口比 B各并[3，4-c]^°坐-5-基}脲；1H-NMR (DMSO-d6) d ppm: 7.9-7.8(m);7.5-7.4(m);4.4-4.3(m);3.8-3.7(m); 1. 29(s) ; 1_ 07(d)。 N-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3 -基} -4-苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.5-7.4(m) ;4.5-4.4(m);3.0(s)。 1^一{5-苯曱蕴基一4,6-二氫〇比'1各并[3,4-(：]'1比11坐-3-基}-4-苯氧苯甲醯胺；1H-NMR (DMSO-d6) d ppin:7.6-7.4(m) ;7·卜6. 9(m) ; 4. 65-4. 5(m)。 N-{5-(l -萘甲醯基）-4,6 -二氫0比0各并[3,4-c] 0比0坐- 3-基}-4 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:8. 1C:\2D-00DE\91-01\90119473.ptd Page 174 1327569 V. INSTRUCTIONS (172) N_{5_(1-Cai-Wing) _4,6_Dinitrogen 0 is more than p[3, 4_c]D is 0 to sit - 3_ kib 4 -th-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 8.0-7. 9(m); 7.9-7.7(m); 7.6- 7.4 (m); 4.8-4.2 (m); 1. 23 (s). N-{5-phenethyl- 4,6-dihydroindole 11 each [3,4-c] n ratio. Sodium-3-yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm·· 7. 9-7· 8 (m); 7.5-7.4 (m); 7.3- 7.2 (m); 4.7-4.4 (m); 3.7-3.6 (m); 1.29 (s). N-phenyl-indole-{3-(4-t-butyl-benzylamino)-4,6-dihydropyridinium [3,4-. ]°比哇-5-基}urea; 111-question 1^(0 elbow 30-(16)(1??111:7. 9-7.8(m); 7.5-7.4(m); 7.3-7.2( m); 6.9-6.8(m); 4. 6-4. 5(m); 1. 27(s). N-isopropyl_N' - {3-(4_t-butyl-benzoquinone) Amine-based 4,6-dihydrogen port ratio B and [3,4-c]^° sit-5-yl}urea; 1H-NMR (DMSO-d6) d ppm: 7.9-7.8 (m) ; 7.5-7.4 (m); 4.4-4.3 (m); 3.8-3.7 (m); 1. 29 (s); 1_ 07 (d). N-{5-nonanesulfonyl-4, 6 - Dihydropyrrolo[3,4-c]indazole-3-yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm: 7.5-7.4 (m); 4.5-4.4 ( m); 3.0(s). 1^-{5-benzoquinone-based 4,6-dihydroindole is more than '1 and [3,4-(:]'1 is 11--3-yl}- 4-phenoxybenzamide; 1H-NMR (DMSO-d6) d ppin: 7.6-7.4 (m); 7·b 6. 9 (m); 4. 65-4. 5 (m). {5-(l-naphthomethyl)-4,6-dihydrogen 0 to 0 each [3,4-c] 0 to 0-s--3-yl}-4-phenoxybenzoquinone; 1H -NMR (DMS0-d6) d ppm: 8. 1

C:\2D-00DE\91-01\90119473.ptd 第175頁 1327569 五、發明說明（173) -7.8(m);7.2-6.9(m);4.9-4.7(m);4.4-4.2(m)。 N-異丙基-Ν’ - {3-(4 -苯氧-苯曱醯胺基）-4,6 -二氫吡咯并[3，4-c]° 比 11 坐-5-基}脲；1H-NMR (DMS〇-d6) d ppm:7.5 -7.4(m);4.3-4.2(m);3.8(m);l.1(d)。 1^-{5-乙醯基-4,6-二氫0比1?各并[3,4-(：]'1比11坐-3-基}-[2-(2-萘基）丙醯胺];111-關1^(0肘50-(16)(1?口111:7.8-7.5(m);4. 6-4. 3(m);4.0(m);2.0(s);l.5(m) 〇 N_異丙基_N’ - {3_胡椒基叛酿胺基）_4，6 -二氫各并[3, 4-(：]吼°坐-5-基}脲；1H-NMR (DMS0-d6) d ppm:7.4-7.7 J®：m);6_l(s);4.7-4.9(m);1.0-l.l(m)。 N-環己基-Ν’ - {3-(4-第三丁基-苯曱醯胺基）-4，6 -二氫口比0各并[3,4-。]°比。坐-5-基}脲；1H-NMR (DMS〇-d6) d ppm: 7.9- 7.8(m);7.5-7.4(m);4.4-4.3(m);1.8-1.0(m); 1.23(s)。 N-乙基- Ν’ - {3-(4-第三丁基-苯曱酿胺基）-4,6 -二氫0比〇各并[3，4-。]°比°坐-5-基}脲；111-關1?(0^180-(16)(1〇口111: 7.9- 7.8(m);7.5-7.4(m);4.4-4.3(m);3.3-3.0(in); 1. 30(s);l.卜1. 0(m)。 g N-(2，6_二乙基苯基）-N’ _{3-(4-第三丁基-苯甲酿胺基） _4，6 -二氫 π比 σ各并[3，4-c] °比 °坐-5_ 基}服；1H-NMR (DMS0-d6) d ppm:7.9-7.8(m);7.5-7.4(m);7.1-7.0(m) ;4.6-4.5(m);2.56(q);1.30(s);l. 11(1:)。 N -環己基-Ν’ - {3-(2-乙基-丁醯胺基）-4, 6 -二氫吡咯并 [3，4-c]ab°坐-5-基}脲；1H-NMR (DMS0-d6) d ppm:4.3C:\2D-00DE\91-01\90119473.ptd Page 175 1327569 V. Description of invention (173) -7.8(m); 7.2-6.9(m); 4.9-4.7(m); 4.4-4.2(m ). N-isopropyl-Ν'-{3-(4-phenoxy-phenylguanidino)-4,6-dihydropyrrolo[3,4-c]° ratio 11 sit-5-yl}urea ;1H-NMR (DMS〇-d6) d ppm: 7.5 - 7.4 (m); 4.3-4.2 (m); 3.8 (m); l.1 (d). 1^-{5-Ethyl-4,6-dihydrogen 0 to 1? each [3,4-(:]'1 to 11-position-3-yl}-[2-(2-naphthyl) Propylamine]; 111-off 1^(0 elbow 50-(16) (1? mouth 111: 7.8-7.5 (m); 4. 6-4. 3 (m); 4.0 (m); 2.0 (s );l.5(m) 〇N_isopropyl _N' - {3_Pepper-based Amine-based)_4,6-Dihydro-[3, 4-(:]吼°--5- 1H-NMR (DMS0-d6) d ppm: 7.4-7.7 J®:m); 6_l(s); 4.7-4.9(m); 1.0-ll(m). N-cyclohexyl-Ν' - {3-(4-Terti-butyl-phenylguanidino)-4,6-dihydrogen port ratio 0 and [3,4-.] ° ratio. Sodium-5-yl}urea; 1H- NMR (DMS〇-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 4.4-4.3 (m); 1.8-1.0 (m); 1.23 (s). N-ethyl- Ν' - {3-(4-Terti-butyl-benzoindolyl)-4,6-dihydrogen 0 is 〇[3,4-.]°°°°-5-yl}urea; 111- Off 1?(0^180-(16)(1〇口111: 7.9- 7.8(m); 7.5-7.4(m); 4.4-4.3(m); 3.3-3.0(in); 1. 30(s L.1. 0(m) g N-(2,6-diethylphenyl)-N' _{3-(4-t-butyl-benzoylamino) _4,6 - dihydro π ratio σ 并 [3,4-c] ° ratio ° sitting -5 _ base}; 1H-NMR (DMS0-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 7.1-7.0(m); 4.6-4.5(m); 2.56(q); 1.30(s);l.11(1:). N -cyclohexyl-fluorene'-{3-(2-ethyl-butylammonium)-4,6-dihydropyrrolo[3,4-c]ab°--5-yl}urea;1H-NMR (DMS0-d6) d ppm: 4.3

C:\2D-C0DE\91-01\90119473.ptd 第176頁 1327569 五、發明說明（174) (m);3.4(m);2.24(m);1.6-1.4(ni);0.8(m)。 1(2,6-二乙基苯基）-『-{3-(胡椒基羧醯胺基）-4,6-二氫响17各并[3，4-〇]°比°坐-5-基}脲；1H-NMR (DMS〇-d6) d ppm:7.5-7. 7(m);7.0-7.2(m);6.l(s);4.4-4.6(m);2.5-2. 6(m);l.0-1.l(t)。 N-2-曱氧苯基-Ν’ - {3-(2 -萘-2 -基-丙醯胺基）-4, 6 -二氫〇比11各并[3，4-(：]°比°坐-5-基}脲；111-關1^(0肘50-(16)(1??111: 7.8-6.8(m);4·5(m);4·0(m);3·8(s);l.5(d)。 1^1-(1-苯基）乙基-^-{3-(2-萘-2-基-丙醯胺基）-4,6-二氫0比°各并[3，4-c]D比 °坐-5-基}脲；1H-NMR (DMSO-d6) d ppm:10.6(s);7.8-7.2(m);6.6(m);4.8(m);4.4(m);4.0(m) ;1.5(d);1.4(d) o N-{5 -苯基醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -萘基 }-3-(2 -萘-2 -基）-丙醯胺；1H-NMR (DMS0-d6) d ppm: 7. 8 -7.5(m);4.4(m);4.0(m);1.4(d) 〇 N-(2，5 -二甲基苯基）-N’-{3-(4-第三丁基-苯曱酿胺基） -4,6-二氫°比11各并[3,4-〇]51比'1坐-5-基丨脲；111-關1^ (DMSO-d6) d ppm : 7.9-7.8(m ) ; 7. 5 - 7. 4(m ) ;7. 1 -6.8(m);4.6-4.5(m);2.23(s);2.16(s);1.30(s)。 N-(2,5 -二甲基苯基）-N’-{3-(2-乙基-丁醯胺基）-4,6-二氫π比l^各并[3，4-c]D比β坐-5-基}脲；lH-NMR(DMSO-d6)d p p m : 7. 1 - 6. 8 (m) ; 4. 5 (m) ; 1. 5 - 1 · 4 ( m) ; 0. 8 (m)。 N-(4-氟苄基）-N’-{3-(2-乙基-丁醯胺基）-4,6 -二氫。比口各并[3，4-c]D 比。坐-5-基}脲；1H-NMR (DMSO-d6) d ppm:7.C:\2D-C0DE\91-01\90119473.ptd Page 176 1327569 V. Description of invention (174) (m); 3.4(m); 2.24(m); 1.6-1.4(ni); 0.8(m) . 1(2,6-diethylphenyl)-"-{3-(piperidylcarboxylamido)-4,6-dihydrophonyl 17 and [3,4-〇]° ratio ° sit-5 -Based urea; 1H-NMR (DMS〇-d6) d ppm: 7.5-7. 7(m); 7.0-7.2(m); 6.l(s); 4.4-4.6(m); 2.5-2 6(m); l.0-1.l(t). N-2-oxophenyl-anthracene - {3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydroindole ratio 11 and [3,4-(:]° Ratio ° ° -5 - base urea; 111 - off 1 ^ (0 elbow 50-(16) (1?? 111: 7.8-6.8 (m); 4 · 5 (m); 4 · 0 (m); 3·8(s);l.5(d). 1^1-(1-phenyl)ethyl-^-{3-(2-naphthalen-2-yl-propionamido)-4,6 - dihydrogen 0 ratio ° [3,4-c]D ratio °-5-yl}urea; 1H-NMR (DMSO-d6) d ppm: 10.6 (s); 7.8-7.2 (m); 6.6 (m); 4.8 (m); 4.4 (m); 4.0 (m); 1.5 (d); 1.4 (d) o N-{5-phenylguanidino-4,6-dihydropyrrolo[3 , 4-c]pyrazole-3-naphthyl}-3-(2-naphthalen-2-yl)-propanamide; 1H-NMR (DMS0-d6) d ppm: 7. 8 -7.5 (m); 4.4 (m); 4.0 (m); 1.4 (d) 〇N-(2,5-dimethylphenyl)-N'-{3-(4-t-butyl-benzoinylamino) - 4,6-dihydrogen ratio 11 and [3,4-〇]51 to '1 sit-5-ylurea urea; 111- Guan 1^ (DMSO-d6) d ppm : 7.9-7.8 (m); 7. 5 - 7. 4(m); 7. 1 -6.8(m); 4.6-4.5(m); 2.23(s); 2.16(s); 1.30(s). N-(2,5 - two Methylphenyl)-N'-{3-(2-ethyl-butylammonium)-4,6-dihydroπ ratio l^[3,4-c]D is β--5- lH-NMR (DMSO-d6) dppm: 7. 1 - 6. 8 (m); 4. 5 (m); 1. 5 - 1 · 4 (m); 0. 8 (m). N-(4-fluorobenzyl)-N'-{3-(2-ethyl-butylguanidino)-4,6-dihydro. Specific ratio of [3,4-c]D. -5-yl}urea; 1H-NMR (DMSO-d6) d ppm: 7.

C:\2D-00DE\91-01\90119473.ptd 第177頁 1327569 五、發明說明（175) 3-7.l(m);4.4(m);4.2(m);l·5-1.4(m);0.8(m) 〇 N-{5-爷基石黃酿基- 4，6 -二氫D比p各并[3，4-c] 0比0坐-3_基} -4-第三丁基苯甲醯胺；111-關1?(0皿50-(16)(1??111:7.9-7-8(m);7.5-7.4(m);7.4-7.3(m);4.6-4.3(m);1.30(s)。 N-2 -氣苯基-N’-{3-(2 -萘-2 -基-丙醯胺基）-4,6 -二氫吡口各并[3，4-c]d 比唾-5-基}脲；1H-NMR (DMS0-d6) d ppm: 7.9-7.l(m);4.5(m);4.0(m);l.5(d) 〇 1^-{5-胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基} -2-(2 -萘基）-丙醯胺；1H-NMR (DMS0-d6) d ppm: 10. 6 d · s);7. 8-7. 5(m);5.8(bs);4. 3(m);4. 0(m);l. 5(d)。 N_{5_(3-曱基-丁酿基）-4，6_二氮n比略并[3，4_c] D比0坐 -3-基}-4_ 笨氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm: 8. 0 -7.4(m);4. 7-4.4(m);0.9(d)。 ^{5-(2-苯基-噻唑-4-基）乙醯基-4,6-二氫吡咯并 [3,4-c]吡唑-3-基}-4 -苯氧苯甲醯胺；1H-NMR (DMS0-d6) d p p m : 8. 1 - 7. 9 (m) ; 7 · 5 - 7. 1 (m) ; 4 · 9 - 4 · 4 (m ) ; 3. 3 ( s )。 N-{5-(2-。塞吩基-乙醯基）-4，6 -二氫各并[3,4-c] °比。坐 -3-基}-4-第三丁基苯甲醯胺；111-題1?(0肘80-(16)(1口_: ^.9-7.8(m);7.5-7.4(m);7.4-7.3(m);7.0-6.9(m);4.8-4 · 4 ( m) ; 4 0 - 3. 9 (m) ; 1 · 3 0 ( s ) 〇 ?»1-{5-(3-〇比〇定基-乙醯基）-4,6-二氫0比略并[3，4-(：]0比0坐 -3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm: 8.4-8.3(m);7.9-7.8(m);7.7-7.3(m);4.8-4.4(m);3.8-3.7(m);l_30(s)。C:\2D-00DE\91-01\90119473.ptd Page 177 1327569 V. Description of invention (175) 3-7.l(m); 4.4(m); 4.2(m); l·5-1.4 ( m);0.8(m) 〇N-{5-Yelkestone Yellow Brewing Base - 4,6-Dihydro D ratio p and [3,4-c] 0 to 0 sitting -3_yl} -4- Tributyl benzamide; 111-off 1? (0 dish 50-(16) (1?? 111: 7.9-7-8 (m); 7.5-7.4 (m); 7.4-7.3 (m); 4.6-4.3 (m); 1.30 (s). N-2 - gas phenyl-N'-{3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydropyrrole And [3,4-c]d than sal-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7.9-7.l (m); 4.5 (m); 4.0 (m); 5(d) 〇1^-{5-Aminocarbonyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-2-(2-naphthyl)-propanoid 1H-NMR (DMS0-d6) d ppm: 10. 6 d · s); 7. 8-7. 5 (m); 5.8 (bs); 4. 3 (m); 4. 0 (m) ;l. 5(d). N_{5_(3-indolyl-butyryl)-4,6-diaza n ratio slightly [3,4_c] D is 0 -3-yl}-4_ oxy Benzoylamine; 1H-NMR (DMS0-d6) d ppm: 8. 0 - 7.4 (m); 4. 7-4.4 (m); 0.9 (d). ^{5-(2-phenyl-thiazole 4-yl)ethinyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide; 1H-NMR (DMS0-d6) dppm : 8. 1 - 7. 9 (m) ; 7 · 5 - 7. 1 (m) ; 4 · 9 - 4 · 4 (m ; 3. 3 ( s ). N-{5-(2-.-Shenyl-ethenyl)-4,6-dihydro-[3,4-c] ° ratio. }-4-Telebutylbenzamide; 111-title 1? (0 elbow 80-(16) (1 port _: ^.9-7.8 (m); 7.5-7.4 (m); 7.4-7.3 (m); 7.0-6.9(m); 4.8-4 · 4 ( m) ; 4 0 - 3. 9 (m) ; 1 · 3 0 ( s ) 〇?»1-{5-(3-〇 ratio 〇定基-Ethyl)-4,6-dihydrogen 0 ratio slightly [3,4-(:]0 to 0--3-yl}-4-t-butylbenzamide; 1H-NMR (DMSO-d6) d ppm: 8.4-8.3 (m); 7.9-7.8 (m); 7.7-7.3 (m); 4.8-4.4 (m); 3.8-3.7 (m); l_30 (s).

C:\2D-CQDE\91-01\90119473.ptd 第178頁 1327569 五、發明說明（176) N-{5-苄基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基}-4 -苯氧苯曱醯胺；111-〇1^(01^0-(16)(1口口111:8.；1-7.9(n〇;7.45-7.1(in);4.5-4.3(n〇;4.6(s)。 N-{5-(2-曱基丙基）羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm: 7.9-7.8(m);7.5-7.4(ni);4.7-4.4(in);2.2-2.1(ni);2.1-2. 0(m) ; 1. 30(s) ; 0. 94(d)。 N-{5-(2-苯基-D比。坐-4-基）乙Si基- 4,6 -二氫吼11各并 [3,4-c]吡唑-3-基}-4 -第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7. 9-7. 8(m);7. 5-7. 4(m) ;4. 9-4. 5 (m);3. 94(s) ; 1 · 30(s)。 N - { 5 - ( 2 -。塞吩基-乙醯基）-4, 6 -二氫°比p各并[3, 4 - c ] 0比。坐 -3-基卜 4-苯氧苯甲醯胺；1H-NMR (DMS0-d6) d ppm:7.9 -7.4(m);4.8-4.4(m);3.9(s) 〇 N-{5-(l -萘）項醯基-4, 6 -二氫吼17各并[3,4-c] D比。坐- 3-基}-環丙基叛醯胺；1H-NMR (DMSO-d6) d ppm:8.7 (m);8.2-8.1(m);7.8-7.6(m);4.6-4.3(m);0.8-0.7(m)。 N-{5-(2-曱氧苯基）-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基}-3-(2 -萘-2 -基）-丙醯胺；1H-NMR (DMS0-d6) d ppm:10.6(s);7.8-7.0(m);4.6-4.2(m);4. 0(m);3.8(s); 1.4(d)。 1{5-(2-〇夫喃甲醯基）-4,6-二氫'1比°各并[3,4-(：]0比〇坐-3-基卜3-(2-萘-2-基）-丙醯胺；1H-NMR (DMS0-d6) d ρρπι:7· 8-6. 6(π〇;4. 9-4. 6(m);4. 0(m); 1. 5(d)。C:\2D-CQDE\91-01\90119473.ptd Page 178 1327569 V. INSTRUCTIONS (176) N-{5-Benzylsulfonyl-4,6-dihydroindole[3, 4- c]pyrazol-3-yl}-4-phenoxybenzamine; 111-〇1^(01^0-(16) (1 mouth 111:8.; 1-7.9 (n〇; 7.45- 7.1 (in); 4.5-4.3 (n〇; 4.6 (s). N-{5-(2-mercaptopropyl)carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole- 3-based}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (ni); 4.7-4.4 (in); 2.2- 2.1(ni); 2.1-2. 0(m) ; 1. 30(s) ; 0. 94(d). N-{5-(2-phenyl-D ratio. sit-4-yl) ethyl Si -4,6-dihydroindole 11-[3,4-c]pyrazol-3-yl}-4-tert-butylbenzamide; 1H-NMR (DMS0-d6) d ppm:7 9-7. 8(m); 7. 5-7. 4(m) ; 4. 9-4. 5 (m); 3. 94(s) ; 1 · 30(s). N - { 5 - ( 2 -. thiophenyl-ethenyl)-4,6-dihydrogen ratio p and [3, 4 - c ] 0 ratio. Sodium-3-yl b 4-phenoxybenzamide; 1H-NMR (DMS0-d6) d ppm: 7.9 - 7.4 (m); 4.8-4.4 (m); 3.9 (s) 〇N-{5-(l-naphthalene)-indolyl-4,6-dihydrogen吼17 each [3,4-c] D ratio. Sodium-3-yl}-cyclopropyl tremamine; 1H-NMR (DMSO-d6) d ppm: 8.7 (m); 8.2-8.1 (m) ;7.8-7.6(m); 4.6-4.3( m); 0.8-0.7 (m) N-{5-(2-indolylphenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-( 2 -Naphthalene-2-yl)-propanin; 1H-NMR (DMS0-d6) d ppm: 10.6 (s); 7.8-7.0 (m); 4.6-4.2 (m); 4. 0 (m); 3.8(s); 1.4(d). 1{5-(2-〇夫喃甲醯基)-4,6-dihydro'1°°[3,4-(:]0 is more than sitting 3-(2-naphthalen-2-yl)-propaninamine; 1H-NMR (DMS0-d6) d ρρπι:7·8-6. 6(π〇; 4. 9-4. 6( m); 4. 0 (m); 1. 5 (d).

C:\2D-00DE\91-01\90119473.ptd 第179頁 1327569 五、發明說明（177) 1^-{5-[5-(卜嗎啉基甲基）呋喃_2-羰基]-4,6-二氫咄咯并[3,4-c] °比唑-3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMS0-d6) d ppm:7. 9-7.8(m);7.5-7.4(m);5. 0-4. 7(m); 3.57(bs);2.42(bs);l.30(s)。 1^-{5-{4-[2-(1-°比咯啶基）乙氧]苯基}乙醯基-4,6-二氫吡咯并[3, 4-c]吡唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm:7. 9-7. 8(m);7. 5-7.4(m);7. 2-7. 1 (m) ；6.9-6.8(m);4.7-4.4(m);4.11(bs);3.7-3.6(m);1.77(bs )丄 30(s)。 N-{5-(l-H-苯并***-5 -羰基）-4,6 -二氫吡咯并[3,4-c] 吼唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm:8.2-7.4(m);4.7-4.6(m);1.26(s)。 N-{5-( °比°各-3-幾基）乙醯基- 4,6 -二氫各并[3,4-c] D比唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.9-7.8(m);7.5-7.4(m);7.3-7.2(m);6. 81(bs);6. 5-6.4(m);4. 9-4. 5(m);l.30(s)。 N-{5-{4-[2 -氧基-2-(1-吼咯啶基）乙氧]苯基}乙醯基 -4, 6-二氫吡咯并[3, 4-c] 0比唑-3-基}-4-苯氧苯曱醯胺； ^1H-NMR (DMSO-d6) d ppm:8. 02(m) ; 4. 66(s);4. 8-4.4(m); 1.9-1.6(in)。 N-{5-(4-曱基磺醯胺基-苯基）乙醯基-4, 6 -二氫吼咯并 [3,4-c]吡唑-3-基卜4-苯氧苯曱醯胺；1H-NMR (DMSO-d6) d ppm:8.0(m);4.8-4.4(m);2.95(s)。 1^-{5-[2-(6-氧基-1(61〇-嗒°井基}乙醯基-4,6-二氫°比咯C:\2D-00DE\91-01\90119473.ptd Page 179 1327569 V. INSTRUCTIONS (177) 1^-{5-[5-(Bumorpholinylmethyl)furan_2-carbonyl]-4 , 6-dihydroindolo[3,4-c] ° oxazol-3-yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 7. 9- 7.8 (m); 7.5-7.4 (m); 5. 0-4. 7 (m); 3.57 (bs); 2.42 (bs); l. 30 (s). 1^-{5-{4-[2-(1-°-pyridyl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 - yl-3-butyl phenyl hydrazide; 1H-NMR (DMSO-d6) d ppm: 7. 9-7. 8 (m); 7. 5-7.4 (m); 7. 2- 7.1 (m); N-{5-(lH-benzotriazol-5-carbonyl)-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-t-butylphenylhydrazine Amine; 1H-NMR (DMSO-d6) d ppm: 8.2-7.4 (m); 4.7-4.6 (m); 1.26 (s). N-{5-(° ratio ° -3-amino) ethyl fluorenyl - 4,6-dihydro-[3,4-c] D-pyrazol-3-yl}-4-t-butyl Benzoylamine; 1H-NMR (DMS0-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 7.3-7.2 (m); 6.81 (bs); 6. 5-6.4 ( m); 4. 9-4. 5(m); l.30(s). N-{5-{4-[2-Oxo-2-(1-oxaridinyl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-c] 0 Bisazo-3-yl}-4-phenoxybenzamine; ^1H-NMR (DMSO-d6) d ppm: 8.2 (m); 4. 66(s); 4. 8-4.4 (m ); 1.9-1.6 (in). N-{5-(4-mercaptosulfonylamino-phenyl)ethenyl-4,6-dihydroindolo[3,4-c]pyrazole-3-ylbu-4-phenyloxybenzene Indoleamine; 1H-NMR (DMSO-d6) d ppm: 8.0 (m); 4.8-4.4 (m); 2.95 (s). 1^-{5-[2-(6-oxy-1(61〇-嗒° well base} ethyl ketone-4,6-dihydrogen ratio)

C:\2D-CODE\91-01\90119473.ptd 第180頁 1327569 五、發明說明（178) 并[3,4-c]吡唑-3-基}-4 -苯氧苯曱醯胺；1H-NMR (D M S 0 - d 6 ) d p p m : 8. 0 - 7 · 4 (m) ; 4 · 9 7 (m ) ; 4 · 8 - 4 · 4 (m )。 N-丨5-(3 -胺基曱醯基甲氧-苯基）乙醯基-4, 6 -二氫吼咯并[3,4-c]吡唑-3-基}-4_苯氧苯甲醯胺；1H-NMR (DMS0-d6) d ppm:7.4-7.2(m);4.8-4.4(m);4.38(s)。 1{5-(4-胺基甲醯基甲氧-苯基）乙醯基-4,6-二氫《比咯并[3,4-c]。比唑-3-基}-4 -苯氧苯甲醯胺；1H-NMR (DMS0-d6) d ppm:7.44(s);7.32(s);7.44-7. 22(m);7.16 -7.19(m);4.85-4.4(m)。 N-{ 5-[4-(1-咄咯啶基）苯基]乙醯基-4, 6-二氫吼咯并 [3,4-c]咄唑-3-基}-4-苯氧苯甲醯胺；1H-NMR (DMS0-d6) d ppm:8. 01(d);7.44(dd);4. 8-.2(m);3. 56(m);3.16(m) ;1 . 9 1 ( m )。 N-{5 -胺基曱醯氧基乙醯基-4,6 -二氫0比洛并[3,4-c] σ比。坐-3-基}-4-苯氧苯甲酸胺；1H-NMR (DMS0-d6) d ppm: 7. 4-7. 2(m) ; 7. 1 (d) ;4· 8-4. 2(m)。 N-{5-{4-[2-(4-曱基哌畊-2 -基）乙氧]苯基}乙醯基 -4,6-二氫咄咯并[3,4-〇]吡唑-3-基}-4-苯氧苯曱醯胺； 1H-NMR (DMS0-d6) d ppm:8. Ο (m);4.8-4.4(m) ; 4.02(m); 3. 64(m) ; 2. 18(s)。 1^-{5-{4-[2-(1-«比咯啶基）乙氧]苯基}乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4 -苯氧苯曱醢胺；1H-NMR (DMS〇-d6) d ppm:8. Ο 2(m) ; 6.88(m ) ; 3. 65(m) ; 2.66(m); 1.71(m)。C:\2D-CODE\91-01\90119473.ptd Page 180 1327569 V. INSTRUCTIONS (178) And [3,4-c]pyrazol-3-yl}-4-phenoxybenzoquinone; 1H-NMR (DMS 0 - d 6 ) dppm : 8. 0 - 7 · 4 (m) ; 4 · 9 7 (m ) ; 4 · 8 - 4 · 4 (m ). N-丨5-(3-aminoguanidinomethoxy-phenyl)ethenyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4_benzene Oxybenzamide; 1H-NMR (DMS0-d6) d ppm: 7.4-7.2 (m); 4.8-4.4 (m); 4.38 (s). 1{5-(4-Aminomethylmercaptomethoxy-phenyl)ethinyl-4,6-dihydro"pyrolo[3,4-c]. Bisazo-3-yl}-4-phenoxybenzamide; 1H-NMR (DMS0-d6) d ppm: 7.44 (s); 7.32 (s); 7.44-7. 22(m); 7.16 -7.19 (m); 4.85-4.4 (m). N-{ 5-[4-(1-Pyryridinyl)phenyl]ethenyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-4-benzene Oxybenzamide; 1H-NMR (DMS0-d6) d ppm: 8. 01 (d); 7.44 (dd); 4. 8-.2 (m); 3. 56 (m); 3.16 (m) ;1 . 9 1 ( m ). N-{5-amino methoxy ethoxyethyl-4,6-dihydro 0-pyloro[3,4-c] σ ratio. Sodium-3-yl}-4-phenoxybenzoic acid amine; 1H-NMR (DMS0-d6) d ppm: 7. 4-7. 2(m); 7. 1 (d); 4· 8-4. 2 (m). N-{5-{4-[2-(4-mercaptopipen-2-yl)ethoxy]phenyl}ethenyl-4,6-dihydroindolo[3,4-anthracene]pyridinium Zyridin-3-yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm: 8. Ο (m); 4.8-4.4 (m); 4.02 (m); 3. 64 ( m) ; 2. 18(s). 1^-{5-{4-[2-(1-«pyrrolidyl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 -1 - phenoxybenzamine; 1H-NMR (DMS 〇-d6) d ppm: 8. Ο 2 (m); 6.88 (m); 3. 65 (m); 2.66 (m); 1.71 (m).

C:\2D-00DE\91-01 \90119473.ptd 第181頁 1327569 五、發明說明（179) N-{5-{4-[2 -氧基-2-U -吼咯啶基）乙氧]苯基}乙醯基 -4, 6 -二氫吡咯并[3,4-c]咄唑-3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMS0-d6) d ppm:7.9-7.8(in);7.5-7.4(m) ；7. 2-6. 8(m);4.8-4. 4(m);4. 66(s) ;3.7-3.4(m);1. 9-1. 7 (m);1.30(s)。 1^1-{5-(4_曱基磺醯胺基-苯基）乙醯基-4,6-二氫吼咯并 [3,4-c]吡唑-3-基}-4_第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7. 9 - 7.8(m);7. 5 - 7.4(m);7. 2 - 7. 1 ( m) ;4.8-4.4(m);3.7-3.6(m);2.94(s);1.30(s)。 N-{5-( 定-3-幾基）-4,6 -二氫 D 比 p各并[3，4-c] °比唾-3- 基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm: 8.7-8.6(m);8.0-7.7(m);7.5-7.4(m);4.8-4.6(m);1.28(s )0 N-{5-(吼。定_3 -幾基）-4，6_ 二氮°比°各弁[3，4-c] °比。坐- 3_ 基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm: 8. 8 -8.6(m);8.：l-7.8(in);7.5-7.4(m);4.8-4.5(m);1.27(s)。 N - { 5 - ( °比咬-4 -幾基）-4，6 -二氫 D比 11各并[3，4 - c ]吼 °坐-3 -基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:8· 8 •-8.7(m);7.9-7.7(m);7.6-7.4(m);4.7-4.5(m);1.27(s)。 N-{5-(2-甲基-吡啶-3 -羰基）-4,6-二氫吡咯并[3,4-〇] 咄唑-3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMS0-d6) d ppm:8.5-8.4(m);8.0-7.7(m);7.6-7.2(m);4. 7-4.4(m); 2.44(s);1·27(s)。 N-{5_(2 -硫曱基_D比咬_3 -幾基卜斗^-二氫吼洛并C:\2D-00DE\91-01 \90119473.ptd Page 181 1327569 V. INSTRUCTIONS (179) N-{5-{4-[2-Oxo-2-U-pyridinyl) ethoxylate Phenyl}ethinyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 7.9-7.8 (in); 7.5-7.4 (m); 7. 2-6. 8 (m); 4.8-4. 4 (m); 4. 66 (s); 3.7-3.4 (m) ;1. 9-1. 7 (m); 1.30 (s). 1^1-{5-(4_decylsulfonylamino-phenyl)ethenyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4_ Tert-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 7. 9 - 7.8 (m); 7. 5 - 7.4 (m); 7. 2 - 7. 1 ( m) ; -4.4 (m); 3.7-3.6 (m); 2.94 (s); 1.30 (s). N-{5-(dine-3-yl)-4,6-dihydro D ratio p and [3,4-c] ° than sparg-3-yl}-4-t-butylphenylhydrazine Amine; 1H-NMR (DMS0-d6) d ppm: 8.7-8.6 (m); 8.0-7.7 (m); 7.5-7.4 (m); 4.8-4.6 (m); 1.28 (s) 0 N-{5 - (吼. 定_3 - several groups) -4,6_ dinitrogen ° ratio ° [3,4-c] ° ratio. -3_yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 8. 8 -8.6 (m); 8.: l-7.8 (in); 7.5-7.4 (m); 4.8-4.5 (m); 1.27 (s). N - { 5 - ( ° ratio bit 4 - several groups) -4,6 - dihydro D ratio 11 and [3,4 - c ] 吼 ° sit -3 -yl}-4-t-butylbenzene Indoleamine; 1H-NMR (DMS0-d6) d ppm: 8·8 •-8.7 (m); 7.9-7.7 (m); 7.6-7.4 (m); 4.7-4.5 (m); 1.27 (s) . N-{5-(2-methyl-pyridin-3-carbonyl)-4,6-dihydropyrrolo[3,4-indole]oxazol-3-yl}-4-t-butylbenzamide Amine; 1H-NMR (DMS0-d6) d ppm: 8.5-8.4 (m); 8.0-7.7 (m); 7.6-7.2 (m); 4. 7-4.4 (m); 2.44 (s); 27(s). N-{5_(2-thiol-yl-D is more than bite_3 - a few bases

C:\2D-C0DE\91-01\90119473.ptd 第182頁 1327569 五、發明說明（180) [3,4-c]吡唑-3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMS〇-d6) d ppm:8. 6-8. 5(m) ; 7. 9 -7. 2(m) ;4. 7-4.4 (m);2.51(s);l.27(s)。 N-{5-( °比°丼-2 -数基）-4, 6 -二氫 °比°各并[3,4-c] D比。坐- 3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMS0-d6) d ppm: 9. l-9. 0(m);8. 8-8. 7(m);7. 9-7. 8(m);7. 6-7. 4(m);4. 9-4. 7(m) ; 1· 29(s)。 N_{5_(3_ 口夫喃甲酿基）_4，6 -二氮0比洛并[3，4_c]D比。坐- 3-基}-4-苯氧苯甲醯胺；1H-NMR (DMSO-d6) d ρρπη 7. 8 -7. 7(m) ; 7. 2-7. 0(m) ; 4. 9-4. 6(m)。 1^-{5-(2-0塞吩曱醯基）-4，6-二氫0比'7各并[3,4-(：]°比°坐-3-基}-4-笨氧苯曱醯胺；111-關尺（〇1^〇-(16)(1??111:8.0-7.7(m);7.4-7.0(m);5.0-4.6(m)。 N-{5-(7-曱氧-苯并°夫。南-2-叛基）-4,6 -二氫π比π各并 [3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7. 9 - 7. 8(m);7. 7 - 7. 0(m);5. 2-4. 6(m) ;4.0-3.9(m);1.31(s)。 ^|-{5-(苯并咬喃-2-羰基）-4,6-二氫°比洛并[3,4-(：]'1比唑 -3 -基}-4 -第三丁基苯甲醯胺；1H-NMR (DMSO-d6) d ppm: 7.9-7.3(m);5.2-4.7(m);l.31(s)。 N-{5-(2 -咳0南曱醯基）-4,6 -二氫吼p各并[3,4-〇]°比〇坐- 3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMSO-d6) d ppni:7.9-7.8(ni);7.5-7.4(in);7.2-7.1(in)；6.7-6.6(m);5. 0-4· 6(m) ; 1, 30(s)。C:\2D-C0DE\91-01\90119473.ptd Page 182 1327569 V. Description of the Invention (180) [3,4-c]pyrazol-3-yl}-4-t-butylbenzamide 1H-NMR (DMS〇-d6) d ppm: 8. 6-8. 5(m) ; 7. 9 -7. 2(m) ; 4. 7-4.4 (m); 2.51(s); .27(s). N-{5-(° ratio °丼-2 - number base)-4,6-dihydrogen ° ratio and [3,4-c] D ratio. Sodium 3-yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 9. l-9. 0(m); 8. 8-8. 7(m) ;7. 9-7. 8(m); 7. 6-7. 4(m); 4. 9-4. 7(m); 1· 29(s). N_{5_(3_ 口夫喃甲甲基)_4,6-Dinitrogen 0 is more than [3,4_c]D ratio. Sodium 3-yl}-4-phenoxybenzamide; 1H-NMR (DMSO-d6) d ρρπη 7. 8 -7. 7(m) ; 7. 2-7. 0(m) ; 9-4. 6(m). 1^-{5-(2-0-thenyl)-4,6-dihydro- 0 is more than '7 and [3,4-(:]° is more than -3-yl}-4- stupid Oxybenzoquinone; 111-closed ruler (〇1^〇-(16) (1??111:8.0-7.7(m); 7.4-7.0(m); 5.0-4.6(m). N-{5 -(7-oxime-benzophene. South-2-rebel)-4,6-dihydropi π-[3,4-c]pyrazol-3-yl}-4-third Butyl benzoguanamine; 1H-NMR (DMS0-d6) d ppm: 7. 9 - 7. 8 (m); 7. 7 - 7. 0 (m); 5. 2-4. 6 (m) ;4.0-3.9(m); 1.31(s).||-{5-(Benzobenzopyran-2-carbonyl)-4,6-dihydro-pyrolo[3,4-(:]'1 Benzazole-3-yl}-4-t-butylbenzamide; 1H-NMR (DMSO-d6) d ppm: 7.9-7.3 (m); 5.2-4.7 (m); l.31 (s) N-{5-(2-cough 0-anthracene)-4,6-dihydroindole p each [3,4-〇]° 〇 - - 3-yl}-4-t-butyl Benzoylamine; 1H-NMR (DMSO-d6) d ppni: 7.9-7.8 (ni); 7.5-7.4 (in); 7.2-7.1 (in); 6.7-6.6 (m); 5. 0-4. 6(m) ; 1, 30(s).

C:\2D-00DE\91-01\90119473.ptd 第183頁 1327569 五、發明說明（181) ^{5-(3-〇夫喃曱醯基）-4，6-二氫°比0各并[3,4-(：]〇比。坐-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:8.3-8.2(m);7.9-7.5(m);6.9-6.8(m);4.8-4.6(m); 1.30(s)。 \-{5-(2-咬喃甲醯基）-4,6-二氫0比11各并[3,4-(：]°比°坐-3-基}-4 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:8. 1 -7. 9(m);7_ 4-7. 0(m);5. 0-4.6(m)。 ?»1-{5-(3-0塞吩甲醯基）-4，6-二氫11比17各并[3，4-(：]〇比〇坐-3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMS0-d6) d ppm:8. 1 <|^7.8(ni);7.6-7.3(m);4.8-4.6(m);l_29(s)。 N - { 5 -(嗜$啉-2 -幾基）-4，6 -二氫°比p各并[3，4 - c ] p比口坐 -3 -基}-4 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ρρπκ 8· 2 -8.15(m);7.5-7.4(m);5.2-4.8(m)。 N-{5-(2-°塞吩基）乙酿基- 4，6 -二氫吼11 各并[3，4-c] °比〇坐 -3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm: 8.0-7.9(m);7.5-7.3(ni);7.0-6.9(ni);4.9-4.5(m);4.40(q );3.99(s);l.34(t);l.30(s)。 N-{5-( °奎琳-6_ 幾基）-4，6 -二氮 D比1^各并[3，4-c] °比 n坐-3_ •基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:9. 0 -8 · 9 5 (m ) ; 7. 1 - 6. 9 (m ) ; 4. 8 - 4. 6 (m ) o ^^-{云-”-咬喃曱醯基卜斗^-二氫吼咯并”^-以吼峻-〗-基}-4-苯氧苯曱醯胺；1H-NMR (DMSO-d6) d ρρπκ7· 5 -7.2(m);4.8-4. 5(m)。 N - { 5 - ( °比 °井-2 -羰基）-4，6 -二氫吼 D各并[3，4 - c ] »比 °坐-3 -C:\2D-00DE\91-01\90119473.ptd Page 183 1327569 V. INSTRUCTIONS (181) ^{5-(3-〇夫喃曱醯)-4,6-Dihydrogen ratio 0 each And [3,4-(:] 〇. sit-3-yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 8.3-8.2 (m); 7.9- 7.5 (m); 6.9-6.8 (m); 4.8-4.6 (m); 1.30 (s). \-{5-(2-bitamosyl)-4,6-dihydro 0 to 11 each [3,4-(:]°°°-3-yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm: 8. 1 -7. 9(m); 7_ 4-7. 0(m); 5. 0-4.6(m). ?»1-{5-(3-0 phenophenanthryl)-4,6-dihydro 11 to 17 and [3, 4-(:]〇〇 -3--3-yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 8.1 <|^7.8(ni); 7.6 -7.3 (m); 4.8-4.6 (m); l_29 (s). N - { 5 - (Iso-phenoline-2 -alkyl)-4,6-dihydrogen ratio p and [3,4 - c ] p is more than -3 -yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ρρπκ 8· 2 -8.15(m); 7.5-7.4(m); 5.2-4.8 (m) N-{5-(2-°Septyl)ethenyl- 4,6-dihydroindole 11 each [3,4-c] ° 〇-3-yl}-4- Tert-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 8.0-7.9 (m); 7.5-7.3 (ni); 7.0-6.9 (ni); 4.9-4.5 (m); 4.40 ( q ); 3.99(s); l.34(t); l.30(s). N-{5-(°奎琳-6_ 千基)-4,6-diaza D ratio 1^ each[3 , 4-c] ° is more than -3 - • yl}-4-t-butylbenzamide; 1H-NMR (DMS0-d6) d ppm: 9. 0 -8 · 9 5 (m ) ; . 1 - 6. 9 (m ) ; 4. 8 - 4. 6 (m ) o ^^-{云-"-咬咬曱醯基卜斗^-Dihydropyrrole and "^- to 吼峻- 〖-yl}-4-phenoxybenzamine; 1H-NMR (DMSO-d6) d ρρπκ7· 5 -7.2(m); 4.8-4. 5(m). N - { 5 - ( ° ratio ° Well-2 -carbonyl)-4,6-dihydroindole D each [3,4 - c ] » than ° sitting -3

C:\2D-C0DE\91-01\90119473.ptd 第184頁 1327569 五、發明說明（182) 基}-4 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:9_：l-8.7 (m);4.9-4.7(m) 〇 1^1-{5-[2-(6-氧基-1(61〇-嗒畊基}乙醯基-4,6-二氫'1比咯并[3，4_c]Ditn坐_3_基}_4-第三丁基苯曱酿胺，1H_NMR (DMS0-d6) d ppm:8. Ο - 7. 9(m);7. 5 - 7. 4(m ) ; 7. Ο - 6. 9(m) ;5.0-4.9(m);4.8-4.5(m);1.30(s) ο N-{ 5-(4-胺基甲醯基甲氧-苯基）乙醯基-4, 6-二氫吡咯并[3,4-c]°比唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm:7. 9 - 7. 8(m ) ;7. 5 - 7. 4(m ) ; 7. 2 - 7. 1(m ); 6_9-6.8(m);4.7-4.4(m);4.37(s);3.7-3.6(m);1.30(s)。 N-{ 5-胺基曱醯基乙醯基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMSO-d6) d ρρπκ 7.9-7.8(m);7.5-7.4(m);4.7-4.4(m);1.30(s)。 N-{5-{4-[2-(4-曱基哌嗜-2 -基）乙氧]苯基}乙醯基 -4,6-二氫吼咯并[3,4-(；]吡唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm:7.9-7_8(m);7.5-7.4(m) ;7.2-6.8(m);4.7-4.4(m);4.1-4.0(m);3.7-3.6(m);2.7-2.6(m);2.5-2.3(m);2.13(s);1.30(s)。 N-{5-(2-甲基磺醯胺基嚷唑-4 -碳基）-4,6 -二氫吡咯并 [3，4-c] 0比0坐_3_基}_4_第三丁基苯曱酿胺；1H-NMR (DMSO-d6) d ppm:7.9-7.8(m);7.5-7.4(m);7.ll(s) ;5.卜4. 5(m);2· 71(s);l. 30(s)。 N-{5-(苯并呋喃-2-羰基）-4,6 -二氫吡D各并[3,4-c]吡唑 -3-基}-4-苯氧苯曱醯胺；1H-NMR (DMSO-d6) d ppm:7_8C:\2D-C0DE\91-01\90119473.ptd Page 184 1327569 V. INSTRUCTIONS (182) yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm:9_: L-8.7 (m); 4.9-4.7(m) 〇1^1-{5-[2-(6-oxy-1(61〇-嗒耕基}ethinyl-4,6-dihydro] 1 咯 -[3,4_c]Ditn sit _3_基}_4-t-butylphenyl hydrazone, 1H_NMR (DMS0-d6) d ppm: 8. Ο - 7. 9(m); - 7. 4(m) ; 7. Ο - 6. 9(m) ; 5.0-4.9(m); 4.8-4.5(m); 1.30(s) ο N-{ 5-(4-aminoformamidine Methoxy-phenyl)ethinyl-4,6-dihydropyrrolo[3,4-c]°bazol-3-yl}-4-t-butylbenzamide; 1H-NMR ( DMSO-d6) d ppm: 7. 9 - 7. 8 (m ) ; 7. 5 - 7. 4 (m ) ; 7. 2 - 7. 1 (m ); 6_9-6.8 (m); 4.7-4.4 (m); 4.37 (s); 3.7-3.6 (m); 1.30 (s). N-{ 5-aminomercaptoacetamido-4,6-dihydropyrrolo[3, 4-c] Pyrazol-3-yl}-4-t-butylbenzamide; 1H-NMR (DMSO-d6) d ρρπκ 7.9-7.8 (m); 7.5-7.4 (m); 4.7-4.4 (m); 1.30(s). N-{5-{4-[2-(4-Mercaptopiperazin-2-yl)ethoxy]phenyl}ethenyl-4,6-dihydroindole[3, 4-(;]pyrazol-3-yl}-4-t-butylbenzamide; 1H-NMR (DMSO-d6) d ppm: 7.9-7_8 (m); 7.5-7.4 (m); 7.2 -6.8( m); 4.7-4.4 (m); 4.1-4.0 (m); 3.7-3.6 (m); 2.7-2.6 (m); 2.5-2.3 (m); 2.13 (s); 1.30 (s). {5-(2-Methylsulfonylcarbazol-4-carboyl)-4,6-dihydropyrrolo[3,4-c] 0 to 0 sitting_3_yl}_4_third Benzoquinone amine; 1H-NMR (DMSO-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 7.ll (s); 5. Bu 4. 5 (m); 71(s);l. 30(s). N-{5-(benzofuran-2-carbonyl)-4,6-dihydropyridinyl D[3,4-c]pyrazol-3-yl }-4-phenoxybenzamine; 1H-NMR (DMSO-d6) d ppm: 7_8

C:\2D-C0DE\91-01\90119473.ptd 第185頁 1327569 五'發明說明（183) -7. 6(m) ; 7. 3-7. 1 (m) ; 5_ 卜4. 7(m)。 N-{5-(吡啶-2 -羰基）-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基}-4-苯氧苯曱醯胺；111-關1?(0^150-(16)(1?口111:8.7-8. 6(m);8.卜7· 8(m);5. 0-4. 6(m)。 N-{5-(2-甲基-吡啶-3 -羰基）-4,6 -二氫吡咯并[3,4-c] 〇比。坐-3-基}-4 -苯氧苯曱醯胺；1H-NMR (DMSO-d6) d ppm: 8.6-8.5(m);4.7-4.3(m);2.5-2.4(s)。 N-{5-( D奎琳-4-羰基）-4, 6 -二氫D比B各并[3, 4-c]吼°坐-3-基}-4-苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:9(m); l-7(m) ;4. 8-4. 3(m)。 N-{5-[4-U -吡咯啶-2 -酮）苯甲醯基]-4, 6 -二氫咄咯并 [3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm:7.9-7.4(m);4.7-4.5(m);3. 9-3.8(m) ;2. 5-2. 4(m);2· 1-2· 0(m) ; 1. 27(s)。 N-{5-苯基乙基- 4，6 -二氫°比口各并[3，4-c] n比。坐—3-基}-4~ 第三丁基苯甲醯胺；111-關1^(0祕80-(16)(1??111:7.9-7.8(m);7.5-7.4(m);7.3-7.1(m);4.0-3.8(m);3.1-2.8(m) ;1.30(s)。 • N -正丁基-Ν’ - {3-(2 -萘-2 -基-丙醯胺基）-4, 6 -二氫吡咯并[3，4-。]吼°坐-5-基}脲；1!1-關1?(0^130-(16)(1??111:7.8 -7. 5(m);6. 2(m);4. 3(m);4. 0(m);3. 0(m);l. 5-1. 3(m);0. 8 (t)° N_異丙基_N’ _{3_(2 -蔡基-丙酿胺基）-4, 6 -二氮n比略并[3，4-c]° 比0坐-5-基}脲；1H-NMR (DMS〇-d6) d ppm:10.6C:\2D-C0DE\91-01\90119473.ptd Page 185 1327569 Five 'Inventions (183) -7. 6(m); 7. 3-7. 1 (m) ; 5_ Bu 4. 7 ( m). N-{5-(pyridine-2-carbonyl)-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide; 111-off 1 (0^150-(16) (1? mouth 111: 8.7-8. 6 (m); 8. Bu 7·8 (m); 5. 0-4. 6 (m). N-{5- (2-methyl-pyridin-3-carbonyl)-4,6-dihydropyrrolo[3,4-c] fluorene. Sodium-3-yl}-4-phenoxybenzoin; 1H-NMR (DMSO-d6) d ppm: 8.6-8.5 (m); 4.7-4.3 (m); 2.5-2.4 (s). N-{5-( D-Quinolin-4-carbonyl)-4,6-dihydrogen D is more than B and [3, 4-c] 吼 °-3-yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm: 9 (m); l-7 ( m) ;4. 8-4. 3(m). N-{5-[4-U-pyrrolidin-2-one)benzimidyl]-4,6-dihydroindole[3,4 -c]pyrazol-3-yl}-4-t-butylbenzamide; 1H-NMR (DMSO-d6) d ppm: 7.9-7.4 (m); 4.7-4.5 (m); -3.8(m); 2. 5-2. 4(m); 2· 1-2· 0(m) ; 1. 27(s). N-{5-phenylethyl-4,6-di Hydrogen ° than the mouth and [3,4-c] n ratio. Sit -3-yl}-4~ T-butylbenzamide; 111- Guan 1^ (0 secret 80-(16) (1? ?111:7.9-7.8 (m); 7.5-7.4 (m); 7.3-7.1 (m); 4.0-3.8 (m); 3.1-2.8 (m); 1.30 (s). • N-n-butyl- Ν' - {3-(2-naphthalen-2-yl-propionamido)-4,6-dihydropyrrolo[3,4-.]吼-5-yl}urea; 1!1-off 1?(0^130-(16)(1??111:7.8 -7. 5(m); 6. 2(m); 4. 3(m) ;4. 0(m);3. 0(m);l. 5-1. 3(m);0. 8 (t)° N_isopropyl_N' _{3_(2 - Caiji- Alkylamino)-4,6-diaza n ratio slightly [3,4-c]° ratio 0 sitting-5-yl}urea; 1H-NMR (DMS〇-d6) d ppm: 10.6

C:\2D-00DE\91-01\90119473.ptd 第186頁 1327569 五、發明說明（184) (s);7.8-7. 5(m);5.9(m);4.3(m);4.0(m);3.8(m);l.5(d); 1.0(d)。 N-{5-乙基胺基叛基_4,6_二氫0比p各并[3，4-c] 0比〇坐- 3-基}-2-萘基丙醯胺；1H-NMR (DMS0-d6) d ppm:7.8-7.5 (m);6. 2(m);4·3(m);4.0(m);3.l(m);l. 5(d);l.0(t)。 1{5-乙氧羰基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基卜3-(2-萘-2-基）-丙醯胺；1H-NMR (DMSO'd6) d ppm:7.8-7. 5(m);4·4(m);4.0(m);l.5(d);l.2-1.0(m) 〇 1{5-(3-甲基丁醯基）-4,6-二氫咄咯并[3,4-〇]咄唑-3-基卜3-(2-萘-2-基）-丙醢胺；1H-NMR (DMSO-d6) d ppm: 10. 6(s);7. 8-7. 5(m);4. 6-4.4(m);4. 0(m);2. 2-2. 0(m );1.5(d);0.9(m)。 1^-{5-胺基羰基曱基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-3-(2-萘-2-基）-丙醯胺；1H-NMR (DMS0-d6) d ppm:7.8-7. 5(m);7.2(bs);7.0(bs);4. 0(m);3.8(m);3.2(s );1·4(d)。 N-{5-( n比0各-3-基幾基）-4，6_二氫n比B各并[3，4-c] u比吐 -3_基}-3-(2-萘-2-基）-丙醯胺；1H-NMR (DMSO-d6) d ppm:7. 8-6. 5(m);4. 8-4. 5(m);4. 0(m); 1. 5(d)。 N-{5_乙氧幾基_4，6 -二氫n比σ各并[3，4-c] 0比11 坐-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.9-7.8 (m);7.5-7.4(m);4.5-4.4(m);4.09(q);1.30(s);1.22(t) ο N— {5—異戌基_4, 6-二氫0比口各并[3，4_c] 0比口坐一3 —基}一4-第C:\2D-00DE\91-01\90119473.ptd Page 186 1327569 V. Description of invention (184) (s); 7.8-7. 5(m); 5.9(m); 4.3(m); 4.0( m); 3.8 (m); l. 5 (d); 1.0 (d). N-{5-ethylamino thiol-4,6-dihydrogen 0 to p each [3,4-c] 0 is more than sino-3-yl}-2-naphthylpropionamine; 1H- NMR (DMS0-d6) d ppm: 7.8-7.5 (m); 6.2 (m); 4·3 (m); 4.0 (m); 3.l (m); l. 5 (d); .0(t). 1{5-ethoxycarbonyl-4,6-dihydropyrrolo[3,4-indenepyrazol-3-ylbu-3-(2-naphthalen-2-yl)-propanamide; 1H-NMR ( DMSO'd6) d ppm: 7.8-7. 5(m); 4·4(m); 4.0(m); l.5(d); l.2-1.0(m) 〇1{5-(3 -methylbutylidene)-4,6-dihydroindolo[3,4-indolyl-3-oxazol-3-(2-naphthalen-2-yl)-propanamide; 1H-NMR (DMSO -d6) d ppm: 10. 6(s); 7. 8-7. 5(m); 4. 6-4.4(m); 4. 0(m); 2. 2-2. 0(m ) ;1.5(d); 0.9(m). 1^-{5-Aminocarbonylmercapto-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-(2-naphthalen-2-yl)-propanamide ;1H-NMR (DMS0-d6) d ppm: 7.8-7. 5 (m); 7.2 (bs); 7.0 (bs); 4. 0 (m); 3.8 (m); 3.2 (s); 4(d). N-{5-(n vs. 0-3-yl-yl)-4,6-dihydron is more than B and [3,4-c]u is more than -3_yl}-3-(2- Naphthyl-2-yl)-propanamide; 1H-NMR (DMSO-d6) d ppm: 7. 8-6. 5(m); 4. 8-4. 5(m); 4. 0(m) ; 1. 5(d). N-{5_ethoxyxyl_4,6-dihydron ratio σ and [3,4-c] 0 to 11 -3--3-yl}-4-t-butylbenzamide; 1H -NMR (DMS0-d6) d ppm: 7.9-7.8 (m); 7.5-7.4 (m); 4.5-4.4 (m); 4.09 (q); 1.30 (s); 1.22 (t) ο N - {5 -isoindolyl _4, 6-dihydrogen 0 than each mouth [3,4_c] 0 than a mouth sitting a 3 - base} a 4-

C:\2D-OODE\91-01\90119473.ptd 第187頁 1327569 五、發明說明（185) 三丁基苯甲醯胺；1H-NMR (DMS0_d6) d ppm: 7. 9-7. 8(m); 7. 5-7.4(m)；4.0-3.8(m);l.7-1. 6(m);l.5-1.4(m);l.30(s );0.90(d)。 N- 丁基-Ν’ - {3-(4-第三丁基-苯甲醯胺基）-4，6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲；1H-NMR (DMSO-d6) d ρρπκ 7.9-7.8(m);7.5-7.4(m);4.4-4.3(m);3.04(q);1.5-1.4(m );1.30(s) ; 0. 87(t)。 N - { 5 - ( °5丨p朵-2 -基）敷基-4，6 -二氫吼p各并[3，4 - c ]哺峻 -3_基}-4-第三丁基苯曱醯胺；1H-NMR (DMSO-d6) d ppm: % 9-7.0(m);5·1-4.7(m);l.31(s)。 1^-{5-(1-甲基-〇5丨°朵-3-基）乙醯基-4，6-二氫〇比略并 [3,4-c]吡唑-3-基}-4-第三丁基苯甲醯胺；1H-NMR (DMSO-d6) d ppm:7.6-7.0(m);3.77(s);3.8-3.7(m) ;1. 30(s卜 1^-{5-[4-(1-味°坐基曱基）苯甲醢基]-4，6-二氫〇比洛并 [3, 4-c]吡唑-3 -基}-4 -苯氧苯甲醯胺；1H-NMR (DMSO-d6) d p p m : 8. 1 - 7. 8 6 (m ) ; 7. 5 - 6. 9 5 (m ) ; 5. 2 (m ) ; 4 · 7 - 4. 4 (m)。 N-{ 5-[4-(卜咪唑基甲基）苯曱醯基]-4, 6 -二氫咄咯并 _3,4-c]咄唑-3-基}-4-苯氧苯曱醯胺；1H-NMR (DMSO-d6) d ppm:7.9-7.1(m);5.2(s);4.7-4.5(in)。 1^-{5-[4-(1-咣略啶-2-酮）苯甲醯基]-4,6-二氫吡咯并 [3,4-c]吡唑-3-基卜4-苯氧苯甲醯胺；1H-NMR (DMSO-d6) d ppm:8.1-7. 6(m);7. 5-6.95(m);4.7-4. 55(m);3.85(m); 2.45(m);2.1(m) oC:\2D-OODE\91-01\90119473.ptd Page 187 1327569 V. INSTRUCTIONS (185) Tributylbenzamide; 1H-NMR (DMS0_d6) d ppm: 7. 9-7. 8( m); 7. 5-7.4(m); 4.0-3.8(m); l.7-1. 6(m); l.5-1.4(m); l.30(s); 0.90(d) . N-butyl-Ν' - {3-(4-t-butyl-benzylamino)-4,6-dihydroindolo[3,4-c]pyrazole-5-yl}urea ;1H-NMR (DMSO-d6) d ρρπκ 7.9-7.8 (m); 7.5-7.4 (m); 4.4-4.3 (m); 3.04 (q); 1.5-1.4 (m); 1.30 (s); 87(t). N - { 5 - ( ° 5 丨 p - 2 -yl)-based -4,6-dihydroindole p and [3,4 - c ]-threating -3 -yl}-4-t-butyl Benzoylamine; 1H-NMR (DMSO-d6) d ppm: % 9-7.0 (m); 5·1-4.7 (m); l.31 (s). 1^-{5-(1-methyl-〇5丨°-3-yl)ethinyl-4,6-dihydroindole than [3,4-c]pyrazol-3-yl} -4-t-butylbenzamide; 1H-NMR (DMSO-d6) d ppm: 7.6-7.0 (m); 3.77 (s); 3.8-3.7 (m); 1. 30 (s) -{5-[4-(1-iso-ytyl) benzylidene]-4,6-dihydroindolebi[3,4-c]pyrazole-3-yl}-4 - Phenoxybenzamide; 1H-NMR (DMSO-d6) dppm : 8. 1 - 7. 8 6 (m ) ; 7. 5 - 6. 9 5 (m ) ; 5. 2 (m ) ; 4 · 7 - 4. 4 (m) N-{ 5-[4-(4-imidazolylmethyl)phenylindolyl]-4,6-dihydroindolo[3,4-c]carbazole-3 -yl}-4-phenoxybenzamine; 1H-NMR (DMSO-d6) d ppm: 7.9-7.1 (m); 5.2 (s); 4.7-4.5 (in). 1^-{5-[ 4-(1-p-acridine-2-one)benzylidene]-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl b-4-phenoxybenzamide; 1H-NMR (DMSO-d6) d ppm: 8.1-7. 6(m); 7. 5-6.95(m); 4.7-4. 55(m); 3.85(m); 2.45(m); 2.1( m) o

C:\2D-C0DE\91-01\90119473.ptd 第 188 頁 1327569 五、發明說明（186) N-{ 5-(2-嗎啉基曱基-5-呋喃曱醯基）-4, 6-二氫吡咯并 [3,4-c]吡唑-3-基}-4 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.4-7.0(m);4.9-4.6(m);2.6-2.4(m) 〇 1^-{5-(5-乙醯胺基_2-呋喃曱醯基）-4,6-二氫°比咯并[3, 4-c]吡唑-3-基}-3-(2 -萘-2 -基）-丙醯胺；1H-NMR (DMS0-d6) d ppm:7. 8-7. 5(m);7. 1 -6. 3(m) ; 4. 8-4. 6(m); 4. 0(m) ; 2. 0(s) ; 1· 5(d)。 N，N-二甲基-N’-{3-(2 -萘-2 -基-丙醯胺基）-4,6 -二氫吡口各并[3，4-(：]°比°坐-5-基}脲；111-〇1^(0^180-(16)(1?口111: 7·8-7.5(m);4.4(m);4. 0(m);2·8(s);l.5(d)。 1{5-(哌畊-1-基）胺基曱醯基-4,6-二氫咣咯并[3,4-(：] 吡唑-3-基}-3-(2 -萘-2 -基）-丙醯胺；1H-NMR (DMS0-d6) d ppm:7.8-7.5(m);4.4(m);4.0(m);3.1(m);1.5(m) 〇 ^^-{5-(4-甲基-派°丼-1-基）乙醯基-4,6-二氫〇比〇各并 [3,4-〇]吡唑-3-基}-3-(2-萘-2-基）-丙醯胺；111-關1^ (DMS〇-d6) d pm :7. 8 - 7. 5(m);4.7 - 4.4(m);4. Ο (m);3. 1(m) ;2.6-2.2(m); l,5(m)。 N — {5-( 0底口定_1 一基）乙醯基-4, 6 -二氫〇比口各并[3，4-c] 〇比〇坐 -3-基}-3-(2 -萘-2 -基）-丙醯胺；1H-NMR (DMSO-d6) d ppm:7. 8-7. 5(m);4. 7-4.4(m);4. 0(m);3. l(m);2. 4(m);l. 4 (m) o N-{5-(0比11各咬-1-基羰基）甲基-4,6-二氫吡°各并[3,4-(：] 吡唑-3-基}-3-(2-萘-2-基）-丙醯胺；1H-NMR (DMSO-d6) d ppm:7. 8-7. 5(m);4. 0(m);3. 8(m) ;3. 5(s);3.4-3. 3(m);C:\2D-C0DE\91-01\90119473.ptd Page 188 1327569 V. INSTRUCTIONS (186) N-{ 5-(2-morpholinylfluorenyl-5-furanyl)-4, 6 -dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm: 7.4-7.0 (m); 4.9-4.6 (m); 2.6-2.4(m) 〇1^-{5-(5-acetamido-2-furanyl)-4,6-dihydrogen ratio [3, 4-c] Pyrazol-3-yl}-3-(2-naphthalen-2-yl)-propanamide; 1H-NMR (DMS0-d6) d ppm: 7. 8-7. 5(m); 7. 1 - 6. 3(m) ; 4. 8-4. 6(m); 4. 0(m) ; 2. 0(s) ; 1· 5(d). N,N-Dimethyl-N'-{3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydropyrryl each [3,4-(:]° ratio ° Sodium-5-urea; 111-〇1^(0^180-(16)(1? mouth 111: 7·8-7.5(m); 4.4(m); 4. 0(m); 2· 8(s);l.5(d). 1{5-(Peptidin-1-yl)aminomercapto-4,6-dihydroindolo[3,4-(:]pyrazole- 3-yl}-3-(2-naphthalen-2-yl)-propanamide; 1H-NMR (DMS0-d6) d ppm: 7.8-7.5 (m); 4.4 (m); 4.0 (m); (m); 1.5(m) 〇^^-{5-(4-methyl-pyrano-1-yl)ethinyl-4,6-dihydroindole 〇[3,4-〇 Pyrazol-3-yl}-3-(2-naphthalen-2-yl)-propanamine; 111- Guan 1^ (DMS〇-d6) d pm : 7. 8 - 7. 5(m); 4.7 - 4.4(m); 4. Ο (m); 3. 1(m); 2.6-2.2(m); l,5(m). N — {5-( 0 底定定_1一基) Acetyl-4,6-dihydroindole is more than [3,4-c] oxime 〇-3-yl}-3-(2-naphthalen-2-yl)-propanamide; 1H- 5(m);3. l. 4 (m) o N-{5-(0 to 11 each bit-1-ylcarbonyl)methyl-4,6-dihydropyridinium each [3,4-(:] pyrazole-3- </ RTI> </ RTI> <RTIgt; 8(m) ; 3. 5(s); 3.4-3. 3(m);

C:\2D-CODE\91-01\90119473.ptd 第189頁 1327569 五、發明說明（187) 1.8(m); 1.4(d)。 N-{5-乙酿基-4，6 -二氫吼17各并[3，4-c] 13比0坐-3-基}-(4_ 0比洛咬-1-基）苯基乙醯胺；1H-NMR (DMS0-d6) d ppm: 7.1-6.5(m);4.6-4.3(m);3.4(s);3.2(m);2.0(s);1.9(m) ο N_{5_乙酿基_4，6 -二氫0比略并[3，4-c] 0比0坐-3_基}_2_ ((4 -吡咯啶-卜基）苯基）丙醯胺；1H-NMR (DMS0-d6) d ppm:7. 1-6. 5(m);4. 6-4.3(m);3. 7(m);3. 2(m);2. 0(s);l. 9 (m);1.3(m) o _ N_{5_乙酿基_4,6_二氮D比p各并[3，4-c] D比0坐-3 -基}- (4-(2 -氧基-吡咯啶-1-基）苯基）乙醯胺；1H-NMR (DMS〇-d6) d ppm:7. 1 -6. 5(m);4. 6 -4.3(m);3. 8 (m); 3. 4(s);2_ 5(m);2. l(m);2_ 0(s)。 N-{5-乙醯基- 4,6 -二氫°比口各并[3，4-c] p比0坐-3-基}-2-(4-(2 -氧基-吡咯啶-1-基）苯基）丙醯胺；1H-NMR (DMS0-d6) d ppm:7. 1 - 6.5(m);. 4. 6-4. 3(m ) ;3. 8 (m ); 2. 4 ( m) ; 2. 0 ( s ) ; 1. 9 ( m) ; 1. 4 (m)。 N-2-曱氧苯基-Ν’ -{2-[4-(2 -氧基-咄咯啶-1-基）苯基]-丙酿胺基_4，6_二氮吼17各并[3，4_c]n比。坐-5-基}脈；1H-NMR (DMS〇-d6) d ppm:7. 6-7.3(m);7. 0 - 6. 8(m);4. 5 ( m ); 3.8(m);2.4(m);2.0(m);1.4(d)。 1^-2,4-二氟苯基-1^’-{2-[4-(2-氧基-吡咯啶-1-基）苯基]-丙醯胺基-4, 6 -二氫0比p各并[3，4-c]"比0坐-5-基}脲； 1H-NMR (DMS0-d6) d ppm:7. 6-7. 0(m);4. 5(m);3.8(m);C:\2D-CODE\91-01\90119473.ptd Page 189 1327569 V. INSTRUCTIONS (187) 1.8(m); 1.4(d). N-{5-ethyl-branched-4,6-dihydroindole 17 and [3,4-c] 13 to 0--3-yl}-(4_0 pirate-1-yl)phenyl Indoleamine; 1H-NMR (DMS0-d6) d ppm: 7.1-6.5 (m); 4.6-4.3 (m); 3.4 (s); 3.2 (m); 2.0 (s); 1.9 (m) ο N_{ 5_乙丁基_4,6-Dihydrogen 0 ratio slightly [3,4-c] 0 to 0 sitting -3_yl}_2_ ((4-pyrrolidinyl)phenyl)propanamine; 1H-NMR (DMS0-d6) d ppm: 7. 1-6. 5(m); 4. 6-4.3(m); 3. 7(m); 3. 2(m); 2. 0(s ); l. 9 (m); 1.3 (m) o _ N_{5_ ethyl ketone _4,6_ dinitrogen D ratio p and [3,4-c] D ratio 0 sitting -3 -yl} - (4-(2-oxy-pyrrolidin-1-yl)phenyl)acetamide; 1H-NMR (DMS〇-d6) d ppm: 7. 1 -6. 5(m); 4. 6 -4.3 (m); 3. 8 (m); 3. 4 (s); 2_ 5 (m); 2. l (m); 2_ 0 (s). N-{5-ethenyl- 4,6-dihydro-° ratio of [3,4-c] p to 0--3-yl}-2-(4-(2-oxy-pyrrolidine) -1-yl)phenyl)propanamine; 1H-NMR (DMS0-d6) d ppm: 7. 1 - 6.5 (m); 4. 4. 4-4. 3 (m ) ; 3. 8 (m ) ; 2. 4 ( m) ; 2. 0 ( s ) ; 1. 9 ( m) ; 1. 4 (m). N-2-nonyloxyphenyl-indole-{2-[4-(2-oxy-indolyl-1-yl)phenyl]-propenylamino-4,6-diazepine 17 And [3,4_c]n ratio. Sitting on a 5-kilo} pulse; 1H-NMR (DMS〇-d6) d ppm: 7. 6-7.3(m); 7. 0 - 6. 8(m); 4. 5 ( m ); 3.8 (m ); 2.4 (m); 2.0 (m); 1.4 (d). 1^-2,4-difluorophenyl-1^'-{2-[4-(2-oxy-pyrrolidin-1-yl)phenyl]-propanylamino-4,6-dihydro 0(p) and [3,4-c]" ratio 0 to 5-base urea; 1H-NMR (DMS0-d6) d ppm: 7. 6-7. 0(m); m); 3.8(m);

C:\2D-OODE\91 -01 \90119473.ptd 第 190 頁 1327569 五、發明說明（188) 2.4(m);2.0(m);1.4(d)。 N-U -苯基）乙基-N’-{2-[4-(2 -氧基-η比咯啶-1-基）苯基]-丙醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲； 1H-NMR (DMS0-d6) d ppm:7. 6-7. 2(m) ; 4.8(m);4.4(m); 3. 8 ( m ) ; 2. 4 (m) ; 2 _ 0 (m) ; 1. 4 (m)。 N-2-甲氧苯基-Ν’ - {2-(4 -吡咯啶-1-基-苯基）-丙醯胺基 _4，6_ 二氮 π比 11 各弁[3，4-c]°ite坐_5_基}脈；1H-NMR (DMS0-d6) d ppm:7. 2 - 6. 5(m);4. 5(m) ; 3.8(s ) ;3. 7(m); 3.2(m);1.9(m);1.3(d)。 N-2,4 -二氟苯基-Ν’ - (2-(4-11比咯啶-1-基-苯基）-丙醯胺基-4,6-二氫吡咯并[3,4-(：]°比唑-5-基}脲；111-01^ (DMS0-d6) d ppm:7. 5-6. 4(m);4. 5(m) ; 3. 7(m) ; 3. 2(m); 1· 9(m);1.3(d)。 N-(卜苯基）乙基-Ν’ - {2-(4 -吼咯啶-卜基-苯基）-丙醯胺基-4，6_ 二氣吼11 各并[3，4-c] °比°坐-5-基}脈；1H-NMR (DMS〇-d6) d ppm:7. 4-6.4(m);4. 8(m);4.4(m) ;3. 7(m); 3 . 2 (m ) ; 1. 9 ( m ) ; 1. 4 ( d ) ; 1. 3 ( d )。 N_{5 -苯基續酿基-4，6_二氮°比p各并[3，4-c] ntb D坐-3_ 基}-2-(4 -吡咯啶-卜基-苯基）丙醯胺；1H-NMR (DMS0-d6) d ppm:7.8-6.4(m);4.4(m);3. 6(m);3.2(m);l.9(m); 1.3(d)。 N-2-甲氧苯基-Ν’ - { [4-(2 -氧基…比咯啶-卜基）-苯基]-乙醯胺基-4,6-二氫咄咯并[3,4-〇]咄唑-5-基}脲；111-題尺 (DMS0-d6) d ppm : 7. 6-6. 8(m) ; 4. 5(m) ;3.8(m);3. 6(s);C:\2D-OODE\91 -01 \90119473.ptd Page 190 1327569 V. INSTRUCTIONS (188) 2.4(m); 2.0(m); 1.4(d). NU-phenyl)ethyl-N'-{2-[4-(2-oxy-n-pyrrolidin-1-yl)phenyl]-propionylamino-4,6-dihydroindole [3,4-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7. 6-7. 2 (m); 4.8 (m); 4.4 (m); 8 ( m ) ; 2. 4 (m) ; 2 _ 0 (m) ; 1. 4 (m). N-2-methoxyphenyl-Ν' - {2-(4-pyrrolidin-1-yl-phenyl)-propaninamine _4,6_ dinitrogen π ratio 11 弁[3,4-c ]°ite sit _5_基} vein; 1H-NMR (DMS0-d6) d ppm: 7. 2 - 6. 5(m); 4. 5(m); 3.8(s); 3. 7(m ); 3.2 (m); 1.9 (m); 1.3 (d). N-2,4-difluorophenyl-indole-(2-(4-11-pyridin-1-yl-phenyl)-propionylamino-4,6-dihydropyrrolo[3,4 -(:]°Bizozol-5-yl}urea; 111-01^ (DMS0-d6) d ppm: 7. 5-6. 4(m); 4. 5(m) ; 3. 7(m) ; 3. 2(m); 1· 9(m); 1.3(d). N-(Phenyl)ethyl-Ν' - {2-(4-oxopentidine-buyl-phenyl)- Propylamine-4,6_dione 11 each [3,4-c] ° ratio -5-based} pulse; 1H-NMR (DMS〇-d6) d ppm: 7. 4-6.4 ( m); 4. 8 (m); 4.4 (m); 3. 7 (m); 3 . 2 (m ) ; 1. 9 ( m ) ; 1. 4 ( d ) ; 1. 3 ( d ). N_{5-phenyl-ternyl-4,6-diazepine ratio p and [3,4-c] ntb D sit-3_yl}-2-(4-pyrrolidine-buyl-phenyl) Propylamine; 1H-NMR (DMS0-d6) d ppm: 7.8-6.4 (m); 4.4 (m); 3. 6 (m); 3.2 (m); l.9 (m); 1.3 (d) N-2-methoxyphenyl-Ν' - { [4-(2-oxy...byrrolidinyl)-phenyl]-acetamido-4,6-dihydroindole[ 3,4-〇]carbazol-5-yl}urea; 111-foot ruler (DMS0-d6) d ppm : 7. 6-6. 8(m) ; 4. 5(m) ;3.8(m); 3. 6(s);

C:\2D-CODE\91-01\90119473.ptd 第191頁 1327569 五、發明說明（189) 2.5(m);2.0(m) 〇 N-2-氯苯基-Ν’ - {[4-(2 -氧基_。比p各咬-1_基）-苯基]_乙醯胺基-4，6-二氫°比11各并[3,4-(：]11比°坐-5-基}脲；1}1-關1^ (DMS〇-d6) d ppm:7.8-7. 1(m) ;4. 5(m);3.8(m);3. 6 (s); 2.5(m);2.0(m)。 N-(l -苯基）乙基_N’ _{[4_(2_氧基一 0比口各口定-1-基）-苯基]-乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲； 1H-NMR (DMS0-d6) d ppm:7. 6-7. 2(m);6. 6(m) ; 4. 8 (m); 4.4(m);3.8(m);3.7(s);2.5(m);2. 0(m);1.4(d) o N -正丁基-N’-{[4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基-4,6 -二氫D比n各并[3,4-c]d比。坐-5-基}脲；1H-NMR (DMS0-d6) d ppm:7. 6 - 7. 3(m) ; 6. 2(m);4.3(m);3. 8 (m); 3. 7(s);3. 0(m);2. 5(m);2· 0(πι);1· 4(m);l. 2(m);0. 8(t)。 N-{5 -苯基續醯基-4, 6 -二氫D比D各并[3, 4-c] °比°坐-3-基}-4-(2 -氧基-吡咯啶-卜基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm:7. 8 - 7. 2(m) ; 4. 4(m);3. 8(m ) ;3. 6 ( s ); 2.5(m);2.0(m)。 N_正丁基-Ν’ _{2-[4-(2_氧基-D比洛°定-1-基）-苯基]-丙 •醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm:7. 6 - 7.3(m) ; 6. 2(m);4. 3(m ) ; 3. 8 ( m); 3.0(m);2.4(m);2.0(m);l.4-1.2(m);0.9(t)。 N-{5 -苯基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-2-[4-(2 -氧基-吡咯啶-1-基）-苯基]-丙醯胺；1H-NMR (DMS0-d6) d ppm:7.8-7.3(m);4.4(m);3.8(m)；2.5(m)；C:\2D-CODE\91-01\90119473.ptd Page 191 1327569 V. Description of invention (189) 2.5(m); 2.0(m) 〇N-2-chlorophenyl-Ν' - {[4- (2 -oxy-.p. each bite -1_yl)-phenyl]-acetamido-4,6-dihydrogen ratio 11 and [3,4-(:]11 than ° sitting- 5-based}urea; 1}1-off 1^ (DMS〇-d6) d ppm: 7.8-7. 1(m); 4. 5(m); 3.8(m); 3. 6 (s); 2.5(m); 2.0(m). N-(l-phenyl)ethyl_N' _{[4_(2_oxy-0-specific -1-yl)-phenyl]-B ( -4 -4 4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7. 6-7. 2(m); 6. 6(m) ; 4. 8 (m); 4.4(m); 3.8(m); 3.7(s); 2.5(m); 2. 0(m); 1.4(d) o N-n-butyl -N'-{[4-(2-oxy-pyrrolidin-1-yl)-phenyl]-acetamido-4,6-dihydro D ratio n[3,4-c] d ratio. sit-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7.6 - 7. 3 (m); 6. 2 (m); 4.3 (m); 3. 8 (m ); 3. 7(s); 3. 0(m); 2. 5(m); 2· 0(πι);1· 4(m); l. 2(m); 0. 8(t) N-{5-phenyl-indolyl-4,6-dihydrogen D ratio D and [3, 4-c] ° ratio of sitting-3-yl}-4-(2-oxy-pyrrolidine) - phenyl-acetamide; 1H-NMR (DMS0-d6) d ppm: 7. 8 - 7. 2 (m); 4. 4 (m); 3. 8 (m); 6 ( s ); 2.5(m); 2.0(m). N_n-butyl-Ν' _{2-[4-(2-oxy-D-Bylo-l-yl)-phenyl]-醯•醯Amino-4,6-dihydroindolo[3,4-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7. 6 - 7.3(m) ; 2. 2(m); 4. 3(m); 3. 8 ( m); 3.0(m); 2.4(m); 2.0(m); l.4-1.2(m); 0.9(t) N-{5-phenylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-[4-(2-oxy-pyrrolidine-1 -yl)-phenyl]-propanamide; 1H-NMR (DMS0-d6) d ppm: 7.8-7.3 (m); 4.4 (m); 3.8 (m); 2.5 (m);

C:\2D-00DE\91-01\90119473.ptd 第192頁 1327569 五、發明說明（190) 2. 0(m) ; 1. 3(d)。 N-{5-胺基羰基-4, 6-二氫吼咯并[3, 4-c]吡唑-3-基} -4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm:7.6-7.2(m);5.8(s);4.3(m);3.8(m); 3.6(s);2.5(m);2.0(m)。 N -正丁基-Ν’ - {2-(4 -吡咯啶-1-基-苯基）-丙醯胺基 -4,6 -二氛吼11各并[3,4-(：]°比°坐-5-基}脲；1H-NMR (DMSO-d6) d ppm:7. 1 -6. 5(m) ;6. 2(m) ; 4. 3(m) ;3.7(m); 3.2(m);3.0(m);1.9(m);1.4-1.2(m);0.8(t)。 N-{5 -胺基M基-4，6 -二氫D比0各并[3，4-c] D比唾-基卜2-(4 -吡咯啶-1-基）-苯基-丙醯胺；1H-NMR (DMSO-d6) d ppm :7. 1 -6. 5(m);5. 8(bs);4. 3(m) ;3. 7 (m);3.2(m);1.9(m);1.3(d)。 N-2-甲氧苯基-Ν’ -{ (4 -吡咯啶-1 -基-苯基）-乙醯胺基 -4，6-二氫11比17各并[3，4-(：]吼°坐-5-基}脲；111-麗尺 (DMS〇-d6) d ppm:10. 5(s);7.8-6. 5(m) ; 4. 5(m);3. 8(s) ;3.5(s);3.2(m);1.9(m)。 N-2 -氣苯基-Ν’ -{ (4 -吡咯啶-1-基-苯基）-乙醯胺基 -4，6 -二氮 π比 p各弁[3，4_c] p比 p坐_5_ 基}脈；1H-NMR (DMS〇-d6) d ppm:10. 5(s);7.8-6. 5(m) ;4. 5(m);3. 4(s) ;3.2(m);1.9(m)。 N-U -苯基）乙基-Ν’ - {(4 -°比咯啶-1-基-苯基）-乙醯胺基 _4，6_ 二氮 B比 ρ各并[3，4_c]D 比 °坐_5_基}脈；1H-NMR (DMSO-d6) d ppm:10.4(s);7.3-6. 4(m);4.8(m);4.4(s)C:\2D-00DE\91-01\90119473.ptd Page 192 1327569 V. Description of invention (190) 2. 0(m) ; 1. 3(d). N-{5-Aminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-(2-oxy-pyrrolidin-1-yl)-benzene --acetamide; 1H-NMR (DMS0-d6) d ppm: 7.6-7.2 (m); 5.8 (s); 4.3 (m); 3.8 (m); 3.6 (s); 2.5 (m); (m). N-n-butyl-indole-{2-(4-pyrrolidin-1-yl-phenyl)-propanylamino-4,6-di-indolyl 11 each [3,4-(:]° ???(5); 3.2(m); 3.0(m); 1.9(m); 1.4-1.2(m); 0.8(t). N-{5-amino M-group-4,6-dihydrogen D is 0 each [ 3,4-c] D is more than salivation-yl-2-(4-pyrrolidin-1-yl)-phenyl-propanamide; 1H-NMR (DMSO-d6) d ppm : 7. 1 -6. 5 (m); 5.8 (bs); 4. 3 (m); 3.7 (m); 3.2 (m); 1.9 (m); 1.3 (d). N-2-methoxyphenyl-fluorene '-{(4-Pyrrolidin-1-yl-phenyl)-acetamido-4,6-dihydro-11 to 17 and [3,4-(:]吼°-5-yl}urea ; 111-Li (DMS〇-d6) d ppm: 10. 5 (s); 7.8-6. 5 (m); 4. 5 (m); 3. 8 (s); 3.5 (s); 3.2 (m); 1.9 (m). N-2 - gas phenyl-Ν'-{(4-pyrrolidin-1-yl-phenyl)-acetamido-4,6-diaza π ratio p弁[3,4_c] p is sitting on the _5_ base} pulse; 1H-NMR (DMS〇-d6) d ppm:10. 5(s);7.8-6. 5(m) ;4. 5(m) ;3. 4(s); 3.2(m); 1.9(m). NU-phenyl)ethyl-Ν' - {(4-°pyrrolidin-1-yl-phenyl)-acetamidamine _4,6_ dinitrogen B ratio ρ and [3,4_c]D ratio ° sitting _5_ base} pulse; 1H-NM R (DMSO-d6) d ppm: 10.4 (s); 7.3-6. 4 (m); 4.8 (m); 4.4 (s)

C:\2D-C0DE\91-01\90119473.ptd 第193頁 1327569 五、發明說明（191) ;3. 5 ( s ) ; 3. 2 (m ) ; 1. 9 (m) ; 1 · 4 ( d)。 N -正丁基-Ν’ - {(4 -咄咯啶-1-基-苯基）-乙醯胺基-4, 6-二氫°比π各并[3，4-c]D比°坐-5-基}脲；lH-NMR(DMSO-d6)d ppm:10.4(s);7.1-6.5(m);6.2(t);4.3(m);3.4(s);3.2(m) ;3. 0(m) ;1· 9(m);1.4-1_ 2(m) ;0. 8(t)。 N-{5 -苯基績醢基-4，6 -二氫n比洛并[3, 4-c] 坐-3- 基}-(4-吡咯啶-卜基-苯基）-乙醯胺；1H-NMR (DMS0-d6) d ppm:7.8-7.6(m);7.0-6.4(m);4.4(m);3.3(s);3.2(m) ;1. 9 (m )。 N-乙基-Ν’ - {[4-(2 -氧基-D比B各咬_1_基）_苯基]_乙酿胺基-4,6 -二氫 °比 p各并[3，4-〇:]°比。坐-5-基}脲；1H-NMR (DMS0-d6) d ppm:7. 9 - 7. 3(m ) ;6. 2(m);4. 5-4. 3 (m); 3.8(m);3. 6(s);3.0(m);2.5(m);2_ 0(t);l. 0(t)。 N -異丙基-Ν’-{[4-(2 -氧基-咄咯啶-1-基）-苯基]-乙醯胺基_4, 6 -二氮β比σ各弁[3，4-c] β比°坐-5_基}脈；1H-NMR (DMS0-d6) d ppm:7. 6 - 7. 3(m ) ; 5. 9(m);4. 3(m ) ; 3. 8 (m); 3. 6 ( s ) ; 2. 5 ( m ) ; 2. 0 (m) ; 1 · 0 (d )。 1'1_{5'-(2_口夫0南曱酿基）-4，6_二氮0比0各弁[3，4_〇]11比〇坐_3_ •基}-4-(2-氧基-吡咯啶-1-基）-苯基-乙醢胺；1H-NMR (DMSO-d6) d ppm:7. 9 - 6. 6(m ) ;4. 9 - 4.6(m);3. 8 (m); 3.6(s);2.5(m);2.0(m)。 N-{5-(2-曱氧苯基）-4,6 -二氫0比口各并[3,4-c] 0比0坐- 3-基}-4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺；1H-NMR (DMS〇-d6) d ppm:10. 6(s) ;7. 6-7. 0(m);4. 6-4. 2(m)C:\2D-C0DE\91-01\90119473.ptd Page 193 1327569 V. Description of invention (191); 3. 5 ( s ) ; 3. 2 (m ) ; 1. 9 (m) ; 1 · 4 (d). N-n-butyl-Ν'-{(4-oxopiperidin-1-yl-phenyl)-acetamido-4,6-dihydrogen ratio π[3,4-c]D ratio ° sit--5-urea urea; lH-NMR (DMSO-d6) d ppm: 10.4 (s); 7.1-6.5 (m); 6.2 (t); 4.3 (m); 3.4 (s); 3.2 (m ; 3. 0 (m) ; 1 · 9 (m); 1.4-1_ 2 (m); 0. 8 (t). N-{5-phenyl-mercapto-4,6-dihydron-biloro[3,4-c]-s--3-yl}-(4-pyrrolidinyl-phenyl)-ethene 1H-NMR (DMS0-d6) d ppm: 7.8-7.6 (m); 7.0-6.4 (m); 4.4 (m); 3.3 (s); 3.2 (m); 1. 9 (m). N-ethyl-Ν' - {[4-(2-oxy-D is more than B each bite_1_yl)-phenyl]-ethylamino-4,6-dihydrogen ratio p and [ 3,4-〇:]° ratio. 5-5. 3 (m); 3.8 (3); (5); m); 3. 6 (s); 3.0 (m); 2.5 (m); 2_ 0 (t); l. 0 (t). N-isopropyl-Ν'-{[4-(2-oxy-indolyl-1-yl)-phenyl]-acetamido- 4,6-diaza β ratio σ 弁 [3 , 4-c] β ratio ° sitting -5_ base} pulse; 1H-NMR (DMS0-d6) d ppm: 7. 6 - 7. 3(m ) ; 5. 9(m); 4. 3(m 3. 8 (m); 3. 6 ( s ) ; 2. 5 ( m ) ; 2. 0 (m) ; 1 · 0 (d ). 1'1_{5'-(2_口夫0南曱制基)-4,6_二氮0-00弁[3,4_〇]11 than 〇3_•基}-4-( 2- oxy-pyrrolidin-1-yl)-phenyl-acetamide; 1H-NMR (DMSO-d6) d ppm: 7. 9 - 6. 6 (m ) ; 4. 9 - 4.6 (m) ; 3. 8 (m); 3.6 (s); 2.5 (m); 2.0 (m). N-{5-(2-indolylphenyl)-4,6-dihydrogen 0 is a ratio of [3,4-c] 0 to 0-position - 3-yl}-4-(2-oxy- Pyridin-1-yl)-phenyl-acetamide; 1H-NMR (DMS〇-d6) d ppm: 10. 6(s); 7. 6-7. 0(m); 4. 6-4 . 2(m)

C:\2D-CODE\91-01\90119473.ptd 第194頁 1327569 五、發明說明（192) ;3. 8 (m) ; 3. 5 ( s ) ; 2. 5 (m ) ; 2. 0 (m )。 1^-{5-胺基羰基曱基-4,6-二氫吼咯并[3,4-(：]吡唑-3-基卜4-(2 -氧基-吡咯啶-卜基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm : 7. 6 - 7. Ο (m ) ; 3. 8(m) ; 3. 5(s ) ; 3. 3(m); 2.5(m);2.0(m)。 N-異丙基-Ν’ - {(4 -吡咯啶-1-基-苯基）-乙醯胺基-4, 6_ 二氫°比°各并[3,4-<:]°比哇-5-基}脲；111-題1^(0心0-(16)(1 ppm:7.1-6.4(m);5. 9(m);4.3(m);3.8(m);3.4(s);3.2(m); 1 · 9(m) ; 1. 0(d)。 N-乙基-Ν’ - {(4 -咄咯啶-1-基-苯基）-乙醯胺基-4, 6 -二氮 π比洛弁[3，4_c]D比 °坐_5_基}脈；1H-NMR (DMSO_d6) d ppm:10.4(s);7.1-6.4(m);6.2(m);4.3(m);3.4(s);3.2(m) ;3.0(m);1.9(m);1.0(t)。 N-{5-胺基裁基曱基-4，6 -二氫°比°各并[3,4-c] 0比。坐- 3-基}-(4 -吡咯啶-卜基-苯基）-乙醯胺；1H-NMR (DMSO-d6) d ppm:10.3(s);7. 0-6.4(m);3.8(m);3.4(s);3.3(s); 3.2(m);1.9(m) o N-{5-(3-曱基丁醯基）-4,6 -二氫吡咯并[3,4-c]咄唑-3-基}-4-(2 -氧基-吡咯啶-卜基）-苯基-乙醯胺；1H-NMR (DMSO-d6) d ppm : 7. 6-7. 3 (m) ; 4. 6-4. 3 (m) ; 3. 8 (m) ; 3. 6 (s);2.5(m);2.2-2.0(m);0.9(m)。 N -正丁基-Ν’ - {3-(2 -萘-2 -基）乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲；1H-NMR (DMSO-d6) d ppm:7. 9 -7. 4(m);6.2(t);4. 3(s);3.8(s);3. 0(m);l. 4-1. 2(m);0. 8C:\2D-CODE\91-01\90119473.ptd Page 194 1327569 V. Description of invention (192); 3. 8 (m) ; 3. 5 ( s ) ; 2. 5 (m ) ; 2. 0 (m). 1^-{5-Aminocarbonylindolyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-ylbu 4-(2-oxy-pyrrolidinyl-bu) -phenyl-acetamide; 1H-NMR (DMS0-d6) d ppm : 7. 6 - 7. Ο (m ) ; 3. 8 (m) ; 3. 5(s ) ; 3. 3(m) ; 2.5(m); 2.0(m). N-isopropyl-Ν'-{(4-pyrrolidin-1-yl-phenyl)-acetamido-4,6-dihydrogen ratio [3,4-<:]° than wow-5-yl}urea; 111-title 1^(0 heart 0-(16) (1 ppm: 7.1-6.4(m); 5. 9(m); 4.3 (m); 3.8 (m); 3.4 (s); 3.2 (m); 1 · 9 (m); 1. 0 (d). N-ethyl-Ν' - {(4 - fluorenidine- 1-yl-phenyl)-acetamido-4,6-diaza pibiloxime [3,4_c]D ratio _5_ yl} pulse; 1H-NMR (DMSO_d6) d ppm: 10.4 ( s); 7.1-6.4(m); 6.2(m); 4.3(m); 3.4(s); 3.2(m); 3.0(m); 1.9(m); 1.0(t). N-{5- Amino-based benzyl-4,6-dihydrogen ratio of [3,4-c] 0. Sodium-3-yl}-(4-pyrrolidine-buyl-phenyl)-acetamidine Amine; 1H-NMR (DMSO-d6) d ppm: 10.3 (s); 7. 0-6.4 (m); 3.8 (m); 3.4 (s); 3.3 (s); 3.2 (m); o N-{5-(3-mercaptobutyl)-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-(2-oxy-pyrrolidine-b Benzyl-acetamide; 1H-NMR (DMSO-d6) d ppm : 7. 6-7. 3 (m) ; 4. 6-4. 3 (m) ; 3. 8 (m) ; 3. 6 (s); 2.5 (m); 2.2-2.0 (m); 0.9 (m). N - n-butyl Ν-Ν' - {3-(2-naphthalen-2-yl)acetamido-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea; 1H-NMR ( DMSO-d6) d ppm: 7. 9 -7. 4 (m); 6.2 (t); 4. 3 (s); 3.8 (s); 3. 0 (m); l. 4-1. 2 ( m);0. 8

C:\2D-00DE\91-01\90119473.ptd 第 195 頁 1327569 五、發明說明（193) (t ) ° N -正丁基- N’-{3-(3_曱基-苯基）乙酿胺基-4，6_二氮°比口各并[3,4-。]°比°坐-5-基}脲；1H-NMR (DMS0-d6) d ppm: 7.2- 7.0(m);6.2(t)；4.3(bs);3.6(s);3.0(m);2.3(s);1.4 -1.2(m);0.8(t)。 N -正丁基-N’_{3-(3-氟-苯基）乙酿胺基-4，6 -二氮D比p各并[3,4-c]n 比 °坐-5-基}脲；1H-NMR (DMS0-d6) d ppm:7.4 -7.0(m);6.2(t);4.3(bs);3.6(s);3.0(m);1.4-1.2(m); 0. 8(t)。 0!'}-正丁基-1'!’-{3-(3-吡啶基）乙醯胺基-4,6-二氫吡咯并 [3, 4-c]吡唑-5 -基丨脲；1^10(0^150-(16)(1??111:7.7-7.3(m);6.2(t);4.3(bs);3.7(s);3.0(m);1.4-1.2(ni);0.8 (t) 〇 N -正丁基-Ν’ - {3-(雙環[4.2.0.]辛 1,3, 5 -三烯-7 -羧醯胺基）-4，6 -二氯吼11 各并[3，4-c] π比。坐-5_基}脈；1H-NMR (DMS〇-d6) d ppm:7.2-7.0(m);6.2(t);4.4(m);4.3(m); 3.3(s);3_ 0(m);l.4-1.2(m);0.8(t)。 N -正丁基-Ν’ - {3-苯氧乙醯胺基-4, 6-二氫吡咯并 •[3, 4-c]吡唑-5 -基}脲；111-關1?(01^0-(16)(1口？111:7.3-6.9(m);6.2(t);4.7(s);4.3(bs);3.0(m);l.4-1.2(m);0.8 (t) ° N -正丁基-Ν’ - {3-(4-曱基-苯基）乙醯胺基-4, 6 -二氫吡口各并[3，4-(：]ηΛ^-5-*}脲；1H-NMR (DMSO-d6) d ppm: 7.2- 7. l(m);6. 2(t);4.3(bs);3. 5(s);3. 0(m);2. 2(s);l. 4C:\2D-00DE\91-01\90119473.ptd Page 195 1327569 V. INSTRUCTIONS (193) (t) ° N-n-butyl-N'-{3-(3_mercapto-phenyl) Ethylamino-4,6-diaza has a specific ratio of [3,4-. [°°°°-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7.2-7.0 (m); 6.2 (t); 4.3 (bs); 3.6 (s); 3.0 (m); 2.3(s); 1.4 -1.2(m); 0.8(t). N-n-butyl-N'_{3-(3-fluoro-phenyl)ethanoamine-4,6-diaza D ratio p and [3,4-c]n ratio °-5- 1H-NMR (DMS0-d6) d ppm: 7.4 - 7.0 (m); 6.2 (t); 4.3 (bs); 3.6 (s); 3.0 (m); 1.4-1.2 (m); 8(t). 0!'}-n-butyl-1'!'-{3-(3-pyridyl)acetamido-4,6-dihydropyrrolo[3,4-c]pyrazole-5-ylindole Urea; 1^10(0^150-(16)(1??111:7.7-7.3(m); 6.2(t); 4.3(bs); 3.7(s); 3.0(m); 1.4-1.2( Ni);0.8 (t) 〇N-n-butyl-Ν' - {3-(bicyclo[4.2.0.] octane 1,3,5-trien-7-carboxyguanidino)-4,6 - Dichloropurine 11 each [3,4-c] π ratio. Sit-5_yl} vein; 1H-NMR (DMS〇-d6) d ppm: 7.2-7.0 (m); 6.2 (t); 4.4 ( m); 4.3(m); 3.3(s); 3_ 0(m); l.4-1.2(m); 0.8(t). N-n-butyl-Ν' - {3-phenoxyacetamide 4- 4,6-dihydropyrrolo-[3,4-c]pyrazol-5-yl}urea; 111-off 1?(01^0-(16) (1 port? 111:7.3-6.9 ( m); 6.2(t); 4.7(s); 4.3(bs); 3.0(m); l.4-1.2(m); 0.8 (t) ° N-n-butyl-Ν' - {3-( 4-mercapto-phenyl)acetamido-4,6-dihydropyryldi[3,4-(:]ηΛ^-5-*}urea; 1H-NMR (DMSO-d6) d ppm : 7.2- 7. l(m); 6. 2(t); 4.3(bs); 3. 5(s); 3. 0(m); 2. 2(s); l. 4

C:\2D-O3DE\91-01\90119473.ptd 第 196 頁 1327569 五、發明說明（194) -1.2(m);0.8(t)。 N-正丁基-Ν’ - {3-(4-氟-苯基）乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ρρπκ7_ 3 -7.1(m);6.2(t);4.3(bs);3.6(s);3.0(m);1.4-1.4(m); 0.8(t)。 N_正丁基-N’_{3_(3，4_二說-苯基）乙酸胺基_4，6_二氮〇比洛并[3,4-〇]°比°坐-5-基}脲；111'^^^(0^!50-(16)(1口口111: 7.4-7.1(m);6.2(t);4.3(bs);3.6(s);3.0(m);1.4-1.2(m) ;0.8(t)。 N-正丁基-Ν’ - {3-(4 -三氟曱氧-苯基）乙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm:7.4-7. 3(m);6.2(t);4. 3(bs);3.6(s);3. 0(m);l.4-1.2(m);0.8(t)。 ^正丁基-…-^-^-甲基-苯基’乙酿胺基-斗^-二氫吼口各并[3，4-c]D 比0坐-5-基}脲；1H-NMR (DMSO-d6) d ppm: 7.2- 7.1(m);6.2(t);4.3(bs);3.6(s);3.0(m);2.2(s);1.4 -1.2(πι);0·8(Ό 〇 N -正丁基-Ν’ - {3-(2 -溴-苯基）乙醯胺基-4, 6 -二氫吡咯并[3，4-。]°比°坐-5-基}脲；111-麗1^(0^180-(16)(1卩卩111: 7.6-7.2(m);6.2(t);4.3(m);3.8(s);3.0(m);l.4-1.2(m); 0.8(t)。 N -正丁基- N’_{3-(2，5 -二氣-苯基）乙醯胺基-4,6 -二氫 0 比 D各并[3，4-c]D 比嗤 _5_基}脲；1H-NMR (DMS〇-d6) d ppm: 7.2- 7.l(m);6.2(t);4.3(m);3.7(s);3.0(m);l.4-1.2(m);C:\2D-O3DE\91-01\90119473.ptd Page 196 1327569 V. Description of invention (194) -1.2(m); 0.8(t). N-n-butyl-Ν'-{3-(4-fluoro-phenyl)acetamido-4,6-dihydropyrrolo[3,4-c]pyrazole-5-yl}urea; 1H - NMR (DMS0-d6) d ρρπκ7_ 3 - 7.1 (m); 6.2 (t); 4.3 (bs); 3.6 (s); 3.0 (m); 1.4-1.4 (m); 0.8 (t). N_n-butyl-N'_{3_(3,4-di-n-phenyl)acetic acid amine _4,6-diazaindolebi[3,4-〇]°°°-5- Urea urea; 111'^^^(0^!50-(16) (1 port 111: 7.4-7.1(m); 6.2(t); 4.3(bs); 3.6(s); 3.0(m) ; 1.4-1.2(m); 0.8(t). N-n-Butyl-Ν' - {3-(4-trifluorooxime-phenyl)acetamido-4,6-dihydropyrrolo[ 3, 4-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7.4-7. 3(m); 6.2(t); 4. 3(bs); 3.6(s 3; 0(m); l.4-1.2(m); 0.8(t). n-Butyl-...-^-^-methyl-phenyl'ethylamino-capryl-dihydrogen The mouth of each [3,4-c]D is 0-5-based urea; 1H-NMR (DMSO-d6) d ppm: 7.2- 7.1 (m); 6.2 (t); 4.3 (bs); 3.6(s); 3.0(m); 2.2(s); 1.4 -1.2(πι); 0·8(Ό 〇N-n-butyl-Ν' - {3-(2-bromo-phenyl)acetamidine Amino-4,6-dihydropyrrolo[3,4-.]°°°-5-yl}urea; 111-Li 1^(0^180-(16)(1卩卩111: 7.6- 7.2(m); 6.2(t); 4.3(m); 3.8(s); 3.0(m); l.4-1.2(m); 0.8(t). N-n-butyl-N'_{3 -(2,5-diox-phenyl)acetamido-4,6-dihydrogen 0 to D and [3,4-c]D to 嗤_5_yl}urea; 1H-NMR (DMS 〇-d6) d ppm: 7.2- 7.l(m); 6.2(t); 4.3(m); 3.7(s); 3.0(m); l.4-1.2( m);

C:\2D-C0DE\91-01\90119473.ptd 第197頁 1327569 五、發明說明（195) 0·8(t)。 N -正丁基-Ν’ -{ 3-(4-(吼咯啶-1-基-羰基甲氧）-苯基）乙酿胺基-4，6_二氫比11 各并[3，4-c] °比。坐-5_基}脈；1H-NMR (DMS0-d6) d ppm:7.2-6.8(m);6.2(t);4. 6(s);4.3(bs) ;3.4(m);3.0(m);l.9-1.7(m);l.4-1.2(m);0.8(t)。 N_正丁基_N’_{3-(3-(胺基幾基甲氧）-苯基）乙酿胺基 -4，6_ 二氮 n比 p各并[3，4-c] °比 °坐_5_ 基}脈；1H-NMR (DMS0-d6) d ppm:7. 5 - 7.3(m ) ; 7. 2 - 6.8(m ) ; 6. 2(t ); 4.4(s);4.3(bs);3.6(s);3.0(m);1.4-1.2(m);0.8(t)。 N -正丁基-N’-{3-(n比。定-4-基-乙酿胺基）-4，6_二氮0比°各并[3，4-。]11比°坐-5-基}脲；111-關1^(0材80-(16)(1??111: 8.6(m);7.4(m);6.2(t);4.3(bs);3.7(s);3.0(m);l.4-1.2 (m);0.8(t)。 N -正丁基-Ν’-{3-(4-(嗎啉-1-基）-苯基）乙醯胺基-4, 6-二氫°比'7各并[3，4-(：]吼°坐-5-基}脲；111-麗1^(0^180-(16)(1 ppm: 7. 2-6. 8(m);6. 2(t);4. 3(bs);3. 7(m);3. 5( s); 3.0(m);1.4-1.2(m);0·8(t)。 N -正丁基-Ν’ - {3-(2-氟-苯基）乙醯胺基-4, 6 -二氫吡咯比嗤-5-基}脲；1H-NMR (DMS〇-d6) d ppm: 0.8(t)。 N_正丁基_N’_{3_(3，5_二氣-苯基）乙酿胺基_4，6_二氮口比0各并[3,4-c]<^°坐-5-基}脲；111-關1?(0^150-(16)(1卩卩111: 7. 1-6. 9(m);6. 2(t);4. 3(bs);3. 7(s);3. 0(m);l.4-1. 2(m)C:\2D-C0DE\91-01\90119473.ptd Page 197 1327569 V. Description of invention (195) 0·8(t). N-n-butyl-Ν'-{ 3-(4-(indolyl-1-yl-carbonylmethoxy)-phenyl)ethanoyl-4,6-dihydrogen ratio 11 each [3, 4-c] ° ratio. Sit 5-5-1 radians; 1H-NMR (DMS0-d6) d ppm: 7.2-6.8 (m); 6.2 (t); 4.6 (s); 4.3 (bs); 3.4 (m); 3.0 ( m); l.9-1.7 (m); l. 4-1.2 (m); 0.8 (t). N_n-butyl _N'_{3-(3-(amino methoxy)-phenyl)ethanoyl-4,6-diaza n ratio p[3,4-c] ° _5_基脉脉;1H-NMR (DMS0-d6) d ppm:7.5 - 7.3(m); 7. 2 - 6.8(m); 6. 2(t); 4.4(s); 4.3 (bs); 3.6 (s); 3.0 (m); 1.4-1.2 (m); 0.8 (t). N-n-butyl-N'-{3-(n ratio. 1,4-yl-ethanoylamino)-4,6-diaza 0 is each [3,4-. 11°°°-5-yl}urea; 111-off 1^(0 material 80-(16)(1??111: 8.6(m); 7.4(m); 6.2(t); 4.3(bs) ; 3.7(s); 3.0(m); l.4-1.2 (m); 0.8(t). N-n-butyl-Ν'-{3-(4-(morpholin-1-yl)-benzene Ethylamino-4,6-dihydrogen ratio '7 each and [3,4-(:]吼° sit-5-yl}urea; 111-丽1^(0^180-(16) (1 ppm: 7. 2-6. 8(m); 6. 2(t); 4. 3(bs); 3. 7(m); 3. 5(s); 3.0(m); 1.4- 1.2(m); 0·8(t). N-n-Butyl-Ν'-{3-(2-fluoro-phenyl)acetamido-4,6-dihydropyrrole than 嗤-5-yl Urea;1H-NMR (DMS〇-d6) d ppm: 0.8(t). N_n-butyl _N'_{3_(3,5_di-phenyl)ethinyl _4,6 _Dinitrogen port ratio 0 and each [3,4-c]<^° sit-5-yl}urea; 111-off 1?(0^150-(16)(1卩卩111: 7. 1- 6. 9(m); 6. 2(t); 4. 3(bs); 3. 7(s); 3. 0(m); l.4-1. 2(m)

C:\2D-CODE\91-01\90119473.ptd 第198頁 1327569 五、發明說明（196) ;0 · 8 (t ) 〇 N-正丁基-N’-{3-(6 -氧基-6H-嗒啡-1-基）乙醯胺基 -4,6-二氫°比11各并[3,4-〇]'1比°坐-5-基}脲；1}1-關1? (DMS0-d6) d ppm:7. 9(m) ; 7. 4(m);6. 9(m);6. 2(t); 4.9(s);4.3(m);3.0(m);1.4-1.2(ni);0.8(t)。 N-{5-甲基°比。定曱醯基-4,6 -二氫°比0各并[3,4-c]吼〇坐- 3-基卜4-(2-氧基-$唑啶-3 -基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm:8. 6 - 7. 25(m);4. 9-4. 6(m) ; 4.4-4. Ο (m); 3.6(s)。 1{5-(°塞吩-2-基）乙醯基-4，6-二氫11比11各并[3,4-(：]'1比〇坐 -3 -基}-4-(2 -氧基-4唑啶-3 -基）-苯基-乙醯胺；1H-NMR (DMSO-d6) d ppm:7.5-6.9(m);4.7-4. 0(m);3.9 (s ) ; 3. 6 ( s )。 [^-{牙-^-咬喃甲醯基卜斗^-二氫吼口各并!^，*-!：]1^^」-基}-4-(2 -氧基-咄唑啶-3 -基）-苯基-乙醯胺；1H-NMR (DMSO-d6) d ppm : 7. 9-6. 6(m) ;4. 9-4. 6(m) ;4. 4-4. Ο (m);3.6(s)。 N-{5-(2_乙氧乙酿基）-4，6 -二氫0比洛并[3,4-c] n比。坐- 3-基卜4-(2 -氧基-ν|唑啶-3 -基）-苯基-乙醯胺；1H-NMR (D M S 0 - d 6 ) d p p m : 7 · 4 (m ) ; 4. 6 - 3. 5 (m ) ; 1. 1 ( m )。 N-{5-(3-曱基-丁酿基）_4，6 -二氫13比p各并[3，4-c] D比。坐 -3-基}-4-(2 -氧基唑啶-3 -基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm : 7.4(m);4. 6-4. 0(m) ; 3. 6(s) ; 2. 2(d);2. 0(ni);0.9(m) oC:\2D-CODE\91-01\90119473.ptd Page 198 1327569 V. INSTRUCTIONS (196); 0 · 8 (t ) 〇N-n-butyl-N'-{3-(6-oxyl -6H-quinone-1-yl)acetamido-4,6-dihydrogen ratio 11 and [3,4-〇]'1 ratio ° sit-5-yl}urea; 1}1-off 1? (DMS0-d6) d ppm: 7. 9 (m); 7. 4 (m); 6. 9 (m); 6. 2 (t); 4.9 (s); 4.3 (m); 3.0 ( m); 1.4-1.2 (ni); 0.8 (t). N-{5-methyl ° ratio.曱醯Mercapto-4,6-dihydrogen ratio 0 and [3,4-c] 吼〇-3-ylbu 4-(2-oxy-$oxazolidine-3-yl)-phenyl - acetamidine; 1H-NMR (DMS0-d6) d ppm: 8.6 - 7. 25 (m); 4. 9-4. 6 (m); 4.4-4. Ο (m); 3.6 (s ). 1{5-(°Cet-2-yl)ethenyl-4,6-dihydro 11 to 11 and [3,4-(:]'1 is more than -33-amino}-4-( 2 -oxy-4-oxazol-3-yl)-phenyl-acetamide; 1H-NMR (DMSO-d6) d ppm: 7.5-6.9 (m); 4.7-4. 0 (m); 3.9 ( s ) ; 3. 6 ( s ). [^-{牙-^-咬甲甲甲基基斗斗--Dihydro 吼口各!^,*-!:]1^^"-基}-4 -(2-oxy-oxazolidine-3-yl)-phenyl-acetamide; 1H-NMR (DMSO-d6) d ppm : 7. 9-6. 6(m) ;4. 9-4 6(m) ;4. 4-4. Ο (m); 3.6(s). N-{5-(2_ethoxyethyl ketone)-4,6-dihydrogen 0 piroxi[3, 4-c] n ratio. Sodium 3-yl b 4-(2-oxy-voxazolidine-3-yl)-phenyl-acetamide; 1H-NMR (DMS 0 - d 6 ) dppm : 7 · 4 (m ) ; 4. 6 - 3. 5 (m ) ; 1. 1 ( m ). N-{5-(3-indolyl-butyl)- 4,6-dihydro 13 to p And [3,4-c] D ratio. Sodium-3-yl}-4-(2-oxoxazolidin-3-yl)-phenyl-acetamide; 1H-NMR (DMS0-d6) d ppm : 7.4(m); 4. 6-4. 0(m) ; 3. 6(s) ; 2. 2(d); 2. 0(ni); 0.9(m) o

C:\2D-00DE\91-01\90]19473. ptd 第199頁 1327569 五、發明說明（197) N-{5- 丁醯基-4, 6 -二氫吡咯并[3,4-c]吡唑-3-基}-4-(2-氧基-1¾唑啶-3 -基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm:7.4(m);4.6-4. 0(m);3. 6(s) ;2.4(m);l. 5(m) ;0. 9 (m )。 N -異丙基-N’-{3-[4-(2 -氧基唑啶-3 -基）-苯基-乙醯胺基]-4，6 -二氫 °比 p各并[3,4-c]W°坐-5-基}脲；1H-NMR (DMS0-d6) d ppm:7.4(m);5. 9(d);4. 4-4. Ο (m);3.8(m); 3.6(s);1.0(m) o N-(正丁基）-N’-{3-[4-(2 -氧基唑啶-3 -基）-苯基-乙 4 ®醯胺基]-4,6 -二氫°比°各并[3,4-〇]°比°坐-5-基}脲；1H-NMR (DMS〇-d6) d ppm:7.4(m);6. 2(t);4. 4-4. 0(m ) ; 3. 6 ( s ); 3· O(m) ; 1. 4-1· 2(m);0. 8(t)。 N-{5-乙氧獄基-4，6 -二氫D比p各并[3，4_c] 坐-3-基} -4-(2 -氧基-g唑啶-3-基）-苯基-乙醯胺；1H-NMR (DMS0-d6) d ppm:7.4(m);4.4-4.0(m);3.6(s);1.2(t)。 N -異丙基-Ν’-{3-[2-(3 -氧基-3,4,4&,83-四氫-2}1-苯并 [1，4]稀'°井-6 -基）乙醯胺基]-4, 6 -二氫0比11 各并[3, 4-c] 唑-5-基}脲；1H-NMR (DMS0-d6) d ppm:6.8(m);5· 9(d) •;4. 5(s);4. 3(bs);3.8(m);3. 5(bs);1.0(m)。 N -異丙基-Ν’ - {3-(3 -溴-苯曱醯胺基）-4,6 -二氫吡咯并 [3，4 - c ] °比 °坐-5 -基}脲 N-{5 -苯項醯基- 4,6 -二氫吼11 各并[3,4-c]吼。坐-3-基}-3-溴苯曱醯胺 N-{5-乙醯基-4,6 -二氫n比p各并[3,4-c]"比。坐-3-基}-C:\2D-00DE\91-01\90]19473. ptd Page 199 1327569 V. INSTRUCTIONS (197) N-{5- Butyryl-4,6-dihydropyrrolo[3,4-c]pyridinium Zyrid-3-yl}-4-(2-oxy-13⁄4-oxazolidine-3-yl)-phenyl-acetamide; 1H-NMR (DMS0-d6) d ppm: 7.4 (m); 0(m); 3. 6(s); 2.4(m); l. 5(m); 0. 9 (m). N-isopropyl-N'-{3-[4-(2-oxoxazolidin-3-yl)-phenyl-acetamido]-4,6-dihydrogen ratio p and [3 , 4-c]W° sit-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 7.4 (m); 5. 9 (d); 4. 4-4. Ο (m); 3.8 (m); 3.6(s); 1.0(m) o N-(n-butyl)-N'-{3-[4-(2-oxoxazolidine-3-yl)-phenyl-ethyl 4®醯Amino]-4,6-dihydrogen ratio °[3,4-〇]°°°-5-yl}urea;1H-NMR (DMS〇-d6) d ppm: 7.4(m) ;6. 2(t);4. 4-4. 0(m) ; 3. 6 ( s ); 3· O(m) ; 1. 4-1· 2(m); 0. 8(t) . N-{5-ethoxyphenanthyl-4,6-dihydro D ratio p and [3,4_c] -3-yl}-4-(2-oxy-goxaridin-3-yl)- Phenyl-acetamide; 1H-NMR (DMS0-d6) d ppm: 7.4 (m); 4.4-4.0 (m); 3.6 (s); 1.2 (t). N-isopropyl-Ν'-{3-[2-(3-oxy-3,4,4&,83-tetrahydro-2}1-benzo[1,4] dilute[°-6 -yl)acetamido]-4,6-dihydrogen 0 to 11 each [3,4-c]oxazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm: 6.8 (m) ;5· 9(d) •; 4. 5(s); 4. 3(bs); 3.8(m); 3. 5(bs); 1.0(m). N-isopropyl-Ν'-{3-(3-bromo-benzoguanidino)-4,6-dihydropyrrolo[3,4 - c ] ° ratio ° sit-5-yl}urea N -{5 -Benzyl fluorenyl- 4,6-dihydroindole 11 each [3,4-c]indole. Sodium-3-yl}-3-bromophenylamine N-{5-ethenyl-4,6-dihydron ratio p and [3,4-c]" ratio. Sitting -3-base}-

C:\2D-C0DE\91-01\90119473.ptd 第200頁 1327569 五、發明說明（198) [4-(1-吡咯啶-2 -酮）苯甲醯胺] N-乙基-N’-{3-(3 -溴-苯曱醯胺基）-4,6 -二氫吡咯并[3, 4 - c ] 〇比0坐-5 -基}脲 N-{5-(8 -嗤琳）績醯基-4，6 -二氫吼洛并[3, 4-c] °比唾-3-基}-對曱苯曱醯胺 N-苯基-Ν’ -{ 3-(3 -溴-苯甲醯胺基）-4, 6 -二氫咄咯并[3, 4-c] °比。坐-5-基}脲 N-{5 -苯確乙醯基-4,6 -二氫"比11各并[3,4-c] D比σ坐-3-基} - 3 -溴苯甲醯胺 ^{5-曱烧石黃醯基-4，6-二氫口比0各并[3,4-。]口比。坐-3-基} - 3 -溴苯曱醯胺 Ν-異丙基-Ν’-{3-[4-(1-吡咯啶-2-酮）-苯基醯胺基]-4, 6 -二氫°比《»各并[3，4-c]吼°坐-5-基}脲 N-{5-(8 -嗤琳）幾基-4，6 -二氫°比略并[3, 4-c]吼°坐- 3-基}-對甲苯曱醯胺 N_{5-(1_蔡）績酿基_4，6 -二氮σ比p各并[3，4-c] D比D坐-3-基}-4-苯基苯甲醯胺 Ν-{5-(1-蔡曱醯基）-4,6 -二氫吼口各并[3,4-c] 0比0坐- 3-基}-4-苯基苯甲醯胺 Ν-{5-(1-萘曱醢基）-4，6 -二氫。比11 各并[3,4-c] D比唾- 3-基}-4-苯氧苯甲醯胺 N-苯基-Ν’ - {3-(4-苯基-苯甲醯胺基）-4,6 -二氫"比咯并 [3, 4-c]"比°坐-5-基}脲 N_{5_苯基乙酿基-4，6_二氮D比0各并[3，4_c] 〇比°坐-3-C:\2D-C0DE\91-01\90119473.ptd Page 200 1327569 V. INSTRUCTIONS (198) [4-(1-Pyrrolidin-2-one)benzamide] N-ethyl-N' -{3-(3-bromo-benzoguanidino)-4,6-dihydropyrrolo[3,4 - c ] 〇 is 0 to 5 -yl}urea N-{5-(8 -嗤琳) 醯基基-4,6-Dihydroindolo[3,4-c] ° than sial-3-yl}-p-benzoquinone N-phenyl-Ν' -{ 3-(3 -Bromo-benzamide amino)-4,6-dihydroindolo[3,4-c] ° ratio. Sodium-5-yl}urea N-{5-phenyl-ethenyl-4,6-dihydro" ratio 11 and [3,4-c] D ratio σ--3-yl}-3-bromo Benzoylamine ^{5-曱烧石黄醯基-4,6-dihydrogen port ratio 0 and [3,4-. ] mouth ratio. Sodium-3-yl}-3-bromophenylamine oxime-isopropyl-Ν'-{3-[4-(1-pyrrolidin-2-one)-phenyldecylamino]-4, 6 -Dihydrogen ratio is lower than "»»[3,4-c]吼°-5-yl}urea N-{5-(8-嗤琳)-based-4,6-dihydrogen ratio 3, 4-c] 吼 ° sitting - 3-yl}-p-toluidine NN_{5-(1_蔡) 酿 _4,6-diazo σ ratio p and [3,4-c ] D is more than D--3-yl}-4-phenylbenzamide Ν-{5-(1-Cetyl)-4,6-dihydropurine each [3,4-c] 0 ratio 0-sodium-3-yl}-4-phenylbenzamide-{5-(1-naphthyl)-4,6-dihydrogen. Ratio of 11 [3,4-c] D to sal-3-yl}-4-phenoxybenzamide N-phenyl-indole - {3-(4-phenyl-benzamide) )-4,6-dihydro"bibromo[3,4-c]" than °°-5-yl}urea N_{5_phenylethyl 4-,6-dinitrogen D ratio 0 Each [3,4_c] 〇°°°-3-

III λ: mIII λ: m

I C:\2D-C0DE\91-01\90119473.ptd 第201頁 1327569 五、發明說明（199) 基卜4-苯基苯甲醯胺 Ν-{5-(1-萘）磺醯基-4,6-二氫°比咯并[3,4-c]吡唑-3-基}-對曱苯曱醯胺 N - { 5 - (1 -萘甲醯基）-4，6 -立:氫11比D各并[3，4 - c ] 口比〇坐-3 -基}-對曱苯甲醯胺 - 乙酿基_4，6_二氮0比略并[3，4_c] 0比0坐-3-基}_3_苯氧苯甲醯胺 N-[5-(4 -氣-2,5-二氟苯曱醯基）-4,6-二氫吡咯并 [3,4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺；1H-NMR *DMS0-d6) d ppm: 7. 9 0-7. 3 0 (m) ; 4. 59(s) ; 4. 39 (s) ; 3· 72(s)。 N - { 5 -[第三丁基羧酸根]-4，6 _二氫吡咯并[3，4 - c ]吡唑 -3 -基}-2-(2 -萘基）乙醯胺；1H-NMR (DMS0-d6) d ρρηκ 7.90-7.75(m);7.55-7.40(m);4.33(s);4.31(s);3.78(s); 1.40(s)。 N-{5-[(l -曱基環丙基）戴基]-4, 6 -二氫0比0各并[3，4-c] 吡唑-3-基}-2-(2 -萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm:7.87(m);7.79(s);7.45(m);4.73(s);4.36(s);3.79 •(s) ; 1. 24(s) ;0. 83(s) ; 0. 52(t)。 1'1-[5-(環丁基幾基）-4,6-二氫13比洛并[3,4-(3]11比°坐-3-基]-2-(2-萘基）乙醯胺；1H-NMR (MSO-d6) d ppm:7.85(m);7. 78(s);7.46(m);4. 46(s);3.78(s);2.20-1· 70(m)。 N-[5-(2-氣苯甲酿基卜斗^-二氫吼^各并^^-^吼哩^-IC:\2D-C0DE\91-01\90119473.ptd Page 201 1327569 V. INSTRUCTIONS (199) Keb 4-phenylbenzimidoxime-{5-(1-naphthalene)sulfonyl-4 ,6-dihydro-pyrolo[3,4-c]pyrazol-3-yl}-p-benzoylamine N-{5-(1-naphthylmethyl)-4,6-立: Hydrogen 11 is more than D and [3,4 - c ] is more than -3 -yl}-p-benzoic acid - E-branched _4,6-dinitrogen 0 is slightly [3,4_c] 0 -3-yl}_3_phenoxybenzamide N-[5-(4- gas-2,5-difluorobenzoinyl)-4,6-dihydropyrrolo[3,4 -c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 1H-NMR *DMS0-d6) d ppm: 7. 9 0-7. 3 0 (m) ; 4. 59 (s) ; 4. 39 (s) ; 3· 72(s). N - { 5 -[t-butylcarboxylate]-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-(2-naphthyl)acetamide; 1H - NMR (DMS0-d6) d ρρηκ 7.90-7.75 (m); 7.55-7.40 (m); 4.33 (s); 4.31 (s); 3.78 (s); 1.40 (s). N-{5-[(l-fluorenylcyclopropyl)-yl]-4,6-dihydro 0- 0 each and [3,4-c]pyrazol-3-yl}-2-(2 - Naphthyl)acetamide; 1H-NMR (DMS0-d6) d ppm: 7.87 (m); 7.79 (s); 7.45 (m); 4.73 (s); 4.36 (s); 3.79 • (s); 24(s); 0. 83(s); 0. 52(t). 1'1-[5-(cyclobutylamino)-4,6-dihydro 13-pyloro[3,4-(3]11-pyran-3-yl]-2-(2-naphthyl) Ethylamine; 1H-NMR (MSO-d6) d ppm: 7.85 (m); 7.78 (s); 7.46 (m); 4. 46 (s); 3.78 (s); 2.20-1·70 (m) N-[5-(2-gas benzoyl thiophene - dihydro hydrazine ^ and ^^-^吼哩^-

C:\2D-OODE\91-Ol\90119473_ptd 第 202 頁 1327569 五、發明說明（200) 基]-2-(2 -萘基）乙酿胺；1H-NMR (DMS〇-d6) d ppm:10.74 (s);7.90-7.23(m);4.32(s);3.80(s)。 N - [ 5 -(。比0定一3 -基親基）_ 4，6 -二氫0比p各并[3，4 - c ] 0比0坐 -3 -基]-2-(2 -萘基）乙醯胺；1H-NMR (DMSO-d6) d ρρπκ 8.75(dd);8.65(m);8.05-7.35(m);4.46(s);3.72(s)。 N - { 5 - [ ( 2，2，2, 3,-四曱基環丙基）羰基]-4, 6 -二氫nb咯并[3,4-c]吡唑-3-基}-2-(2 -萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm:7.86(m);7. 79(s);7.45(m);4. 73(s); 4. 57(s) ; 3. 79(s) ; 1. 22(n〇 ; 1. 12(m)。 N-[5-(2,4, 5 -三氟苯曱酿基）-4, 6 -二氫口比洛并[3,4-c] 〇比°坐-3 -基]-2-(2 -蔡基）乙醯胺；1H-NMR (DMSO-d6) d ppm:10.76(s);7.90-7.35(m);4.47(s);4.37(s);3.72(s) ο Ν-[5- (2-甲基戊-4 -稀醯基）-4,6 -二氫ϋ比口各并[3,4 — c] o坐-3-基]-2-.(2-蔡基）乙醯胺；lH-NMR(DMS0-d6)dppπl: 7.86(m);7.78(s);7.46(m);5.71(ni)；4.97(m);4.61(s);4. 35(s);3.78(s);2.63(m);2.28(m);2.05(m);1.22(m);1.0( t ) ° N — [5 —（環丙基乙醯基）-4，6_二氫〇比0各并[3，4-c] ϋ比0坐_3_ 基]-2-(2-萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm:7.90-7.40(m);3.77(s);2.21(t);0.96(m);0.42(m)。 N-[5_(5-氟一2-曱基苯曱醯基）-4,6 -二氫口比口各并[3,4-c] 吡唑-3 -基]-2-(2 -萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm:.7· 90-7_ 10(m);4. 20(s);2. 16(s)。C:\2D-OODE\91-Ol\90119473_ptd Page 202 1327569 V. Description of the Invention (200) Group]-2-(2-naphthyl)ethinamine; 1H-NMR (DMS〇-d6) d ppm: 10.74 (s); 7.90-7.23 (m); 4.32 (s); 3.80 (s). N - [ 5 - (. is more than 0 - 1 -yl-based) - 4,6 - dihydrogen 0 to p each [3,4 - c ] 0 to 0 -3 -yl]-2-(2 -naphthyl)acetamide; 1H-NMR (DMSO-d6) d ρρπκ 8.75 (dd); 8.65 (m); 8.05-7.35 (m); 4.46 (s); 3.72 (s). N - { 5 - [ ( 2,2,2, 3,-tetradecylcyclopropyl)carbonyl]-4,6-dihydronb-[3,4-c]pyrazol-3-yl}- 2-(2-naphthyl)acetamide; 1H-NMR (DMS0-d6) d ppm: 7.86 (m); 7.79 (s); 7.45 (m); 4. 73 (s); 4. 57 (s) ; 3. 79(s) ; 1. 22(n〇; 1. 12(m). N-[5-(2,4,5-trifluorobenzoquinone)-4, 6 - two Hydrogen port piroxi[3,4-c] 〇 ratio -3 -yl]-2-(2-cacoyl)acetamide; 1H-NMR (DMSO-d6) d ppm: 10.76(s); 7.90-7.35(m); 4.47(s); 4.37(s); 3.72(s) ο Ν-[5-(2-methylpent-4-yl-indenyl)-4,6-dihydroanthracene Each [3,4 - c] o--3-yl]-2-.(2-caiyl)acetamide; lH-NMR (DMS0-d6) dppπl: 7.86 (m); 7.78 (s); 7.46(m); 5.71(ni); 4.97(m); 4.61(s); 4.35(s); 3.78(s); 2.63(m); 2.28(m); 2.05(m); 1.22(m) );1.0( t ) ° N — [5 —(cyclopropylethylhydrazino)-4,6-dihydroindole ratio 0 each and [3,4-c] ϋ is 0 _3_ ki]-2- (2-Naphthyl)acetamide; 1H-NMR (DMS0-d6) d ppm: 7.90-7.40 (m); 3.77 (s); 2.21 (t); 0.96 (m); 0.42 (m). [5_(5-Fluoro- 2-indolylphenylhydrazolyl)-4,6-dihydrogen-portion [3,4-c]pyrazol-3-yl]-2-(2-naphthyl) Ethylamine; 1H-NMR (DMS0-d6) d ppm:.7· 90-7_ 10(m); 4. 20(s); 2.16(s).

C:\2D-C0DE\91-01\90119473.ptd 第203頁 1327569 五、發明說明（201) N-{5-[2-氟-5-(三氟曱基）苯甲醯基]-4, 6 -二氫吡咯并 [3,4-c]吡唑-3-基}-2-(2 -萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm:10.75(s);7. 97-7.35(m);4.60(s) ;4.35(s);3. 71(s)。 N-{5-[(3-曱氧環己基）羰基]-4, 6 -二氫吼咯并[3, 4-c] 吡唑-3 -基}-2-(2 -萘基）乙醯胺；1H-NMR (DMSO-d6) d ppm: 10.78(s);7.85(m);7.78(s);7.45(m);3.78(s) ;3.21(s);2.40-2.65(m);2.05-0.95(in)。C:\2D-C0DE\91-01\90119473.ptd Page 203 1327569 V. INSTRUCTIONS (201) N-{5-[2-Fluoro-5-(trifluoromethyl)benzimidyl]-4 , 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-(2-naphthyl)acetamide; 1H-NMR (DMS0-d6) d ppm: 10.75 (s); 7. 97-7.35(m); 4.60(s); 4.35(s); 3.71(s). N-{5-[(3-oxocyclohexyl)carbonyl]-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-2-(2-naphthyl)B Indoleamine; 1H-NMR (DMSO-d6) d ppm: 10.78 (s); 7.85 (m); 7.78 (s); 7.45 (m); 3.78 (s); 3.21 (s); 2.40-2.65 (m) ;2.05-0.95 (in).

N-[5-(2,4 -二氯-5-氟苯曱醯基）-4,6 -二氫吼咯并 •[3,4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm: 0. 76(s);7. 96 - 7. 38 (m ) ; 4. 57(s ) ; 4. 27 (s) ; 3.80(s)。 !^-[5-(2-氯-4,5-二氟苯曱醯基）-4,6-二氫吼咯并 [3，4-c]0比0坐-3_ 基]-2-(2 -蔡基）乙酿胺；1H-NMR (DMSO-d6) d ppm: 10. 78(s);7. 90 - 7.35 (m);4. 58(s ); 4_ 27(s);3. 71(s)。 N-{5-[4-(lH- 0米0坐-1-基）苯曱酿基]-4，6 -二氯D比0各并 [3, 4-c]吡唑-3 -基}-2-(2 -萘基）乙醯胺；1H-NMR 蠢 (DMS0-d6) d ppm:7.90-7.20(m);4.52(s);3.78(s)。 N-{5-[4-(胺基磺醯基）丁醯基]-4, 6-二氫吼咯并 [3,4-c]吼唑-3-基}-2-(2 -萘基）乙醯胺；1H-NMR (DMSO-d6) d ppm:7.85(m);7. 78(s ) ; 7.46(m);4. 53(s ); 3. 78(s);2.98(m);2.25(t);l.93(m)。 N-{5-[(8 -氧基-5, 6, 7，8 -四氫萘-2 -基）数基]-4，6 -二氫N-[5-(2,4-dichloro-5-fluorobenzoinyl)-4,6-dihydroindolo[3,4-c]pyrazole-3-yl]-2-( 2-naphthyl)acetamide; 1H-NMR (DMS0-d6) d ppm: 0. 76(s); 7.96 - 7.38 (m); 4. 57(s); 4. 27 (s ); 3.80(s). !^-[5-(2-chloro-4,5-difluorobenzoinyl)-4,6-dihydroindolo[3,4-c]0 is 0 to 0-based]-2- (2 - Cai Ke) Ethylamine; 1H-NMR (DMSO-d6) d ppm: 10.78(s); 7.90 - 7.35 (m); 4.58(s); 4_ 27(s); 3. 71(s). N-{5-[4-(lH- 0m0-1-yl)phenyl hydrazide]-4,6-dichloro D ratio 0 and [3, 4-c]pyrazole-3-yl }-2-(2-naphthyl)acetamide; 1H-NMR silly (DMS0-d6) d ppm: 7.90-7.20 (m); 4.52 (s); 3.78 (s). N-{5-[4-(Aminosulfonyl)butanyl]-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-2-(2-naphthyl) Acetamine; 1H-NMR (DMSO-d6) d ppm: 7.85 (m); 7.78 (s); 7.46 (m); 4. 53 (s); 3. 78 (s); 2.98 (m) ; 2.25(t); l.93(m). N-{5-[(8-oxy-5, 6, 7,8-tetrahydronaphthalen-2-yl)yl]-4,6-dihydro

C:\2D-CODE\91-01\90119473.ptd 第204頁 1327569 五、發明說明（202) 0比p各并[3,4-c]n比。坐-3-基}-2-(2 -萘基）乙醯胺；1H-NMR (DMSO-d6) d ppm:8. 05-7. 33(m);4.44(s) ;3. 80(s) ; 2. 95 (m);2. 60(m) ; 2· 05(m)。 N — (5 -丙酮醯基6 -二氫0比0各并[3，4一 c] 0比0坐一3 -基）一 2-(2_蔡基）乙酿胺 N-[5-(2,2 -二甲基丙醯基）-4，6 -二氫吼11 各并[3,4-c] π比唑-3-基]-2-(2-萘基）乙醯胺；1H-NMR (DMSO-d6) d ρρπκ 7. 90-7.40(m);3.80(s);l.20(s)。 N-(5 - 丁一2 -醯基-4, 6 -二氫 0比 D各并[3, 4_c] 口比0坐一3 -基）— 2-(2-萘基）乙醯胺；1H-NMR (DMS0-d6) d ppm:7.90 -7.40(m) ;3. 80(s) ; 1. 20(s)。 N-[5-(3 -碘-4-曱基苯曱醯基）-4,6 -二氫吼咯并[3,4-c] 吡唑-3 -基]-2-(2 -萘基）乙醯胺；1H-NMR (DMSO-d6) d ppm:10.72(s);8.05-7.35(m);4.45(s);3.710(s);2.37(s) o N-{5-[( _基氧）乙醯基]-4，6 -二氫n比p各并[3,4-c]吼〇坐 -3-基}-2-(2-萘基）乙醯胺；1H-NMR (DMS0-d6) d ρρηκ 7.90-7.20(m);4.25-4.70(m);4.20(s);3.80(s)。 N-{5-(2- H-2 -苯基乙醯基）-4，6 -二氫吼17各并[3, 4-c] 口比唑-3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7.8-8.0(m);7.4-7.6(m);6.0-6·5(m);4.2-5.0(m)。 N-{5-(2_氣-2-苯基乙酿基）-4, 6_二氮D比略并[3, 4-c] 0比唑-3-基}-4-苯氧苯甲醯胺；1H-NMR (DMS0-d6) d ppm: 7.8-8.0(m);7.4-7.6(m);4.2-5.0(m)。C:\2D-CODE\91-01\90119473.ptd Page 204 1327569 V. INSTRUCTIONS (202) 0 is more than p and [3,4-c]n ratio. -3--3-yl}-2-(2-naphthyl)acetamide; 1H-NMR (DMSO-d6) d ppm: 8. 05-7. 33(m); 4.44(s); 3.80 ( s) ; 2. 95 (m); 2. 60 (m) ; 2 · 05 (m). N — (5 -acetone fluorenyl 6 - dihydrogen 0 to 0 each [3,4 a c] 0 to 0 sitting a 3-base) a 2-(2_Caiji) ethylamine N-[5- (2,2-dimethylpropionyl)-4,6-dihydroindole 11 each [3,4-c] π-pyrazol-3-yl]-2-(2-naphthyl)acetamide ;1H-NMR (DMSO-d6) d ρρπκ 7. 90-7.40 (m); 3.80 (s); l.20 (s). N-(5-butyl-2-indolyl-4,6-dihydrogen 0 to D each [3, 4_c] is 0-group than 0) 2-(2-naphthyl)acetamide; 1H-NMR (DMS0-d6) d ppm: 7.90 - 7.40 (m); 3.80 (s); 1. 20 (s). N-[5-(3-iodo-4-mercaptophenyl)-4,6-dihydroindolo[3,4-c]pyrazol-3-yl]-2-(2-naphthalene) Acetylamine; 1H-NMR (DMSO-d6) d ppm: 10.72 (s); 8.05-7.35 (m); 4.45 (s); 3.710 (s); 2.37 (s) o N-{5-[ ( _ yloxy) ethinyl]-4,6 -dihydro n ratio p and [3,4-c] 吼〇-3-yl}-2-(2-naphthyl)acetamide; 1H - NMR (DMS0-d6) d ρρηκ 7.90-7.20 (m); 4.25-4.70 (m); 4.20 (s); 3.80 (s). N-{5-(2-H-2-phenylethenyl)-4,6-dihydroindole 17 and [3, 4-c]-portazol-3-yl}-4-third Benzoguanamine; 1H-NMR (DMS0-d6) d ppm: 7.8-8.0 (m); 7.4-7.6 (m); 6.0-6·5 (m); 4.2-5.0 (m). N-{5-(2_ gas-2-phenylethyl)-4,6-diaza D ratio slightly [3, 4-c] 0-pyrazol-3-yl}-4-phenoxybenzene Formamide; 1H-NMR (DMS0-d6) d ppm: 7.8-8.0 (m); 7.4-7.6 (m); 4.2-5.0 (m).

C:\2D-C0DE\91-01\90119473.ptd 第205頁 1327569 五、發明說明（203) N-{5-(2-°S吩基-乙醞基）—4，6 -二氫0比11 各并[3,4-c] 0比0坐 -3-基}-4-(4-甲基哌啡基）笨甲醯胺；1H_NMR (DMS〇_d6) d PPm：7.8-8.0(m)；6.8-7.〇(m)；4. 6-4.8(d);4.4-4.5(d); 3.7(s);2.3(s)。 N-{5-(3-甲基-丁醢基）_4，6_二氳n比洛并[3，4_c] 0比0坐 -3-基）-4-(4-曱基哌畊基）笨曱醯胺；1H_NMR (DMS〇_d6) d ppm:7. 8-8. 0(m)；6.8-7. 〇(m);4. 6-4.8(m);4. 4-4. 5(m); 2.3(t);2.1-2.0(m)。 N-{5-(2 -咬喃甲醯基）一4, 6_二氫吡咯并[3, 4_c]吡唑_3_ ^•基}-4-(4-曱基旅畊基）苯甲醯胺；1H_NMR (DMS〇_d6) d ppm:7.8-8. 0(m)；7.2-7.4(m)；6. 8-7.0(m);5. 0-4.8(d); 4.6-4.7(d);2.l(s)。 N-{5 -苯基乙酿基-4, 6—二氫吡咯并[3, 4_c]吡唑_3_ 基}-4-(4-甲基旅畊基）苯甲醯胺；1H_NMR (DMS〇_d6) d ppm:7.8-8.0(m)；6.8-7.〇(m)；5.0-4.8(m);4. 6-4. 7(m)； 3.7(s)。 N-{5 -苯磺醯基-4, 6 -二氫吡咯并[3, 4_c]吡唑_3_基} -4-(4-甲基呢喷基）笨甲醯胺；1H_NMR (MS〇_d6) ^ ppm: .7. 8-8.0(m);7.5-7.7(m);7.2-7.3(m)。 N-(2’6_—乙基苯基卜n，_{3_[4_(4_曱基哌畊基）苯甲醯 (DMSO-d6) d PPm：7.8-8.0(m)；7.0-7.2(m);2.5-2.6(ni) ;1.1-1.2(m)。 N-乙基-Ν’ -{3-[4-(4-甲基哌畊基）苯曱醯胺]_4, 6_二氫C:\2D-C0DE\91-01\90119473.ptd Page 205 1327569 V. INSTRUCTIONS (203) N-{5-(2-°S-Benyl-ethenyl)-4,6-dihydrogen 0 Ratio of 11 to [3,4-c] 0 to 0--3-yl}-4-(4-methylpiperidinyl) benzoic acid; 1H_NMR (DMS〇_d6) d PPm: 7.8-8.0 (m); 6.8-7. 〇 (m); 4. 6-4.8 (d); 4.4-4.5 (d); 3.7 (s); 2.3 (s). N-{5-(3-methyl-butylindolyl)_4,6-dioxin npiroxi[3,4_c] 0 to 0--3-yl)-4-(4-mercapto-peptidyl)曱醯amine; 1H_NMR (DMS〇_d6) d ppm: 7. 8-8. 0(m); 6.8-7. 〇(m); 4. 6-4.8(m); 4. 4-4. (m); 2.3(t); 2.1-2.0(m). N-{5-(2-N-carbamoyl)- 4,6-dihydropyrrolo[3,4_c]pyrazole_3_^•yl}-4-(4-anthracenyl)醯amine; 1H_NMR (DMS〇_d6) d ppm: 7.8-8. 0(m); 7.2-7.4(m); 6. 8-7.0(m); 5. 0-4.8(d); 4.6-4.7 (d); 2.l(s). N-{5-phenylethyl-brom-4,6-dihydropyrrolo[3,4_c]pyrazole-3-yl}-4-(4-methyl bridging) benzalkonium; 1H_NMR (DMS 〇_d6) d ppm: 7.8-8.0 (m); 6.8-7. 〇 (m); 5.0-4.8 (m); 4. 6-4. 7 (m); 3.7 (s). N-{5-Benzenesulfonyl-4,6-dihydropyrrolo[3,4_c]pyrazole-3-yl}-4-(4-methylthyl)pyridylcarboxamide;1H_NMR (MS 〇_d6) ^ ppm: .7. 8-8.0(m); 7.5-7.7(m); 7.2-7.3(m). N-(2'6--ethylphenylbu-n, _{3_[4_(4_decylpiperyl)benzamide (DMSO-d6) d PPm: 7.8-8.0 (m); 7.0-7.2 ( m); 2.5-2.6(ni); 1.1-1.2(m). N-ethyl-Ν'-{3-[4-(4-methylpipedyl)benzamine]_4, 6_2 hydrogen

C:\2D-Q0DE\91-01\90119473.ptd 第206頁 1327569 五、發明說明（204) 吡咯并[3, 4-c]咄唑-5 -基}脲；1H-NMR (DMSO-d6) d ρρπκ 7.8-8.0(m);6.9-7.1(m);3.0-3,l(m);l.；l-1.2(m)。 N-{5-(2-氟-2-苯基乙醯基）-4，6 -二氫0比洛并[3，4-c] 口比唑-3-基}-[4-(卜吡咯啶-2 -酮）苯曱醯胺];1H-NMR (DMSO-d6) d ppm:7.9-8. 1(m)；7. 7-7. 8(m) ;3.8-4. 0(m); 2.5-2_ 6(m);2. 1-2.0(s)。 N-{5-(2-氟_2 -苯基乙醯基）-4，6 -二氫°比17各并[3, 4-c] 0比唑-3-基}-4-(4-甲基哌畊基）苯曱醯胺 N-{5-(2-°塞冷基乙酿基）-4,6 -二氫°比〇各并[3,4-c] °比吐 -3 -基}-胡椒基醯胺；111-關1^(〇15〇-(16)(10口111:7.6〇-6.96(m，6H);6.11(s，2H);4.77-4.48(in，4H);3.95(m，2H)。 N-{5-(3-甲基-丁醯基）-4,6 -二氫吼洛并[3,4-c]B比嗤 _3-基}-胡椒基酿胺；1H-NMR (DMSO-d6) d ppm:12.35 (1H);10. 70(m, 1H), 7. 56-7. 00(m, 3H), 6. 10(s, 2H), 4. 65-4 • 45(m，4H)，2.21-2.05(m，3H),0.93(6H)。 N-{5-(2 -咬喃曱醯基）_4,6 -二氫11比11 各并[3,4-(：]〇比〇坐-3-基}-胡椒基醯胺；111-關1^(1)材50-(16)(1?口111:7.93-7. 89(m, 1H);7. 57-7. 49(m, 2H), 7. 14-7. 00(m, 2H), 6. 67(m, lH),6.10(s，2H)，5.01-4.67(m，4H) ° N-{5 -苯基乙醯基）_4, 6 -二氫D比咯并[3, 4-c]咄唑-3-基 }-胡椒基醯胺；1H-NMR (DMS0-d6) d ppm: 7.61-7.00(m， 8H), 6. l〇(s，2H)，4. 74-4. 47(m，4H)，3. 72(2H) ° N-{5_苯磺醯基）_4, 二氩°比咯并[3,4_c] e比哇基卜胡椒基醯胺；1H-NMR (DMSO-d6) d ρρπκ 7.88-6.98C:\2D-Q0DE\91-01\90119473.ptd Page 206 1327569 V. INSTRUCTIONS (204) Pyrrolo[3,4-c]oxazol-5-yl}urea; 1H-NMR (DMSO-d6 d ρρπκ 7.8-8.0 (m); 6.9-7.1 (m); 3.0-3, l (m); l.; l-1.2 (m). N-{5-(2-fluoro-2-phenylethenyl)-4,6-dihydro- 0-l-[3,4-c]-port-azol-3-yl}-[4-(b Pyrrrolidine-2-one phenyl hydrazide]; 1H-NMR (DMSO-d6) d ppm: 7.9-8. 1 (m); 7. 7-7. 8 (m); 3.8-4. 0 ( m); 2.5-2_ 6(m); 2. 1-2.0(s). N-{5-(2-fluoro-2-phenylethenyl)-4,6-dihydrogen ratio 17 and [3, 4-c] 0-pyrazol-3-yl}-4-(4 -methylpipedyl) benzoguanamine N-{5-(2-°Sexy-ethylidene)-4,6-dihydrogen ratio 〇[3,4-c] ° ratio spit 3-based}-piperidinylamine; 111- Guan 1^(〇15〇-(16)(10-port 111:7.6〇-6.96(m,6H); 6.11(s,2H);4.77-4.48(in , 4H); 3.95 (m, 2H). N-{5-(3-methyl-butenyl)-4,6-dihydroindolo[3,4-c]B is more than 嗤3-3-} Piperamine; 1H-NMR (DMSO-d6) d ppm: 12.35 (1H); 10.70 (m, 1H), 7. 56-7. 00(m, 3H), 6. 10(s, 2H ), 4. 65-4 • 45 (m, 4H), 2.21-2.05 (m, 3H), 0.93 (6H). N-{5-(2 - 咬曱醯 ))_4,6-dihydrogen 11 More than 11 each [3,4-(:]〇〇 -3--3-yl}-piperonyl decylamine; 111-off 1^(1) material 50-(16) (1? mouth 111:7.93-7 89(m, 1H); 7. 57-7. 49(m, 2H), 7. 14-7. 00(m, 2H), 6. 67(m, lH), 6.10(s, 2H), 5.01-4.67 (m, 4H) ° N-{5-phenylethenyl)_4,6-dihydro D is more than [<">> 1H-NMR (DMS0-d6) d ppm: 7.61-7.00 (m, 8H), 6. l〇(s, 2H), 4. 74-4. 47(m, 4H), 3. 72(2H) ° N-{5_phenylsulfonyl)_4, Ar ° and slightly more than [3,4_c] e ratio wow Jibu piperonyl Amides; 1H-NMR (DMSO-d6) d ρρπκ 7.88-6.98

C:\2D-O0DE\91-Ol\9O119473.ptd 第207頁 1327569 五、發明說明（205) (m，8H), 6. ll(s，2H)，4. 48-4. 34(m，4H) ° N-{5-(2-三氟甲基）苯續醯基_4，6-二氫°比0各并[3,4-c] "比《坐-3-基}-胡椒基醯胺；1H-NMR (DMSO-d6) d ppm: 8. 04-6· 98(m，7H), 6. 12(m，2H)，4. 64-4. 49(m，4H)。 N-乙基-Ν’ -{3-胡椒基羧醯胺基-4, 6-二氫吡咯并 [3, 4-c]咄唑-5 -基}脲；111-01{(01^0-(16)〇1??111:7.62-6.98(m，3H);6.1(s，2H)，4.41-4.38(m，4H)，3.2(m，2H)，1.0 l(t，3H)。 N-{5_乙酿基- 4，6 -二氫π比咯并[3，4-c] °比0坐_3_基}_乙酿 .胺； N-{5-乙酿基_4，6 -二氫p比p各并[3，4-c] 0比0坐-3-基丨-環丙烷羧醯胺； N-{5-乙醯基_4，6 -二氫0比0各并[3，4-c] 0比°坐-3-基}-異丁醯胺； N_{5-乙酿基_4，6 -二氫d比p各并[3，4-c] 坐_3_基}-環戍烷羧醯胺； N-{5-乙酿基_4，6-二氫〇比嘻并[3，4-c] D比ρ坐- 3-基}-苯曱醯胺； _ Ν-{5-乙酿基_4，6 -二氫0比ρ各并[3，4-c] 0比坐-3_基}_曱基 P吡啶甲醯胺； N-{5-乙酿基_4，6_二氫〇比洛并[3，4_c] 坐_3-基}_於驗醯胺； 1^-{5-乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-異菸鹼醯胺；C:\2D-O0DE\91-Ol\9O119473.ptd Page 207 1327569 V. Description of invention (205) (m, 8H), 6. ll(s, 2H), 4. 48-4. 34(m, 4H) ° N-{5-(2-trifluoromethyl)benzene hydrazino group _4,6-dihydrogen ratio 0 and [3,4-c] " than "sit-3-yl}- Piperonyl decylamine; 1H-NMR (DMSO-d6) d ppm: 8. 04-6·98 (m, 7H), 6. 12 (m, 2H), 4. 64-4. 49 (m, 4H) . N-ethyl-Ν'-{3-piperylcarboxylamido-4,6-dihydropyrrolo[3,4-c]indazol-5-yl}urea; 111-01{(01^0 - (16) 〇1?? 111: 7.62-6.98 (m, 3H); 6.1 (s, 2H), 4.41-4.38 (m, 4H), 3.2 (m, 2H), 1.0 l (t, 3H). N-{5_乙牛基-4,6-dihydropi-pyrene-[3,4-c] ° is 0 _3_基}_乙乙.amine; N-{5-乙酿基_ 4,6-dihydrop ratio p and each [3,4-c] 0 to 0--3-ylindole-cyclopropanecarboxamide; N-{5-ethenyl_4,6-dihydrogen 0 Ratio of 0 to [3,4-c] 0 to ° -3-yl}-isobutylamine; N_{5-ethyl-branched _4,6-dihydro d ratio p and [3,4- c] sit _3_yl}-cyclodecanecarboxamide; N-{5-ethyl aryl-4,6-dihydroindole 嘻[3,4-c] D ratio ρ sit-3-yl }-benzoguanamine; _ Ν-{5-ethyl-branched _4,6-dihydro- 0-ratio ρ[3,4-c] 0 than sitting -3_yl}-mercapto P-pyridine Amine; N-{5-ethyl-branched _4,6-dihydroindolebi[3,4_c] sitting _3-yl}-in testin; 1^-{5-ethinyl-4, 6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-isonicotinamine amide;

C:\2D-CDDE\91-01\90119473.ptd 第208頁 1327569 五、發明說明（206) N_{5_乙酿基_4，6_二氮0比11 各弁[3，4-c] 0比0坐_3_基}_3_曱基-2-呋喃曱醯胺； N_{5_乙酿基_4，6 -二氮°比°各并[3，4-c] D比。坐-3-基}_°塞吩 -2-羧醯胺； N-{5-乙醯基- 4,6 -二氫D比0各并[3,4-c] °比°坐-3-基}-°塞吩 _ 3 _叛胺； N-{5_乙酿基_4，6_二氮0比°各弁[3，4_c] °比0坐_3-基}_鄰_ 曱苯曱醯胺； N-{5-乙醯基-4, 6 -二氫吼11各并[3, 4-c] D比。坐-3-基}-間-曱苯曱醯胺； ^1-{5-乙醢基-4，6-二氫0比17各并[3，4-(：]11比。坐-3-基}-對-曱苯甲醯胺； N_{5-乙酿基_4，6—二氫°比口各并[3，4-c] D比0坐_3 -基}—水楊醯胺； N_{5-乙酿基-4，6_二氮11比11 各并[3，4_c] D比°坐-3-基}_2-氟苯甲醯胺； N - { 5 -乙醯基-4，6 -二II 0比0各并[3，4 - c ]吼°坐-3 -基} - 3 -氟苯甲醯胺； N-{5-乙醯基- 4,6 -二氫吼。各并[3,4-c] °比。坐-3-基}-4-氟苯曱醯胺； 1^-{5-乙醯基-4，6-二氫吼>1各并[3,4-(：]°比〇坐-3-基}-17塞吩 -2-乙醯胺； N_{5-乙酿基_4，6_二氮'各并[3，4_c] °比°坐-3-基}_°塞吩 -3-乙醯胺；C:\2D-CDDE\91-01\90119473.ptd Page 208 1327569 V. Description of invention (206) N_{5_乙酿基_4,6_Dinitrogen 0 to 11 弁[3,4-c ] 0 to 0 sitting _3_ base}_3_mercapto-2-furoamine; N_{5_ethyl-branched _4,6-diaza ratio ° and [3,4-c] D ratio . Sodium-3-yl}_°cephen-2-carboxamide; N-{5-ethenyl- 4,6-dihydrogen D is 0 and each [3,4-c] °°°-3 -基}-°cetin _ 3 _ defensin; N-{5_ethyl ketone _4,6_dinitrogen 0 ratio ° 弁 [3,4_c] ° ratio 0 sitting _3-base}_ neighbor _ Anthranilamide; N-{5-ethinyl-4,6-dihydroindole 11 each [3, 4-c] D ratio. -3--3-yl}-m-p-benzoylamine; ^1-{5-ethenyl-4,6-dihydrogen 0 to 17 each [3,4-(:]11 ratio. sitting-3 -基}-p-nonylbenzamide; N_{5-ethyl-branched _4,6-dihydrogen ratio each [3,4-c] D ratio 0 sitting_3 -yl}-salt Indoleamine; N_{5-ethenyl-4,6-diaza 11 to 11 each [3,4_c] D ratio °-3-yl}_2-fluorobenzamide; N - { 5 - B Mercapto-4,6-di II 0 to 0 each [3,4 - c ]吼° sitting -3 -yl} - 3 -fluorobenzamide; N-{5-ethenyl- 4,6 - indoline, each [3,4-c] ° ratio, sit-3-yl}-4-fluorobenzamide; 1^-{5-ethinyl-4,6-dihydroanthracene ;1 each [3,4-(:]° than 〇 -3-yl}-17 cephen-2-yl decylamine; N_{5-ethyl-branched _4,6-dinitrogen] 3,4_c] °°°-3-yl}_°cetin-3-acetamide;

C:\2D-C0DE\91-01\90119473.ptd 第209頁 1327569 五、發明說明（207) 1^-{5-乙醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-苯基丙炔醯胺； !^-{5-乙醯基-4，6-二氫0比11各并[3,4-(：]':1比11坐_3-基}-3-氰基苯甲醯胺； N-{5-乙醯基- 4,6 -二氫p比p各并[3,4-c] 0比0坐-3-基}-4-氰基苯甲醯胺； N-{5-乙醯基- 4,6 -二氫n比p各并[3,4-c]吼吐-3-基}-反-桂皮醯胺； N - { 5 -乙醯基-4，6 -二氫D比0各并[3，4 - c ] σ比唾-3 -基}-順-桂皮醯胺； Ν-{5_乙酿基_4，6_二氮吼17各并[3，4-c] 0比0坐_3-基}-3_ (3 -吡啶基）丙烯醯胺； Ν_{5_乙酿基_4，6_二氮。比*7各并[3，4_c] 0比α坐_3 -基}_3_ (4 -吡啶基）丙烯醯胺； Ν-{5-乙酿基-4，6_二氫ρ比略并[3，4-c] π比0坐-3-基}-2 -苯基丙醯胺； Ν-{5-乙酿基-4,6 -二氫吼11各并[3，4-c] °比哇-3-基}-鄰-甲苯基乙醯胺； N-{5_乙酿基_4，6_二氫°比略并[3，4~*c]"比。坐-3-基}-間-胃曱苯基乙醯胺； N-{5-乙醯基-4,6-二氫°比洛并[3,4-c] °比°坐-3-基}-對-曱苯基乙醯胺； ^{5-乙醯基-4,6-二氫吡咯并[3,4-(：]呲唑-3-基}-鄰-茴香醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 209 1327569 V. INSTRUCTIONS (207) 1^-{5-Ethyl-4,6-dihydropyrrolo[3,4-〇] Pyrazol-3-yl}-phenylpropynylamine; !^-{5-ethenyl-4,6-dihydrogen 0 to 11 each [3,4-(:]': 1 to 11 sitting _3-yl}-3-cyanobenzamide; N-{5-ethenyl- 4,6-dihydrop ratio p and [3,4-c] 0 to 0--3-yl }-4-cyanobenzamide; N-{5-ethinyl- 4,6-dihydron ratio p and [3,4-c]pyrid-3-yl}-anti-cassia Amine; N - { 5 -ethinyl-4,6 -dihydro D ratio 0 each and [3,4 - c ] σ than sal -3 -yl}-cis-cinnamin; Ν-{5_B Brewing base_4,6_diazepine 17 and [3,4-c] 0 to 0 sitting _3-yl}-3_(3-pyridyl)propenylamine; Ν_{5_乙酿基_4 , 6_ dinitrogen. Ratio *7 each and [3,4_c] 0 than α sitting _3 -yl}_3_ (4-pyridyl) acrylamide; Ν-{5-ethyl aryl-4,6_2 The hydrogen ρ ratio is slightly [3,4-c] π is 0 -3-yl}-2-phenylpropanamide; Ν-{5-ethyl aryl-4,6-dihydroindole 11 each [ 3,4-c] ° than wow-3-yl}-o-tolylacetamide; N-{5_ethyl-branched _4,6-dihydrogen ratio slightly [3,4~*c] "比.坐-3-基}-Inter-gastric phenylacetamide; N-{5-B Mercapto-4,6-dihydro-pyrolo[3,4-c] ° ratio -3-yl}-p-indole phenyl acetamide; ^{5-ethenyl-4,6 - dihydropyrrolo[3,4-(:]oxazol-3-yl}-o-anisylamine;

C:\2D-CODE\91-01\90119473.ptd 第210頁 1327569 五、發明說明（208) N-{5-乙酿基- 4,6 -二氮°比洛并[3，4 - c] °比〇坐_3-基}_3-甲氧苯甲醯胺； N-{5-乙醯基-4, 6 -二氫吡咯并[3, 4-c] °比唑-3 -基}-對-茴香醯胺； N-{5-乙酿基- 4,6 -二氫吼11 各并[3,4-c] °比°坐-3-基}-苯氧乙醯胺； N-{5-乙醢基-4, 6 -二氫°比°各并[3, 4-c] °比°坐-3 -基}-2-氟苯基乙醯胺； N-{5_乙酿基_4，6 -二氮0比°各并[3，4-c] π比。坐-3-基}_3-氟苯基乙醯胺； Ν-{5-乙酿基-4，6 -二氮D比ρ各并[3，4-c] 0比。坐-3-基}-4_氟苯基乙醯胺； 1{5-乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3-(2 -噻吩基）丙烯醯胺； N-{5_乙酿基_4，6_二氮0比17各弁[3，4-c] D比。坐_3-基}_3-(3 -嘍吩基）丙烯醯胺； N_{5_乙酿基_4，6_二氮D比11 各并[3，4_c] D比。坐-3-基}_3_ (2 -嘍吩基）丙醯胺；苯甲醯胺； N-{5-乙酿基-4，6 -二氮0比p各并[3，4_c] π比°坐-3 -基}-3_氯苯曱醯胺； Ν-{5_乙酿基-4，6_二氮0比ρ各并[3，4_c]吼〇坐-3-基}_4~氯苯甲醯胺；C:\2D-CODE\91-01\90119473.ptd Page 210 1327569 V. INSTRUCTIONS (208) N-{5-Ethyl- 4,6-diaza-pyrolo[3,4-c ° ° 〇 _3-yl}_3-methoxybenzamide; N-{5-ethinyl-4,6-dihydropyrrolo[3, 4-c] ° azole-3-yl }-p-anisoleamine; N-{5-ethyl-bromo- 4,6-dihydroindole 11 each [3,4-c] ° ratio of -3-yl}-phenoxyacetamide; N-{5-ethinyl-4,6-dihydrogen ratio °[3, 4-c] ° ratio -3 -yl}-2-fluorophenylacetamide; N-{5 _ B-based 4,6-diaza 0 ratio ° [3,4-c] π ratio. -3--3-yl}_3-fluorophenylacetamide; Ν-{5-ethyl-branched-4,6-diaza D ratio ρ and [3,4-c] 0 ratio. -3--3-yl}-4_fluorophenylacetamide; 1{5-acetamido-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3- (2-thiophenyl) acrylamide; N-{5_ethyl-branched _4,6-diaza 0 to 17 弁[3,4-c] D ratio. Sit _3-基}_3-(3 -nonyl)propenylamine; N_{5_ethylidene_4,6-dinitrogen D ratio 11 and [3,4_c] D ratio. Sodium-3-yl}_3_ (2-anthracenyl) Propylamine; benzepidine; N-{5-ethenyl-4,6-diaza 0 to p and [3,4_c] π ratio ° sit-3-yl}-3_chlorophenylhydrazine Amine; Ν-{5_乙牛基-4,6_二氮0 ratio ρ和[3,4_c]吼〇-3-yl}_4~chlorobenzamide;

C:\2D-O0DE\91-01\9O119473.ptd 第211頁 1327569 五、發明說明（209) N-{5-乙酿基_4，6_二氮π比p各并[3，4_c] D比0坐_3-基}-1-口瓜。定丙酿胺； N-{5-乙酿基-4，6 -二氫吼11 各并[3，4-c] D比〇坐-3-基}-2-乙醯基苯曱醯胺； N-{5-乙酿基- 4,6 -二氫0比D各并[3，4-c] °比°坐-3-基}_4-乙醯基苯曱醯胺； N_{5-乙酿基-4，6_二氮π比σ各弁[3，4_c] D比σ坐-3~基}-1_ 曱醯胺； Ν_{5_乙酿基_4，6 -二氮°比ρ各并[3，4-c] °比〇坐_3_基}_2_ •曱醢胺； ^{5-乙醯基-4，6-二氫0比洛并[3，4-(：]0比°坐-3-基}-3-苯曱醯基丙醯胺； Ν-{5-乙酿基-4,6 -二氫各并[3，4-c] °比°坐-3-基}-4-乙醯胺基苯甲醯胺； N-{5-乙醢基-4,6 -二氫D比洛并[3，4-c] 0比。坐-3-基}-2，5-二甲氧苯曱醯胺； N-{5_ 乙酿基-4，6 -二氫0比 p各并[3，4-c] p比0坐-3-基}-2，6-二甲氧苯甲醯胺； —N-{5-乙酿基_4，6_二氮D比卩各弁[3，4-c] °比〇坐-3-基}-3，4-w二甲氧苯曱醯胺； N_{5_ 乙酿基-4，6_ 二氮 °比 17各弁[3，4_c] D比0坐_3_ 基}-3，5-二甲氧苯甲醯胺； N-{5_乙酿基-4，6_二氮0比洛弁[3，4-c] 0比〇坐-3-基}_3_ (2-噻吩甲醯基）-丙醯胺；C:\2D-O0DE\91-01\9O119473.ptd Page 211 1327569 V. INSTRUCTIONS (209) N-{5-Ethyl _4,6_Dinitrogen π ratio p[3,4_c] D is 0 to _3-base}-1-mouth. Acrylamine; N-{5-ethyl-branched-4,6-dihydroindole 11 each [3,4-c] D is more than 〇-3-yl}-2-ethenylbenzamide ; N-{5-ethyl-branched- 4,6-dihydrogen 0 to D each [3,4-c] ° ratio sit-3-yl}_4-ethylmercaptobenzamine; N_{5 -B-Bry-based-4,6_Dinitrogen π ratio σ[3,4_c] D ratio σ sitting -3~yl}-1_ decylamine; Ν_{5_乙酿基_4,6-diaza ° ratio ρ and [3,4-c] ° ratio 〇3_基}_2_ • guanamine; ^{5-acetamido-4,6-dihydro 0 piroxi[3,4- (:]0°°-3-yl}-3-phenylmercaptopropylamine; Ν-{5-ethyl-branched-4,6-dihydro-[3,4-c] ° ratio Sodium-3-yl}-4-acetamidobenzamide; N-{5-ethinyl-4,6-dihydro Dbi-l[3,4-c] 0 ratio. -yl}-2,5-dimethoxybenzamine; N-{5_ethyl-branched-4,6-dihydrogen 0 to p and [3,4-c] p is 0--3-yl }-2,6-dimethoxybenzamide; —N-{5-ethyl-branched _4,6-diaza D is more than 卩[3,4-c] ° 〇-3-yl }-3,4-w-dimethoxybenzamine; N_{5_ ethyl-branched-4,6-diaza ratio 17 弁[3,4_c] D ratio 0 sitting_3_ base}-3,5- Dimethoprimamide; N-{5_ethyl-branched-4,6-diaza-pyrene [3,4-c] 0 is more than 〇-3-yl}_3_(2-thienylmethyl)-propanamine;

C:\2D-C0DE\91-01\90119473.ptd 第212頁 1327569 五、發明說明（210) N-{5 -乙酿基-4，6 -二氮°比°各并[3，4-c] °比°坐_3_基}-1_ 基乙醯胺； N_{5-乙酿基-4，6 -二氫11比p各并[3，4-c] p比0坐_3_基}-4-苯基笨曱醯胺； N-{5-苄基-4, 6 -二氫σ比0各并[3，4-c]吼。坐-3-基}-乙酸胺； Ν-{5-窄基-4, 6 -二氫吼ρ各并[3,4-c] °比°坐-3-基}-環丙烧羧醯胺； N-{5-苄基-4，6 -二氫°比0各并[3，4-c] D比。坐-3-基}-異丁酸胺； N-{5-窄基-4，6 -二氫°比0各并[3，4-c] °比°坐-3-基}-環戊烧羧醯胺； N-{5-芊基-4，6-二氫11比0各并[3，4-c] °比〇坐-3-基}-苯曱醯胺； N-{5-苄基- 4,6 -二氫吼17各并[3，4-c] °比0坐-3-基卜曱基°比啶甲醯胺； N-{5-窄基-4，6 -二氫吼11 各并[3,4-c] n比°坐-3-基}-於驗酿胺； 1^-{5-爷基-4，6-二氫11比略并[3，4-(：]'3比°坐-3-基}-異於驗醯胺； 1^-{5-芊基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-3-曱基 -2 -咳喃曱醯胺； N-{5-辛基-4, 6 -二氫D比ρ各并[3,4-c] °比。坐-3-基}-°塞吩 -2 -叛酿胺；C:\2D-C0DE\91-01\90119473.ptd Page 212 1327569 V. INSTRUCTIONS (210) N-{5-Ethyl-4,6-diaza°°°[3,4- c] ° ratio ° sitting _3_ base}-1_ acetylamine; N_{5-ethyl aryl-4,6-dihydro 11 ratio p and [3,4-c] p ratio 0 sitting_3 _ yl}-4-phenyl azelaamine; N-{5-benzyl-4,6-dihydro σ ratio 0 and [3,4-c] oxime. -3--yl}-acetic acid amine; Ν-{5-narrow-based-4,6-dihydroindole ρ[3,4-c] ° ratio of sitting-3-yl}-cyclopropanone Amine; N-{5-benzyl-4,6-dihydrogen ratio 0 and [3,4-c] D ratio. Sodium-3-yl}-isobutyric acid amine; N-{5-narrow base-4,6-dihydrogen ratio 0 and [3,4-c] ° ratio sit-3-yl}-cyclopentyl Carbarylamine; N-{5-mercapto-4,6-dihydrogen 11 to 0 each [3,4-c] ° 〇-3-yl}-benzoguanamine; N-{5 -benzyl- 4,6-dihydroanthracene 17 each [3,4-c] ° is 0--3-dibupyridylpyridylpyridylamine; N-{5-narrow base-4,6-two Hydroquinone 11 and [3,4-c] n ratio °-3-yl}-in the amine; 1^-{5-yote-4,6-dihydro 11 ratio slightly [3,4 -(:]'3 is more than -3 yl} - different from proline; 1^-{5-mercapto-4,6-dihydropyrrolo[3,4-anthracene]pyrazole-3 -yl}-3-mercapto-2-c-decylamine; N-{5-octyl-4,6-dihydrogen D ratio ρ and [3,4-c] ° ratio. Base}-°cetin-2 - apoemic amine;

C:\2D-OODE\91 -01\90119473.ptd 第213頁 1327569 五、發明說明（211) 1{5-苄基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-噻吩 -3 -羧醯胺； N-{5-苄基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-鄰-甲苯曱醯胺； N-{5_辛基_4，6_二氨°比0各弁[3，4_c] 0比0坐_3_基}_間-曱苯曱醯胺； N-{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-對-曱苯曱醯胺； N-{5-苄基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}-苯基乙蜃醢胺； N-{5_窄基_4，6_二氮吼11 各弁[3，4_〇]°比吐_3_基}_水楊酿胺； N-{5_窄基_4，6_二氯°比σ各弁[3，4_c] °比σ坐_3_基}_2-氣苯甲醯胺； Ν_{5_辛基_4，6 -二氫〇比ρ各并[3，4-c] 0比0坐-3-基}-3-氟苯曱醯胺； Ν_{5_罕基_4，6 -二氫吼D各并[3，4_c] °比°坐-3 -基}-4-氟苯曱醯胺； • N-{5-辛基_4，6_二氮n比p各弁[3，4-c] 0比0坐-3-基}_β塞吩 2 -乙醯胺； Ν_{5-罕基-4，6 -二氫吼11 各并[3，4-c] °比°坐-3-基}-D塞吩 -3 -乙醯胺； N-{5_节基_4，6 -二氫D比p各并[3，4-c] °比〇坐-3-基}-苯基丙炔醯胺；C:\2D-OODE\91 -01\90119473.ptd Page 213 1327569 V. INSTRUCTIONS (211) 1{5-Benzyl-4,6-dihydropyrrolo[3,4-(:]carbazole -3-yl}-thiophene-3-carboxycarboxamide; N-{5-benzyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-o-toluene Amine; N-{5_octyl_4,6-diamine ° ratio 0 弁 [3,4_c] 0 to 0 sitting _3_ base}_m-phenylhydrazine; N-{5-benzyl 4-,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-p-nonylbenzamide; N-{5-benzyl-4,6-dihydropurine And [3,4-(:]carbazol-3-yl}-phenylacetamide; N-{5_narrow base_4,6-diazaindole 11 弁[3,4_〇]°比吐_3_基}_水杨胺胺; N-{5_Narrow base_4,6_Dichloro ° ratio σ 弁 [3,4_c] ° ratio σ sit _3_ base}_2-gas benzene Methionine; Ν_{5_octyl_4,6-dihydroindole ratio ρ[3,4-c] 0 to 0 -3-yl}-3-fluorophenylamine; Ν_{5 _Hanji_4,6-dihydroindole D each [3,4_c] ° ratio sit-3-yl}-4-fluorobenzamine; • N-{5-octyl_4,6_ Diazo-n ratio p 弁[3,4-c] 0 to 0 -3-yl}_β-cetin 2 -acetamide; Ν_{5-罕基-4,6-dihydroindole 11 each [ 3,4-c] ° ratio -3-yl}-D cephene-3-acetamide; N-{ 5_ nodal group _4,6-dihydrogen D ratio p and [3,4-c] ° ratio 〇-3-yl}-phenylpropynyl decylamine;

C:\2D-O0DE\91-0I\9O119473.ptd 第214頁C:\2D-O0DE\91-0I\9O119473.ptd第214页

J 1327569 五、發明說明（212) N-{5 -苄基-4,6-二氫咄咯并[3,4-〇]咄唑-3-基}-3-氰基苯甲醯胺； 1^-{5-窄基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}-4-氰基苯甲醯胺； N-{5 -苄基-4,6-二氫咄咯并[3,4-〇]°比唑-3-基}-反-桂皮醯胺； N - { 5 -苄基-4，6 -二氫°比p各并[3，4 - c ] D比0坐-3 -基}-順-桂皮醯胺； N-{5 -苄基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-3-(3-吡啶基）丙烯醯胺； ^{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3-(4-0比π定基）丙稀醯胺； Ν-{5-窄基-4，6_二氫吼ρ各并[3，4-c] °比〇坐-3-基}-2 -苯基丙趨胺； Ν-{5 -苄基-4，6 -二氫0比ρ各并[3,4-c] D比。坐-3-基}-鄰-曱苯基乙醯胺； N_{5_窄基—4，6_二氫〇比口各并[3，4_c] 0比。坐―3-基}一間-甲苯基乙醯胺； N-{5_窄基_4，6_二氮0比洛并[3，4_c] π比°坐-3-基}-對-甲苯基乙醯胺； Ν-{5_窄基_4，6_二氮0比ρ各并[3，4 - c] °比〇坐-3-基}_鄰-菌香醯胺； Ν-{5-窄基- 4,6 -二氫吼口各并[3,4-c] °比〇坐-3-基}-3-甲氧苯甲醯胺；J 1327569 V. INSTRUCTION DESCRIPTION (212) N-{5-Benzyl-4,6-dihydroindolo[3,4-indolyl]oxazol-3-yl}-3-cyanobenzamide; 1^-{5-Narrow-based-4,6-dihydroindolo[3,4-(:]oxazol-3-yl}-4-cyanobenzamide; N-{5-benzyl -4,6-dihydroindolo[3,4-indenyl]-pyrazol-3-yl}-trans-cinsinamide; N-{5-benzyl-4,6-dihydrogen ratio p And [3,4 - c ] D is 0-base}-cis-cinnamate; N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]pyrazole- 3-yl}-3-(3-pyridyl)propenylamine; ^{5-benzyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3- (4-0 to π-based) acrylamide; Ν-{5-narrow-based-4,6-dihydroindole ρ[3,4-c] ° than 〇-3-yl}-2 - Phenylpropenamine; Ν-{5-benzyl-4,6-dihydrogen 0 to ρ and [3,4-c] D ratio. Sodium-3-yl}-o-indole phenylacetamide N_{5_Narrow base-4,6-dihydroindole has a ratio of [3,4_c] 0. Sit-3-yl}-m-tolylacetamide; N-{5_narrow base_ 4,6_Dinitrogen 0biol[3,4_c] π ratio °-3-yl}-p-tolylacetamide; Ν-{5_narrow base_4,6_diazo 0 ratio ρ Each [3,4 - c] ° is more than -3-yl}-o-bacteria; Ν-{5-narrow- 4,6-dihydropurine each [3,4-c] ° than 〇-3-yl}-3-methoxybenzamide;

C:\2D-CODE\91-01\90119473.ptd 第215頁 1327569 五、發明說明（213) N-{5-辛基-4, 6 -二氫0比σ各并[3,4-c] 0比。坐-3-基}-對-茴香醯胺； N-{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-苯氧乙醯胺； N-{5-节基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基卜2-氟苯基乙醯胺； N-{5 -辛基-4, 6 -二氫吡咯并[3,4-c]吡唑-3 -基卜3 -氟苯基乙醯胺； N_{5-牟基-4, 6 -二氫0比°各并[3，4-c] p比0坐-3-基}-4_氟苯 I®基乙醯胺； N-{5-辛基-4，6 -二氫 D比洛并[3，4_c]"比〇坐-3 -基}-3_(2_ 噻吩基）丙烯醯胺； N-{5-窄基-4，6 -二氮 π比 17各并[3，4-c] 0比 0坐 _3_ 基}-3-(3-噻吩基）丙烯醯胺； Ν_{5-辛基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-3-(2-噻吩基）丙酿胺； Ν-{5 -苄基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-2-氯苯甲醯胺； _ Ν-{5-窄基_4，6_二氮π比ρ各弁[3，4-c] 0比0坐_3_基}-3 -氣苯 ¥甲醯胺； Ν-{5-辛基-4，6 -二氫吼11 各并[3, 4-c] °比π坐-3-基}-4-氯苯曱醯胺； N_{5_辛基_4，6_二氮°比°各弁[3，4-c] °比d坐-3-基}_1_派°定丙酿胺；C:\2D-CODE\91-01\90119473.ptd Page 215 1327569 V. INSTRUCTIONS (213) N-{5-octyl-4,6-dihydrogen 0 to σ each [3,4-c ] 0 ratio. -3-yl}-p-anisylamine; N-{5-benzyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-phenoxyacetamide N-{5-nodal-4,6-dihydroindolo[3,4-(:]oxazol-3-yl-2-fluorophenylacetamide; N-{5-octyl- 4,6-dihydropyrrolo[3,4-c]pyrazol-3-yloxa-3-fluorophenylacetamide; N_{5-mercapto-4,6-dihydro- 0 ratio °[ 3,4-c] p is 0--3-yl}-4_fluorophenyl I® acetylamine; N-{5-octyl-4,6-dihydro D is more than [3,4_c] "比〇-3-3-yl}-3_(2_thienyl)propenylamine; N-{5-narrow base-4,6-diazo π ratio 17 and [3,4-c] 0 to 0 _3_yl}-3-(3-thienyl)propenylamine; Ν_{5-octyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3- (2-thienyl)propanol; Ν-{5-benzyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-2-chlorobenzamide; _ Ν-{5-Narrow base_4,6_Dinitrogen π ratio ρ弁[3,4-c] 0 to 0 sitting _3_基}-3 - benzene Benzene carbamide; Ν-{5- Octyl-4,6-dihydroindole 11 each [3, 4-c] ° ratio π-3-yl}-4-chlorophenylamine; N_{5_octyl_4,6_two Nitrogen ° ratio ° 弁 [3,4-c] ° ratio d sitting -3- base} _1 _ _ ° 定酿酿酿 ;;

C:\2D-OODE\91-Ol\90119473_ptd 第 216 頁 1327569 五、發明說明（214) N-{5-辛基-4，6 -二氮0比0各弁[3，4_c] 11比。坐_3_基}_2_乙酿基苯甲醯胺； N-{5-苄基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-4-乙醯基苯甲醯胺； N-{5-爷基-4, 6 -二氫n比0各并[3，4-c] 口比0坐-3-基}-1-蔡曱醯胺； 1{5-爷基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-2-萘曱醢胺； N-{5-辛基-4,6-二氫°比咯并[3,4-(：]吡唑-3-基}-3-苯甲酿基丙酿胺； N-{5-苄基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-4-乙醯胺基苯曱醯胺； N-{5-亨基-4，6 -二氫吼11各并[3,4-c] 口比。坐-3-基}-2，5 -二甲氧苯曱醯胺； N_{5_ 窄基-4，6_ 二氮 °比 ρ各并[3，4-c] 0 比 π坐 _3-基}-2，6 -二甲氧苯甲醯胺； Ν-{5_ 罕基 -4，6_ 二氮0比洛弁[3，4-c] 0比 °坐-3 -基}-3，4_ 二曱氧苯甲醯胺； Ν-{5-辛基-4，6 -二氫0比°各并[3，4-c]吼〇坐-3-基}-3，5 -二曱氧苯甲醯胺； Ν-{5_ 辛基_4，6_ 二氳0比 °各并[3，4_c] 0比0坐-3-基}-3-(2-噻吩甲醯基）-丙醯胺； Ν-{5_亨基_4，6_二氫各并[3，4-c] 0比唾-3-基}-2 -蔡基乙醯胺；C:\2D-OODE\91-Ol\90119473_ptd Page 216 1327569 V. INSTRUCTIONS (214) N-{5-octyl-4,6-diaza 0 to 0 弁[3,4_c] 11 ratio. _3_基}_2_Ethylbenzamide; N-{5-benzyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-4-B Mercaptobenzamide; N-{5-yote-4,6-dihydron-n to 0-[3,4-c] to 0--3-yl}-1-cainamide; 1{ 5-aryl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-2-naphthylamine; N-{5-octyl-4,6-di Hydrogen ratio of [3,4-(:]pyrazol-3-yl}-3-benzylidene propylamine; N-{5-benzyl-4,6-dihydropyrrolo[3, 4-c]pyrazol-3-yl}-4-acetamidobenzoguanamine; N-{5-henyl-4,6-dihydroindole 11 and [3,4-c] ratio -3-3-yl}-2,5-dimethoxybenzamine; N_{5_ narrow base-4,6_ dinitrogen ratio ρ and [3,4-c] 0 ratio π sitting_3- }}-2,6-dimethoxybenzamide; Ν-{5_ 罕基-4,6_二氮0比洛弁[3,4-c] 0°°坐-3 -基}-3, 4_ dioxobenzoguanamine; Ν-{5-octyl-4,6-dihydrogen 0 ratio °[3,4-c] 吼〇-3-yl}-3,5-di Oxybenzamide; Ν-{5_ octyl _4,6_ 氲0 ～°[3,4_c] 0 to 0 -3-yl}-3-(2-thienylmethyl)-propyl Indoleamine; Ν-{5_henyl_4,6-dihydro-[3,4-c] 0 is more than saliva-3- } -2 - CAI group as acetamide;

C:\2D-C0DE\91-01\90119473.ptd 第217頁 1327569 五、發明說明（215) N-{5-窄基-4，6 -二氫吼11各并[3，4-c] 0比0坐-3-基}-1-萘基乙醯胺； N-{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-苯基苯曱醯胺； Ν~·{5 -苯基乙基- 4,6 -二氫吼11 各并[3，4_c] D比。坐-3-基}_乙醯胺； N-{5 -苯基乙基-4，6 -二氫°比略并[3,4-c] °比°坐-3-基}-環丙烷羧醯胺； ^{5-笨基乙基-4,6-二氫咄咯并[3,4-〇]咄唑-3-基}-異丁醢胺； N-{5 -苯基乙基-4，6 -二氫吼11 各并[3，4_c] °比β坐_3-基}-環戊烷羧醯胺； Ν_{5_苯基乙基-4，6_二氮吼11各并[3，4_c] **比°坐-3-基}-苯甲醯胺； N-{5 -苯基乙基_4，6_二氮°比。各弁[3，4-c]吼〇坐_3 -基}_曱基咄啶甲醯胺； N-{5 -苯基乙基-4，6_二氫η比0各并[3.，4-c] **比〇坐-3-基}-终驗醯胺； • !'}-{5-苯基乙基-4,6_二氫°比洛并[3，4-〇]11比〇坐-3-基}-異於驗醯胺； Ν-{5 -苯基乙基-4，6_ 二氫 Btbp各并[3，4-c] 0比0坐-3-基}-3-甲基-2-呋喃甲醯胺； N-{5 -苯基乙基-4，6_二氫吼0各并[3，4-c] 0比0坐-3-基}-0塞吩-2 _缓醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 217 1327569 V. INSTRUCTIONS (215) N-{5-Narrow-based-4,6-dihydroindole 11 and [3,4-c] 0 to 0--3-yl}-1-naphthylacetamide; N-{5-benzyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}- 4-phenylbenzamide; Ν~·{5-phenylethyl-4,6-dihydroindole 11 each [3,4_c] D ratio. Sodium-3-yl}-acetamide; N -{5-phenylethyl-4,6-dihydrogen ratio slightly [3,4-c] ° ° sit-3-yl}-cyclopropane carboxamide; ^{5-stupylethyl -4,6-dihydroindolo[3,4-indene]oxazol-3-yl}-isobutylamine; N-{5-phenylethyl-4,6-dihydroindole 11 [3,4_c] ° is more than β _3-yl}-cyclopentane carboxamide; Ν_{5_phenylethyl-4,6-diazaindole 11 and [3,4_c] ** ratio ° Sodium-3-yl}-benzamide; N-{5-phenylethyl-4,6-diaza ratio. 弁[3,4-c]吼〇_3 -基}_曱Acridine carbenamide; N-{5-phenylethyl-4,6-dihydro-n ratio 0 and [3.,4-c] ** than 〇-3-yl}-final test Amine; • !'}-{5-phenylethyl-4,6-dihydro-pyrolo[3,4-〇]11 than 〇--3-yl}-different to decylamine; {5-Phenylethyl-4,6-dihydro Btbp And [3,4-c] 0 to 0--3-yl}-3-methyl-2-furancarboxamide; N-{5-phenylethyl-4,6-dihydroindole 0 each [3,4-c] 0 to 0 -3-yl}-0 phenan-2 _ valine amine;

C:\2D-OODE\91-Ol\90119473.ptd 第218頁 1327569 五、發明說明（216) N-{5 -苯基乙基-4,6-二氫°比咯并[3,4-(：]°比唑-3-基}-噻吩-3 -羧醯胺； 1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-鄰 -曱苯曱醯胺； N-{5-苯基乙基-4,6-二氫吼咯并[3,4-〇]吡唑-3-基}-間 -曱苯甲醯胺； 1\1-{5-苯基乙基-4,6-二氫"比咯并[3,4-〇]吡唑-3-基}-對 -曱苯曱醯胺； ^{5-苯基乙基-4,6-二氫°比咯并[3,4-〇]°比唑-3-基}-苯基乙醯胺； N-{5-苯基乙基-4，6 —二氫0比p各并[3，4-c] 0比0坐一3-基}-水楊醯胺； N-{5 -苯基乙基-4, 6 -二氮〇比σ各并[3, 4-c] 0比0坐-3-基丨- 2-氟苯曱醯胺； Ν-{5 -苯基乙基-4, 6 -二氫。比17各并[3, 4-c] ρ比。坐-3-基}-3-氟笨甲醯胺； Ν - {5_苯基乙基_4，6_二氮吼11 各弁[3，4_c] 11比哇-3-基}_4 -氟苯曱醯胺； N-{5 -苯基乙基- 4,6 -二氮°比0各并[3，4_c] 0比°坐_3-基}-°塞吩-2-乙醯胺； 1^-{5-苯基乙基-4,6-二氫0比11各并[3,4-。]'»比。坐-3-基}-0塞吩-3-乙醢胺； N_{5_苯基乙基_4，6_二氮〇比p各并[3，4_c] 0比0坐-3_基}_苯基丙炔醯胺；C:\2D-OODE\91-Ol\90119473.ptd Page 218 1327569 V. INSTRUCTIONS (216) N-{5-Phenylethyl-4,6-dihydrogen ratio [3,4- (:]°Bizozol-3-yl}-thiophene-3-carboxycarboxamide; 1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-anthracene]pyrazole- 3-yl}-o-nonylbenzamide; N-{5-phenylethyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-m-indole Benzalamine; 1\1-{5-phenylethyl-4,6-dihydro"bido[3,4-indolepyrazol-3-yl}-p-nonylbenzamide ;^{5-phenylethyl-4,6-dihydro-pyrolo[3,4-〇]°bazol-3-yl}-phenylacetamide; N-{5-phenylethyl Base-4,6-dihydrogen 0 to p each [3,4-c] 0 to 0 sit a 3-yl}-salicylimine; N-{5-phenylethyl-4,6-di The ratio of nitrogen to yttrium is σ[3, 4-c] 0 to 0 -3- 丨丨- 2-fluorophenyl hydrazide; Ν-{5-phenylethyl-4,6-dihydro. Each [3, 4-c] ρ ratio. Sodium-3-yl}-3-fluorobenzamide; Ν - {5_phenylethyl_4,6-diazepine 11 弁 [3, 4_c] 11-wow-3-yl}_4-fluorophenylguanamine; N-{5-phenylethyl-4,6-diaza ratio 0 and [3,4_c] 0 ratio ° sitting_3 -基}-°Cetene-2-acetamide; 1^-{5-phenylethyl-4,6- Hydrogen 0 to 11 and [3,4-.]'» ratio. Sodium-3-yl}-0-cetin-3-acetamide; N_{5_phenylethyl-4,6-diazepine Ratio p[3,4_c] 0 to 0 sitting -3_yl}_phenylpropynylamine;

C:\2D-OODE\91-01\90119473.ptd 第219頁 1327569 五、發明說明（217) N-{5 -苯基乙基_4，6_二氫°比ρ各并[3，4_c] °比。坐-3_基}-3_ 氰基苯曱醯胺； N-{5 -苯基乙基-4, 6 -二氫°比°各并[3,4-c] °比°坐-3-基}-4-氰基苯甲醯胺； N-{5 -苯基乙基- 4,6 -二氫°比°各并[3,4-c] °比。坐-3-基}-反 -桂皮醯胺； N - { 5 -苯基乙基-4，6 -二氫°比D各并[3，4 - c ] D比0坐-3 -基丨-順 -桂皮酿胺； N-{5 -苯基乙基-4，6 -二氫π比略并[3，4-c] °比〇坐-3-基}_3_ 馨C 3 -吡啶基）丙烯醯胺； Ν_{5 -苯基乙基_4，6_二氫D比略并[3，4_c] °比σ坐-3 -基}-3_ (4 -吡啶基）丙烯醯胺； Ν-{5 -苯基乙基-4，6 -二氫°比Β各并[3，4-c] °比°坐-3 -基}-2-苯基丙醯胺； Ν-{5 -苯基乙基-4，6 -二氫0比Β各并[3，4-c] °比°坐-3*~基}-鄰 -甲苯基乙醯胺； N-{5 -苯基乙基-4，6 -二氫。比17各并[3，4-c] 0比0坐-3-基}-間 -甲苯基乙醯胺；龜N-{5 -苯基乙基-4，6 -二氫0比σ各并[3，4-c] 0比0坐-3-基}-對 t甲苯基乙醯胺； N-{5 -苯基乙基-4，6 -二氫0比σ各并[3，4-c] 0比0坐-3-基}-鄰 -茴香醯胺； N_{5 -苯基乙基-4，6 -二氫吼π各并[3，4-c] 0比〇坐-3-基}-3-曱氧苯甲醯胺；C:\2D-OODE\91-01\90119473.ptd Page 219 1327569 V. INSTRUCTIONS (217) N-{5-Phenylethyl_4,6-dihydrogen ratio ρ[3,4_c ° ° ratio. Sitting -3_yl}-3_cyanobenzoguanamine; N-{5-phenylethyl-4,6-dihydrogen ratio ° and [3,4-c] ° ratio -3- } _ cyanobenzamide; N-{5-phenylethyl-4,6-dihydrogen ratio of [3,4-c] °. Sodium-3-yl}-trans-cinnamate; N-{5-phenylethyl-4,6-dihydrogen ratio D and [3,4 - c ] D ratio 0 sitting -3 -based - cis-casin amine; N-{5-phenylethyl-4,6-dihydroπ ratio slightly [3,4-c] ° 〇-3-yl}_3_ 馨 C 3 -pyridyl Acrylamide; Ν_{5-phenylethyl-4,6-dihydrogen D ratio slightly [3,4_c] ° ratio σ sitting -3 -yl}-3_ (4-pyridyl) acrylamide; Ν-{5-Phenylethyl-4,6-dihydrogen ratio Β[3,4-c] ° ratio of sitting -3 -yl}-2-phenylpropanamide; Ν-{5 -Phenylethyl-4,6-dihydrogen 0 is Β[3,4-c] °°°-3*~yl}-o-tolylacetamide; N-{5-phenyl Ethyl-4,6-dihydrogen. Ratio of 17 to [3,4-c] 0 to 0--3-yl}-m-tolylacetamide; turtle N-{5-phenylethyl-4,6-dihydro- 0 σ And [3,4-c] 0 is 0-O--3-yl}-p-t-tolylacetamide; N-{5-phenylethyl-4,6-dihydro- 0 is σ[3, 4-c] 0 to 0--3-yl}-o-anisamine; N_{5-phenylethyl-4,6-dihydroindole π[3,4-c] 0 -3-yl}-3-oxobenzoylamine;

C:\2D-CODE\91-01\90119473.ptd 第220頁 1327569 五、發明說明（218) 1^-{5-苯基乙基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-對 -茴香醯胺； N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-〇]。比唑-3-基}-苯氧乙醯胺； N-{5 -苯基乙基-4，6 -二氫0比σ各并[3，4-c] D比0坐-3 -基丨- 2-氟苯基乙醯胺； N-{5_苯基乙基-4，6 -二氮0比17各并[3，4-c] °比。坐-3-基丨-3-氟苯基乙醯胺； 1^-{5-苯基乙基-4,6-二氫。比咯并[3,4-(：]吡唑-3-基}-4-氟苯基乙醯胺； ^{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-3-(2 -噻吩基）丙烯醯胺； N_{5_苯基乙基_4，6_二氮D比洛弁[3，4_c] π比°坐_3_基}_3_ (3 -噻吩基）丙烯醯胺； ^1-{5-苯基乙基-4,6-二氫吼咯并[3,4-(：]吼唑-3-基}-3-(2 -噻吩基）丙醯胺； Ν-{5 -苯基乙基-4,6-二氫吼咯并[3,4-c]吼唑-3-基}-2-氯苯甲醯胺； Ν-{5 -苯基乙基-4，6 -二氮0比σ各并[3，4_c] °比〇坐-3-基}-3-氣苯甲醯胺； N-{5 -苯基乙基-4,6-二氳》比咯并[3,4-cレ比唑-3-基}-4-氣苯甲醯胺； 1^-{5-苯基乙基-4,6-二氫吼咯并[3,4-〇]吼唑-3-基}-：1-p底咬丙酿胺；C:\2D-CODE\91-01\90119473.ptd Page 220 1327569 V. INSTRUCTIONS (218) 1^-{5-Phenylethyl-4,6-dihydroindole[3,4- (:]pyrazol-3-yl}-p-anisylamine; N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-indole].Biazol-3-yl} -phenoxyacetamide; N-{5-phenylethyl-4,6-dihydrogen 0 to σ each [3,4-c] D to 0-spin-3-ylindole-2-fluorophenyl Acetamine; N-{5_phenylethyl-4,6-diaza 0 to 17 each [3,4-c] °. Sodium-3-ylindole-3-fluorophenylacetamide ; 1^-{5-phenylethyl-4,6-dihydro. Biorido[3,4-(:]pyrazol-3-yl}-4-fluorophenylacetamide; ^{5 -phenylethyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-(2-thienyl)propenylamine; N_{5_phenylethyl_ 4,6_Dinitrogen D is more than 弁 [ [3,4_c] π ratio ° sitting _3_基}_3_ (3 -thienyl) acrylamide; ^1-{5-phenylethyl-4,6- Dihydroindolo[3,4-(:]oxazol-3-yl}-3-(2-thiophenyl)propanamine; Ν-{5-phenylethyl-4,6-dihydroanthracene [3,4-c]oxazol-3-yl}-2-chlorobenzamide; Ν-{5-phenylethyl-4,6-diaza 0 to σ each [3,4_c ° ° 〇 -3-yl}-3- gas benzyl amide; N-{5 - benzene Benzyl-4,6-diindole-pyrolo[3,4-cindolozol-3-yl}-4-oxabenzamide; 1^-{5-phenylethyl-4, 6-Dihydroindolo[3,4-indolyl]oxazol-3-yl}-:1-p-bottom propylamine;

C:\2D-Q0DE\91-01\90119473.ptd 第 221 頁 1327569 五、發明說明（219) N-{5-苯基乙基- 4,6 -二氫π比0各并[3，4-c]。比。坐-3-基}-2-乙醯基苯甲醯胺； N-{5 -苯基乙基-4，6 -二氫吼11 各并[3，4-c] 0比0坐-3_基}-4-乙醯基苯甲醯胺； N-{5-苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-l-萘曱醯胺； N-{5-笨基乙基-4，6 -二氫°比°各并[3，4-c] °比唾-3_基}_2-萘甲醯胺； N-{5-苯基乙基_4，6 -二氫0比p各并[3，4-c] °比°坐_3_基}_3->苯曱醯基丙醯胺； N-{5 -苯基乙基-4, 6 -二氫吡咯并[3,4-c]吡唑-3 -基卜4-乙醯胺基苯甲醯胺； N-{5 -苯基乙基- 4, 6- 二氫口比咯并[3, 4- -c ] 0比〇坐-3 -基} -2， 5- ，二甲氧苯甲醯胺 9 N-{5 -苯基乙基- 4, 6 - .二氫口比咯并[3, 4- -C ] 0比〇坐_ 3 -基} - 2， 6· 二曱氧苯甲醯胺 9 N-{5 -苯基乙基- 4, 6- 二氫口比咯并[3, 4- -C] 0比〇坐-3 -基}-3, 4- -二曱氧苯甲醯胺 f | N-{5 -苯基乙基- 4， 6- 二氫口比咯并[3, 4- -C] 口比口坐-3 -基} - 3， 5- -二曱氧苯曱醯胺 9 Ν-{5· -苯基乙基-4， 6- 二氫口比咯并[3, 4- -C ] 0比唑-3 -基} -3- (2 -噻吩甲醯基）-丙醯胺； N-{5 -苯基乙基-4，6_二氫。比17各并[3，4-c] π比嗤-3-基}-2-萘基乙醯胺；C:\2D-Q0DE\91-01\90119473.ptd Page 221 1327569 V. INSTRUCTIONS (219) N-{5-Phenylethyl-4,6-dihydroπ is 0 and each [3,4 -c]. ratio. Sodium-3-yl}-2-ethenylbenzamide; N-{5-phenylethyl-4,6-dihydroindole 11 each [3,4-c] 0 to 0 sitting-3 _yl}-4-ethenylbenzamide; N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-l-naphthalene Indoleamine; N-{5-stupylethyl-4,6-dihydrogen ratio °[3,4-c] ° than saliva-3_yl}_2-naphthylcarboxamide; N-{ 5-phenylethyl_4,6-dihydrogen 0 to p each [3,4-c] ° ratio _3_yl}_3-> phenylhydrazine propylamine; N-{5 -Phenylethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-ylpyridyl 4-acetamidobenzamide; N-{5-phenylethyl-4 , 6-dihydrogen pyrrolo[3,4- -c ] 0 is more than -3 -yl} -2, 5-, dimethoxybenzamide 9 N-{5-phenylethyl- 4, 6 - . Dihydrogen port is more than s-[3, 4- -C ] 0 is more than 〇 3 -yl} - 2, 6· dioxobenzoguanamine 9 N-{5 -phenylethyl - 4, 6-dihydro-portion pyrrolo[3,4- -C] 0 is more than stilbene -3 -yl}-3,4-dioxabenzophenamide f | N-{5 -phenyl Ethyl- 4,6-dihydro-porto-pyrolo[3,4- -C] mouth-specific 3-amino}- 3,5-dioxabenzoquinone 9 Ν-{5·-Phenylethyl-4,6-dihydro-portion-[3,4--C] 0-pyrazol-3-yl}-3-(2-thiophenanthryl)-propyl Indoleamine; N-{5-phenylethyl-4,6-dihydrogen. Ratio of [3,4-c] π to 嗤-3-yl}-2-naphthylacetamide;

C:\2D-OODE\91-Ol\90119473.ptd 第222頁 1327569 五、發明說明（220) N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-：l-萘基乙醯胺； !^-{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]咄唑-3-基}-4-苯基苯甲醯胺； 1{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-乙醯胺； 1{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-環丙烷羧醯胺； N - {5-曱烧確酿基-4，6_二氮0比σ各并[3，4-c] D比0坐-3 -基}-異丁醯胺； 1'1-{5-曱烧石黃醯基-4，6-二氫〇比11各并[3,4-(：]°比°坐-3-基}-環戊烷羧醯胺； N_{5-曱烧石黃酿基_4，6_二氮0比〇各并[3，4-c] D比0坐-3-基}-苯甲醯胺； 1^-{5-曱烷磺醯基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}-甲基吡啶甲醯胺； N_{5_曱烧續酿基-4，6_二氮ϊI比0各并[3，4-c]D比o坐-3-基}-於臉醯胺； N_{5_曱烧石黃酿基-4，6_二氮吼*7各并[3，4_c]D比°坐-3-基}-異菸鹼醯胺； N-{5-甲烧石黃酿基-4，6 -二氫〇比°各并[3，4-c] D比0坐-3-基} -3-曱基-2 -呋喃曱醯胺； N-{5-甲烧石黃醢基-4, 6 -二氫吼0各并[3,4-c] 0比。坐-3-基}-噻吩-2-羧醯胺；C:\2D-OODE\91-Ol\90119473.ptd Page 222 1327569 V. INSTRUCTIONS (220) N-{5-Phenylethyl-4,6-dihydropyrrolo[3,4-c] Pyrazol-3-yl}-:l-naphthylacetamide; !^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-indole]oxazol-3-yl} -4-phenylbenzamide; 1{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-acetamide; 1{ 5-methanesulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-cyclopropanecarboxamide; N-{5-曱烧烧--4,6 _Dinitrogen 0 ratio σ and [3,4-c] D ratio 0 sitting -3 -yl}-isobutylamine; 1'1-{5-曱石石黄醯基-4,6-dihydroindole ratio 11 each [3,4-(:]° ratio ° sit-3-yl}-cyclopentane carboxamide; N_{5- 曱石石黄 _4,6_二 0 0 〇 [3,4-c] D is 0--3-yl}-benzamide; 1^-{5-nonanesulfonyl-4,6-dihydroindole[3,4-(: ] oxazol-3-yl}-methylpyridinecarboxamide; N_{5_曱续酿 -4 -4,6_diazepine I ratio 0 and [3,4-c]D ratio o sitting-3 -基}- 醯醯 ;; N_{5_ 曱石石黄基-4,6_diazepine*7 and [3,4_c]D ratio ° sit-3-yl}-isonicotin 醯Amine; N-{5-metharestone yellow-branched-4,6-dihydroindole ratio And [3,4-c] D is 0--3-yl}-3-mercapto-2-furoamine; N-{5-methyst-xanthine-4,6-dihydroindole 0 [3,4-c] 0 ratio. Sodium-3-yl}-thiophene-2-carboxamide;

C:\2D-G0DE\91-01\90119473.ptd 第223頁 1327569 五、發明說明（221) 1^-{5-甲烧石黃醯基-4,6-二氫〇比洛并[3，4-0：]〇比〇坐-3-基}-噻吩-3-羧醯胺； N-{5-曱烷磺醯基-4, 6 -二氫"比咯并[3, 4-c]吼唑-3 -基}-鄰-曱苯曱醯胺； ?^-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-間-曱苯曱醯胺； N-{5-曱烧石黃酸基- 4,6 -二氫°比0各并[3,4-c] D比。坐-3-基}-對-曱苯曱醯胺； ?'1-{5-甲競)石黃醯基-4,6-二氫0比'7各并[3,4-(：]0比°坐-3-基}-0苯基乙醯胺； ^{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基}-水楊醯胺； 1^-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}- 2- 氟苯甲醯胺； N-{ 5-曱烷磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3 -基}- 3- 氟苯甲醯胺； N - {5-甲烧石黃酿基-4，6_二氫D比11 各并[3，4-c] π比p坐-3-基}- 4- 氟苯甲醯胺； • 1^-{5-甲烷磺醯基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}- 塞吩-2-乙醯胺； 1^-{5-甲烷磺醯基-4,6-二氳吡咯并[3,4-〇]吡唑-3-基}-噻吩-3-乙醯胺； 1^-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-苯基丙炔醯胺；C:\2D-G0DE\91-01\90119473.ptd Page 223 1327569 V. INSTRUCTIONS (221) 1^-{5-甲烧石黄醯基-4,6-Dihydroindolebi[3,4 -0:] 〇〇 -3- -3-yl}-thiophene-3-carboxamide; N-{5-nonanesulfonyl-4,6-dihydro " bis-[3, 4-c Indazole-3-yl}-o-nonylbenzamide; ?^-{5-methanesulfonyl-4,6-dihydropyrrolo[3,4-(:]carbazol-3-yl }-m-p-benzoylamine; N-{5-anthraquinone- 4,6-dihydrogen ratio 0 and [3,4-c] D ratio. sit-3-yl}- p-Phenylbenzamine; ?'1-{5-Ai Jing) sulphate-4,6-dihydrogen 0 to '7 each and [3,4-(:]0 to ° sit-3-yl} -0 phenylacetamide; ^{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-salicylide; 1^- {5-decanesulfonyl-4,6-dihydropyrrolo[3,4-indole:]pyrazol-3-yl}- 2-fluorobenzamide; N-{ 5-decanesulfonate Base-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}- 3-fluorobenzamide; N - {5-methadite yellow wine-4,6_ Dihydrogen D ratio 11 and [3,4-c] π ratio p--3-yl}- 4-fluorobenzamide; • 1^-{5-methanesulfonyl-4,6-dihydrogen咄[3,4-(:]oxazol-3-yl}-cephen-2-ylamine; 1 ^-{5-Methanesulfonyl-4,6-dipyrido[3,4-indolylpyrazol-3-yl}-thiophene-3-acetamide; 1^-{5-methanesulfonate 4-,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-phenylpropynylamine;

C:\2D-C0DE\91-01\90119473.ptd 第224頁 1327569 五、發明說明（222) 1^-{5-曱炫)續醯基-4,6-二氫0比|1各并[3,4-(：]0比唑-3-基}-3 -氰基苯甲醯胺； 1^-{5-曱烧續酿基-4，6-二氫0比0各并[3，4-(：]0比°坐-3-基}-4-氰基苯甲醯胺； N-{5-曱烧石黃醯基- 4,6 -二氫°比0各并[3,4-c] °比。坐-3_基}-反-桂皮酿胺； ?'1-{5-甲院石黃醯基-4,6-二氫11比17各并[3,4-(：]0比〇坐-3-基}-順-桂皮醯胺； ^{5-曱烧石黃醯基-4,6-二氫0比《1各并[3,4-〇]0比。坐-3-基}-3 - ( 3 - °比啶基）丙烯醯胺； ^{旦-甲烧石黃醯基-斗^-二氫吼洛并^^-^吼吐^-基}-3-(4-°比啶基）丙烯醯胺； 1^-{5-甲烷磺醯基-4,6-二氫°比咯并[3,4-〇]吡唑-3-基}- 2- 苯基丙醯胺； ^'1-{5-曱烧石黃醯基-4,6-二氫0比'1各并[3,4-(：]0比〇坐-3-基}-鄰-甲苯基乙醯胺； N - {5-甲烧石黃酿基_4，6_二氮0比略弁[3，4-c]0比0坐-3-基}-間-甲苯基乙醯胺； 1{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-對-曱苯基乙醯胺； N-{5-曱烧石黃醯基- 4,6 -二氫吼口各并[3,4-c] 〇比0坐-3-基}-鄰-茴香醯胺； 1^-{5-曱烧石黃醯基-4，6-二氫0比略并[3，4-(：]°比〇坐-3-基}- 3- 甲氧苯甲醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 224 1327569 V. Description of invention (222) 1^-{5-曱炫) Continued thiol-4,6-dihydrogen 0 ratio|1 each [3,4-(:]0-pyrazol-3-yl}-3-cyanobenzamide; 1^-{5-曱续酿 -4 -4,6-dihydro 0 to 0 each [ 3,4-(:]0 is more than -3-yl}-4-cyanobenzamide; N-{5-曱石石黄醯基- 4,6-dihydrogen is 0 and each [3, 4-c] ° ratio. Sitting -3_ base}-anti-casin amine; ?'1-{5-A hospital scutellaria-4,6-dihydro 11 to 17 each [3,4-(: ]0 is more than 〇 -3- 基 - - 顺顺桂 ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- -3- 3-yl}-3 - (3 - ° pyridyl) acrylamide; ^{旦-甲烧石黄醯基-斗^-二氢吼洛和^^-^吼吐^-基}-3-( 4-°-pyridyl) acrylamide; 1^-{5-methanesulfonyl-4,6-dihydropyr-[3,4-indolylpyrazol-3-yl}- 2-benzene Propionamide; ^'1-{5-曱石石黄醯基-4,6-dihydrogen 0 to '1 each [3,4-(:]0 is more than 〇-3-yl}-o-toluene Ethyl acetamide; N - {5-carbaceous yellow broth _4,6_diaza 0 ratio slightly 弁[3,4-c]0 to 0 -3-yl}-m-tolyl oxime Amine; 1{5-methanesulfonyl-4,6-dihydropyrrolo[ 3,4-(:]pyrazol-3-yl}-p-indole phenylacetamide; N-{5-曱石石黄醯基- 4,6-dihydropurine each [3,4-c ] 〇 is 0 -3-yl}-o-anisoleamine; 1^-{5-曱石石黄醯基-4,6-dihydro 0 is slightly more than [3,4-(:]° -3-yl}- 3-methoxybenzamide;

C:\2D-00DE\91-01\90119473.ptd 第225頁 1327569 五、發明說明（223) N - {5-曱烧石黃酿基- 4,6 -二氫0比0各并[3，4-c]B比0坐-3-基}-對-茴香醯胺； 1'1-{5-曱烧石黃醯基-4,6-二氫0比?1各并[3，4-(：]'1比〇坐-3-基}-苯氧乙醯胺； N-{5-曱烷磺醯基-4, 6 -二氫咄咯并[3, 4-c]。比唑-3 -基}- 2- 氟苯基乙醯胺； N-{5-曱烧石黃醯基- 4,6 -二氫D比σ各并[3，4-c] 0比0坐-3-基}- 3- 氟苯基乙醯胺； 1^-{5-曱烧石黃醯基-4,6-二氫0比略并[3,4-(：]0比〇坐-3-基}- 麵氟苯基乙醯胺； N-{5_曱烧石黃酿基-4，6_二氮D比略并[3，4_c]d比。坐-3-基}_ 3-(2 -噻吩基）丙烯醯胺； 1^-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-3-(3 -噻吩基）丙烯醯胺； ^1-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-3 - ( 2 -噻吩基）丙醯胺； 1^-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-2-氯苯曱醯胺； • N-{5-曱烧石黃酿基- 4,6 -二氫吼口各并[3，4-c] 0比0坐-3-基}-’3-氯苯曱醯胺； N-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3,4-c]吡唑-3 -基ΙΑ- 氯苯曱醯胺； Ν-{5-曱烧石黃醯基-4，6-二氫"比0各并[3，4-c] 〇比0坐-3-基}-1 -派。定丙醯胺；C:\2D-00DE\91-01\90119473.ptd Page 225 1327569 V. INSTRUCTIONS (223) N - {5-曱烧石黄毛基 - 4,6 - Dihydrogen 0 to 0 each [3 , 4-c]B is 0--3-yl}-p-anisylamine; 1'1-{5-曱石石黄醯基-4,6-dihydro- 0 ratio-1 each [3,4- (:]'1 than 〇--3-yl}-phenoxyacetamide; N-{5-nonanesulfonyl-4,6-dihydroindolo[3,4-c]. -3 -yl}- 2-fluorophenylacetamide; N-{5-anthracene-xanthine- 4,6-dihydrogen D ratio σ and [3,4-c] 0 to 0 -3- }}- 3-fluorophenylacetamide; 1^-{5-曱石石黄醯基-4,6-dihydro 0 ratio slightly [3,4-(:]0 is more than 〇-3-yl} - fluorophenyl acetamidine; N-{5_ 曱石石黄基-4,6_二氮D ratio slightly [3,4_c]d ratio. sit-3-yl}_ 3-(2 -thienyl)propenylamine; 1^-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-(3-thiophenyl) Acrylamide; ^1-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazol-3-yl}-3 -(2-thienyl)propene Indoleamine; 1^-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazol-3-yl}-2-chlorobenzoin; {5-曱烧石黄毛基 - 4,6 - Dihydrogen [3,4-c] 0 to 0--3-yl}-'3-chlorophenylguanamine; N-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4- c]pyrazole-3-ylindole-chlorobenzoin; Ν-{5-曱烧石黄醯基-4,6-dihydro" ratio 0 and [3,4-c] 〇 is 0 sitting- 3-yl}-1 - sent.

C:\2D-0ODE\91-01\90119473.ptd 第226頁 1327569 五、發明說明（224) N-{5_甲烧石黃醯基_4,6_二氫0比洛并[3,4-(：]°比°坐-3-基}-2-乙醯基苯曱醯胺； N-{5-甲烧石黃醯基- 4,6 -二氫0比口各并[3,4-c] D比°坐-3 -基ΙΑ- 乙醯基苯曱醯胺； Ν-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}- 1- 萘甲醯胺； Ν-{5_甲烧石黃醢基- 4,6 -二氫。比11各并[3,4-c] D比0坐-3-基}- 2- 萘曱醯胺； N-{5-曱烧石黃酿基- 4,6 -二氫°比口各并[3，4-c]D比0坐-3-基}- 3- 笨曱醯基丙醯胺； N-{5-曱烧石黃醯基- 4,6 -二氫0比略并[3,4-c] 0比。坐-3-基ΙΑ- 乙醯胺基苯甲醯胺； Ν-{ 5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}-2, 5-二曱氧苯甲醯胺； ^{云-曱烧石黃醯基-斗^-二氫吼洛并!^，^。]1^0^·^-*}- 2, 6-二曱氧苯甲醯胺； Ν_{5_曱烧續酿基_4，6_二氮0比0各弁[3，4_〇]°比〇坐_3_基}- 3, 4-二曱氧苯曱醯胺； 1'1-{5-曱烧石黃醯基-4,6-二氫吼洛并[3,4-(：]吼〇坐-3-基}-3, 5-二曱氧苯曱醯胺； 1^-{5-曱烧確醢基-4，6-二氫0比0各并[3，4-(：]0比°坐-3-基}- 3-(2-噻吩曱醯基）-丙醯胺； 1{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-(：]吼唑-3-基}-2 -萘基乙醢胺；C:\2D-0ODE\91-01\90119473.ptd Page 226 1327569 V. INSTRUCTIONS (224) N-{5_甲烧石黄醯基_4,6_Dihydro 0 Biluo[3,4- (:]°°°-3-yl}-2-ethylmercaptobenzamine; N-{5-carbaceous scutellaria- 4,6-dihydrogen 0-portion [3,4-c ] D ratio ° -3 - hydrazine - ethenyl benzoguanamine; Ν-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 }}- 1-naphthylamine; Ν-{5_甲烧石黄醢基- 4,6-dihydrogen. Ratio 11 and [3,4-c] D to 0 -3-yl}- 2- Naphthylamine; N-{5-曱石石黄-based - 4,6-dihydrogen ratios [3,4-c]D ratio 0 sitting-3-yl}- 3- awkward Propionamide; N-{5-anthracene-xanthine- 4,6-dihydrogen 0 to slightly [3,4-c] 0 ratio. sit-3-ylindole-acetamidobenzamide ;Ν-{ 5-decanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2, 5-dioxalylbenzamide; ^{云- 曱烧石黄醯基-斗^-二氢吼洛和!^,^.]1^0^·^-*}- 2,6-dioxabenzoguanamine; Ν_{5_曱烧续Base _4,6_Dinitrogen 0 to 0 弁[3,4_〇]° 〇 _3_基}- 3, 4-dioxabenzoquinone; 1'1-{5-曱Burnt stone scutellaria base-4,6- Hydroquinone [3,4-(:] 吼〇-3-yl}-3, 5-dioxabenzoquinone; 1^-{5-曱烧醢醢-4,6-二Hydrogen 0 to 0 each and [3,4-(:]0 is more than -3-yl}- 3-(2-thienyl)-propanamine; 1{5-decanesulfonyl-4 ,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-2-naphthylacetamide;

C:\2D-C0DE\91-01\90119473. ptd 第227頁 1327569 五、發明說明（225) N-{5-曱烧石黃醯基_4，6 -二氫π比11 各并[3，4-c] 0比。坐-3-基}-1 -萘基乙醯胺； N-{5-甲院石黃醯基- 4,6 -二氫°比0各并[3,4-c] 0比0坐-3-基ΙΑ-苯基苯甲醯胺； Ν-{5-乙基胺基数基-4, 6 -二氫°比°各并[3，4-c] °比。坐- 3-基}-乙醯胺； N-{5-乙基胺基叛基-4,6 -二氫°比p各并[3，4-c] °比°坐_3_ 基}-環丙烷羧醯胺； N-{5_乙基胺基裁基-4,6 -二氮吼15各弁[3,4-c] °比0坐_3_ _基}-異丁醯胺； N-{5-乙基胺基羰基-4，6 -二氫D比π各并[3，4_c]吼。坐- 3-基}-環戊烷羧醯胺； N-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-苯曱醯胺； N-{5_乙基胺基幾基-4，6_二氫吼11各并[3，4_c] °比0坐- 3-基}-甲基吡啶曱醯胺； N-{5_乙基胺基叛基-4, 6 -二氮B比0各并[3，4-c] π比。坐-3_ 基}-菸鹼醯胺； • Ν-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-c]吡唑-3- 基}_異於驗酿胺； Ν-{5-乙基胺基叛基-4，6 -二氫吼17各并[3,4-c] °比°坐-3-基}-3-曱基-2-呋喃甲醯胺； N-{5_乙基胺基幾基-4，6 -二氫吼11各并[3，4-c] 0比°坐-3-基}-噻吩-2-羧醯胺；C:\2D-C0DE\91-01\90119473. ptd Page 227 1327569 V. INSTRUCTIONS (225) N-{5-曱烧石黄醯基_4,6-Dihydro-π ratio 11 and [3,4 -c] 0 ratio. -3--3-yl}-1 -naphthylacetamide; N-{5-甲院石黄醯基- 4,6-dihydrogen ratio 0 and [3,4-c] 0 to 0 sitting -3- Base ΙΑ-phenylbenzamide; Ν-{5-ethylamino group-4,6-dihydrogen ratio of [3,4-c] °. Sodium 3-yl}-acetamide; N-{5-ethylamino-based defensyl-4,6-dihydrogen ratio p and [3,4-c] ° ratio °_3_ base}- Cyclopropanecarboxamide; N-{5-ethylamine-based cleavage-4,6-diazaindole 15 弁[3,4-c] ° ratio 0 _3_ _ yl}-isobutylamine; N-{5-ethylaminocarbonyl-4,6-dihydrogen D is π[3,4_c]吼. Sodium 3-yl}-cyclopentane carboxamide; N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-phenylhydrazine Indoleamine; N-{5-ethylaminomethyl-4,6-dihydroindole 11 each [3,4_c] ° ratio 0--3-yl}-methylpyridinium; N-{ 5-Ethylamino-t-based-4,6-diaza B is 0 and each [3,4-c] π ratio. -3 - yl}-nicotinamide; • Ν-{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl} Amine amine; Ν-{5-ethylamino thiol-4,6-dihydroanthracene 17 each [3,4-c] ° ratio sit-3-yl}-3-mercapto-2-furan Methionine; N-{5-ethylaminomethyl-4,6-dihydroindole 11 and [3,4-c] 0 ratio °-3-yl}-thiophene-2-carboxamide ;

C:\2D-roDE\91-01\90119473.ptd 第228頁 1327569 五、發明說明（226) N-{5-乙基胺基羰基-4, 6 -二氫咄咯并[3,4-c]吡唑- 3-基卜噻吩-3-羧醯胺； 1{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基卜間-曱苯曱醯胺； N-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}-對-曱苯曱醯胺； N-{5-乙基胺基羰基-4, 6 -二氫n比咯并[3,4-c]吼唑-3-基}-水楊醯胺； N-{5-乙基胺基羰基-4, 6 -二氫17比11 各并[3,4-c] D比唑- 3-基丨苯曱酿胺； N-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3,4-c] D比唑- 3-基}_3_氣苯甲酿胺； ^{5-乙基胺基羰基-4,6-二氫吡。各并[3,4-(：]0比唑-3-基}-4_氟苯甲醯胺； N-{5-乙基胺基幾基-4，6 -二氫吼11 各并[3，4-c] D比。坐_3-基}-噻吩-2-乙醯胺； N-{5-乙基胺基幾基-4，6_二氫D比略并[3，4-c] °比°坐- 3-基}-噻吩-3-乙醯胺； 1'1-{5-乙基胺基羰基-4,6-二氫咄11各并[3,4-<:]°比唑-3-基}-苯基丙炔醯胺； N-{5-乙基胺基羰基-4, 6 -二氫吼11各并[3, 4-c] D比唑- 3-基}_3-氰基苯甲酿胺； N-{5-乙基胺基幾基-4，6 -二氫11比11 各并[3，4-c] 0比峻- 3-基}-4-氰基苯甲酿胺；C:\2D-roDE\91-01\90119473.ptd Page 228 1327569 V. INSTRUCTIONS (226) N-{5-Ethylaminocarbonyl-4,6-dihydroindole[3,4- c]pyrazole-3-ylthiophene-3-carboxamide; 1{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl Benzyl-nonylphenylamine; N-{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-p-indole Amine; N-{5-ethylaminocarbonyl-4,6-dihydron-pyrolo[3,4-c]oxazol-3-yl}-salicylimamine; N-{5-ethyl Aminocarbonyl-4,6-dihydrogen 17 to 11 each [3,4-c] D-pyridyl-3-ylindole benzoate; N-{5-ethylaminocarbonyl-4,6- Dihydropyrrolo[3,4-c] D-pyridyl-3-yl}_3_gasbenzamide; ^{5-ethylaminocarbonyl-4,6-dihydropyridyl. Each [3, 4-(:]0-pyrazol-3-yl}-4-fluorobenzamide; N-{5-ethylaminodido-4,6-dihydroindole 11 each [3,4-c D ratio. sit _3-yl}-thiophene-2-acetamide; N-{5-ethylamino benzyl-4,6-dihydro D ratio slightly [3,4-c] ° ratio ° sit-3-yl}-thiophene-3-acetamide; 1'1-{5-ethylaminocarbonyl-4,6-dihydroindole 11 each [3,4-<:]° ratio Zyridin-3-yl}-phenylpropynylamine; N-{5-ethyl Alkylcarbonyl-4,6-dihydroindole 11 each [3,4-c] D-biazole-3-yl}_3-cyanobenzamide; N-{5-ethylamino group-4 , 6-dihydrogen 11 to 11 each [3,4-c] 0 to ternary 3-yl}-4-cyanobenzamide;

C:\2D-00DE\91-01\90119473.ptd 第229頁 1327569 五、發明說明（227) N-{5-乙基胺基叛基_4，6_二氫°比°各并[3，4-c] °比。坐- 3-基丨-反-桂皮酿胺； ^{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-順-桂皮醯胺； N-{5-乙基胺基幾基-4，6 -二氫°比σ各并[3,4-c] n比。坐- 3- 基}-3-(3 -吡啶基）丙烯醯胺 N_{5_乙基胺基獄基_4，6-基}-3-(4-°比啶基）丙烯醯胺 N-{5-乙基胺基羰基-4, 6-基}-2 -苯基丙醯胺； N-{5-乙基胺基幾基-4，6-基}-鄰-曱苯基乙醯胺； N-{5-乙基胺基羰基-4, 6-基}-間-甲苯基乙醯胺； N_{5_乙基胺基幾基_4, 6-基}-對-曱苯基乙醯胺； N-{5-乙基胺基幾基- 4,6-基}-鄰-茴香醢胺； N-{5-乙基胺基幾基-4，6-基}-3-曱氧苯曱醯胺； N-{5-乙基胺基幾基-4，6-基}-對-茴香醯胺； N-{5-乙基胺基羰基-4, 6-基卜苯氧乙醯胺；氫0比p各并[3，4 - c ]吼°坐-3 -氫°比π各并[3，4 - c ] °比°坐-3 -氫0比11各并[3，4 - c ] °比°坐-3 -氫0比D各并[3，4 - c ] °比。坐-3 -氫'π各并[3，4 - c ]吼。坐-3 -氫°比σ各并[3，4 - c ]吼。坐-3 -氫吼ρ各并[3，4 - c ] D比°坐-3 -氫11比B各并[3，4 - c ]吼°坐-3 -氫°比略并[3，4 - c ] °比吐-3 -C:\2D-00DE\91-01\90119473.ptd Page 229 1327569 V. INSTRUCTIONS (227) N-{5-Ethylamino-based thiol-4,6-dihydrogen ratio °[3 , 4-c] ° ratio. Sodium 3-carbo-anti-cinnabarin; ^{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-cis-cassia Indoleamine; N-{5-ethylaminomethyl--4,6-dihydrogen ratio σ and [3,4-c] n ratio. Sodium-3-yl}-3-(3-pyridyl) Acrylamide N_{5_ethylamine-based Pegyl-4,6-yl}-3-(4-°-pyridyl)propenylamine N-{5-ethylaminocarbonyl-4,6- N-{5-ethylamino benzyl-4,6-yl}-o-indole phenylacetamide; N-{5-ethylaminocarbonyl- 4,6-yl}-m-tolylacetamide; N_{5-ethylaminomethyl- 4,6-yl}-p-indole phenylacetamide; N-{5-ethylamine Alkyl- 4,6-yl}-o-anisylamine; N-{5-ethylaminomethyl-4,6-yl}-3-nonylbenzophenone; N-{5- Ethylaminomethyl-4,6-yl}-p-anisylamine; N-{5-ethylaminocarbonyl-4,6-ylphenoxyacetamide; hydrogen 0 to p each [ 3,4 - c ]吼° sitting -3 - hydrogen ° ratio π and [3,4 - c ] ° ratio ° sitting -3 - hydrogen 0 to 11 each and [3,4 - c ] ° ratio ° sitting - 3 - Hydrogen 0 is more than D and [3,4 - c ] ° ratio. Sitting -3 - hydrogen 'π each and [3,4 - c ] 吼. Sitting -3 - hydrogen ° ratio σ [3,4 - c ]吼. Sitting -3 -吼ρ和[3,4 - c ] D ratio ° sitting -3 - hydrogen 11 ratio B and [3,4 - c ]吼° sitting -3 - hydrogen ° ratio slightly [3,4 - c ] ° Than tob-3 -

C:\2D-CODE\91-0l\90119473.ptd 第230頁 1327569 五、發明說明（228) N-{5-乙基胺基獄基-4，6_二氫°比°各并[3，4-〇] 11比°坐_3-基}-2-氟苯基乙酿胺； N-{5-乙基胺基叛基-4，6_二氫0比°各并[3，4-c] °比°坐_3-基}-3-氟苯基乙醯胺； N-{5-乙基胺基幾基-4，6 -二氫D比p各并[3,4-c] n比嗤-3-基}_4_氣苯基乙酿胺； N-{5-乙基胺基幾基_4，6_二氮0比洛弁[3，4-c] °比°坐_3-基}-3-(2-噻吩基）丙烯醯胺； N-{5-乙基胺基幾基-4，6 -二氮0比σ各并[3，4-c] 0比。坐_3-基}-3_(3-°塞D分基）丙稀酿胺； N-{5-乙基胺基幾基-4，6 -二氫吼11各并[3, 4-c] D比0坐- 3-基}-3-(2 -噻吩基）丙醯胺； N_{5-乙基胺基獄基- 4,6 -二氫吼17各并[3,4-c] 10比0坐- 3-基}_2 -氯苯甲酿胺； N-{5-乙基胺基裁基- 4,6 -二氫吼11各并[3,4-c] °比。坐- 3-基}-3_氯苯甲酿胺； ^{5-乙基胺基羰基-4,6-二氫吼咯并[3,4-〇]吡唑-3-基}-4-氯苯甲醯胺； N-{5_乙基胺基艘基-4，6_二氫吼。各并[3，4-c] °比°坐- 3-基丨-1-°辰咬丙醯胺； N-{5-乙基胺基幾基-4，6 -二氫°比0各并[3,4-c] 11比0坐- 3-基}-2-乙醯基苯曱醯胺； N-{5-乙基胺基藏基-4，6 -二氫。比17各并[3，4-c] °比°坐- 3-基}-4-乙醯基苯曱醯胺；C:\2D-CODE\91-0l\90119473.ptd Page 230 1327569 V. INSTRUCTIONS (228) N-{5-Ethylamine Peptyl-4,6-Dihydrogen °°[3 , 4-〇] 11°° _3-yl}-2-fluorophenylethylamine; N-{5-ethylamino thiol-4,6-dihydrogen 0°°[3, 4-c] ° ratio _3-yl}-3-fluorophenylacetamide; N-{5-ethylamino benzyl-4,6-dihydro D ratio p and [3,4 -c] n is more than -3--3-}}_4_ phenyl phenylamine; N-{5-ethylamino yl 4,6-diaza 0 弁弁 [3,4-c] ° ～3-yl}-3-(2-thienyl)propenylamine; N-{5-ethylamino benzyl-4,6-diaza 0 to σ[3,4-c ] 0 ratio. Sitting _3-yl}-3_(3-° plug D-based) acrylamide; N-{5-ethylamino-based-4,6-dihydroindole 11 and [3, 4-c D is 0 to sit - 3-yl}-3-(2-thienyl)propanamine; N_{5-ethylamine-prison- 4,6-dihydroindole 17 and [3,4-c ] 10 to 0 sitting - 3-yl}_2-chlorobenzamide; N-{5-ethylamino-based - 4,6-dihydroindole 11 each [3,4-c] ° ratio. -3-yl}-3_chlorobenzamide; ^{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazol-3-yl}-4 - chlorobenzamide; N-{5-ethylaminosyl-4,6-dihydroanthracene. Each [3,4-c] ° ratio sits - 3-based 丨-1-° itch propylamine; N-{5-ethylamino benzyl-4,6-dihydrogen ratio 0 And [3,4-c] 11 to 0--3-yl}-2-ethylmercaptobenzamine; N-{5-ethylamino)-4,6-dihydro. Ratio of 17 to [3,4-c] ° ° -3-yl}-4-ethylmercaptobenzamine;

C:\2D-O0DE\91-Ol\9OU9473.ptd 第231頁 1327569 五、發明說明（229) 1^-{5-乙基胺基叛基-4，6-二氫°比°各并[3，4-〇]°比°坐-3-基}-1-萘曱醯胺； 1^-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基} -2-萘曱醯胺； 1^-{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基卜3 -苯甲醯基丙醯胺； 1{5-乙基胺基羰基-4,6-二氫咄咯并[3,4-〇:]咄唑-3-基}-4-乙醯胺基苯曱醯胺； N_{5_乙基胺基叛基-4，6_二氫π比0各并[3,4-c] °比°坐-3-<_基}-2, 5-二甲氧苯甲醯胺； ^丨云-乙基胺基裁基-斗^-二氫吼洛并!^,*-。]11!：!:0^··^-基}-2,6 -二曱氧苯甲醢胺； N-{5-乙基胺基叛基-4，6 -二氫0比p各并[3，4-c] °比°坐- 3-基}-3, 4-二甲氧苯甲醯胺； ^{5-乙基胺基叛基-4,6-二氫°比11各并[3,4-(：]0比°坐-3-基} -3, 5-二甲氧苯曱醯胺； N-{5-乙基胺基羰基- 4,6 -二氫吼11 各并[3,4-c] °比°坐- 3-基}-3-(2 -噻吩曱醯基）-丙醯胺； _1'1-{5-乙基胺基幾基-4，6-二氫吼略并[3，4-(：]11比〇坐-3-基}-2 -萘基乙酿胺； N-{5-乙基胺基叛基- 4,6 -二氫吼p各并[3，4-c] °比°坐- 3-基}-卜萘基乙醯胺； N-{5-乙基胺基幾基- 4,6 -二氫D比略并[3,4-c] 〇比°坐-3-基} -4-苯基苯甲醯胺；C:\2D-O0DE\91-Ol\9OU9473.ptd Page 231 1327569 V. INSTRUCTIONS (229) 1^-{5-Ethylamino-based thiol-4,6-dihydrogen ratio °[ 3,4-〇]°°°-3-yl}-1-naphthylamine; 1^-{5-ethylaminocarbonyl-4,6-dihydroindole[3,4-〇 Pyrazol-3-yl}-2-naphthylamine; 1^-{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazole-3- 3b-5-ethylmercaptopropylamine; 1{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-anthracene]-3-oxazol-3-yl}-4-B醯Aminobenzoguanamine; N_{5_ethylamino-based t-group-4,6-dihydro-π ratio 0 and [3,4-c] ° ratio °-3-<_ base}- 2, 5-Dimethoxybenzamide; ^丨云-ethylamine-based base-bucket^-dihydroindole and ^^,*-.]11!:!:0^··^-based }-2,6-dioxabenzoguanamine; N-{5-ethylamino-based tetamine-4,6-dihydrogen 0 to p each [3,4-c] °°° - 3 -yl}-3,4-dimethoxybenzamide; ^{5-ethylamino-based defensyl-4,6-dihydrogen ratio 11 and [3,4-(:]0 than ° sitting -3-yl}-3, 5-dimethoxybenzamine; N-{5-ethylaminocarbonyl-4,6-dihydroindole 11 each [3,4-c] ° - 3-yl}-3-(2-thiophenanthryl)-propanamide; _1'1-{5-B Aminoamino-4,6-dihydroanthracene [3,4-(:]11 than sino-3-yl}-2-naphthylethylamine; N-{5-ethylamino Rebel- 4,6-dihydroindole p each [3,4-c] ° ratio -3-yl}-p-naphthylacetamide; N-{5-ethylamino group - 4,6 - dihydrogen D ratio slightly [3,4-c] 〇 ratio ° sitting-3-yl}-4-phenylbenzamide;

C:\2D-CODE\91-01\90119473.ptd 第232頁 1327569 五、發明說明（230) N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-乙醯胺； N-{5 -苯基胺基羰基-4,6-二氫°比咯并[3,4-c]吡唑-3-基}-環丙烷羧醯胺； 1{5-苯基胺基羰基-4,6-二氫吼咯并[3,4-(：]°比唑-3-基卜異丁醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吼唑-3-基}-環戊烷羧醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3-基}-苯曱醯胺； N-{5_苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基卜甲基吡啶甲醯胺； ^{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吼唑-3-基}-於驗醯胺； N-{5 -苯基胺基叛基-4，6_二氮吼11 各弁[3，4-c] π比°坐- 3-基}-異於驗醯胺； Ν_{5_苯基胺基幾基-4, 6**二氮吼ρ各弁[3，4_c] °比°坐-3_ 基卜3-曱基-2-呋喃曱醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫11比p各并[3, 4-c] °比°坐- 3-基卜噻吩-2-羧醯胺； 1^-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基卜噻吩-3 -羧醯胺； N-{5-苯基胺基羰基-4,6-二氫咄咯并[3,4-c]咄唑-3-基}-鄰-曱苯甲醯胺；C:\2D-CODE\91-01\90119473.ptd Page 232 1327569 V. INSTRUCTIONS (230) N-{5-Phenylaminocarbonyl-4,6-dihydropyrrolo[3, 4-c Pyrazol-3-yl}-acetamide; N-{5-phenylaminocarbonyl-4,6-dihydropyrolo[3,4-c]pyrazol-3-yl}-cyclo Propane carboxamide; 1{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-(:]° oxazol-3-yl-isobutyl decylamine; N-{5 - Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-cyclopentancarboxamide; N-{5-phenylaminocarbonyl-4,6 -dihydroindolo[3,4-c]pyrazol-3-yl}-benzoguanamine; N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3, 4- c]pyrazole-3-ylpyridiniumcarbamide; ^{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}- Indoleamine; N-{5-phenylamino-t-radyl-4,6-diazaindole 11 弁[3,4-c] π ratio ° sit--3-yl}-different to decylamine; Ν_{ 5_Phenylamino group - 4, 6 ** diazepine ρ [3,4_c] ° ratio ° -3 - kib 3-mercapto-2-furanthamine; N-{5 - Phenylaminocarbonyl-4,6-dihydrogen 11 is more than [3, 4-c] °°- 3-ylthiophene-2-carboxamide; 1^-{5-phenylamine Carbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-ylthiophene-3-carboxycarboxamide; N-{5-phenylaminocarbonyl-4,6-dihydro Berzo[3,4-c]oxazol-3-yl}-o-nonylbenzamide;

C: \2D-C0DE\91 -01\90119473.ptd 第233頁 1327569 五、發明說明（231) N-{5-苯基胺基羰基-4, 6 -二氫吼σ各并[3, 4-c]"比。坐- 3-基}-間-甲苯曱醯胺； 1{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基卜對-曱苯甲醯胺； Ν-{5 -苯基胺基羰基-4, 6 -二氫吼11 各并[3,4-c]吼。坐- 3-基}-苯基乙醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫吼11 各并[3, 4-c] °比°坐- 3-基}-水揚醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3,4-c]咄唑-3-基}_2-氟苯甲蕴胺； N-{5 -苯基胺基獄基- 4,6 -二氫吼17各并[3,4-〇]°比°坐-3-基}-3-氟苯曱醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫。比11 各并[3,4-c] °比°坐- 3-基} -4-氟苯曱醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫吡D各并[3, 4-c] °比唾- 3-基}-噻吩-2-乙醯胺； N-{5_苯基胺基数基-4，6-二氫°比略并[3,4-c] p比°坐- 3-基}-喀吩-3-乙醯胺； N-{5 -苯基胺基羰基- 4,6 -二氫D比咯并[3,4-c] °比。坐- 3-’基}-苯基丙炔醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫11比洛并[3, 4-c] °比。坐- 3-基}_3-氰基苯曱酿胺； N-{5 -苯基胺基獄基-4，6-二氫°比°各并[3,4-c] °比。坐- 3-基}_4-氰基苯甲酿胺；C: \2D-C0DE\91 -01\90119473.ptd Page 233 1327569 V. INSTRUCTIONS (231) N-{5-Phenylaminocarbonyl-4,6-dihydroindole σ[3, 4 -c]" ratio. Sodium 3-yl}-m-toluidine; 1{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl-p-anthracene Benzalamine; Ν-{5-phenylaminocarbonyl-4,6-dihydroindole 11 each [3,4-c]indole.sodium-3-yl}-phenylacetamide; N- {5-Phenylaminocarbonyl-4,6-dihydroindole 11 each [3, 4-c] ° ratio -3 -yl}-water decylamine; N-{5-phenylamino group Carbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}_2-fluorobenzamide; N-{5-phenylamine-phenyl)-4,6-dihydrogen吼17 each [3,4-〇]° ratio 坐-3-yl}-3-fluorophenylguanamine; N-{5-phenylaminocarbonyl-4,6-dihydrogen. And [3,4-c] ° ratio sit--3-yl}-4-fluorophenylguanamine; N-{5-phenylaminocarbonyl-4,6-dihydropyridyl D each [3, 4-c] ° than saliva-3-yl}-thiophene-2-acetamide; N-{5-phenylamino group-4,6-dihydrogen ratio slightly [3,4-c] p Ratio of -3 -yl}-carbo-3-acetamide; N-{5-phenylaminocarbonyl- 4,6-dihydrogen D than octoh [3,4-c] °. - 3-'yl}-phenylpropynylamine; N-{5-phenylaminocarbonyl-4,6-dihydro-11-pyrolo[3,4-c] ° ratio }_3-cyanobenzoquinone; N-{5-phenyl Amine base 4,6-dihydrogen ratio of [3,4-c] °. Sodium 3-yl}_4-cyanobenzamide;

C:\2D-C0DE\91-01\90119473.ptd 第234頁 1327569 五、發明說明（232) N-{5 -苯基胺基獄基-4, 6_二氫D比17各并[3，4-c] °比°坐-3-基卜反-桂皮醯胺； N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基} _順-桂皮酿胺； N-{5 -苯基胺基幾基_4, 6_二氫°比D各并[3，4-c] °比σ坐-3-基}_3_(3_11比11定基）丙稀胺； 1{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基} - 3 - ( 4 -吡啶基）丙烯醯胺； ?^-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-2 -苯基丙醯胺； Ν-{5 -苯基胺基幾基_4，6 -二氯°比Β各并[3，4-c] °比。坐_3-基}-鄰-曱苯基乙醯胺； Ν-{5-苯基胺基羰基-4, 6-二氫。比咯并[3, 4-c]咄唑-3-基卜間-曱苯基乙醯胺； Ν-{5 -苯基胺基幾基-4，6_二氮吼1*各并[3，4-c] °比°坐- 3-基}-對-曱苯基乙醯胺； Ν-{5 -苯基胺基叛基-4，6 -二氫D比D各并[3，4-c] °比°坐- 3-基}-鄰-茴香醯胺； N-{5 -苯基胺基幾基- 4,6 -二氫B比σ各并[3，4-c] °比。坐- 3-基}-3_甲氧苯曱醯胺； N-{5-苯基胺基幾基- 4，6 -二氫吼11 各并[3,4-c]吼°坐-3-基}-對-茴香醯胺； N-丨5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-苯氧乙醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 234 1327569 V. INSTRUCTIONS (232) N-{5-Phenylamine-based Prison-4, 6-Dihydro-D is 17 and [3] , 4-c] ° ratio - -3- keb-trans-cinnamate; N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3 -基} _ cis-casin amine; N-{5-phenylamino group _4, 6-dihydrogen ratio D and [3,4-c] ° ratio σ sit-3-yl}_3_ (3_11 to 11 base) acrylamide; 1{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-3-(4-pyridine Acrylamide; ?--{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-2-phenylpropanamide; Ν-{5-Phenylamino-based _4,6-dichloro- Β Β [3,4-c] ° ratio. Sodium _3-yl}-o- phenyl phenyl acetamide; Ν -{5-phenylaminocarbonyl-4,6-dihydro.pyrolo[3,4-c]oxazol-3-yl-b-phenylphenylamine; Ν-{5-phenyl Aminomethyl-4,6-diazaindole 1* each [3,4-c] °°-3-yl}-p-indole phenylacetamide; Ν-{5-phenylamine Baseline-4,6-dihydrogen D ratio D and [3,4-c] ° ratio sit-3-yl}-o-anisoleamine; N-{5-phenylamino group- 4, 6-dihydrogen B ratio σ and [3,4-c] ° ratio. Sodium-3-yl}-3-methoxybenzoguanamine; N-{5-phenylamino group - 4,6 - indoline 11 each [3,4-c]吼?-3-yl}-p-anisylamine; N-丨5-phenylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-phenoxyacetamide;

C:\2D-C0DH\91-01\90119473.ptd 第235頁 1327569 五、發明說明（233) N-{5 -苯基胺基羰基-4, 6 -二氫吼11各并[3, 4-c] n比哇- 3-基}_2-氟苯基乙酿胺； N-{5 -苯基胺基羰基-4, 6 -二氫咄B各并[3, 4-c] D比嗤- 3-基}-3-氟苯基乙醯胺； 1^-{5-苯基胺基羰基-4,6-二氫°比咯并[3,4-<:]吡唑-3-基}-4_氟苯基乙酿胺； N-{5 -苯基胺基幾基-4，6 -二氫吼洛并[3，4-c] °比。坐-3_ 基}-3-(2 -噻吩基）丙烯醯胺； N-{5 -苯基胺基羰基- 4,6 -二氫p比咯并[3,4-c]吡唑-3-,_基}-3-(3-噻吩基）丙烯醯胺； N-{5 -苯基胺基羰基-4,6_二氫吡咯并[3,4-c]吼唑-3-基}_3_(2_°塞吩基）丙酿胺； 1{5-苯基胺基羰基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}-2-氯苯甲醯胺； N-{5-苯基胺基戴基-4，6 -二氫°比°各并[3, 4-c] °比°坐-3-基卜3 -氯苯曱醯胺；卜{5-苯基胺基錄基-4,6-二氫11比17各并[3,4-〇:]'1比°坐-3-基}-4-氣苯甲醯胺； • N-{5 -苯基胺基幾基- 4,6 -二氫吼17各并[3，4-c]吼°坐-3- _基} - 1 -哌啶丙醯胺； N-{5 -苯基胺基幾基-4，6-二氫吼11各并[3，4-c] π比°坐-3-基} -2-乙醯基苯曱醯胺； Ν-{5 -苯基胺基幾基-4，6 -二氫°比°各并[3，4-c] η比。坐-3 -基}-4-乙醯基苯甲醯胺；C:\2D-C0DH\91-01\90119473.ptd Page 235 1327569 V. INSTRUCTIONS (233) N-{5-Phenylaminocarbonyl-4,6-dihydroindole 11 each [3, 4 -c] n-wow-3-yl}_2-fluorophenylethylamine; N-{5-phenylaminocarbonyl-4,6-dihydroindole B each [3, 4-c] D ratio嗤-3-yl}-3-fluorophenylacetamide; 1^-{5-phenylaminocarbonyl-4,6-dihydropyrano[3,4-<:]pyrazole- 3-yl}-4_fluorophenylethylamine; N-{5-phenylaminodino-4,6-dihydroindolo[3,4-c] ° ratio. -3-yl}-3-(2-thienyl)propenylamine; N-{5-phenylaminocarbonyl- 4,6-dihydrop-pyrolo[3,4-c]pyrazole-3 -, _ yl}-3-(3-thienyl) acrylamide; N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl }_3_(2_°secenyl) propylamine; 1{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-(:]carbazol-3-yl}-2- Chlorobenzamide; N-{5-phenylaminodyl-4,6-dihydrogen ratio °[3, 4-c] ° ratio -3--3-b 3-chlorophenylhydrazine Indoleamine; b{5-phenylamino-based 4-,6-dihydrogen 11 to 17 each [3,4-〇:]'1°°-3-yl}-4-benzophenone Amine; N-{5-phenylamino-yl- 4,6-dihydroindole 17 and [3,4-c]吼°-3-yl}-1 -piperidinepropionamide; N-{5-Phenylamino-yl-4,6-dihydroindole 11 and [3,4-c] π ratio °-3-yl}-2-ethylmercaptobenzamine; -{5-Phenylamino-yl--4,6-dihydrogen ratio of [3,4-c] η ratio. Sodium-3-yl}-4-ethenylbenzamide;

C:\2D-C0DE\91-01\90119473.ptd 第236頁 1327569 五、發明說明（234) N-{5-苯基胺基羰基-4, 6 -二氫°比洛并[3,4-c] D比唑- 3-基}-1-萘曱醯胺； N-{5-苯基胺基毅基-4, 6 -二氫吼11 各并[3,4-c] D比唾- 3-基}-2 -萘曱醯胺； ^{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基} - 3 -苯曱醯基丙醯胺； N-{5 -苯基胺基幾基_4，6_二氫各并[3，4-c]"比。坐_3-基}-4-乙醯胺基苯甲醯胺； N-{5 -苯基胺基艘基-4，6 -二氫吼略并[3, 4-c] °比°坐- 3-基}-2,5-二曱氧苯曱醢胺； N_{5 -苯基胺基獄基_4，6_二氫p比p各并[3，4-c] °比β坐- 3-基}-2, 6-二曱氧苯曱醯胺； Ν-{5 -苯基胺基羰基-4,6-二氫°比咯并[3,4-c]°比唑-3-基卜3,4-二甲氧苯甲醯胺； Ν-{5 -苯基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基}-3，5 -二甲氧苯曱酿胺； Ν-{5 -苯基胺基幾基-4，6-二氫吼11各并[3，4-c] D比°坐- 3-基}-3-(2-噻吩曱醯基）-丙醯胺； N-{5 -苯基胺基幾基-4，6-二氫"比略并[3，4-c] °比°坐-3-基}-2-萘基乙醯胺； [^-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]°比唑-3-基}-1-萘基乙酿胺； !^-{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-苯基苯曱醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 236 1327569 V. INSTRUCTIONS (234) N-{5-Phenylaminocarbonyl-4,6-dihydropyrazine [3,4 -c] D-biazole-3-yl}-1-naphthylamine; N-{5-phenylamino-yl-4,6-dihydroindole 11 each [3,4-c] D ratio Salic-3-yl}-2-naphthylamine; ^{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-benzene Mercaptopropionamide; N-{5-phenylamino-based _4,6-dihydro-[3,4-c]" ratio. Sit _3-yl}-4-acetamidobenzamide; N-{5-phenylamine-based 4,6-dihydroanthracene [3, 4-c] ° - 3-yl}-2,5-dioxabenzoquinone; N_{5-phenylamine-based prison group _4,6_dihydrop ratio p and [3,4-c] ° ratio β Sodium 3-yl}-2,6-dioxabenzoquinone; Ν-{5-phenylaminocarbonyl-4,6-dihydropyrano[3,4-c]° azole -3- kib 3,4-dimethoxybenzamide; Ν-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl }-3,5-Dimethoxybenzoquinone; Ν-{5-phenylamino-based-4,6-dihydroindole 11 and [3,4-c] D ratio °- 3- }}-3-(2-thienyl)-propanamine; N-{5-phenylamino-based-4,6-dihydro" ratio [[3,4-c] °坐-3-yl}-2-naphthylacetamide; [^-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]°bazole-3- }}-1-naphthylethylamine; !^-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-benzene Benzimidamide;

C:\2D.C0DE\91-01\90119473.ptd 第237頁 1327569 五、發明說明（235) 1^-{5-辛基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-乙醯胺； N-{5-亨基胺基幾基- 4,6 -二氫吼17各并[3，4-c] °比〇坐-3-基}-環丙烷羧醯胺； N - {5_辛基胺基幾基-4，6_二氫°比p各并[3，4-c] °比。坐_3_ 基卜異丁醯胺； N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-環戊烷羧醯胺； N-{ 5-辛基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑-3-瞻基卜苯曱醯胺； N-{5-辛基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基}-甲基吡啶曱醯胺； N-{5-亨基胺基幾基- 4,6 -二氫吼11 各并[3,4-c] D比。坐- 3-基}-菸鹼醯胺； N-{5-亨基胺基幾基-4，6_二氫吼17各并[3，4-c] °比0坐-3-基}-異菸鹼醯胺； N-{5-辛基胺基幾基-4，6_二氫n比11 各并[3，4-c] σ比0坐- 3-基}-3-曱基-2-呋喃曱醯胺； Ν-{5-苄基胺基幾基- 4,6 -二氫0比σ各并[3,4-c]吼〇坐- 3-•基卜噻吩-2-羧醯胺； 1'1-{5-爷基胺基幾基-4,6-二氫11比洛并[3,4-〇]°比°坐-3-基}-嘍吩-3 -羧醯胺； 1^-{5-辛基胺基裁基-4,6-二氫〇比11各并[3,4-(：]'1比。坐-3-基卜鄰-曱苯曱醯胺；C:\2D.C0DE\91-01\90119473.ptd Page 237 1327569 V. INSTRUCTIONS (235) 1^-{5-octylaminocarbonyl-4,6-dihydropyrrolo[3,4- (:]pyrazol-3-yl}-acetamide; N-{5-henylamino-yl-4,6-dihydroindole 17 each [3,4-c] ° 〇 sitting-3 -yl}-cyclopropanecarboxamide; N-{5-octylamino group-4,6-dihydrogen ratio p and [3,4-c] ° ratio. sitting _3_ Indoleamine; N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-cyclopentanecarboxamide; N-{ 5-octyl Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-thylbenzamide; N-{5-octylaminocarbonyl-4,6-dihydrogen咄[3,4-c]pyrazol-3-yl}-methylpyridiniumamine; N-{5-henylamino-yl-4,6-dihydroindole 11 each [3, 4-c] D ratio. Sodium-3-yl}-nicotinium amide; N-{5-Hexylamino-based-4,6-dihydroindole 17 each [3,4-c] ° ratio 0--3-yl}-isonicotinamine amide; N-{5-octylamino group-4,6-dihydron ratio 11 and [3,4-c] σ ratio 0 sitting - 3 -yl}-3-mercapto-2-furoamine; Ν-{5-benzylaminomethyl- 4,6-dihydro- 0-σ and [3,4-c] squat- 3-• thiophene-2-carboxyindole ; 1'1-{5-L-ylamino-yl-4,6-dihydro- 11 piroxi[3,4-〇]°°--3-yl}-porphin-3-carboxamide ; 1^-{5-octylamino-based cleavage-4,6-dihydroindole ratio 11 and [3,4-(:]'1 ratio. Sodium-3-kib-o-phenylphthalamide ;

II

IIII

i C:\2D-OODE\91-Ol\90119473.ptd 第238頁 1327569 五、發明說明（236) N-{5-节基胺基幾基-4，6-二氫°比p各并[3，4-c] n比0坐- 3-基卜間-曱苯曱醯胺； N-{5-辛基胺基幾基-4, 6_二氫吼17各并[3，4-c] °比〇坐- 3-基}-對-曱苯曱醯胺； 1{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-〇]咄唑-3-基}-水楊醯胺； N-{5_辛基胺基叛基_4，6_二氯°比0各并[3，4-c] °比。坐_3_ 基}_2~氟苯曱酿胺； N-{5-窄基胺基叛基_4，6 -二氫°比0各并[3，4-c] 〇比0坐- 3-基}_3-敗苯甲酿胺； 1\1-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基丨-4-乱苯甲酿胺； N - {5-窄基胺基裁基-4，6_二氮°比洛并[3，4_c] °比。坐- 3-基}-噻吩-2-乙醯胺； 1^-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-噻吩-3-乙醯胺； N-{5_爷基胺基幾基_4，6_二氮π比17各弁[3，4_c]吼°坐_3_ 基}-苯基丙炔醯胺； N-{5-苄基胺基叛基-4，6 -二氫D比嘻并[3, 4-c] »比。坐- 3-基}-3-氰基苯曱酿胺； N-{5-窄基胺基叛基-4，6_二氮吼11 各并[3，4-c]吼〇坐- 3-基}-4-氰基苯曱醯胺； N-{5-辛基胺基戴基- 4,6 -二氣p比11 各并[3，4-c] °比°坐-3-基}-反-桂皮醯胺；i C:\2D-OODE\91-Ol\90119473.ptd Page 238 1327569 V. INSTRUCTIONS (236) N-{5-nodal amino group-4,6-dihydrogen ratio p and [ 3,4-c] n is 0-position - 3-yl-bu-p-benzoguanamine; N-{5-octylamino-based-4,6-dihydroindole 17 each [3,4- c] ° than squat - 3-yl}-p-nonyl benzoguanamine; 1{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]carbazole-3 -yl}-salicylimamine; N-{5-octylamino-based thiol-4,6-dichloro-pyrene ratio 0 and [3,4-c] ° ratio. Sit _3_ base}_2~ fluorobenzoquinone; N-{5-narrow-based amine-based _4,6-dihydrogen ratio 0 and [3,4-c] 〇 ratio 0 sitting - 3- Base}_3- benzoylamine; 1\1-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-ylindole-4-chaotic Benzoylamine; N-{5-narrowylamino-based base-4,6-diaza-pyrylene[3,4_c] °.sodium-3-yl}-thiophene-2-acetamide; 1^-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-thiophene-3-acetamide; N-{5_爷基胺基基基_4,6_Dinitrogen π ratio 17 弁[3,4_c]吼° _3_ ki}-phenylpropynyl decylamine; N-{5-benzylamine thiol- 4,6-dihydrogen D is more than 嘻[3,4-c]». Sodium-3-yl}-3-cyanobenzoquinone; N-{5-narrowylamino-based-4 6_diazepine 11 each [3,4-c] sino-3-yl}-4-cyanobenzoquinone; N-{5-octylaminodyl- 4,6-di Gas p is more than 11 and [3,4-c] ° ratio of -3-yl}-trans-cinnafloxacin;

C:\2D-O0DE\91-01\90119473.ptd 第239頁 1327569 五、發明說明（237) ^^-苄基胺基羰基-彳^-二氫吡洛并”：斗-^吼唑·^-基}-順-桂皮醯胺； ^{5-爷基胺基羰基-4,6-二氫°比°各并[3,4-(：]°比唑-3-基}_3_(3_®比咬基）丙稀酿胺； N-{5-爷基胺基叛基_4，6_二氫吼0各并[3，4-c] °比〇坐- 3-基卜3-(4-°比啶基）丙烯醯胺； N-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-c]吼唑-3-基卜2-苯基丙醯胺； N-{5-苄基胺基獄基- 4,6 -二氫D比17各并[3，4-c] °比°坐- 3-<_基}-鄰-甲苯基乙醯胺； N-{5-爷基胺基羰基-4,6-二氫。比咯并[3,4-c]吡唑-3-基}-間-曱苯基乙醯胺； ^'1-{5-苄基胺基幾基-4,6-二氫°比°各并[3，4-(：]°比。坐-3-基卜對-甲苯基乙醯胺； N-{5-节基胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3-基卜鄰-茴香醯胺； 1'1-{5-:¥:基胺基獄基-4，6-二氫°比洛并[3，4-(：]0比。坐-3-基}-3-甲氧苯曱醯胺； N-{5-辛基胺基羰基- 4,6 -二氫"比17各并[3,4-c] °比°坐- 3- 基}-對-茴香醯胺； 1^-{5-亨基胺基羰基-4,6-二氫咄咯并[3,4-(：]咣唑-3-基}-苯氧乙醯胺； N-{5-爷基胺基幾基- 4,6 -二氫各并[3，4-c]。比吐-3-基}_2_氟苯基乙酿胺；C:\2D-O0DE\91-01\90119473.ptd Page 239 1327569 V. INSTRUCTIONS (237) ^^-Benzylaminocarbonyl-彳^-dihydropyrromethene: bucket-^-carbazole ^-基}-cis-cinnafloxacin; ^{5-argylaminocarbonyl-4,6-dihydrogen ratio °[3,4-(:]°pyrazol-3-yl}_3_( 3_® than bite base) acrylamide; N-{5-ylamino-based t-base-4,6-dihydroindole 0 each [3,4-c] ° 〇 sitting - 3-kib 3 -(4-°-pyridyl)propenylamine; N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl-2-phenyl Propionamide; N-{5-benzylamine-based prison base - 4,6-dihydro D ratio 17 and [3,4-c] ° ratio sit - 3-<_base}-o- Tolylacetamide; N-{5-argylaminocarbonyl-4,6-dihydro.pyrolo[3,4-c]pyrazol-3-yl}-m-decylphenylacetamide ; ^'1-{5-benzylaminomethyl-4,6-dihydrogen ratio °[3,4-(:]° ratio. sit-3-carbo-tolylacetamide N-{5-nodylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl-o-anisylamine; 1'1-{5-:¥: Amino-based pegyl-4,6-dihydro-pyrolo[3,4-(:]0 ratio. sit-3-yl}-3-methoxybenzamine; N-{5-octyl Aminocarbonyl-4,6-dihydrogen " than 17 each [3,4-c] ° ratio - 3-yl}-p-anisamine; 1^-{5-heterylaminocarbonyl-4,6-dihydroindole [3,4-(:]oxazol-3-yl}-phenoxyacetamide; N-{5-ylaminomethyl- 4,6-dihydro-[3,4-c]. Bis-3-yl}_2_fluorophenylethylamine;

C:\2DOODE\91-01\90119473.ptd 第 240 I 1327569 五、發明說明（238) N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] °比唑-3-基}-3-1苯基乙酿胺； N-{5-窄基胺基羰基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}_4_氣苯基乙酿胺， N-{5 -苄基胺基羰基-4,6-二氫咄咯并[3,4-〇]呲唑-3_ 基}-3-(2 -喀吩基）丙烯醯胺； N-{5-笮基胺基羰基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}_3_(3_°塞吩基）丙稀酿胺； N-{5-苄基胺基羰基-4,6-二氫吼咯并[3,4-c]吡唑-3-基卜3-(2-噻吩基）丙醯胺； N-{5-辛基胺基羰基-4,6-二氫吼咯并[3,4-c]咄唑-3-基}_2-氯苯甲酿胺； N-{5 -爷基胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}_3_氣苯曱酿胺； N-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}_4_氯苯曱酿胺； !^-{5-苄基胺基羰基-4,6-二氫吼咯并[3,4-(：]吼唑-3-基} -1 -哌啶丙醯胺； N-{5-爷基胺基叛基-4，6 -二氫π比D各并[3，4-c]吼。坐- 3-基}-2-乙醯基苯甲醯胺； N_{5_窄基胺基幾基-4，6_二氯0比11 各并[3，4_c] °比〇坐- 3-基}-4-乙醯基苯甲醯胺；基卜；!-萘甲醯胺；C:\2DOODE\91-01\90119473.ptd 240 I 1327569 V. INSTRUCTIONS (238) N-{5-Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c] ° Bisazo-3-yl}-3-1 phenylethylamine; N-{5-narrowylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl} _4_ gas phenylethylamine, N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-indolyl]carbazole-3-yl}-3-(2-introduction Acrylamide; N-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}_3_(3_°secenyl) propylene Amine; N-{5-benzylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-ylbu-3-(2-thienyl)propanamine; N- {5-octylaminocarbonyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl}_2-chlorobenzamide; N-{5-ylaminocarbonyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}_3_ gas benzoquinone; N-{5-benzylaminocarbonyl-4,6-dihydropyrrole [3,4-c]pyrazol-3-yl}_4_chlorobenzoquinone; !^-{5-benzylaminocarbonyl-4,6-dihydroindole[3,4-(: ] oxazol-3-yl} -1 -piperidine propylamine; N-{5-yl-amino-denyl-4,6-dihydro-π ratio D and [3,4-c] oxime. - 3-yl}-2-ethylmercaptobenzamide; N _{5_Narrow-based amino-based group-4,6-dichloro- 0 to 11 each [3,4_c] ° than sitting - 3-yl}-4-ethylmercaptobenzamide; !-naphthylamine;

C:\2D-C0DE\91-01\90119473.ptd 第241頁 1327569 五、發明說明（239) 1^-{5-苄基胺基羰基-4,6-二氫吡11各并[3,4-(：]吼°坐-3-基}-2 -蔡甲酿胺； N-{5-窄基胺基幾基-4,6 -二氫吼11 各并[3，4-c] n比0坐-3_ 基}-3-苯曱醯基丙醯胺； 1^-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-4-乙醯胺基苯曱醯胺； N-{5_亨基胺基幾基_4，6_二氮D比p各弁[3,4-c] 0比0坐_3_ 基}-2,5 -二曱氧苯甲醯胺； ^{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]咄唑-3-|^基}-2, 6-二曱氧苯甲醯胺； N-{5_爷基胺基幾基_4，6_二氮0 各弁[3，4_c] 0比11 坐-3_ 基} -3, 4-二曱氧苯曱醯胺； ?^-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3, 5-二曱氧苯甲醯胺； Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-3-(2-噻吩曱醯基）-丙醯胺； Ν-{5_爷基胺基截基-4，6_二氮0比略弁[3，4-c] π比。坐- 3-基}_2_蔡基乙酿胺； • Ν-{5-窄基胺基幾基- 4，6 -二氫〇比0各并[3,4-c] η比°坐-3- 基}-1-蔡基乙酿胺； Ν-{5-爷基胺基叛基-4,6 -二氫吼*7各并[3，4-c] °比。坐-3-基} -4-苯基苯甲醯胺； 1{5-苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-〇]°比唑 -3-基}-乙醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 241 1327569 V. INSTRUCTIONS (239) 1^-{5-Benzylaminocarbonyl-4,6-dihydropyrene 11 each [3, 4-(:]吼° sitting-3-yl}-2-Calamine; N-{5-narrowylamino-based-4,6-dihydroindole 11 each [3,4-c] n is 0 to 0 -3}-3-phenylmercaptopropylamine; 1^-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3 -yl}-4-acetamidobenzoylamine; N-{5_henylamino group _4,6-diaza D ratio p 弁[3,4-c] 0 to 0 sitting_ 3_yl}-2,5-dioxabenzoguanamine; ^{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]carbazole-3-| }-2,6-dioxabenzoguanamine; N-{5_ arylamino group _4,6-diaza 0 弁[3,4_c] 0 to 11 sit-3_ base} -3 , 4-dioxabenzoquinone; ?^-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3, 5 - dioxobenzoguanamine; Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-(2-thiophene oxime醯-) propylamine; Ν-{5_ 贵基胺基基基-4,6_二氮0 ratio slightly [3,4-c] π ratio. Sit-3-yl}_2_蔡基乙Amine; • Ν-{5-narrowylamino group - 4 6-dihydroindole ratio 0 and [3,4-c] η ratio 坐-3-yl}-1-caiyl ethene; Ν-{5- arylamino thiol-4,6-dihydrogen吼*7 each [3,4-c] ° ratio. Sodium-3-yl}-4-phenylbenzamide; 1{5-phenylhydrazinocarbonyl-4,6-dihydroanthracene And [3,4-〇]°boxazol-3-yl}-acetamide;

C:\2D-CODE\91-01\90119473_ptd 第242頁 1327569 五、發明說明（240) ^丨卩-苯曱醯基胺基羰基“^-二氫吼洛并^^-以吡唑 -3 -基}-環丙烧缓酿胺； 1^-{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基卜異丁醯胺； 1{5-苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-(：]吡唑 -3-基}-環戊烷羧醯胺； N-{ 5 -笨曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-苯曱醯胺； 1{5-苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇:]吡唑 -3 -基卜甲基吡啶曱醯胺； N-{ 5-苯甲醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-菸鹼醯胺； 1{5-苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-(：]吡唑 _3 -基}·~異於驗酿胺； 1^-{5-苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-〇]吡唑 -3-基}-3-曱基_2 -呋喃曱醯胺； Ν-{5-苯甲醯基胺基羰基-4, 6-二氫呲咯并[3, 4-c]吡唑 -3-基}-噻吩-2-羧醯胺；卜{5-笨甲醯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-噻吩-3-羧醯胺； 1{5-苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-鄰-甲苯曱醯胺； Ν-{5-笨曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_間-曱苯甲酿胺；C:\2D-CODE\91-01\90119473_ptd Page 242 1327569 V. INSTRUCTIONS (240) ^丨卩-Benzylaminocarbonylcarbonyl^^-dihydroindole and ^^-pyrazazole-3 -yl}-cyclopropanol slow-acting amine; 1^-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-ylpyridin Guanidine; 1{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-cyclopentanecarboxamide; N-{ 5 - alkalylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-benzoguanamine; 1{5-benzhydrylaminocarbonyl- 4,6-dihydropyrrolo[3,4-anthracene]pyrazol-3-ylpyridiniumamine; N-{5-benzylidenylaminocarbonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazol-3-yl}-nicotinium amide; 1{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydroindolo[3,4-(:]pyrazole _3 -基}·~ is different from the amine; 1^-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl} -3-mercapto-2-furoylamine; Ν-{5-benzhydrylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}- Thiophene-2-carboxamide; b{5- benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyridyl -3-yl}-thiophene-3-carboxamide; 1{5-benzylidenylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}- O-toluidine; Ν-{5- azainylcarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-m-indole benzamide ;

C:\2D-G0DE\91-01\90119473.ptd 第243頁 1327569 五、發明說明（241) 1^-{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 - 3 -基}-對-曱苯甲醯胺； 1\}-{5-苯曱醯基胺基羰基-4,6-二氫吡略并[3,4-(：]吡唾 _3_基丨-苯基乙酿胺； N-{5 -苯曱醯基胺基羰基- 4,6 -二氫D比略并[3,4-c] °比°坐 -3_基}_水楊酿胺； N-{5 -笨曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-2 -氣苯甲酿胺； 1^-{5-苯曱醯基胺基羰基-4,6-二氫°比咯并[3,4-〇]咄唑 3 -基丨-3-氣苯曱酿胺； N_{5_苯曱酿基胺基叛基_4，6_二氮吼11 各并[3，4_c] D比0坐 _3-基}-4-氟苯曱酿胺； N-{5 -苯曱醯基胺基叛基- 4，6 -二氫吼17各并[3，4-c] D比吐 -3 -基}-噻吩-2-乙醯胺； N-{5-苯曱酿基胺基幾基- 4,6 -二氫D比洛并[3,4-c] °比°坐 -3-基}-噻吩-3-乙醯胺； N-{5-苯曱醯基胺基幾基- 4,6 -二氫"比17各并[3,4-c] 0比0坐 _3_基}_苯基丙快酿胺； N-{5-苯曱醯基胺基羰基-4,6-二氫"比咯并[3,4-(：]"比唑 _3-基}-3-氛基苯曱酿胺； N-{5 -苯甲酿基胺基幾基-4，6 -二氫"比11各并[3，4-c] 0比0坐 -3-基}-4-氰基苯甲醯胺； N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3-基卜反-桂皮醢胺；C:\2D-G0DE\91-01\90119473.ptd Page 243 1327569 V. INSTRUCTIONS (241) 1^-{5-Benzenylaminocarbonyl-4,6-dihydropyrrolo[3, 4-〇]pyrazole-3-yl}-p-nonylbenzamide; 1\}-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrano[3,4-( :]pyrazine_3_ylindole-phenylethylamine; N-{5-phenylhydrazinocarbonyl- 4,6-dihydrogen D ratio slightly [3,4-c] ° -3_基}_水杨胺胺; N-{5 - alkalylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-2 - gas Benzoylamine; 1^-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrolo[3,4-indole]carbazole-3-ylindole-3-p-benzoquinone ; N_{5_苯苯胺基基基基基_4,6_二吼吼11 each [3,4_c] D ratio 0 _3-yl}-4-fluorobenzoquinone; N-{ 5-Benzylamino-amino-derivative- 4,6-dihydroindole 17-[3,4-c] D-pyr-3-yl}-thiophene-2-acetamide; N-{5- Benzene arylamino-yl, 4,6-dihydro D, pirodi[3,4-c] ° ratio, sit-3-yl}-thiophene-3-acetamide; N-{5-benzene Mercaptoalkylamino- 4,6-dihydro" ratio 17 and [3,4-c] 0 to 0 sitting _3_yl}-phenylpropanol; N-{5-benzene Mercaptoamine Benzyl-4,6-dihydro"bi[3,4-(:]"biazole-3-yl}-3-ylphenyl benzoate; N-{5-benzamide Ketosyl-4,6-dihydro" ratio 11 and [3,4-c] 0 to 0--3-yl}-4-cyanobenzamide; N-{5-benzoquinone Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl b- cinnamate;

C:\2D-C0DE\91-01\90119473.ptd 第244頁 1327569 五、發明說明（242) 1^-{5-苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-〇]°比唑 -3 -基卜順-桂皮醯胺； 1{5-苯曱醯基胺基羰基-4,6-二氫°比咯并[3,4-(：]吡唑 _3_基}_3_(3_ °比咬基）丙稀酿胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫咄咯并[3, 4-c] 0比唑 -3-基}-3-(4-°比啶基）丙烯醯胺； N-{5-苯甲醯基胺基羰基-4, 6-二氫咄咯并[3, 4-c]吡唑 _3_基}_2_苯基丙酿胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫咄咯并[3, 4-c]吡唑 -3 -基}-鄰-曱苯基乙酿胺； N-{5 -苯甲醯基胺基幾基- 4,6 -二氫°比琳}[3，4-〇] °比0坐 _3-基}_間-甲苯基乙酿胺； ^}-{5-苯甲醯基胺基羰基-4,6-二氫呲咯并[3,4-(：]吡唑 -3-基}-對-曱苯基乙醯胺； 1{5-苯甲醯基胺基羰基-4,6-二氫吼咯并[3,4-(：]"比唑 -3-基卜鄰-茴香醯胺； N-{5 -苯甲醯基胺基羰基-4,6 -二氫°比咯并[3,4-c] °比唑 -3-基}-3-甲氧苯甲醯胺； N-{5-苯甲醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]咄唑 _3-基}-對-菌香酿胺； N-{5 -苯甲醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_苯氧乙酿胺； N-{5 -苯甲醯基胺基羰基-4,6-二氫°比咯并[3,4-(：]吡唑基丨-2_說苯基乙酿胺；C:\2D-C0DE\91-01\90119473.ptd Page 244 1327569 V. INSTRUCTIONS (242) 1^-{5-Benzenylaminocarbonyl-4,6-dihydroindole[3 , 4-〇]°Bizozol-3-kibsuccinyl-cinnamate; 1{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydro-pyrano[3,4-(:]pyridyl Azole_3_yl}_3_(3_° ratio) propylene amine; N-{5-benzoguanidinocarbonyl-4,6-dihydroindolo[3,4-c] 0 ratio Zyridin-3-yl}-3-(4-°-pyridyl)propenylamine; N-{5-benzhydrylaminocarbonyl-4,6-dihydroindolo[3,4-c] Pyrazole_3_yl}_2_phenylpropanol; N-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl }-o-indole phenylethylamine; N-{5-benzhydrylamino group - 4,6-dihydro-pyrene}[3,4-〇] ° ratio 0 _3-based }_m-tolylethylamine; ^}-{5-benzhydrylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-pair - phenyl phenyl acetamide; 1 {5-benzhydrylaminocarbonyl-4,6-dihydroindolo[3,4-(:]"biazol-3-yl-o-anion Amine; N-{5-benzhydrylaminocarbonyl-4,6-dihydropyrolo[3,4-c] °pyrazol-3-yl}-3-methoxybenzamide; N- {5-Benzyldecylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}-p-bacteria; N-{5-benzhydryl Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-phenoxyethylamine; N-{5-benzhydrylaminocarbonyl-4,6- Dihydrogen ratio [3,4-(:]pyrazolylindole-2_ phenyl phenylamine;

C:\2D-00DE\91-01\90119473.ptd 第245頁 1327569 五、發明說明（243) N-{5-苯曱醯基胺基羰基-4, 6-二氫咄咯并[3, 4-c]咄唑 -3 -基}-3-氣苯基乙酿胺， N-{5-苯曱醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-4-氟苯基乙醯胺； !^-{5-苯曱醯基胺基羰基-4,6-二氫吡°各并[3,4-(：]°比。坐 -3-基卜3-(2-噻吩基）丙烯醯胺； N-{5 -苯曱酿基胺基羰基- 4,6 -二氫D比洛并[3,4-c] °比°坐 -3-基}-3-(3-噻吩基）丙烯醯胺； 1^-{5-苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 ^-3-基}-3-(2 -噻吩基）丙醯胺； 1^-{5-苯曱醯基胺基叛基-4,6-二氫吡0各并[3,4-(：]〇比。坐 _3-基}-2 -氣苯曱酿胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫°比咯并[3, 4-c]吼唑 _3-基}-3 -氯苯曱酿胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-4-氣苯甲醯胺； N-{5 -苯曱醯基胺基羰基-4,6 -二氫°比咯并[3,4-c]吡唑 -3 -基} - 1 -哌啶丙醯胺； φ N-{5-笨曱醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c] °比唑 _3_基}_2_乙酿基苯曱酿胺； 1\1-{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}_4_乙酿基苯曱酿胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-1-萘曱醯胺；C:\2D-00DE\91-01\90119473.ptd Page 245 1327569 V. INSTRUCTIONS (243) N-{5-Benzenylaminocarbonyl-4,6-dihydroindole[3, 4-c]carbazole-3-yl}-3-phenylphenylethylamine, N-{5-phenylhydrazinocarbonyl-4,6-dihydropyrrolo[3,4-c]pyridin Zyridin-3-yl}-4-fluorophenylacetamidine; !^-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyridyl[3,4-(:]° ratio -3-Ki 3-(2-thienyl)propenylamine; N-{5-benzoquinoneaminocarbonyl- 4,6-dihydro Dbi-l[3,4-c] ° °-3-yl}-3-(3-thienyl)propenylamine; 1^-{5-benzhydrylaminocarbonyl-4,6-dihydropyrrolo[3,4-(: Pyrazol-3-yl}-3-(2-thienyl)propanamine; 1^-{5-phenylhydrazino-amino-derivative-4,6-dihydropyridinol[3, 4-(:]〇 ratio. Sit _3-yl}-2 - gas benzoquinone; N-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydrogen ratio [3, 4 -c]carbazole-3-yl}-3-chlorobenzoquinone; N-{5-phenylhydrazinocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole- 3-yl}-4-oxobenzamide; N-{5-phenylhydrazinocarbonyl-4,6-dihydropyr-[3,4-c]pyrazole-3-yl} - 1 - piperidine; φ N-{5- albino aminocarbonyl-4,6-dihydropyrrolo[3,4-c] °biazole_3_yl}_2_ethyl phenyl benzoate; 1\1 -{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}_4_ethylphenylbenzoate; N-{5- Benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-1-naphthylamine;

C:\2D-CODE\91-01\90119473.ptd 第246頁 1327569 五、發明說明（244) N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3,4-c]吡唑 -3-基}-2 -萘曱醯胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫咣咯并[3, 4-c]咄唑 -3-基}-3 -苯曱醯基丙醯胺； ^{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-4-乙醯胺基苯曱醯胺； 1{5-苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 _3-基}-2，5_二甲氧苯曱酿胺； N-{ 5-苯曱醯基胺基羰基-4, 6-二氫咄咯并[3, 4-c]吡唑 -3-基}-2,6 -二曱氧苯甲醯胺； N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吼咯并[3,4-c] °比唑 _3-基}-3，4_二甲氧苯甲酿胺； N-{5-苯曱醯基胺基羰基-4, 6-二氫咄咯并[3, 4-c]吡唑 -3-基}-3, 5-二曱氧苯甲醯胺； ]\1-{5-苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-(：]吼唑 -3-基}-3-(2-噻吩甲醯基）-丙醯胺； N-{5-苯甲醯基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 _3-基}-2 -蔡基乙酿胺； N-{5 -苯曱醯基胺基羰基-4,6 -二氫°比咯并[3,4-c]吡唑 _3_基}-1-蔡基乙酿胺； 1^-{5-苯甲醯基胺基羰基-4,6-二氫咄咯并[3,4-(：]咣唑 -3-基}-4-苯基苯甲醯胺； 1'1-{5-胺基獄基-4,6-二氫〇比'1各并[3,4-(：]11比°坐-3-基}-乙醯胺；C:\2D-CODE\91-01\90119473.ptd Page 246 1327569 V. INSTRUCTIONS (244) N-{5-Benzenylaminocarbonyl-4,6-dihydropyrrolo[3,4 -c]pyrazol-3-yl}-2-naphthylamine; N-{5-phenylhydrazinocarbonyl-4,6-dihydroindolo[3,4-c]carbazole- 3-yl}-3-phenylmercaptopropylamine; ^{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}- 4-acetamidobenzoguanamine; 1{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}-2,5 _Dimethoxybenzoquinone; N-{ 5-phenylhydrazinocarbonylcarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-2,6- Diphenoxybenzamide; N-{5-benzoguanidinocarbonyl-4,6-dihydroindolo[3,4-c] °biazole-3-yl}-3,4_ Dimethoxybenzoic acid; N-{5-benzoguanidinocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-3, 5-di [0,4-(:]oxazol-3-yl}-3-( 2-thiophenemethyl)-propanamine; N-{5-benzhydrylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-2 Cai Jiyi, Amine; N-{ 5-Benzylaminocarbonyl-4,6-dihydropyrolo[3,4-c]pyrazole-3-yl}-1-caiyldiamine; 1^-{5-benzamide Aminocarbonyl-4,6-dihydroindolo[3,4-(:]oxazol-3-yl}-4-phenylbenzamide; 1'1-{5-amine base -4,6-dihydroanthracene is more than '1, and [3,4-(:]11 is more than -3-yl}-acetamide;

C:\2D-00DE\91-01\90119473.ptd 第247頁 1327569 五、發明說明（245) N-{5 -胺基羰基-4,6-二氫吼11各并[3,4-〇:]°比°坐-3-基}-環丙烷羧醯胺； N_{5 -胺基獄基_4, 6_二氫吼D各并[3，4-c] °比。坐-3_基}_異丁醯胺； N-{5 -胺基幾基- 4,6 -二氫吼11各并。，斗-以吼唾^-基卜環戊烷羧醯胺； N_{5 -胺基獄基-4，6 -二氫°比p各并[3，4-c] °比°坐-3 -基}-苯甲醯胺； N-{5 -胺基幾基- 4,6 -二氫吼11各并[3，4-c] °比0坐-3-基}-曱 •基吡啶甲醯胺； N-{5 -胺基叛基-4，6 -二氫°比p各并[3，4-c] σ比°坐-3 -基}_於驗醯胺； N-{5 -胺基獄基-4，6 -二氫11比ρ各并[3，4-c] °比。坐-3 -基丨-異菸鹼醯胺； Ν-{5 -胺基幾基-4, 6 -二氫°比Β各并[3，4-c] ρ比。坐-3-基}-3-甲基-2-呋喃曱醯胺； Ν-{5 -胺基幾基-4，6 -二氫D比ρ各并[3,4-c]吼°坐-3-基卜0塞吩-2-羧醯胺； N-{5 -胺基截基- 4,6 -二氫D比p各并[3,4-c] 11比唾-3-基丨-D塞吩-3 -缓酿胺； N-{5 -胺基幾基-4，6 -二氫D比p各并[3，4-c]"比°坐-3 -基}-鄰 -甲苯甲醯胺； N-{5 -胺基獄基-4，6 -二氫吼11 各并[3，4-c] 〇比。坐-3-基}-間 -甲苯曱醯胺；C:\2D-00DE\91-01\90119473.ptd Page 247 1327569 V. INSTRUCTIONS (245) N-{5-Aminocarbonyl-4,6-dihydroindole 11 and [3,4-〇 :]°°°-3-yl}-cyclopropanecarboxamide; N_{5-amine-based prison group_4,6-dihydroindole D each [3,4-c] ° ratio. Sitting -3_yl}-isobutylamine; N-{5-aminodido-4,6-dihydroindole 11 each. , bucket - 吼 ^ ^ - kib cyclopentane carboxamide; N_{5 - amine phenyl group-4,6 - dihydrogen ratio p and [3,4-c] ° ratio sit-3 -yl}-benzamide; N-{5-amino-yl- 4,6-dihydroindole 11 each [3,4-c] ° 0--3-yl}-purinyl-pyridine Methionine; N-{5-amino thiol-4,6-dihydrogen ratio p and [3,4-c] σ ratio ° sit-3 -yl}_in the test amine; N-{ 5-amino-based pegyl-4,6-dihydrogen 11 is more than [3,4-c] °. Sitting on -3 -ylindole-isonicotinium amide; Ν-{5-aminoglycol-4,6-dihydrogen ratio Β[3,4-c] ρ ratio. Sodium-3-yl}-3-methyl-2-furanium; Ν-{5-amino-based-4,6-dihydro D ratio ρ[3,4-c]吼° -3- kib 0-cephen-2-carboxyindole; N-{5-amino-based- 4,6-dihydro-D ratio p-[3,4-c] 11-syn-3-yl丨-D ceto-3 - slow-acting amine; N-{5-amino benzyl-4,6-dihydro D ratio p and [3,4-c]" than ° sitting -3 -yl} - o-toluamylamine; N-{5-amino-p-phenyl-4,6-dihydroindole 11 each [3,4-c] fluorene ratio. Sodium-3-yl}-m-toluidine;

C:\2D-C0DE\91-01\90119473_ptd 第248頁 1327569 五、發明說明（246) N-{5 -胺基獄基-4, 6 -二氫吼11各并[3，4-c] °比唾-3 -基卜對 -曱苯甲醯胺； N-{5 -胺基幾基-4，6_二氫°比略并[3，4-c]吼°坐-3-基}-苯基乙醯胺； N-{5 -胺基叛基-4, 6 -二氫°比°各并[3，4-c] °比°坐-3-基卜水楊醯胺； N-{5 -胺基裁基_4，6_二氫D比σ各并[3，4-c]吼°坐-3_基}-2-氟苯曱醯胺； Ν-{5 -胺基叛基-4，6_二氫D比17各并[3，4-c] °比°坐-3-基}-3-氟苯曱醯胺； N-{5 -胺基叛基-4，6 -二氫°比11 各并[3，4-c] °比°坐-3-基}-.4-氟苯甲醯胺； N-{5 -胺基羰基-4，6 -二氫吼17各并[3, 4-c] °比°坐-3-基} - 0塞吩-2-乙醯胺； N-{5 -胺基幾基_4，6 -二氫。比11各并[3，4-c]"比11 坐-3-基}_°塞吩-3-乙醯胺； N-{5 -胺基羰基-4，6 -二氫吼11各并[3, 4-c]吼唾-3-基丨-苯基丙炔醯胺； N-{5 -胺基羰基-4, 6 -二氫吼11各并[3, 4-c] °比°坐-3-基}-3-氰基苯甲醯胺； N-{5 -胺基幾基-4，6 -二氫°比°各并[3, 4-c] °比**坐-3_基丨- 4-氰基苯曱醯胺； N-{5_胺基幾基_4，6 -二氫°比11 各并[3，4-c] π比。坐-3_基}-反 _桂皮酿胺；C:\2D-C0DE\91-01\90119473_ptd Page 248 1327569 V. INSTRUCTIONS (246) N-{5-Amine Prison-4,6-Dihydroindole 11 and [3,4-c] ° than salivation-3-yl b-p-benzamide; N-{5-amino-based-4,6-dihydrogen ratio slightly [3,4-c]吼°-3-yl }-Phenylacetamide; N-{5-amino-based t-group-4,6-dihydrogen ratio °[3,4-c] ° ratio of -3- benzyl salicylamine; N-{5-amino-based _4,6-dihydrogen D ratio σ and [3,4-c] 吼 ° sitting -3_yl}-2-fluorobenzamide; Ν-{5 - Amino-based 4-,6-dihydro D ratio of 17 and [3,4-c] ° ratio of -3-yl}-3-fluorobenzamine; N-{5-amino thiol -4,6-dihydrogen ratio 11 each [3,4-c] ° ratio -3-yl}-.4-fluorobenzamide; N-{5-aminocarbonyl-4,6 - indoline 17 each [3, 4-c] ° ratio -3-yl} - 0 cephene-2-acetamide; N-{5-aminol-yl 4,6-dihydrogen . More than 11 and [3,4-c]" than 11 -3-yl}_°cetin-3-acetamide; N-{5-aminocarbonyl-4,6-dihydroindole 11 And [3, 4-c]pyridin-3-ylindole-phenylpropynylamine; N-{5-aminocarbonyl-4,6-dihydroindole 11 each [3, 4-c] ° °-3-yl}-3-cyanobenzamide; N-{5-amino-based-4,6-dihydrogen ratio °[3, 4-c] ° ratio** Sitting -3_ylindole- 4-cyanobenzoquinone; N-{5-amino-based _4,6-dihydrogen ratio 11 and [3,4-c] π ratio. Sit -3_base}-reverse _ cinnabarine amine;

C:\2D-C0DE\91-01\90119473.ptd 第249頁 1327569 五'發明說明（247) N - { 5 -胺基羰基-4，6 -二氫吡咯并[3，4 - c ]吡唑-3 -基}-順 -桂皮醯胺； N-{5 -胺基羰基-4，6 -二氫D比p各并[3，4-c] °比°坐-3-基}-3-(3 -吡啶基）丙烯醯胺； N-{5 -胺基叛基-4，6 -二氫π比°各并[3，4-c] °比°坐-3-基}_ 3_(4_π比咬基）丙稀酿胺， N-{5 -胺基羰基-4, 6 -二氫^比。各并[3,4-c]吼°坐-3-基}-2-苯基丙醯胺； N-{5 -胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基}-鄰甲笨基乙醯胺； N-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3 -基卜間 -曱苯基乙醯胺； N-{5 -胺基叛基_4，6 -二氫°比11 各并[3，4-c]吼。坐基卜對 -曱苯基乙醯胺； N-{5 -胺基幾基-4，6 -二氫p比略并[3，4-c] 11比σ坐-3-基}-鄰 -茴香酿胺； Ν_{5_胺基叛基-4, 6_二氫吼11 各弁[3，4-c] °比°坐-3_基}_3-曱氧苯甲醯胺； _ N-{5_胺基幾基-4，6 -二氮°比p各弁[3，4-c] D比°坐-3_基}-對 -茴香醯胺； N-{5 -胺基幾基- 4，6 -二氫D比洛并[3,4-〇]°比°坐-3-基}-苯氧乙醯胺； N-{5 -胺基羰基-4, 6 -二氫17比11 各并[3,4-c]吼°坐-3 -基}-2-氟苯基乙醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 249 1327569 V'Inventive Description (247) N - { 5 -Aminocarbonyl-4,6-dihydropyrrolo[3,4 - c ]pyridin Zyridin-3-yl}-cis-cinnamate; N-{5-aminocarbonyl-4,6-dihydrogen D ratio p[3,4-c] ° ratio sit-3-yl}- 3-(3-Pyridyl)propenylamine; N-{5-amino-t-radyl-4,6-dihydro-π ratio °[3,4-c] °°°-3-yl}_ 3_(4_π than bite) acrylamide, N-{5-aminocarbonyl-4,6-dihydrogen ratio. Each [3,4-c]吼°-3-yl}-2-phenylpropanamine; N-{5-aminocarbonyl-4,6-dihydroindole[3,4-indole Pyrazol-3-yl}-o-phenylideneacetamide; N-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl - phenyl phenyl acetamide; N-{5-amino thiol-4,6-dihydrogen ratio 11 and [3,4-c] oxime.基卜对曱曱曱曱 ; ; ;; N-{5 -amino-based benzyl-4,6-dihydro p ratio slightly [3,4-c] 11 than σ sitting-3-yl}-neighbor - anise-brown amine; Ν_{5_amino-based thiol-4,6-dihydroanthracene 11 弁[3,4-c] ° ratio ° sitting -3 _} 曱曱曱苯 ; ;; N-{5_Aminomethyl-4,6-diazot ratio p 弁[3,4-c] D ratio ° sitting -3 yl}-p-anisylamine; N-{5-amine Alkyl- 4,6-dihydro-D-Bisto[3,4-〇]°°°-3-yl}-phenoxyacetamide; N-{5-aminocarbonyl-4,6- Dihydrogen 17 to 11 each [3,4-c] 吼 ° -3 -yl}-2-fluorophenylacetamide;

C:\2D-C0DE\91-01\90119473.ptd 第250頁 1327569 五、發明說明（248) N-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]咄唑-3 -基}-3-氟苯基乙醯胺； N-{5 -胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吼唑-3 -基}-4-氟笨基乙醯胺； N-{5 -胺基幾基-4, 6 -二氫D比11 各并[3，4-c] °比°坐-3-基}-3 -(2-噻吩基）丙烯醯胺； N-{5 -胺基幾基-4, 6 -二氫σ比洛并[3，4-c]吼峻^-基}^ -(3 -噻吩基）丙烯醯胺； Ν-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c] °比吐-3-基}-3 -(2 -噻吩基）丙醯胺； Ν-{5 -胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3~基卜2-氯笨曱醯胺； 1{5-胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-3-氯笨曱醯胺； Ν-{5 -胺基幾基-4，6 -二氫°比σ各并[3, 4-c]吼°圭-3 -基}-4-氯笨甲醯胺； Ν-{5 -胺基叛基-4，6 -二氮吼17各弁[3，4_c]"比°坐_3_基}_1- 啶丙醯胺； N-{5 -胺基幾基-4，6 -二氫°比11 各并[3，4-c] °比°生-3 -基}-2-乙醯基苯曱醯胺； N-{5 -胺基幾基-4，6 -二氫°比p各并[3，4-c] °比°圭基}-4-乙醯基苯曱醯胺； 1^1-{5-胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-：1-萘甲醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 250 1327569 V. INSTRUCTIONS (248) N-{5-Aminocarbonyl-4,6-dihydroindolo[3,4-c] Oxazol-3-yl}-3-fluorophenylacetamide; N-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c]carbazole-3-yl}- 4-fluorophenylacetamide; N-{5-amino-based-4,6-dihydro-D ratio 11 and [3,4-c] ° ratio -3-yl}-3 - ( 2-thienyl)propenylamine; N-{5-amino-based-4,6-dihydro-σ-pyrolo[3,4-c]吼^^-yl}^-(3-thiophenyl) Acrylamide; Ν-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c]°-dose-3-yl}-3-(2-thienyl)propanamide; Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3~yl-2-chlorobenzamide; 1{5-aminocarbonyl-4,6 -dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-chlorobenzamide; Ν-{5-aminol-yl-4,6-dihydrogen ratio σ[ 3, 4-c]吼°圭-3 -yl}-4-chlorobenzamide; Ν-{5-amino thiol-4,6-diazepine 17 弁[3,4_c]" °3_基}_1- pyridine propylamine; N-{5-amino benzyl-4,6-dihydrogen ratio 11 and [3,4-c] ° ratio -3 - } -2- 醯醯 phenyl hydrazide; N-{5-amino-based group-4,6-dihydrogen ratio p and [3,4-c] ° ratio 圭基}-4-acetamidobenzoin; 1^1-{ 5-aminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-: 1-naphthylcarboxamide;

C:\2D-CDDE\91-01\90119473.ptd 第251頁 1327569 五、發明說明（249) N-{5 -胺基羰基-4,6-二氫吡咯并[3,4-c]呲唑-3-基}-2-萘曱醯胺； N-{5 -胺基幾基-4，6 -二氫D比p各并[3，4-c] D比σ坐-3-基}-3-苯曱醯基丙醯胺； & N-{5 -胺基幾基-4，6 -二氫π比17各并[3，4-c]吼°坐-3 -基}-4-乙醯胺基苯曱醯胺； 1{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-2, 5 -二曱氧苯曱醯胺； Ν_{5_胺基獄基_4，6 -二氯η比σ各弁[3，4-c] °比°坐-3_基}_2, 二甲氧苯曱醯胺； N-{5 -胺基羰基-4, 6 -二氫吼σ各并[3,4-c] °比。坐-3-基}-3, 4 -二甲氧苯甲醯胺； N_{5_胺基幾基-4，6 -二氫D比p各并[3，4-c] °比°坐-3 -基}-3, 5-二曱氧苯曱醯胺； N-{5 -胺基幾基-4, 6 -二氫吼p各并[3, 4-c] °比σ坐-3-基}-3 - ( 2 -噻吩曱醯基）-丙醯胺； ?^-{5-胺基羰基-4,6-二氫吼咯并[3,4-(：]吡唑-3-基}-2-萘基乙醯胺； Ν-{5_胺基獄基-4，6_二氮吼11 各并[3，4_c] η比Β坐-3-基}-1-萘基乙醯胺； Ν-{5 -胺基幾基-4，6 -二氫π比11 各并[3，4-c]吼°坐-3-基}-4 -苯基苯曱醯胺； N-{5 -胺基續醯基-4，6 -二氫吼11各并[3, 4-c]吼°坐-3 -基}-乙醯胺；C:\2D-CDDE\91-01\90119473.ptd Page 251 1327569 V. INSTRUCTIONS (249) N-{5-Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]indole Zyrid-3-yl}-2-naphthylamine; N-{5-amino-based-4,6-dihydro D ratio p and [3,4-c] D ratio σ--3-yl }-3-phenylmercaptopropylamine; & N-{5-amino-based-4,6-dihydroπ ratio 17 and [3,4-c]吼°-3 -yl} -4-acetamidobenzoin; 1{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-2,5-diindole Oxalbenzamine; Ν_{5_amine-based prison base_4,6-dichloro-n-ratio σ[3,4-c] ° ratio ° sitting -3_}}, methoxybenzoquinone Amine; N-{5-aminocarbonyl-4,6-dihydroindole σ and [3,4-c] ° ratio of sitting-3-yl}-3,4-dimethoxybenzamide; N_{5_Aminomethyl-4,6-dihydrogen D ratio p and [3,4-c] ° ratio -3 -yl}-3,5-dioxabenzoquinone; N -{5-amino-based-4,6-dihydroindole p and [3, 4-c] ° ratio σ-3-yl}-3 - (2-thiophenanthryl)-propanamide ;^-{5-aminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-2-naphthylacetamide; Ν-{5-amine Kiba base-4,6_diazepine 11 each [3,4_c] η than Β -3--3-yl}-1-naphthylacetamide; Ν-{5-amino-based-4,6-dihydroπ ratio 11 and [3,4-c]吼°-3-yl }-4-Phenylbenzamide; N-{5-Amino-indenyl-4,6-dihydroindole 11 and [3,4-c]吼°3 -yl}-acetamidine amine;

C:\2D-CODE\91-01\90119473.ptd 第252頁 1327569 五、發明說明（250) N-{5 -胺基項醯基-4，6 -二氫°比D各并[3，4-c]吼α坐-3-基}-環丙烷羧醯胺； Ν-{5 -胺基續醯基-4，6 -二氫吼11 各并[3, 4-c]吼11 坐-3-基}-異丁醯胺； Ν-{5 -胺基續酿基_4，6 -二氫°比0各并[3, 4-c] °比°坐-3-基}-環戊烷羧醯胺； Ν-{5_胺基續醯基_4, 6 -二氫°比略并[3，4-c] °比。坐-3_基}-苯甲醯胺； Ν - {5 -胺基續酿基-4，6_二氫π比η各弁[3，4-c] β比。坐-3-基}-曱基吡啶甲醯胺； Ν-{5 -胺基續醯基-4, 6 -二氫°比略并[3, 4-c] D比哇-3-基}-菸鹼醯胺； N-{5 -胺基續醯基-4,6-二氫β比p各并[3,4-c]吡°坐-3-基}-異菸鹼醯胺； N-{5 -胺基續醯基-4，6 -二氫吼11 各并[3, 4-c]吼。坐-3-基}-3-甲基-2 -呋喃甲醯胺； N-{5 -胺基項醢基-4, 6 -二氫β比略并[3, 4-c] °比°坐-3-基Ια塞吩 _ 2 - 缓酿胺； Ν-{5 -胺基績醯基- 4,6 -二氫各并[3,4-c]1^。坐-3-基}-噻吩-3-羧醯胺； N-{5 -胺基續醯基-4，6 -二氫D比略并[3, 4-c]吼°坐-3-基}-鄰-甲苯曱醯胺； N-{5 -胺基續醯基-4, 6 -二氫β比洛并[3, 4-c] 11比°坐-3-基}-間-曱苯曱酿胺；C:\2D-CODE\91-01\90119473.ptd Page 252 1327569 V. INSTRUCTIONS (250) N-{5-amine-based fluorenyl-4,6-dihydrogen ratio D and [3, 4-c]吼α-yl-3-yl}-cyclopropanecarboxamide; Ν-{5-amino sulfonyl-4,6-dihydroindole 11 each [3, 4-c]吼11 -3-yl}-isobutylamine; Ν-{5-amino aryl group _4,6-dihydrogen ratio 0 and [3, 4-c] ° ratio sit-3-yl}- Cyclopentane carboxamide; Ν-{5_amino group 醯 _4,6-dihydrogen ratio slightly [3,4-c] ° ratio. Sitting on -3_yl}-benzamide; Ν - {5-amino aryl--4,6-dihydro-π ratio η [3,4-c] β ratio. -3--yl}-mercaptopyridinecarbamamine; Ν-{5-amino sulfonyl-4,6-dihydrogen ratio slightly [3, 4-c] D than wow-3-yl} - nicotine decylamine; N-{5-amino sulfonyl-4,6-dihydro-β ratio p and [3,4-c]pyridin-3-yl}-isonicotinamine; N-{5-Amino-indenyl-4,6-dihydroindole 11 each [3,4-c]indole. -3--3-yl}-3-methyl-2-furancarboxamide; N-{5-amine-based fluorenyl-4,6-dihydro-β ratio slightly [3, 4-c] ° ratio Sodium-3-yl hydrazone alpha thiophene _ 2 - slow-acting amine; Ν-{5-amino fluorenyl- 4,6-dihydro-[3,4-c]1^. -3--3-yl}-thiophene-3-carboxamide; N-{5-amino sulfonyl-4,6-dihydro D ratio slightly [3, 4-c] 吼 °-3-yl }-o-toluidine; N-{5-amino sulfonyl-4,6-dihydrobeta-pyrolo[3,4-c] 11 ratio °-3-yl}-m-anthracene Benzoquinone

C:\2D-C0DE\91-01\90119473.ptd 第253頁 1327569 五、發明說明（251) N-{5 -胺基續醯基-4，6 -二氫吼^各并[3，4-c] °比。圭-3 -基}-對-甲苯曱醯胺； N-{5 -胺基績醯基_4，6 -二氫°比p各并[3，4-c]吼°坐-3-基}-苯基乙醯胺； N-{5 -胺基續醯基-4，6 -二氫σ比11 各并[3, 4-c] °比α坐-3-基}-水楊醯胺； Ν-{5_胺基石黃酿基_4，6_二氫D比洛并[3，4_c]吼σ坐-3_基}_ 2 -氟苯曱醯胺； Ν_{5_胺基石黃醯基_4, 6 -二氫0比口各弁[3，4 — c] 0比0坐_3-基}_ 1^8-氟苯曱醯胺； Ν-{5 -胺基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3 -基ΙΑ- 氟苯曱醯胺； Ν-{5 -胺基績醯基-4，6 -二氫°比0各并[3,4-c]吼°坐-3-基}-噻吩-2-乙醯胺； N-{5 -胺基續醯基-4, 6 -二氫吼11 各并[3, 4-c]吼°坐-3 -基}-噻吩-3-乙醯胺； N-{5_胺基績酿基-4，6_二氫B比p各并[3, 4-c] **比°坐-3-基}-苯基丙炔醯胺； I N-{5 -胺基續醯基-4,6 -二氫吼11 各并[3,4-c] °比唾-3 -基}-’3-氰基苯甲醯胺； N-{5 -胺基續酿基-4, 6 -二氫°比°各并[3, 4-c] °比。坐-3-基Ι-ΐ- 氰基苯曱醯胺； Ν-{5 -胺基續醯基-4，6 -二氫吼ρ各并[3，4-c]吼°坐-3 -基}-反-桂皮酿胺；C:\2D-C0DE\91-01\90119473.ptd Page 253 1327569 V. INSTRUCTIONS (251) N-{5-Amino-indenyl-4,6-dihydroanthracene[3,4 -c] ° ratio.圭-3-yl}-p-toluidine; N-{5-amino fluorenyl _4,6-dihydrogen ratio p and [3,4-c]吼°-3-yl }-Phenylacetamide; N-{5-aminothio-indenyl-4,6-dihydro-sigma ratio 11 and [3, 4-c] ° ratio α--3-yl}-salt Amine; {5_amine stone yellow wine base_4,6_ dihydrogen Dbiol[3,4_c]吼σ sit-3_yl}_ 2-fluorophenylguanamine; Ν_{5_amine Basestone Astragalus _4,6-Dihydrogen 0 is more than 口[3,4 — c] 0 to 0 sits _3-yl}_ 1^8-fluorobenzoguanamine; Ν-{5-aminosulfonamide 4-,6-dihydroindolo[3,4-c]pyrazol-3-ylindole-fluorophenyl hydrazide; Ν-{5-amino fluorenyl-4,6-dihydrogen More than 0 each [3,4-c] 吼 ° sit-3-yl}-thiophene-2-acetamide; N-{5-amino sulfonyl-4,6-dihydroindole 11 each [ 3, 4-c]吼° sitting -3 -yl}-thiophene-3-acetamide; N-{5_amine-based base-4,6-dihydro-B ratio p and [3, 4- c] ** is more than -3-yl}-phenylpropynylamine; I N-{5-amino sulfonyl-4,6-dihydroindole 11 each [3,4-c] ° Specific ratio of salino-3-yl}-'3-cyanobenzamide; N-{5-amino aryl- 4,6-dihydrogen ratio of [3, 4-c] °. -3--3-ylindole-ΐ-cyanobenzoquinone; Ν-{5-amino sulfonyl-4,6-dihydroindole ρ[3,4-c]吼°-3 - Base}-anti-cassia

C:\2D-CODE\91-01\90119473.ptd 第254頁 1327569 五、發明說明（252) N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-順-桂皮醯胺； N-{5 -胺基績醯基-4，6 -二氫°比17各并[3, 4-c] °比°坐-3-基}-3-(3 -吡啶基）丙烯醯胺； N-{5 -胺基續醢基-4, 6 -二氫D比π各并[3, 4-c] °比哇-3 -基}-3-(4-吡啶基）丙烯醯胺； N-{5 -胺基續醯基-4, 6 -二氫吼11 各并[3，4-c]吼°坐-3 -基}- 2- 笨基丙醯胺； N-{5 -胺基續醯基-4，6 -二氫D比p各并[3，4-c] -基}- 鄰-曱苯基乙醯胺； Ν_{5 -胺基續醯基-4，6_二氫β比11 各并[3，4-c]吼峻^-基}-間-曱苯基乙醯胺； Ν-{5 -胺基續醯基-4，6-二氫°比°各并[3, 4-c] D比。坐-3-基}-對-曱苯基乙醯胺； N-{5 -胺基績酿基-4，6 -二氮D比11 各并[3，4-c] °比°坐-3_基}-鄰-茴香醯胺； N-{5 -胺基石黃酿基-4, 6_二氫D比σ各并[3，4-c] °比。坐-3_基}- 3- 曱氧苯甲醯胺； Ν - {5 -胺基續酿基-4，6_二氮π比ρ各弁[3，4_c] D比°坐_3_基}-對-茴香醯胺； N-{5 -胺基續醢基-4，6_二氫吼11 各并[3，4-c]吼°坐-3 -基}-苯氧乙醯胺； N-{5 -胺基項醯基-4, 6 -二氫B比p各并[3，4-c]吼°坐-3_基}-2-氟苯基乙醯胺；C:\2D-CODE\91-01\90119473.ptd Page 254 1327569 V. INSTRUCTIONS (252) N-{5-Aminosulfonyl-4,6-dihydropyrrolo[3,4-c Pyrazol-3-yl}-cis-cinnamate; N-{5-aminol-alkyl-4,6-dihydrogen ratio 17 and [3, 4-c] °° sitting-3 -yl}-3-(3-pyridyl)propenylamine; N-{5-amino sulfonyl-4,6-dihydrogen D ratio π and [3, 4-c] ° than wow-3 -yl}-3-(4-pyridyl)propenylamine; N-{5-aminothio-indenyl-4,6-dihydroindole 11 each [3,4-c]吼°3 - }}- 2- phenyl propylamine; N-{5-amino sulfonyl-4,6-dihydro D ratio p and [3,4-c]-yl}-o- phenylene Indoleamine; Ν_{5-amino group thiol-4,6-dihydrobeta ratio 11 each [3,4-c]吼^^yl}-m-decylphenylacetamide; Ν-{ 5-Amino-indenyl-4,6-dihydrogen ratios are each [3, 4-c] D ratio. Sodium-3-yl}-p-indole phenylacetamide; N-{5-amino-based base-4,6-diaza D ratio 11 and [3,4-c] ° ratio - 3_yl}-o-anisoleamine; N-{5-amino sulfonyl-4,6-dihydrogen D ratio σ and [3,4-c] ° ratio. Sitting -3_yl}- 3- phenoxybenzamine; Ν - {5-amino styrene-4,6_dinitrogen π ratio ρ[3,4_c] D ratio ° sitting_3_ }--p-anisole; N-{5-amino sulfonyl-4,6-dihydroindole 11 each [3,4-c] 吼 ° -3 -yl}-phenoxy oxime Amine; N-{5-amine-based fluorenyl-4,6-dihydro-B ratio p and [3,4-c] 吼 ° -3 -yl}-2-fluorophenylacetamide;

第255頁 C:\2D-G0DE\91-01\90119473.ptd 1327569 五、發明說明（253) N-{5-胺基磺醯基-4, 6-二氫吡咯并[3,4-c]吡唑-3-基}-3-氟苯基乙醯胺； N-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基Ι-ΐ- 氟苯基乙醯胺； Ν_{5_胺基確基-4，6 -二氫吼ρ各并[3，4-c] β比°坐-3_基}-3-(2 -噻吩基）丙烯醯胺； N-{5 -胺基績醯基-4, 6 -二氫11比17各并[3, 4-c] °比。坐-3-基}- 3- (3 -噻吩基）丙烯醯胺； N-{5 -胺基績醯基-4, 6 -二氫n比0各并[3，4-c] °比。坐-3 -基}-^8-(2-噻吩基）丙醯胺； N-{5 -胺基績醯基-4, 6 -二氫咄σ各并[3,4-c]吼。坐-3-基}- 2 -氯苯曱醯胺； N-{5_胺基續酿基_4，6 -二氮吼p各并[3，4-c] °比。坐-3_基}- 3 -氯苯甲醯胺； N_{5_胺基項酿基-4，6_二氮°比B各弁[3, 4_c] °比α坐_3_基ΙΑ - 氯苯曱醯胺； Ν-{5 -胺基續醯基-4, 6 -二氫吼°各并[3, 4-c]吼唾-3 -基}-1 - 底咬丙醯胺； Ν-{5 -胺基確醢基-4, 6 -二氫Β比洛并[3,4-c] η比唾-3-基}->2-乙醯基苯曱醯胺； ~-{5-胺基續醯基-4，6-二氫°比1>各并[3,4-(：]°比°坐-3-基}- 4- 乙醯基苯曱醯胺； Ν_{5 -胺基續酿基_4，6 -二氫°比ρ各并[3，4-c] °比α坐-3-基}-1-萘甲醯胺；Page 255 C:\2D-G0DE\91-01\90119473.ptd 1327569 V. INSTRUCTIONS (253) N-{5-Aminosulfonyl-4,6-dihydropyrrolo[3,4-c Pyrazol-3-yl}-3-fluorophenylacetamide; N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl Ι-ΐ-fluorophenylacetamide; Ν_{5_amino-based 4,6-dihydroindole ρ[3,4-c] β ratio ° sitting -3_}} 2 -Thienyl)propenylamine; N-{5-Amino-alkyl-4,6-dihydro 11 to 17 and [3, 4-c] ° ratio. -3--3-yl}- 3-(3-thiophenyl)propenylamine; N-{5-amino benzyl-4,6-dihydron- to 0-[3,4-c] ° ratio . Sodium-3-yl}-^8-(2-thienyl)propanamine; N-{5-aminodinyl-4,6-dihydroindole σ[3,4-c]indole. Sodium-3-yl}-2-hydroxybenzoguanamine; N-{5-amino aryl group 4,6-diazepine p each [3,4-c] ° ratio. Sitting -3_yl}- 3 - chlorobenzamide; N_{5_amine-based base-4,6-diazepine ratio B 弁[3, 4_c] ° ratio α sitting_3_基ΙΑ - chlorpheniramine; Ν-{5-amino sulfonyl-4,6-dihydroindole °[3,4-c] oxime-3-yl}-1 - acetophene Ν-{5-Amino-decyl-4,6-dihydroindolebi[3,4-c] η than sparg-3-yl}->2-ethylmercaptobenzamine; ~-{5-Amino-indenyl-4,6-dihydrogen ratio 1> Each [3,4-(:]°°°-3-yl}- 4-ethylmercaptobenzamine Ν_{5-amino aryl group _4,6-dihydrogen ratio ρ and [3,4-c] ° ratio α--3-yl}-1-naphthylcarboxamide;

C:\2D-OODE\91-Ol\90119473.ptd 第256頁 1327569 五、發明說明（254) N-{5_胺基確酿基-4，6_二氫D比**各弁[3，4_c] °比°坐-3_基}_ 2- 萘甲醯胺； N-{5 -胺基確醢基-4, 6 -二氫11比略并[3, 4-c] n比。坐-3-基}-3 -苯曱醯基丙醯胺； N-{5_胺基項酿基_4，6_二氫π比p各弁[3，4_c]吼°坐-3-基}_ 4-乙醯胺基苯甲醯胺； N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}- 2.5- 二甲氧苯曱醯胺； N-{5 -胺基續醯基- 4,6-二氫ϊ^比p各并[3,4-c]ι^比ι^坐-3-基}- 2.6- 二曱氧苯曱醯胺； N-{5 -胺基項醯基-4,6-二氫吼。各并[3,4-c] °比°坐-3-基}-3 ,4 -二曱氧苯甲醢胺； N-{5 -胺基確酿基_4，6_二氮°比p各并[3, 4_c] D比。坐-3_基}-3, 5-二曱氧苯曱醯胺； 1^-{5-胺基磺醯基-4,6-二氫吼咯并[3,4-(：]吡唑-3-基}- 3- (2 -噻吩曱醯基）-丙醯胺； N-{5 -胺基項醯基- 4,6 -二氫°比°各并[3,4-c]°比。坐-3-基}-2-萘基乙醯胺； N-{5 -胺基續醯基-4, 6 -二氫β比略并[3, 4-c] °比°坐-3-基} -1-萘基乙醯胺； Ν_{5 -胺基績醯基-4, 6 -二氫°比ρ各并[3, 4-c] ρ比嗤-3-基}- 4- 苯基苯曱醯胺； Ν-{5-甲笨磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}-乙醯胺；C:\2D-OODE\91-Ol\90119473.ptd Page 256 1327569 V. INSTRUCTIONS (254) N-{5_Amino-based 4-,6-dihydro-D ratio **[3] , 4_c] °°°−3_yl}_ 2-naphthylcarmine; N-{5-amino-decyl-4,6-dihydro 11 ratio slightly [3, 4-c] n ratio . -3--3-yl}-3-phenylmercaptopropylamine; N-{5_amine-based aryl-4,6-dihydro-π ratio p弁[3,4_c]吼° sitting-3- _ 4-Ethylaminobenzamide; N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}- 2.5- Dimethoxybenzamine; N-{5-aminodinyl- 4,6-dihydroanthracene ratio p and [3,4-c]ι^ than ι^ sit-3-yl}- 2.6- Dioxalylbenzamine; N-{5-amine-based mercapto-4,6-dihydroindole. Each [3,4-c] ° ratio of -3-yl}-3,4-dioxabenzamide; N-{5-aminol-branched _4,6-diazepine ratio p each and [3, 4_c] D ratio. -3-yl}-3,5-dioxabenzoquinone; 1^-{5-aminosulfonyl-4,6-dihydroindolo[3,4-(:]pyrazole -3-yl}- 3-(2-thiophenanthryl)-propanamine; N-{5-amine-based fluorenyl- 4,6-dihydrogen ratio °[3,4-c] ° ratio. sit-3-yl}-2-naphthylacetamide; N-{5-amino group hydrazino-4,6-dihydro-β ratio slightly [3, 4-c] ° ratio ° -3-yl}-1-naphthylacetamide; Ν_{5-amino fluorenyl-4,6-dihydrogen ratio ρ and [3, 4-c] ρ than 嗤-3-yl} 4- 4-phenylbenzamide; Ν-{5-methyl sulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-acetamide;

C:\2D-CODE\91-01\90119473_ptd 第257頁 1327569 五、發明說明（255) 1{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}- 環丙烷羧醯胺； N-{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-異丁醯胺； N-{5-曱苯績酿基_4，6 -二氫0比p各并[3，4_〇]°比〇坐_3_基}-環戊烷羧醯胺； N_{5_曱苯石黃酿基_4，6_二氮0比p各并[3，4_c] D比0坐_3_基}_ 苯曱醯胺； N-{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}- ·甲基吡啶曱醯胺； N-{5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}-菸鹼醯胺； ^»1-{5-曱苯績醯基-4，6-二氫°比17各并[3,4-(：]'1比°坐-3-基}-異菸鹼醯胺； 1^-{5-甲苯石黃醯基-4,6-二氫0比0各并[3,4-(：]11比°坐-3-基}-3-曱基-2-呋喃甲醯胺； N-{5-曱苯石黃醯基-4，6-二氫τ^比^I各并[3，4-c]°比o坐-3-基}-噻吩-2-羧醯胺； N-{5-曱苯石黃醯基- 4,6 -二氫D比0各并[3，4-c] °比〇坐-3-基}- •噻吩-3-羧酿胺； ^{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑-3-基}-鄰-曱苯曱醯胺； \-{5-曱苯石黃醯基-4,6-二氫吼〇各并[3,4-0：]〇比°坐-3-基}-間-曱苯曱醯胺；C:\2D-CODE\91-01\90119473_ptd Page 257 1327569 V. Description of the invention (255) 1{5-Toluenesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole -3-yl}-cyclopropanecarboxamide; N-{5-toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-isobutylamine; N-{5- 曱绩酿 _ 4,6 - dihydrogen 0 ratio p and [3,4_〇] ° than sitting _3_ base}-cyclopentane carboxamide; N_{5_ Benzene yellow wine base _4,6_ dinitrogen 0 ratio p and [3,4_c] D ratio 0 sitting _3_ base}_ benzoguanamine; N-{5-toluenesulfonyl-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-methylpyridinium; N-{5-toluenesulfonyl-4,6-dihydropyrrolo[3, 4-c]pyrazol-3-yl}-nicotinium amide; ^»1-{5-曱醯醯 -4-4,6-dihydrogen ratio 17 and [3,4-(:]' 1 than ° sit-3-yl}-isonicotinium amide; 1^-{5-tolyl xanthine-4,6-dihydro 0 to 0 each [3,4-(:]11 than ° sitting- 3-yl}-3-mercapto-2-furancarbamide; N-{5-bestone xanthene-4,6-dihydro-tau^^^^[3,4-c]° ratio o Sodium-3-yl}-thiophene-2-carboxamide; N-{5-bepholine xanthine- 4,6-dihydrogen D is 0 and each is [3,4-c] ° Base}- • thiophene-3-carboxylamine; ^{5- Phenylsulfonyl-4,6-dihydropyrrolo[3,4-indolyl-3-oxazol-3-yl}-o-nonylbenzamide; \-{5-bepholine xanthine-4,6- Dihydroindole each [3,4-0:] 〇 ratio 坐-3-yl}-m- phenyl hydrazine;

C:\2D-CODE\91-01\90119473.ptd 第258頁 1327569 五、發明說明（256) N-{5-甲苯磺醯基-4,6-二氫吼咯并[3,4-c]°比唑-3-基}-對-曱苯曱醯胺； ^{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-水楊醯胺； N-{5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3 -基}-2 -氟苯曱醯胺； ^{5-曱苯磺醯基-4,6-二氫吡咯并[3,4_〇]吡唑-3-基}- 3- 氟苯曱醯胺； ^^-{云-甲苯石黃醯基-斗^-二氫吼洛并^^-^吼峻^-基}- 4- 氟苯曱醯胺； ^{5-曱苯石黃醢基-4，6-二氫0比°各并[3,4-(：]〇比〇坐-3-基}-噻吩-2-乙醯胺； N_{5_曱苯項酿基_4，6_二氯0比B各弁[3，4_c] 0比0坐-3_基}-噻吩-3 -乙醯胺； N-{5-曱苯續醯基- 4,6 -二氫吼0各并[3,4-c] 0比。坐-3-基}-苯基丙炔醯胺； 1{5-曱苯磺醯基-4,6-二氫"比咯并[3,4-(：]"比唑-3-基}-3-氰基苯曱醯胺； N-{5-曱苯磺醯基-4,6 -二氫吡咯并[3, 4-c]吡唑-3 -基ΙΑ- 氰基苯甲醯胺； 1{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-反-桂皮酿胺； Ν-{5-曱苯磺醯基-4, 6 -二氫咄咯并[3,4-c]咄唑-3 -基}-順-桂皮醯胺；C:\2D-CODE\91-01\90119473.ptd Page 258 1327569 V. INSTRUCTIONS (256) N-{5-Toluenesulfonyl-4,6-dihydroindole[3,4-c ]°Bizozol-3-yl}-p-nonylbenzamide; ^{5-toluenesulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}- Salicylamine; N-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-c]indazol-3-yl}-2-fluorobenzoguanamine; ^{5 - Benzene sulfonyl-4,6-dihydropyrrolo[3,4_〇]pyrazol-3-yl}-3-fluorobenzamide; ^^-{cloud-toluene xanthine-bucket^ -Dihydrofuran and ^^-^吼君^-yl}- 4-fluorophenyl hydrazide; ^{5-bepholine xanthine-4,6-dihydrogen 0 ratio °[3,4- (:] 〇〇 -3- -3-yl}-thiophene-2-acetamide; N_{5_ benzene benzene base _4,6_ dichloro 0 to B 弁 [3,4_c] 0 to 0 Sitting -3_yl}-thiophene-3-acetamide; N-{5-nonylbenzene fluorenyl- 4,6-dihydroindole 0 and [3,4-c] 0 ratio. }}-phenylpropynylamine; 1{5-nonylbenzenesulfonyl-4,6-dihydro"bido[3,4-(:]"biazol-3-yl}-3 -cyanobenzamine; N-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-ylindole-cyanobenzamide; {5-nonphenylsulfonyl-4,6-dihydrogen Pyrrolo[3,4-indolylpyrazol-3-yl}-trans-cinnamin; Ν-{5-nonylsulfonyl-4,6-dihydroindolo[3,4-c] Carbazole-3-yl}-cis-cinnamate;

C:\2D-OODE\91-Ol\90119473.ptd 第259頁 1327569 五、發明說明（257) 1^-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3 - ( 3 -吡啶基）丙烯醯胺； ^{5-曱苯磺醯基-4,6-二氫0比咯并[3,4-(：]°比唑-3-基} -3-(4-吡啶基）丙烯醯胺； N-{5-曱苯石黃醯基- 4,6 -二氫吼0各并[3，4-c] D比0坐-3-基}- 2- 笨基丙醯胺； N-{5-曱苯石黃醯基- 4,6 -二氫0比17各并[3，4-c] 0比0坐-3_基}-鄰-曱苯基乙醯胺； N-{5-曱苯續醯基-4，6 -二氫°比°各并[3，4-c] 0比。坐-3-基}-間-曱苯基乙醯胺； N-{5-曱苯磺醯基-4,6 -二氫°比咯并[3,4-c]"比唑-3 -基}-對-曱苯基乙醯胺； N-{5_甲苯石黃酿基_4，6_二氫吼11 各并[3，4-c] °比°坐-3-基}-鄰-茴香醯胺； 1{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}- 3- 甲氧苯曱醯胺； Ν-{5-曱苯石黃酿基_4，6 -二氮0比11 各并[3，4-c] 0比0坐-3-基}_ 對-茴香醯胺； _^{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}_ 苯氧乙醯胺； Ν-{5-曱苯績酿基- 4,6 -二氫吼11 各并[3，4-c]°比0坐~3_基}_ 2- 氟苯基乙醯胺； N-{5-曱苯續醯基-4, 6 -二氫0比°各并[3, 4-c] °比。坐-3-基}- 3- 氟苯基乙醯胺；C:\2D-OODE\91-Ol\90119473.ptd Page 259 1327569 V. INSTRUCTIONS (257) 1^-{5-Phenylsulfonyl-4,6-dihydropyrrolo[3,4- (:]pyrazol-3-yl}-3 -(3-pyridyl)propenylamine; ^{5-nonylsulfonyl-4,6-dihydro- 0-pyrano[3,4-(: ]°Bizozol-3-yl}-3-(4-pyridyl)propenylamine; N-{5-beanthine-glycosyl- 4,6-dihydroindole 0-[3,4-c] D -3-yl}- 2- streptopropylamine; N-{5-bepholine xanthine- 4,6-dihydrogen 0 to 17 each [3,4-c] 0 to 0 sitting- 3_基}-o-indole phenylacetamide; N-{5-nonylbenzene fluorenyl-4,6-dihydrogen ratio °[3,4-c] 0 ratio. }--m-phenyl phenyl acetamide; N-{5-nonyl benzene sulfonyl-4,6-dihydro-pyrano[3,4-c]"biazole-3-yl}- P-Phenyl phenyl acetamide; N-{5_toluene yellow aryl-4,6-dihydroindole 11 each [3,4-c] ° ratio of sitting-3-yl}-o-fennel Guanidine; 1{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-methoxybenzamine; Ν-{5 - indimen yellow base _4,6-diaza 0 to 11 each [3,4-c] 0 to 0 -3-yl} _ p-anisoleamine; _^{5-nonylbenzenesulfonate Mercapto-4,6-dihydropyrrolo[3,4-〇 Pyrazol-3-yl}-phenoxyacetamide; Ν-{5-曱绩酿 - - 4,6-dihydroindole 11 each [3,4-c] ° than 0 sitting ~3_ _} 2-fluorophenylacetamide; N-{5-nonylbenzene fluorenyl-4,6-dihydrogen 0 ratio °[3, 4-c] ° ratio. - 3-fluorophenylacetamide;

C:\2D-GODE\91-01\90119473.ptd 第260頁 1327569 五、發明說明（258) N_{5_曱苯石黃酿基_4，6_二氮0比17各弁[3，4-c]D比0坐_3_基}-4 -氟苯基乙醯胺； N-{5-曱苯續酿基_4，6_二氮0比p各弁[3，4 - c]Dtb。坐-3_基}-3_(2_嘆喻基）丙稀酿胺； 1^-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑-3-基}-3 _ ( 3 _ D塞吩基）丙稀酿胺； N - {5_曱苯石黃酿基_4，6_二氫0比11 各并[3，4-c]D比0坐-3_基}- 3- (2 -噻吩基）丙醯胺； 1\1-{5-甲苯磺醯基-4,6-二氫°比咯并[3,4-〇]咄唑-3-基}- 2 -氣苯曱醯胺； ^{5-曱苯石黃醯基-4,6-二氫吡°各并[3,4-(：]0比〇坐-3-基}- 3 -氯苯甲醯胺； 1{5-曱苯石黃醯基-4，6-二氫〇比17各并[3，4-(：]0比°坐-3-基}- 4- 氯苯曱醯胺； ^{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-1 -派π定丙醢胺； Ν-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-2-乙醯基苯曱醯胺； Ν-{5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]呲唑-3 -基ΙΑ- 乙醯基苯曱醯胺； 1{5-曱苯磺醯基-4,6-二氫0比咯并[3,4-(：]吼唑-3-基}- 1- 萘曱醯胺； Ν-{ 5-曱苯石黃醯基-4, 6 -二氫口比。各并[3, 4-c] 口比峻一3 -基}- 2- 萘甲醢胺；C:\2D-GODE\91-01\90119473.ptd Page 260 1327569 V. Description of invention (258) N_{5_ indimen yellow base _4,6_dinitrogen 0 to 17 弁 [3, 4-c]D is 0 to _3_yl}-4-fluorophenylacetamide; N-{5-nonylbenzene is styling _4,6_dinitrogen 0 to p 弁[3,4 - c] Dtb. Sit -3_base}-3_(2_story base) acrylamide; 1^-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]carbazole 3-yl}-3 _ (3 _ D-sepyl) acrylamide; N - {5_ benzophenone yellow aryl-4,6_dihydrogen 0 to 11 each [3,4-c] D is 0 to 0-based}- 3-(2-thiophenyl)propanamine; 1\1-{5-toluenesulfonyl-4,6-dihydrogen ratio [3,4-〇 ] oxazol-3-yl}- 2 - benzophenone; ^{5-beanthine xanthyl-4,6-dihydropyridyl each [3,4-(:]0 is more than 〇3 -yl}- 3 - chlorobenzamide; 1 {5-bepholine xanthine-4,6-dihydroindole ratio 17 and [3,4-(:]0 ratio °-3-yl}- 4-chlorobenzoin; ^{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-1 -pyridine Ν-{5-nonphenylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-ethenylbenzamide; Ν-{5- Indenesulfonyl-4,6-dihydroindolo[3,4-c]carbazole-3-ylindole-ethenylbenzamide; 1{5-nonylsulfonyl-4, 6-Dihydro 0-pyrolo[3,4-(:]oxazol-3-yl}- 1-naphthylamine; Ν-{ 5-pyrene-xanthine-4,6-dihydroport ratio. Each [3, 4-c] is more than 3 - yl} 2- 2-naphthylamine;

C:\2D-C0DE\91-01\90119473.ptd 第261頁 1327569 五、發明說明（259) N-{5-甲苯石黃醯基_4，6 -二氫吼11 各并[3，4_c]D比0坐-3_基} -3-苯甲醯基丙醯胺； N-{5_甲苯石黃醯基_4，6 -二氫°比0各并[3，4-c]0比0坐-3_基ΙΑ- 乙醯胺基苯曱醯胺； Ν - {5-曱苯續酿基-4，6_二氫0比11 各并[3，4 - c]0比0坐-3_基}-2, 5-二甲氧苯甲醯胺； Ν-{5-曱苯磺醯基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}-2,6-二曱氧苯曱醯胺； Ν_{5_曱苯確隨基_4，6_二氮Β比口各并[3，4_c]0比0坐_3_基}_ ，4 -二曱氧苯甲醯胺； N-{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-3,5-二甲氧苯曱醯胺； 1^-{5-甲苯續醯基-4，6-二氫0比17各并[3,4-〇]0比°坐-3-基}-3-(2 -嘍吩曱醯基）-丙醯胺； ^{云-曱苯石黃酿基-斗^-二氫吼口各并^^-^吼唾^-基}-2-萘基乙醯胺； N-{5-曱苯石黃醯基- 4,6 -二氫°比0各并[3,4-c] 0比。坐-3-基}-1-萘基乙醯胺； • ^{5-甲苯磺醯基-4,6-二氫吼咯并[3,4-〇]。比唑-3-基}- _4-苯基苯甲醯胺； N-{5_辛基續酿基-4，6_二氮°比11 各并[3，4_c]吼°坐-3_基}_ 乙醯胺； 1{5-苄基磺醯基-4,6-二氫咄咯并[3,4-(：]"比唑-3-基}-環丙烷羧醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 261 1327569 V. INSTRUCTIONS (259) N-{5-Tolylxanthine_4,6-dihydroindole 11 each [3,4_c]D ——-3-3-yl}-3-benzhydrylpropionamide; N-{5_toluene xanthine _4,6-dihydrogen ratio 0 and [3,4-c]0 to 0 sit -3_基ΙΑ- acetaminophen hydrazide; Ν - {5- fluorene Benzene-4,6_ dihydrogen 0 to 11 each [3,4 - c]0 to 0 sitting -3 _ base}-2, 5-dimethoxybenzamide; Ν-{5-nonylbenzenesulfonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl} -2,6-dioxabenzoquinone; Ν_{5_曱苯 indeed with the base _4,6_diazepine than the mouth [3,4_c]0 to 0 sitting _3_base}_, 4-dioxabenzamide; N-{5-toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3,5-dimethoxy Benzoylamine; 1^-{5-toluene fluorenyl-4,6-dihydrogen 0 to 17 and [3,4-〇]0 ratio ° sits-3-yl}-3-(2 -喽曱醯 ) ) ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ -{5-bepholine xanthine - 4,6-dihydrogen ratio 0 and [3,4-c] 0 ratio. -3--3-yl}-1-naphthylacetamide; • ^{5-toluenesulfonyl-4,6-dihydroindolo[3,4-indole]. Bizol-3-yl}- _4-phenylbenzamide; N-{5_octyl continuation-4,6-diazepine ratio 11 each [3,4_c]吼° sitting-3_ } _ acetamide; 1{5-benzylsulfonyl-4,6-dihydroindolo[3,4-(:]"pyrazol-3-yl}-cyclopropanecarboxamide;

C:\2D-CODE\91-01\901l9473.ptd 第262頁 1327569 五、發明說明（260) N-{ 5-苄基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3 -基}-異丁醯胺； N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-環戊烷羧醯胺了- ' 4 _ c ] 0比0坐- 3 -基} -4 - c ]吼。坐-3 -基}-4 - c ]吼 °坐-3 -基}-4 - c ] D比口坐 _ 3 - 基}_ 4 - c ] °比。坐-3 -基}-4 - c ]吼口坐-3 -基} _ 4 - c ] D比口坐 - 3 _ 基}-4 - c ] 0比口坐-3 _ 基 ΙΑ _ c ] n 比0坐 _ 3 - 基 } _ 4 - c ] 0比0坐-3 _ 基} - 氫°比咯并[3，氫nb ρ各并[3 , 氫D比ρ各并[3，氫吼D各并[3，氫°比°各并[3，氫吼13各并[3 , 氫吼ρ各并[3，氫°比各并[3，氫D比咯并[3，氫吼洛并[3 , N-{5-苄基磺醯基-4, 6-二苯曱酿胺； N_{5_节基石黃酿基_4，6-二曱基吼啶甲醯胺； N-{5-苄基磺醯基-4, 6-鹼醯胺； N-{5- ¥基磺醯基-4, 6- 異菸鹼醯胺；基磺醯 σ夫喃曱基磺醯醯胺；基磺醯醯胺；基磺醯醯胺；基磺醯醯胺；基磺醯醯胺；基-4,6-二醯胺；基-4, 6-二基-4, 6-二基-4, 6-二基-4, 6-二基-4, 6-二 N _ { 5 _ 辛 3-曱基-2-N-{5-芊 D塞吩-2 -叛 N-{5-苄 °塞吩_ 3 -叛 N-{5- ¥ 鄰-甲苯曱 N-{5-苄間-甲苯曱 N-{5-苄對-甲苯曱C:\2D-CODE\91-01\901l9473.ptd Page 262 1327569 V. INSTRUCTIONS (260) N-{ 5-Benzylsulfonyl-4,6-dihydroindole[3, 4- c]pyrazol-3-yl}-isobutylamine; N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-cyclo Pentane Carboxamide - - ' 4 _ c ] 0 is 0 - 0 - yl} -4 - c ] 吼. Sit -3 - ki}-4 - c ] 吼 ° sit -3 - base} -4 - c ] D sit _ 3 - base}_ 4 - c ] ° ratio. Sit -3 - ki}-4 - c ] 吼口 -3 - 基} _ 4 - c ] D Sit-on - 3 _ base}-4 - c ] 0 than mouth -3 _ base _ c ] n is sitting at 0 _ 3 - ki} _ 4 - c ] 0 is 0 - 0 _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _吼D each [3, hydrogen ° ° ° [3, hydroquinone 13 each [3, hydroquinone ρ and [3, hydrogen ° ratio of each [3, hydrogen D ratio and [3, hydroquinone洛和[3 , N-{5-benzylsulfonyl-4,6-diphenyl hydrazine; N_{5_基基石黄-based 4,6-dimercaptocarboxamide; N -{5-benzylsulfonyl-4,6-alkaline decylamine; N-{5- ¥ sulfamoyl-4,6-isonicotinamide; sulfonamide 醯夫曱曱 sulfoxime Amine; sulfonamide; sulfonamide; sulfonamide; sulfonamide; keto-4,6-diamine; keto-4,6-diyl-4, 6-di Base-4,6-diyl-4,6-diyl-4,6-di-N _ { 5 _ octyl 3-mercapto-2-N-{5-芊D thiophene-2 - renegade N-{ 5-Benzene ° 塞 _ 3 - Rebel N-{5- ¥ o-toluene N-{5-benzyl-toluene N-{5-benzyl p-toluene

C:\2D-OODE\91-Ol \90119473.ptd 第263頁 1327569 五'發明說明（261) N-{5-苄基磺醯基-4,6 -二氫°比咯并[3,4-c]吡唑-3 -基卜苯基乙醯胺；択-丨5-苄基磺醯基-4,6-二氫吼咯并[3,4-〇]咄唑-3-基}-水揚醯胺； 1^-{5-苄基磺醯基-4,6-二氫咄咯并[3,4-(：]咄唑-3-基}- 2 -氟苯甲醯胺； N -丨5-窄基石黃醯基-4, 6 -二氫。比p各并[3，4-c] 0比。坐-3-基}- 3 -氟苯甲醯胺； N-{5-节基續醯基-4，6-二氛°比°各并[3，4-c] °比°坐-基} -#4 -氟苯甲醯胺； N-{5-辛基績醯基-4，6 -二氫ϋ比p各并[3，4-c]吼〇坐-3 -基}-噻吩-2-乙醯胺； N-{5-辛基石黃醯基-4，6_二氫°比p各并[3，4-c] c比。坐-3_基}-噻吩-3-乙醯胺； N-{5—辛基石黃醯基一 4,6 -二氫。比口各并[3，4_c] °比。坐一3_基苯基丙炔醯胺； N-{5-辛基石黃醯基-4，6-二氫吼13各并[3，4-c] °比。坐-3 -基} -3 -氰基苯甲醯胺； N-{5-苄基磺醯基-4,6-二氫咄咯并[3,4-c]吡唑_3-基}-I4-氰基苯曱醯胺； N - {5-辛基續醯基- 4,6 -二氫吼11各并[3，4-c] °比〇坐-3-基}-反-桂皮醯胺； 1^一{5-:¥:基石黃醢基一4，6-二氫0比口各并[3，4_〇]°比〇坐_3-基}_ 順-桂皮醯胺；C:\2D-OODE\91-Ol \90119473.ptd Page 263 1327569 V'Inventive Description (261) N-{5-Benzylsulfonyl-4,6-dihydrogen ratio [3,4 -c]pyrazole-3-phenylphenethylamine; 択-丨5-benzylsulfonyl-4,6-dihydroindolo[3,4-indole]oxazol-3-yl} - hydrazine; 1^-{5-benzylsulfonyl-4,6-dihydroindolo[3,4-(:]oxazol-3-yl}-2-fluorobenzamide N-丨5-narrow sulphate xanthyl-4,6-dihydrogen. Ratio of p to [3,4-c] 0. Sodium-3-yl}- 3-fluorobenzamide; N-{5 -Nu-5- octyl -4,6-dihydroindole ratio p and [3,4-c] stilbene-3 -yl}-thiophene-2-acetamide; N-{5-octyl sulphate-4,6_2 The ratio of hydrogen to p is [3,4-c] c. Sodium-3-yl}-thiophene-3-acetamide; N-{5-octyl sulphate- 4,6-dihydrogen. And [3,4_c] ° ratio. sit a 3-phenylphenylpropynylamine; N-{5-octyl sulphate-4,6-dihydroindole 13 each [3,4-c] ° ratio. -3 - yl} -3 -cyanobenzamide; N-{5-benzylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl} -I4-cyano Benzoylamine; N - {5-octyl fluorenyl- 4,6-dihydroindole 11 each [3,4-c] ° 〇-3-yl}-trans-cinnamin; 1 ^一{5-:¥: Cornerstone Astragalus a 4,6-dihydrogen 0 than each mouth [3,4_〇]° than 〇3-基}_ cis-cinnamate;

C:\2D-OODE\91-0]\90]19473.ptd 第264頁 1327569 五、發明說明（262) N-{5-辛基石黃醯基_4，6-二氫口比0各并[3, 4_c] 口比0坐_3_基}_ 3 - ( 3 -咄啶基）丙烯醯胺； N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-3-(4-吡啶基）丙烯醯胺； 1{5-苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吼唑-3-基}- 2- 苯基丙醯胺； N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-間-曱苯基乙醢胺； N_{5-苄基磺醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-對-曱苯基乙醯胺； 1{5-苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-鄰-茴香醯胺； ^{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}- 3- 甲氧苯甲醯胺； N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}-對-菌香醯胺； N-{5-苄基項酿基- 4,6 -二氫D比略并[3，4-c] D比0坐-3-基}-苯氧乙醯胺； N-{5-苄基確酿基-4，6 -二氫0比p各并[3，4 - c ] °比。坐-3 -基}- 2- 氟苯基乙醯胺； ^{5-苄基磺醯基-4,6-二氫°比咯并[3,4-(：]吼唑-3-基}- 3- 氟苯基乙醯胺； 1^-{5-苄基績醯基-4,6-二氫0比°各并[3,4-〇]°比°坐-3-基}- 4- 氟苯基乙醯胺；C:\2D-OODE\91-0]\90]19473.ptd Page 264 1327569 V. Description of invention (262) N-{5-octyl sulphate _4,6-dihydrogen port ratio 0 each [3 , 4_c] 比3_基}_ 3 - (3 - aridinoyl) acrylamide; N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4- c]pyrazol-3-yl}-3-(4-pyridyl)propenylamine; 1{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-(:]carbazole -3-yl}- 2-phenylpropanamide; N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-m- Phenyl phenyl acetamide; N_{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-p-indole phenylacetamide; {5-Benzylsulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-o-anisylamine; ^{5-benzylsulfonyl-4 ,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-3-methoxybenzamide; N-{5-benzylsulfonyl-4,6-dihydropyrrole [3,4-c]pyrazol-3-yl}-p-bacteria; N-{5-benzylyl-branched- 4,6-dihydro-D ratio slightly [3,4-c] D is 0 -3-yl}-phenoxyacetamide; N-{5-benzyl aryl-4,6-dihydrogen 0 to p and [3,4 - c] ° ratio. 3-based}- 2-fluorophenylacetamide; ^{5-benzyl Sulfhydryl-4,6-dihydropyrolo[3,4-(:]oxazol-3-yl}-3-fluorophenylacetamide; 1^-{5-benzyl fluorenyl -4,6-dihydrogen 0 ratio °[3,4-〇]° ratio °-3-yl}- 4-fluorophenylacetamide;

C:\2D-C0DE\91-01\90119473.ptd 第265頁 1327569 五、發明說明（263) N-{5-辛基石黃醯基-4，6_二氫吼11 各并[3，4-c] °比〇坐-3-基}-3 - ( 2 -噻吩基）丙烯醯胺； N-{5-爷基石黃醯基_4,6_二氫0比°各并[3，4-c] n比。坐-3-基}-3-(3-噻吩基）丙烯醯胺； N_{5-芊基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3 -基}-3-(2 -喀吩基）丙醯胺； 1{5-苄基磺醯基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基}-2 -氯苯曱醯胺； N-{5-苄基石黃醢基-4,6-二氫0比略并[3,4-c] °比。坐-3-基}--氯苯曱醯胺； Ν-{5-芊基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基ΙΑ - 氣苯曱醯胺； Ν-{5-笮基石黃醯基- 4,6 -二氫吼11 各并[3,4-c] °比吐-3 -基}-1 - B底咬丙醯胺； N-{5-芊基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3 -基}-2-乙醯基苯曱醯胺； N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基ΙΑ- 乙醯基苯曱醯胺； • Ν-{5-辛基磺醯基-4, 6 -二氫吼咯并[3, 4-c]"比唑-3 -基}- ’；1 -萘曱醯胺； ^1-{5-爷基續酿基-4，6-二氫〇比0各并[3，4-〇]°比〇坐-3-基}- 2- 萘曱醯胺； Ν - {5_辛基石黃酿基_4，6_二氮πΛ»ρ各并[3,4-c] D比0坐_3 -基}- 3- 苯曱醯基丙醯胺；C:\2D-C0DE\91-01\90119473.ptd Page 265 1327569 V. INSTRUCTIONS (263) N-{5-octyl sulphate-4,6-dihydroindole 11 each [3,4-c ° ° 〇 -3-yl}-3 - ( 2 -thienyl) acrylamide; N-{5-Yellowstone sulphate _4,6_ dihydrogen 0 ° ° each [3,4-c] n ratio. -3-yl}-3-(3-thienyl)propenylamine; N_{5-mercaptosulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3 }}-3-(2-carboxyphenyl)propanamine; 1{5-benzylsulfonyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}- 2-Chlorobenzoquinone; N-{5-benzyl schistyl-4,6-dihydro 0 ratio slightly [3,4-c] ° ratio. -3--3-yl}-chlorobenzoin; Ν-{5-mercaptosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-ylindole-gasbenzene Indoleamine; Ν-{5-fluorenyl fluorenyl- 4,6-dihydroanthracene 11 each [3,4-c] ° than sp -3 -yl}-1 - B bottom propylamine; N- {5-decylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-2-ethenylbenzamine; N-{5-benzyl Sulfomethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-ylindole-ethenylbenzamide; • Ν-{5-octylsulfonyl-4, 6 -dihydroindolo[3,4-c]"Bizozol-3 -yl}- ';1-naphthylamine; ^1-{5-Germanyl-4,6-dihydrogen 〇 0 0 0 0 0 0 0 0 0 0 And [3,4-c] D is 0 to _3 -yl}- 3-phenylmercaptopropylamine;

C:\2D-CODE\91-01\90119473.ptd 第266頁 1327569 五、發明說明（264) ^1-{5-苄基石黃醯基-4，6-二氫0比*7各并[3,4-(：]'1比°坐-3-基}-4-乙醯胺基苯甲醯胺； N-{5-窄基石黃酿基-4,6-二氫11比0各并[3，4_c] °比°坐-3-基}-2,5 -二曱氧苯曱醯胺； N-{5-窄基續酿基- 4，6 -二氫0比p各并[3，4-c] 0比0坐-3-基}- 2, 6 -二甲氧苯甲醯胺； N-{5 -窄基績酿基_4，6 -二氫吼11各并[3，4-c] π比。坐-3-基}-3,4 -二曱氧苯曱醯胺； Ν-{5 -辛基石黃酿基_4，6 -二氮D比0各并[3，4-c]"比°坐-3 -基}_ 3, 5 -二甲氧苯曱醯胺； N-{5-辛基石黃酿基-4，6 -二氫°比°各并[3，4-c]吼°坐-3_基}-3-(2 -噻吩曱醯基）-丙醯胺； N-{5 -苄基石黃醯基一4,6_二氫"比口各并[3,4-c] 口比唾-3 -基}-2-萘基乙醯胺； ^{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-1 -萘基乙醯胺； N-{5-爷基續酿基-4，6 -二氮口比11 各并[3，4-c] 0比0坐-3_基ΙΑ - 笨基苯曱醯胺； Ν-{5-乙醯基-4，6 -二氫0比0各并[3, 4-c] °比。坐-3-基}，『-(4-氯牟基）脈； Ν-{5-亨基-4, 6 -二氫0比 ρ各并[3，4_c] °比〇坐-3 -基}，Ν’ - (4-氣苄基）脲； Ν-{5 -苯基-4,6-二氫吼咯并[3,4-cレ比唑-3-基}，N’-(4-氣芊基）脲；C:\2D-CODE\91-01\90119473.ptd Page 266 1327569 V. INSTRUCTIONS (264) ^1-{5-Benzyl sulphate-4,6-dihydrogen 0 to *7 each [3, 4-(:]'1 ratio °-3-yl}-4-acetamidobenzamide; N-{5-narrow ketone yellow-4,6-dihydro 11 to 0 each [ 3,4_c] ° ratio -3-yl}-2,5-dioxabenzoquinone; N-{5-narrow base aryl- 4,6-dihydrogen 0 to p each [3 , 4-c] 0 to 0 -3-yl}- 2,6-dimethoxybenzamide; N-{5 - narrow base _4,6-dihydroindole 11 each [3 , 4-c] π ratio. Sodium-3-yl}-3,4-dioxabenzoquinone; Ν-{5 - octyl sulphate _4,6-diaza D ratio 0 each [ 3,4-c]"比°-3 -yl}_ 3,5-dimethoxybenzamine; N-{5-octyl sallow-based-4,6-dihydrogen ratio And [3,4-c]吼°--3_yl}-3-(2-thiophenanthryl)-propanamine; N-{5-benzyl sulfonyl- 4,6-dihydro" Mouth [3,4-c] is more than sal-3-yl}-2-naphthylacetamide; ^{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4- 〇]pyrazol-3-yl}-1-naphthylacetamide; N-{5-yl-based aryl-4,6-diaza ratio 11 and [3,4-c] 0 to 0 Sit -3_base - stupid benzoquinone Indoleamine; Ν-{5-ethinyl-4,6-dihydrogen 0 to 0 each [3, 4-c] ° ratio. Sodium-3-yl}, "-(4-chloroindolyl) vein ; Ν-{5-Henki-4,6-dihydrogen 0 is more than ρ[3,4_c] ° than 〇-3-yl}, Ν'-(4-gasbenzyl)urea; Ν-{ 5-phenyl-4,6-dihydroindolo[3,4-cindolozol-3-yl}, N'-(4-carbazyl)urea;

C:\2D-C0DE\91-01\90119473.ptd 第267頁 1327569 五、發明說明（265) N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3 -基}, Ν’ -（4-氣牟基）服； ~-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基丨，Ν’ -(4-氣苄基）脲； Ν-{5-曱烧石黃醯基- 4,6 -二氫°比°各并[3,4-c] 〇比。坐-3-基}， N’~(4-氣辛基）服； N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]呲唑-3 -基}， N -(4 -氣辛基）服； N-{5-甲苯石黃酿基-4，6-二氫0比17各并[3，4-(：]〇比。坐-3_基}， -(4-氣苄基）脲； N-{5 -苄基胺基羰基_4,6_二氫吡咯并[3,4-c]吡唑-3-基}，Ν’ - (4 -氯罕基）服；以及 Ν-{5 -苯基胺基羰基-4，6 -二氫°比°各并[3, 4-c]吼°坐- 3-基} , Ν’ -(4-氯苄基）脲。實施例1 3 Ν-{3-苯乙醯胺基-5-(第三丁酯基）-4,5, 6, 7 -四氫咄啶 [4, 3-c]吼唑-1-基}，Ν’-甲基聚苯乙烯脲之製備苯乙醯氣（24. 08毫莫耳，3. 18毫升）於10毫升無水二氯 @曱烷溶液逐滴添加至先前於90毫升無水二氯曱烷及16. 5毫 _#DIEA( 9 6. 32毫莫耳）溶脹的N-{3 -胺基-5-(第三丁酯基）-4,5,6,7 -四氫咄啶[4,3-c]吡唑-1-基}^’-曱基聚苯乙烯脲（3. 01毫莫耳，3. 5克）。結果所得懸浮液於2 2 °C溫和攪拌1 8小時。然後樹脂經過濾，以二氯曱烷、曱醇洗滌及於真空脫水。C:\2D-C0DE\91-01\90119473.ptd Page 267 1327569 V. INSTRUCTIONS (265) N-{5-Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]indole Oxazol-3 -yl}, Ν'-(4-a gas-based); ~-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3 - 丨, - '4-(4-benzylidene) urea; Ν-{5-曱石石黄醯基- 4,6-dihydrogen ratio ° and [3,4-c] 〇 ratio. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}, N-(4- gas octyl) service; N-{5-toluene yellow-branched-4,6-dihydrogen 0 to 17 each [3,4-(:] 〇 ratio. sitting -3_ base} , -(4-gasbenzyl)urea; N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl},Ν' - (4 - chloroanthryl); and Ν-{5-phenylaminocarbonyl-4,6-dihydrogen ratio °[3, 4-c]吼°-3-yl}, Ν'-( 4-chlorobenzyl)urea. Example 1 3 Ν-{3-phenethylamino-5-(t-butyl ester)-4,5,6-7-tetrahydroacridine [4, 3- Preparation of phenyl oxazolidine (24. 08 mmol, 3. @曱烷溶液 was added dropwise to N-{3-amino-5-(third butyl) previously swelled in 90 ml of anhydrous dichloromethane and 16.5 mM _#DIEA (9 6. 32 mM) Esteryl)-4,5,6,7-tetrahydroacridine[4,3-c]pyrazol-1-yl}^'-mercaptopolystyrene urea (3.11 mmol, 3. 5 The resulting suspension was gently stirred at 22 ° C for 18 hours. The resin was then filtered, washed with dichloromethane, methanol and dried in vacuo.

C:\2D-CODE\91-01\90119473.ptd 第268頁 1327569 五、發明說明（266) 以類似方式，經由使用適當醯基氣可製備下列化合物： N-{3-乙醯胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫吡啶[4, 3-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3 -環丙烷羧醯胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫吡啶[4，3 - c ] °比唑-1 -基}，N ’ -曱基聚苯乙烯脲 N-{3 -異丁醯胺基-5-(第三丁酯基）-4,5, 6, 7-四氫吡啶 [4,3-c]吡唑-1-基}，『-甲基聚苯乙烯脲 N-{3 -環戊烷羧醯胺基-5-(第三丁酯基）-4,5，6, 7-四氫吡啶[4,3-c]咄唑曱基聚苯乙烯脲 N-{3 -苯甲醯胺基-5-(第三丁酯基）-4,5,6,7-四氫咄啶 [4,3-c]吡唑-1-基}，『-甲基聚苯乙烯脲 N—{3-曱基口比咬曱醯胺基-5-(第三丁酯基）-4, 5, 6, 7-四氮°比咬[4，3-c] °比。坐-1_基}，1^’-曱基聚苯乙稀服 N-{3 -菸鹼醯胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫吡啶 [4,3-c]吼唑-1-基}，『-曱基聚苯乙烯脲 N-{3 -異菸鹼醯胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫吼啶[4,3-c]吡唑-1-基},N’-曱基聚苯乙烯脲 N-{3-(3-曱基一2 -口夫喃）一醯胺基一5_(第三丁 S旨基）一 4，5，6，7 -四氫0比。定[4，3-c] 0比0坐-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-( °塞吩-2-叛酿胺基）-5-(第三丁 S旨基）-4, 5，6，7 -四氫吡啶[4,3-c]咄唑-1-基}，1^’-甲基聚苯乙烯脲 N-{3-(噻吩-3 -羧醯胺基）-5-(第三丁酯基）-4,5,6,7 -四氫吡啶[4,3-〇]吡唑-1-基}^’-甲基聚苯乙烯脲C:\2D-CODE\91-01\90119473.ptd Page 268 1327569 V. INSTRUCTIONS (266) In a similar manner, the following compounds can be prepared via the use of an appropriate hydrazine base: N-{3-acetamido- 5-(t-butyl ester)-4, 5, 6, 7-tetrahydropyridine [4, 3-c]pyrazol-1-yl}, N'-methyl polystyrene urea N-{3 - Cyclopropane carboxylamido-5-(t-butylester)-4, 5, 6, 7-tetrahydropyridine [4,3 - c ] °biazole-1 -yl},N '-fluorenyl group Styrene urea N-{3 -isobutylammonium-5-(t-butylester)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, 『-Methyl polystyrene urea N-{3 -cyclopentanecarboxy carbamoyl-5-(t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]咄Zindolyl polystyrene urea N-{3-benzamide-5-(t-butyl ester)-4,5,6,7-tetrahydroacridine [4,3-c]pyrazole- 1-yl}, "-methyl polystyrene urea N-{3-曱 base mouth ratio biting amidino-5-(t-butyl ester group)-4, 5, 6, 7-tetrazole ratio Bite [4,3-c] ° ratio. Sit -1_base}, 1^'-mercaptopolystyrene N-{3 -nicotinoguanamine-5-(t-butylester)-4, 5, 6, 7-tetrahydropyridine [4,3-c]oxazol-1-yl}, "-mercaptopolystyrene urea N-{3-isonicotin amide amino-5-(t-butyl ester)-4, 5, 6 , 7-tetrahydroacridine [4,3-c]pyrazol-1-yl}, N'-mercaptopolystyrene urea N-{3-(3-indolyl-2-ylenyl)-anthracene The amine group is a 5,5,6,7-tetrahydrogen 0 ratio. [4,3-c] 0 to 0 sitting -1-yl}, Ν'-methyl polystyrene uranium-{3-( ° cenet-2-densylamino)-5- (third -4,5,6,7-tetrahydropyridine [4,3-c]oxazol-1-yl}, 1^'-methylpolystyrene urea N-{3-(thiophene- 3-carboxycarboxamide)-5-(t-butylester)-4,5,6,7-tetrahydropyridine[4,3-indolyl]pyrazole-1-yl}^'-methylpolyphenyl Ethylene urea

C:\2D-OODE\91-01\90119473.ptd 第269頁 1327569 五、發明說明（267) N-{3-(鄰曱苯曱醯胺基）-5-(第三丁酯基）-4,5,6,7 -四氫吡啶[4, 3-c]吡唑-1-基}，Ν’ -曱基聚笨乙烯服 Ν_{3-(間甲苯曱醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4,3-c]吼唑曱基聚笨乙烯脲 N-{3-(對甲苯曱醯胺基）-5-(第三丁酯基）-4,5,6,7 -四氫吡啶[4, 3-c]咄唑-1-基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3 -水楊醯胺基-5-(第三丁酯基）-4, 5, 6, 7 -四氫吡啶 [4,3-c]咄唑曱基聚苯乙烯脲 N_{3-(2-氟苯曱醢胺基）-5-(第三丁酯基）-4,5,6,7-四 |氫吡啶[4,3-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 N-{3-(3-氟苯甲醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4,3-c]吡唑-1-基}，N’-甲基聚笨乙烯脲 N-{3-(4-氟苯曱醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫吼啶[4,3-c]咄唑-1-基}，『-曱基聚苯乙烯脲 N-{3-(噻吩-2-乙醯胺基）-5-(第三丁酯基）-4,5,6,7 -四氫吼啶[4,3-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 N-{3-(噻吩-3-乙醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4,3-c]吡唑-1-*}，N’-甲基聚苯乙烯脲 | N-{3 -苯基丙炔醯胺基-5-(第三丁酯基）-4,5,6,7-四氫 ^比啶[4,3-c]咄唑-1-基}，N’-曱基聚苯乙烯脲 N-{3-(3-氰基苯甲酿胺基）-5-(第三丁 S旨基）-4，5，6, 7-四氫°比°定[4,3-c] D比0坐-1-基}，N’-曱基聚苯乙稀脲 N-{3-(4-氰基苯曱醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫0比咬[4, 3-c] 17比0坐- l-基},Ν’ -甲基聚笨乙稀脲C:\2D-OODE\91-01\90119473.ptd Page 269 1327569 V. INSTRUCTIONS (267) N-{3-(o-phthalazinyl)-5-(t-butyl ester)- 4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, Ν'-fluorenyl polystyrene Ν{{3-(m-toluamino)-5- (t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]oxazolyl polyphenylene urea N-{3-(p-tolylamino)-5- (tert-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]oxazol-1-ylindole, Ν'-mercaptopolystyrene uranium-{3 - salicyl Amidino-5-(t-butyl ester)-4, 5, 6, 7-tetrahydropyridine [4,3-c]oxazolyl polystyrene urea N_{3-(2-fluorophenylhydrazine Amidino)-5-(t-butylester)-4,5,6,7-tetrahydropyridyl[4,3-c]pyrazole-1-*}, N'-mercaptopolystyrene Urea N-{3-(3-fluorobenzylidinium)-5-(t-butylester)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-1- N,{'-methyl polystyrene urea N-{3-(4-fluorophenylguanidino)-5-(t-butyl ester)-4,5,6,7-tetrahydroacridine [4,3-c]oxazol-1-yl}, "-mercaptopolystyrene urea N-{3-(thiophene-2-ethinyl)-5-(t-butyl ester)-4 ,5,6,7-tetrahydroacridine [4,3-c]pyridyl -1-*}, N'-mercaptopolystyrene urea N-{3-(thiophene-3-ethinyl)-5-(t-butyl ester)-4,5,6,7-tetra Hydropyridine [4,3-c]pyrazole-1-*}, N'-methyl polystyrene urea|N-{3-phenylpropynylguanidino-5-(t-butyl ester)- 4,5,6,7-tetrahydropyridinium [4,3-c]oxazol-1-yl}, N'-mercaptopolystyrene urea N-{3-(3-cyanobenzoate Amino)-5-(Third-butylene)-4,5,6,7-tetrahydrogen ratio [4,3-c] D is 0-position-1-yl}, N'-曱Polystyrene-urea N-{3-(4-cyanobenzoguanamine)-5-(t-butylester)-4,5,6,7-tetrahydro- 0 ratio bite [4, 3 -c] 17 to 0 sitting - l-base}, Ν'-methyl polystyrene

C:\2D-00DE\91-01\90119473.ptd 第270頁 1327569C:\2D-00DE\91-01\90119473.ptd Page 270 1327569

C:\2D-C0DE\9I-01\90119473.ptd 第271頁 1327569 五、發明說明（269) N-{3-苯氧乙醯胺基-5-(第三丁酯基）-4, 5, 6, 7 -四氫吡啶[4,3-c]吡唑-1-基}，ΙΓ -曱基聚苯乙烯脲 Ν-{3-(2-氟苯基乙醯胺基）-5-(第三丁酯基）-4,5，6, 7-四氫吡啶[4, 3-c]吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν - {3-(3-氟苯基乙酿胺基）_5-(第三丁醋基）-4，5，6，7-四氫咄啶[4, 3-c]吡唑-1-基}，Ν’.-甲基聚苯乙烯脲 Ν-{3_(4-氟苯基乙酿胺基）-5-(第三丁自旨基）-4，5，6, 7-四氫吡啶[4, 3-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 N-{3-[3-(2 -噻吩基）丙烯醯胺基]-5-(第三丁酯基）-丨.，5,6,7-四氫咄啶[4,3-(：]咄唑-1-基}，1^-曱基聚苯乙烯脲 N-{3-[3-(3 -噻吩基）丙烯醯胺基]-5-(第三丁酯基）-4, 5, 6, 7-四氫吡啶[4, 3-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-[3-(2 -噻吩基）丙醯胺基]-5-(第三丁酯基）-4，5，6，7 -四'氫°比°定[4,3-(：] 0比0坐- l- 基}，！^’-曱基聚苯乙稀脲 N-{3-[2 -氯苯曱醢胺基]-5-(第三丁酯基）_4,5,6,7-四 g氫0比咬[4，3-c] °比〇坐-1-基}，1^’-甲基聚苯乙稀脲 N-{3-[3 -氣苯曱醯胺基]-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4,3-c]咄唑-1-基}，！^’-甲基聚苯乙烯脲 N-{3-(4-氯苯甲醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫°比啶[4,3-(：]吡唑-1-基}，~’-曱基聚苯乙烯脲 Ν-{3-(1-^π定丙酿胺基）_5-(第三丁醋基）-4，5, 6，7-四C:\2D-C0DE\9I-01\90119473.ptd Page 271 1327569 V. INSTRUCTIONS (269) N-{3-phenoxyethylamino-5-(t-butyl ester)-4, 5 , 6, 7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, fluorenyl-mercaptopolystyrene-ruthenium-{3-(2-fluorophenylethylamino)-5- (t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-ylindole, Ν'-methyl polystyrene uranium - {3-(3 -fluorophenylethylamino)_5-(tributylacetate)-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-1-yl}, Ν'.- Methyl polystyrene urea-{3_(4-fluorophenylethylamino)-5-(t-butylidene)-4,5,6,7-tetrahydropyridine [4, 3-c Pyrazole-1-*}, N'-mercaptopolystyrene urea N-{3-[3-(2-thiophenyl)propenylamino]-5-(t-butyl ester)-oxime. ,5,6,7-tetrahydroacridine [4,3-(:]carbazol-1-yl}, 1^-mercaptopolystyrene urea N-{3-[3-(3-thiophenyl) Acrylamide]-5-(t-butylester)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene Urea-{3-[3-(2-thiophenyl)propanylamino]-5-(t-butyl ester)-4,5,6,7-tetrahydrogen ratio [4,3 -(:] 0 to 0 sitting - l- base },!^'-曱-based polystyrene urea N-{3-[2-chlorophenylguanidinosyl]-5-(t-butyl ester)_4,5,6,7-tetrahydrogen Than the bite [4,3-c] ° 〇-1-yl}, 1^'-methyl polystyrene urea N-{3-[3 - gasbenzamine]-5- (the first Tributyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]oxazol-1-yl}, !^'-methyl polystyrene urea N-{3-(4- Chlorobenzylamino)-5-(t-butylester)-4,5,6,7-tetrahydropyridinium [4,3-(:]pyrazol-1-yl},~'- Mercapto-polystyrene urea-{3-(1-^π-butylamino)_5-(third butyl vine)-4,5, 6,7-four

C:\2D-OODE\91-Ol\90119473.ptd 第272頁 1327569 五、發明說明（270) 氫吡啶[4, 3-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(2-乙醯基苯曱醯胺基）-5-(第三丁酯基）-4, 5, 6, 7-四氫咄啶[4, 3-c]吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν-{3-(4-乙醯基苯甲醯胺基）-5-(第三丁酯基）- 4.5.6.7- 四氫吡啶[4,3-c]咣唑-1-基}^’-曱基聚苯乙烯脲 Ν-{3-(1-萘曱醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫吼啶[4,3-c]吡唑-1-*}，N’-甲基聚苯乙烯脲 N-{3-(2-萘曱醯胺基）-5-(第三丁酯基）-4,5,6,7 -四氫吡啶[4,3-c]吡唑-1-基}，N’ -甲基聚苯乙烯脲 N-{3-(3-苯甲醯基丙醯胺基）-5-(第三丁酯基）- 4.5.6.7- 四氫吡啶[4,3-(：]吡唑-1-基}^’-曱基聚苯乙烯脲 N-{3-(4-乙醯胺基苯曱醯胺基）-5-(第三丁酯基）-4, 5, 6, 7-四氫吡啶[4, 3-c]吡唑-l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(2,5 -二甲氧苯甲醯胺基）-5-(第三丁酯基）- 4.5.6.7- 四氫吡啶[4,3-。]吡唑-1-基}，1^’-曱基聚苯乙烯脲 1^-{3-(2，6-二曱氧苯曱酿胺基）_5-(第三丁5旨基）- 4，5，6,7-四氫〇比咬[4，3-(：]〇比〇坐-1-基}，1^’-甲基聚苯乙稀脲 N_ {3-(3,4 -二曱氧苯曱醯胺基）-5-(第三丁酯基）-C:\2D-OODE\91-Ol\90119473.ptd Page 272 1327569 V. INSTRUCTIONS (270) Hydropyridine [4, 3-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene Urea-{3-(2-ethylmercaptophenylamino)-5-(t-butylester)-4, 5, 6, 7-tetrahydroacridine [4, 3-c]pyrazole -1-ylindole, Ν'-methyl polystyrene uranium-{3-(4-ethylmercaptobenzylamino)-5-(t-butyl ester)- 4.5.6.7-tetrahydropyridine [4,3-c]oxazol-1-yl}^'-mercaptopolystyrene urea-{3-(1-naphthylamino)-5-(t-butyl ester)-4, 5,6,7-tetrahydroacridine [4,3-c]pyrazole-1-*}, N'-methyl polystyrene urea N-{3-(2-naphthylamino)-5 -(t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, N'-methyl polystyrene urea N-{3-( 3-benzylidene propylamino)-5-(t-butyl ester)- 4.5.6.7-tetrahydropyridine [4,3-(:]pyrazol-1-yl}^'-fluorenyl Styrene urea N-{3-(4-acetamidobenzoguanamine)-5-(t-butyl ester)-4, 5, 6, 7-tetrahydropyridine [4, 3-c] Pyrazole-l-yl}, Ν'-methyl polystyrene urea-{3-(2,5-dimethoxybenzamide)-5-(t-butyl ester)- 4.5.6.7 - tetrahydropyridine [4, 3-.]pyrazol-1-yl}, 1^'-mercaptopolystyrene urea 1^-{3-(2,6-dioxabenzoquinone-based amine)_5-(third butyl 5 Base) - 4,5,6,7-tetrahydroindole ratio bite [4,3-(:]〇〇 -1--1-yl}, 1^'-methylpolystyrene urea N_ {3-( 3,4-dioxabenzoguanamine)-5-(t-butyl ester)-

C:\2D-C0DE\91-01\90119473.ptd 第273頁 1327569 五、發明說明（271) 曱基聚苯乙烯 4, 5, 6, 7-四氫。比啶[4, 3-C]吡唑-1-基}，|^，脲， N-{3-(3,5-二曱氧苯曱醯胺基）_5_(第三丁酯基）_4 5 6’ = ^7[4’3^“_1_基}，^甲基聚苯乙稀脲， N-{3-3-(2-噻吩醯）_丙醯胺基_5_(第三丁酯基）_4 5 6 '四m4,3、c卜比嗤+基}，n’-甲基聚*乙豨脲’ ’ ’ N-{3-(2-秦基乙醯胺基）-5-(第三丁 s旨基）_4 5 6 四氫吼咬[4, 3-c]。比唑_；!-基}，Ν’ -曱基聚笨乙稀脲 ’ N-{3-U-萘基乙醯胺基）-5-(第三丁酿基卜4,5,6 7_四氫吼咬[4, 3-c]吡唑-1-基}，N，-甲基聚笨乙稀脲 N-{ 3-(4-苯基笨曱醯胺基）-5-(第三丁酯基）_4, 56, 了― 四氫吼咬[4,3-c]吡唑-1-基}^’-甲基聚笨乙稀脲 N-{3-(2-吱喃醯胺基）-5-(第三丁酯基）_4, 5, 6, 四吡啶[4, 3-c]咄唑-；[-基}，N，-曱基聚苯乙烯脲 ’ & N-{3-(4-笨氧苯甲醯胺基）-5-(第三丁酯基）_4,5 6 7_ 四氫吡啶[4,3-c]咄唑-1-基}，『-曱基聚笨乙稀脲’ ’ N-{3-(3-苯氧苯曱酿胺基）-5-(第三丁酯基）_4,5 6 γ 四氫nb°^[4，3-c] 〇比吐- l-基}，！^’ -曱基聚笨乙稀脲 I N-{3-(4-第三丁基-苯曱酿胺基）_5-(第三丁 g旨基）_ 4, 5，6, 7 -四氫咄啶[4, 3-c]吡唑-I-基丨，Ν’ -曱基聚笨乙稀脲 Ν-{3 -胡椒基羧醯胺基-5-(第三丁酯基）-4,5,6,7-四氣 0比。定[4，3-c]0比0圭_1_*}，N _甲基聚本乙稀服 N-{3-(2-萘）丙醢胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫C:\2D-C0DE\91-01\90119473.ptd Page 273 1327569 V. INSTRUCTIONS (271) Mercapto-based polystyrene 4, 5, 6, 7-tetrahydrogen. Bis[4,3-C]pyrazol-1-yl},|^, urea, N-{3-(3,5-dioxabenzoquinone)_5_(t-butyl ester)_4 5 6' = ^7[4'3^"_1_yl}, ^Methylpolystyrene, N-{3-3-(2-thiophene)-propanylamine_5_(third Ester group)_4 5 6 'four m4,3,c b 嗤+ base}, n'-methyl poly*acetamidine ' ' ' N-{3-(2-methyl acetyl amide)-5 - (third s s base) _4 5 6 tetrahydrobite [4, 3-c]. azole _;!-yl}, Ν'-mercapto polystyrene' N-{3-U -naphthylacetamido)-5-(third butyl keb 4,5,6 7_tetrahydroindene [4,3-c]pyrazol-1-yl}, N,-methyl poly Stupid ethyl diurea N-{ 3-(4-phenyl amidino)-5-(t-butyl ester)_4, 56, - tetrahydrobite [4,3-c]pyrazole- 1-yl}^'-methyl polyethylidene urea N-{3-(2-indolyl)-5-(t-butyl ester)_4, 5, 6, tetrapyridine [4, 3 -c]carbazole-;[-yl},N,-mercaptopolystyrene urea & N-{3-(4- oxabenzoguanidino)-5-(t-butyl ester) _4,5 6 7_tetrahydropyridine [4,3-c]oxazol-1-yl}, "-mercaptopolyethylidene" 'N-{3-(3-phenoxybenzoinyl) -5-(t-butyl ester group)_4, 5 6 γ tetrahydronb°^[4,3-c] 〇吐吐 - l-基}, !^' - fluorenyl polyethylidene I N-{3-(4-t-butyl-benzene Brewed amine)_5-(third butyl group)_ 4, 5,6,7-tetrahydroacridine [4,3-c]pyrazole-I-ylindole, Ν'-mercapto group Ethylene uranium-{3 -piperonylcarboxylamido-5-(t-butyl ester)-4,5,6,7-tetragas 0 ratio. [4,3-c]0 to 0 gui _1_*}, N _ methyl polybenzidine N-{3-(2-naphthalene)propanylamino-5-(t-butyl ester)-4, 5, 6, 7-tetrahydrogen

C:\2D-00DE\91-0U90119473.ptd 第274頁 1327569 五、發明說明（272) 吼啶[4, 3-c] °比唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(6-甲氧-2-萘）丙醯胺基-5-(第三丁酯基）-4,5,6, 7 -四氫吡啶[4,3-c]吡唑-1-基}，N’ -甲基聚苯乙烯脲 N-{3-(2-乙基丁醯胺基）-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4, 3-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(4 -吡咯啶-1-基-苯基）丙醯胺基-5-(第三丁酯基） -4,5,6,7_四氫吡啶[4,3-〇]吡唑-1-基},1^’-曱基聚苯乙烯脲 N-{3-(2-氧基比咯啶-1-基）苯基}丙醯胺基-5-(第三丁酯基）-4,5,6,7-四氮吡啶[4,3-(：]吡唑-1-基}，1^-曱基聚苯乙烯脲 N-{3-(雙環[4. 2. 0]辛-1，3, 5 -三稀-7-缓酿胺基）-5-(第三丁酯基）-4,5,6,7 -四氫咄啶[4, 3-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(2 -氧基-吡咯啶-1-基）苯乙醯胺基- 5- (第三丁酯基）-4,5, 6, 7-四氫吡啶[4，3-c]咄唑-l-基}，Ν’ -甲基聚苯乙稀脲 Ν-{3-(4 - °比11各0定-1-基）苯乙醯胺基-5-(第三丁 S旨基）-4， 5, 6, 7 -四氫吡啶[4, 3-c]吡唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν-{3-(4 -三氟^甲基）苯乙醯胺基-5-(第三丁 S旨基）-4，5，6，7-四氫〇比咬[4,3-(：]〇比〇坐-1-基}，1^’-甲基聚苯乙烯脲 Ν-{3-(2 -漠）苯乙酿胺基- 5- (第三丁 S旨基）_4，5, 6, 7-四氫吡啶[4,3-c]吡唑-1-基}，N’-曱基聚苯乙烯脲C:\2D-00DE\91-0U90119473.ptd Page 274 1327569 V. INSTRUCTIONS (272) Acridine [4, 3-c] °Biazol-1-yl}, Ν'-methyl polystyrene Ν-{3-(6-methoxy-2-naphthalene)propanylamino-5-(t-butylester)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole -1-yl}, N'-methyl polystyrene urea N-{3-(2-ethylbutylamido)-5-(t-butyl ester)-4,5,6,7-tetra Hydropyridine [4,3-c]pyrazol-1-yl}, Ν'-methyl polystyrene-indole-{3-(4-pyrrolidin-1-yl-phenyl)propanamido-5 -(t-butyl ester) -4,5,6,7-tetrahydropyridine [4,3-indolyl]pyrazole-1-yl},1^'-mercaptopolystyrene urea N-{3- (2-oxypyrrolidin-1-yl)phenyl}propanylamino-5-(t-butyl ester)-4,5,6,7-tetrazinidine [4,3-(:] Pyrazol-1-yl}, 1^-mercaptopolystyrene urea N-{3-(bicyclo[4. 2. 0] octane-1,3,5-tris-7-yano-yl)- 5-(t-butyl ester)-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene uranium-{3 -(2-oxy-pyrrolidin-1-yl)phenylethylamino-5-(t-butylester)-4,5,6,7-tetrahydropyridine[4,3-c]carbazole -l-yl}, Ν'-methyl polystyrene uranium-{3- (4 - ° ratio of 11 to 0 -1-yl) phenethylamino-5-(t-butylene)-4, 5, 6, 7-tetrahydropyridine [4, 3-c]pyridyl Zin-1-ylindole, Ν'-methyl polystyrene-indole-{3-(4-trifluoromethyl)phenethylamino-5-(t-butyl)--4,5 ,6,7-tetrahydroindole ratio bite [4,3-(:]〇〇 -1--1-yl}, 1^'-methyl polystyrene uranium-{3-(2 - desert) phenyl Amine-based 5-(Tertiary S-based)_4,5, 6, 7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, N'-mercaptopolystyrene

C:\2D-Q0DE\91-01\90119473.ptd 第275頁 1327569 五、發明說明（273) N-{3-[4-(吡咯啶-1-基-羰基甲氧基）]苯乙醯胺基-5-(第三丁 S旨基）-4，5，6，7-四氫0比咬[4，3-c] π比0坐-1_基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-[3-(胺基羰基曱氧）苯乙醯胺基]-5-(第三丁酯基） -4,5,6,7-四氫吼啶[4,3-(：]吡唑-1-基}，^-曱基聚苯乙烯脲 N-{3-[4-(2 -氧基唑啶-3 -基）苯乙醯胺基]-5-(第三丁酯基）-4,5,6,7-四氫吡啶[4,3-c]吡唑-曱基聚苯乙烯脲 4 N-{3-[4-(4-甲基哌畊基）苯乙醯胺基]-5-(第三丁酯基） -4, 5,6, 7-四氫吡啶[4, 3-c]吡唑-l-基}, Ν’ -甲基聚苯乙烯脲 Ν-{3-(苯并[1，3]二氧伍圜-5-基）乙醯L胺基-5-(第三丁酯基）-4, 5, 6, 7 -四氫吡啶[4, 3-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-[4-(2-氧基唑啶-3 -基）苯乙醯胺基]-5-(第三丁酯基）-4，5，6，7 -四氫 11 比0定[4,3-c] 0 比0坐-1-*},N’ -曱基聚苯乙烯脲 I N-{3-(2 -苯基-1,3 -噻唑-4 -基）乙醯胺基-5-(第三丁酯 _基）-4,5,6,7-四氫吡啶[4,3-〇]吡唑-1-基}，1'}’-甲基聚苯乙烯脲 N-{3_[4-(l-B比ϋ各咬-2-嗣）苯甲酿胺基]- 5-（第三丁 S旨基）-4,5,6,7 -四氫。比啶[4,3-c]吼唑曱基聚苯乙稀脈C:\2D-Q0DE\91-01\90119473.ptd Page 275 1327569 V. INSTRUCTIONS (273) N-{3-[4-(Pyrrolidin-1-yl-carbonylmethoxy)]phenylacetamidine Amino-5-(Third-butyl group)-4,5,6,7-tetrahydro- 0 ratio bite [4,3-c] π ratio 0 sitting -1_yl}, Ν'-fluorenyl group Styrene-urea-{3-[3-(aminocarbonyl oxime) phenethylamino]-5-(t-butyl ester)-4,5,6,7-tetrahydroacridine [4, 3-(:]pyrazol-1-yl},^-mercaptopolystyrene urea N-{3-[4-(2-oxoxazolidin-3-yl)phenylethylamino]-5- (t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazole-decyl polystyrene urea 4 N-{3-[4-(4-methylper Plough base) phenethylamino]-5-(t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazole-l-yl}, Ν'- Polystyrene uranyl-{3-(benzo[1,3]dioxoindol-5-yl)ethyl hydrazine L-amino-5-(t-butyl ester)-4, 5, 6, 7 -tetrahydropyridine [4, 3-c]pyrazol-1-yl}, Ν'-methyl polystyrene-indole-{3-[4-(2-oxoxazolidine-3-yl)phenyl Amidino]-5-(t-butylester)-4,5,6,7-tetrahydrol 11 is determined to be [4,3-c] 0 to 0-l-*}, N'-曱Polystyrene urea I N-{3-(2-phenyl-1,3 - Zin-4-yl)acetamido-5-(t-butyl ester-yl)-4,5,6,7-tetrahydropyridine [4,3-indolyl]pyrazole-1-yl}, 1' }'-Methyl styrene urea N-{3_[4-(lB ϋ ϋ 嗣嗣嗣嗣苯苯苯苯 ] ] ] ] ] ] ] -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 ,7-tetrahydro.pyridinyl[4,3-c]oxazolyl-based polystyrene

C:\2D-C0DE\91-01\90119473.ptd 第 276 頁 1327569C:\2D-C0DE\91-01\90119473.ptd Page 276 1327569

C:\2D-OODE\91-Ol\90119473.ptd 第277頁 1327569C:\2D-OODE\91-Ol\90119473.ptd Page 277 1327569

1327569 五、發明說明（276) 基丨，Ν’ -甲基聚苯乙烯脲 !^-{3-環戊烧叛醯胺基-4，5，6,7-四氫°比。定[4，3-〇]°比〇坐甲基聚苯乙稀脈 N-{3-苯曱醯胺基-4，5，6，7-四氫0比咬[4, 3-c] 0比0坐基}，Ν’ -曱基聚苯乙烯脲 !^-{3-甲基0比。定曱酸胺基-4，5，6，7-四氫0比〇定[4，3-(：]0比唑-1-基}，Ν’ -曱基聚苯乙烯脲 1^-丨3-於驗醯胺基-4，5，6，7-四氫'3比〇定[4，3-(：]°比°坐-1- 基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -異於驗醯胺基-4, 5，6，7-四氫ρ比咬[4，3-c] °比°坐-1-基}，Ν’ -曱基聚苯乙烯脲 ^{3-(3-曱基-2-呋喃）-醯胺基-4,5,6,7-四氫吼啶 [4，3_c] 0比。坐_1-基}，1^’_曱基聚苯乙稀脈 N-{3-( °塞吩-2-緩酿胺基）-4，5，6，7_四氮11比。定[4，3-c] 0比唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-( π塞吩-3-缓醯胺基）-4，5，6，7-四氫吼咬[4，3-c] D比唑-l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(鄰曱苯曱醯胺基）-4,5,6, 7 -四氫吡啶[4,3-c]咄 °坐-1-基}，1^’_曱基聚苯乙稀脈 N-{3-(間甲苯甲醯胺基）-4,5,6,7 -四氫吼啶[4,3-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(對曱苯曱醯胺基）-4, 5,6, 7 -四氫吡啶[4,3-c]吡唑-l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -水楊醯胺基-4，5，6，7-四氫〇比咬[4，3-0]°比°坐-1-1327569 V. INSTRUCTIONS (276) Base, Ν'-methylpolystyrene urea ^^-{3-cyclopentanthene sulfhydryl-4,5,6,7-tetrahydrogen ratio. Determine [4,3-〇]° than 〇甲基 methyl polystyrene ring N-{3-benzoguanamine-4,5,6,7-tetrahydro 0 ratio bite [4, 3-c] 0 to 0 sitting base}, Ν '-mercaptopolystyrene urea! ^-{3-methyl 0 ratio.曱胺 -4 -4 -4 -4 -4 -4 -4 -4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 [4,3-(:] 3- in the test of amidino-4,5,6,7-tetrahydro'3 ratio [4,3-(:] ° ratio °-1-yl}, Ν'-methyl polystyrene Ν-{3 - is different from the test of amidino-4, 5,6,7-tetrahydro ρ than bite [4,3-c] ° °-1-yl}, Ν'-mercaptopolystyrene Urea^{3-(3-mercapto-2-furan)-nonylamino-4,5,6,7-tetrahydroacridine [4,3_c] 0 ratio. Sitting _1-yl}, 1^' _ 曱聚 polystyrene oxime N-{3-( ° cecn-2-pyramine)-4,5,6,7_tetranitrogen 11 ratio. [4,3-c] 0 azole -l-yl}, Ν'-mercaptopolystyrene-ruthenium-{3-( π-cetin-3- sulfhydryl)-4,5,6,7-tetrahydro hydrazine [4,3- c] D-biazole-l-yl}, Ν'-methyl polystyrene-ruthenium-{3-(o-phthalazinyl)-4,5,6,7-tetrahydropyridine [4,3 -c]咄°坐-1-yl}, 1^'_曱-based polyphenylethylene ring N-{3-(m-toluamylamino)-4,5,6,7-tetrahydroacridine [ 4,3-c]pyrazol-1-yl},Ν'-methylpolystyrene-indole-{3-(p-benzoylamino)-4,5,6,7-tetrahydropyridine [ 4,3-c]pyrazole-l-yl}, Ν'-methyl polyphenyl Ethylene urea Ν-{3 - salicylamine-4,5,6,7-tetrahydroanthracene than bite [4,3-0]°°°-1-

C:\2D-00DE\91-01\90119473.ptd 第279頁 1327569 五、發明說明（277) 基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(2-氟苯甲醯胺基）-4, 5,6, 7 -四氫吡啶[4,3-c]吼唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν_{3-(3-氟苯曱醯胺基）-4,5,6, 7 -四氫咄啶[4,3-c] 0比唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-氟苯甲醯胺基）-4,5,6, 7 -四氫吼啶[4,3-c] 口比唑-1-基丨，Ν’ -曱基聚苯乙烯脲 1{3-(°塞吩-2-乙醯胺基）-4,5,6,7-四氫吡°定[4,3-〇]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲私Ν-{3-( °塞吩-3-乙醯胺基）-4, 5, 6, 7 -四氫Β比0定[4，3-c] 口比唑-l-基},Ν’ -甲基聚苯乙烯脲 1^-{3-苯基丙炔酿胺基-4，5,6,7-四氫吼〇定[4，3-0：]〇比〇坐 -l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(3-氰基苯曱醯胺基）-4,5,6,7-四氫口比啶[4,3-c] 吡唑-1 -基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4 -氰基苯曱醯胺基）-4,5,6,7-四氫口比啶[4,3-c] »比口坐一1_基}，N，一甲基聚苯乙烯脲 !'}-{3-反桂皮醯胺基-4,5,6,7-四氫°比咬[4,3-〇:]°比°坐-1- _基}, Ν’ -甲基聚苯乙烯脲 Ν - { 3 -順桂皮醢胺基-4，5，6, 7 -四氫°比σ定[4，3 - c ] °比0坐-1 -基}，Ν’ -曱基聚苯乙烯脲 1{3-[3-(3-吡啶基）丙烯醯胺基]-4,5,6,7-四氫吡啶 [4, 3_c] 0比0坐_1_基}，1^’_甲基聚苯乙稀脈 \-{3-[3-(4-咄啶基）丙烯醯胺基]-4,5,6,7-四氫吼啶 C:\2D-00DE\91-01\90119473.ptd 第280頁 _1__ 1327569 五、發明說明（278) [4,3-c]吡唑-1-基}，N’_甲基聚苯乙烯脲 N-{3-(2 -苯基丙醯胺基）-4, 5, 6, 7-四氫咄啶[4, 3-c]吡唑-1-基丨，Ν’ -曱基聚苯乙烯脲 ^{3-鄰曱苯基乙醯胺基-4,5,6,7-四氫吡啶[4,3-(：]吡 β坐_1_基}，|^’-曱基聚苯乙稀脈 1{3-間曱苯基乙醯胺基-4,5,6,7-四氫吡啶[4,3-(：]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 1{3-對曱苯基乙醯胺基-4,5,6,7-四氫吡啶[4,3-(：]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3 -鄰菌香酿胺基-4，5，6，7_四氫π比咬[4，3-c] Β比°坐-1-基}，Ν’ -曱基聚苯乙烯脲 N—{3-(3-甲氧苯曱醢胺基）—4, 5, 6, 7-四氫°比咬[4, 3-c] 咄唑-1-基}，Ν’ -曱基聚苯乙烯政 !^-{3-對茴香醢胺基-4，5，6，7-四氫〇比咬[4，3-(：]0比°坐-1- 基}，Ν’ -甲基聚苯乙烯脲 Ν-{3 -苯氧乙醯胺基-4, 5, 6, 7-四氫咄啶[4, 3-c]吡唑-1-基}，Ν’ -甲基聚笨乙烯脲 Ν-{3-(2-氟苯基乙醯胺基）-4, 5, 6,7 -四氫咄啶[4, 3-c] 吼唑-1 -基}，Ν，-曱基聚苯乙烯脲 1{3-(3-氟苯基乙醯胺基）-4,5,6,7-四氫°比啶[4,3-(：] 吡唑-l-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(4- II苯基乙酿胺基）-4，5，6，7 -四氫ρ比°定[4，3-c] 吡唑-1-基}，Ν，-曱基聚苯乙烯脲 Ν-{3-[3-(2-°塞吩基）丙烯醯胺基]-4, 5, 6，7-四氫0比咬C:\2D-00DE\91-01\90119473.ptd Page 279 1327569 V. INSTRUCTIONS (277) BASE}, Ν'-mercaptopolystyrene urea-{3-(2-fluorobenzamide -4,5,6,7-tetrahydropyridine [4,3-c]oxazol-1-yl}, Ν'-methyl polystyrene ruthenium _{3-(3-fluorophenylguanamine -4,5,6,7-tetrahydroacridine [4,3-c] 0-pyridyl-l-yl}, Ν'-mercaptopolystyrene urea-{3-(4-fluorobenzene Methionine)-4,5,6,7-tetrahydroacridine [4,3-c] Oroxazol-1-ylindole, Ν'-mercaptopolystyrene urea 1{3-(° stopper吩-2-Ethylamino)-4,5,6,7-tetrahydropyridin [4,3-〇]pyrazole-l-yl},Ν'-mercaptopolystyrene urea- {3-( ° thiophene-3-ethinylamino)-4, 5, 6, 7 -tetrahydroindole ratio 0 [4,3-c] oxazole-l-yl}, Ν'- Polystyrene urea 1^-{3-phenylpropynylamino-4,5,6,7-tetrahydroindole [4,3-0:] 〇〇 - -l- yl}, Ν'-mercaptopolystyrene-indole-{3-(3-cyanobenzoguanamine)-4,5,6,7-tetrahydropyridinium [4,3-c]pyrazole-1 -based, Ν'-mercaptopolystyrene-indole-{3-(4-cyanobenzoguanamine)-4,5,6,7-tetrahydropyrazine [4,3-c] »Sit a 1_base}, N, monomethyl Polystyrene urea!'}-{3-Anti-guinea amidino-4,5,6,7-tetrahydrogen ratio bite [4,3-〇:]° ratio ° sitting -1- _ base}, Ν '-Methylpolystyrene uranium - { 3 -cis cinnamyl-4,5,6,7 -tetrahydrogen ratio σ [4,3 - c ] ° ratio 0 sitting -1 -yl}, Ν'-mercapto polystyrene urea {{3-[3-(3-pyridyl) acrylamido]-4,5,6,7-tetrahydropyridine [4, 3_c] 0 to 0 sitting _1 _ base}, 1^'_methyl polystyrene pulse \-{3-[3-(4-acridinyl) acrylamide]-4,5,6,7-tetrahydroacridine C: \2D-00DE\91-01\90119473.ptd Page 280_1__ 1327569 V. Description of invention (278) [4,3-c]pyrazol-1-yl}, N'-methyl polystyrene urea N -{3-(2-phenylpropionamido)-4, 5, 6, 7-tetrahydroacridine [4, 3-c]pyrazol-1-ylindole, Ν'-mercaptopolystyrene Urea^{3-o-indole phenylacetamido-4,5,6,7-tetrahydropyridine[4,3-(:]pyridin-1-yl},|^'-fluorenyl polyphenyl Ethyl sulphate 1{3-m-phenyl phenylacetamido-4,5,6,7-tetrahydropyridine [4,3-(:]pyrazol-1-yl}, Ν'-methyl polyphenyl Ethylene urea 1{3-p-phenyl phenyl acetamino-4,5,6,7-tetrahydropyridine [4,3-(:]pyrazol-1-yl}, fluorene-fluorenyl polystyrene Urea Ν-{3 - arbuscular scented amine -4,5,6,7_tetrahydropyrene ratio bite [4,3-c] Β ratio ° sit-1-yl}, Ν'-mercaptopolystyrene urea N-{3-(3-methoxy Benzoguanamine)-4, 5, 6, 7-tetrahydrogen ratio [4, 3-c] carbazol-1-yl}, Ν'-mercaptopolystyrene!^-{3- Pair of anisoleamine-4,5,6,7-tetrahydroindole ratio bite [4,3-(:]0 to °-1-yl}, Ν'-methylpolystyrene uranium-{3 -phenoxyethylamino-4,5,6,7-tetrahydroacridine[4,3-c]pyrazol-1-yl}, Ν'-methyl polystyrene uranyl-{3-( 2-fluorophenylethylamino)-4,5,6,7-tetrahydroacridine[4,3-c]carbazole-1 -yl}, fluorene,-mercaptopolystyrene urea 1{3 -(3-fluorophenylethylamino)-4,5,6,7-tetrahydropyridinium [4,3-(:] pyrazole-1-yl}, Ν'-methyl polystyrene Urea Ν-{3-(4-IIphenylethylamino)-4,5,6,7-tetrahydro ρ ratio [4,3-c]pyrazol-1-yl}, hydrazine, - Mercapto polystyrene uranium-{3-[3-(2-°-septyl) acrylamido]-4, 5, 6,7-tetrahydro 0-bit

C:\2D-00DE\91-01\90119473.ptd 第281頁 1327569 五、發明說明（279) [4,3-c]吡唑-1-*}，N’-曱基聚苯乙烯脲 1^-{3-[3-(3-噻吩基）丙烯醯胺基]-4,5,6,7-四氫"比啶 [4,3-c]吡唑-1-*}，N’-甲基聚苯乙烯脲 1{3-[3-(2-噻吩基）丙醯胺基]-4,5,6,7-四氫°比啶 [4,3-c]咄唑-1-*}，N’-甲基聚苯乙烯脲 1^-{3-[2-氣苯曱醯胺基]-4，5，6,7-四氫〇比咬[4，3-〇]口比唑-1-基}，Ν’ -曱基聚苯乙烯脲 1^-{3-[3-氣苯甲醯胺基]-4，5,6，7-四氫〇比咬[4，3-(：]0比唑-1-基}，Ν，-曱基聚苯乙烯脲 Ν-{3-(4 -氯苯甲醯胺基）-4,5,6,7-四氫吡啶[4,3-c]咄唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3_(1_旅咬丙酿胺基）-4，5，6，7 -四氫0比咬[4，3-c] 口比唑-1-基}，1^’-甲基聚苯乙烯脲 Ν-{3-(2-乙醯基苯曱醯胺基）-4, 5, 6, 7-四氫吡啶 [4,3-c]吡唑-1-基}，Ν’_甲基聚苯乙烯脲 1^-{3-(4-乙醯基苯曱醯胺基）-4,5,6,7-四氫吡啶 [4,3-c]吡唑-1-基}，Ν’-甲基聚苯乙烯脲 Ν-{3-(1-萘曱醯胺基）-4，5，6，7-四氫0比咬[4，3-c] 0比〇坐 1_S}，N’-甲基聚苯乙稀脈 1^-{3-(2-萘曱醯胺基）-4,5，6,7-四氫0比〇定[4，3-(：]0比口坐 _1_基}，1^’-曱基聚苯乙稀脈 N-{3-(3 -苯甲醯基丙醯胺基）-4, 5,6,7-四氫吡啶 [4,3-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3-(4—乙醯胺基苯曱醯胺基）-4,5,6,7 -四氫口比口定C:\2D-00DE\91-01\90119473.ptd Page 281 1327569 V. Description of invention (279) [4,3-c]pyrazole-1-*}, N'-mercaptopolystyrene urea 1 ^-{3-[3-(3-Thienyl)acrylamido]-4,5,6,7-tetrahydro"bipyridyl[4,3-c]pyrazole-1-*}, N '-Methyl polystyrene urea 1{3-[3-(2-thienyl)propanamido]-4,5,6,7-tetrahydropyridinium [4,3-c]carbazole- 1-*}, N'-methyl polystyrene urea 1^-{3-[2-phenylamino]-4,5,6,7-tetrahydroindole ratio [4,3-〇 ]poroxazol-1-yl}, Ν'-mercaptopolystyrene urea 1^-{3-[3-gasbenzamide]-4,5,6,7-tetrahydroindole ratio bite [ 4,3-(:]0-pyrazol-1-yl}, fluorene,-mercaptopolystyrene-indole-{3-(4-chlorobenzamide)-4,5,6,7-tetra Hydropyridine [4,3-c]oxazol-1-yl}, Ν'-mercaptopolystyrene uranium-{3_(1_Big acylamino)-4,5,6,7-four Hydrogen 0 is like biting [4,3-c] port-azol-1-yl}, 1^'-methylpolystyrene-indole-{3-(2-ethylmercaptobenzamide)-4, 5, 6, 7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, Ν'_methyl polystyrene urea 1^-{3-(4-ethylmercaptophenyl hydrazino )-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, Ν'-A Polystyrene-uranium-{3-(1-naphthylamino)-4,5,6,7-tetrahydro- 0 ratio bite [4,3-c] 0 than squat 1_S}, N'-A Polyphenylene sulfonate 1^-{3-(2-naphthylamino)-4,5,6,7-tetrahydro 0 ratio [4,3-(:]0 than mouth sitting_1 _ base}, 1^'-mercaptopolyphenylene oxide N-{3-(3-benzylidene propylamino)-4,5,6,7-tetrahydropyridine [4,3-c Pyrazol-1-yl}, N'-methyl polystyrene urea N-{3-(4-acetamidobenzoguanamine)-4,5,6,7-tetrahydro port set

C:\2D-C0DE\91-01\90119473.ptd 第282頁 1327569 五、發明說明（280) [4，3_c] 0比0圭-1-基}，1^’_甲基聚苯乙稀脈 N-{3-(2,5 -二曱氧苯曱醯胺基）-4,5,6,7-四氫吼啶 [4,3-c]吡唑-1-基}，1^’ -甲基聚苯乙烯脲 N-{3-(2,6 -二曱氧苯曱醯胺基）-4,5,6,7 -四氫吡啶 [4,3-c]吡唑-1-基}，N’ -曱基聚苯乙烯脲 1{3-(3,4-二曱氧苯曱醯胺基）-4,5,6,7-四氫吡啶 [4,3-c]吡唑-1-*}，N’ -曱基聚苯乙烯脲 N-{3-(3,5 -二曱氧苯曱醯胺基）-4,5,6,7 -四氫吼啶 [4,3-c]吡唑-1-基}，N’ -曱基聚苯乙烯脲 1^-{3-3-(2-噻吩醯）-丙醯胺基-4,5,6,7-四氫吡啶 [4,3-c]吡唑-1-基}，『-曱基聚苯乙烯脲 N-{3-(2 -蔡基乙醯胺基）-4，5，6，7-四氫°比。定[4，3-c] D比唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(1-蔡基乙醯胺基）-4，5，6，7-四氫°比°定[4，3-c] 口比。坐基丨，Ν’ -甲基聚苯乙稀服 Ν-{3-(4 -苯基苯曱醯胺基）-4，5, 6,7-四氫吼°定[4，3-〇] 咄唑-1-基丨，Ν’ -甲基聚苯乙烯脲 Ν - { 3 - ( 2 -呋喃醯胺基）-4，5, 6, 7 -四氫吡啶[4，3 - c ]吡唑曱基聚苯乙稀脈 N-{3-(4 -苯氧苯甲醯胺基）-4, 5, 6, 7 -四氫吼啶[4, 3-c] 吡唑- l-基},Ν’ -曱基聚苯乙烯脲 1{3-(3-苯氧苯曱醯胺基）-4,5,6,7-四氫吼啶[4,3-〇] 咄唑-1-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-第三丁基-苯曱醯胺基）-4,5,6,7-四氫吡啶[4,C:\2D-C0DE\91-01\90119473.ptd Page 282 1327569 V. Description of invention (280) [4,3_c] 0 to 0 gui-1-yl}, 1^'_methyl polystyrene N-{3-(2,5-dioxabenzoguanamine)-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-1-yl}, 1^ '-Methylpolystyrene urea N-{3-(2,6-dioxabenzoguanamine)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazole-1 -yl},N'-mercaptopolystyrene urea {{3-(3,4-dioxobenzoguanamine)-4,5,6,7-tetrahydropyridine [4,3-c] Pyrazole-1-*}, N'-mercaptopolystyrene urea N-{3-(3,5-dioxabenzoquinone)-4,5,6,7-tetrahydroacridine 4,3-c]pyrazol-1-yl},N'-mercaptopolystyrene urea 1^-{3-3-(2-thiophene)-propanylamino-4,5,6,7 -tetrahydropyridine [4,3-c]pyrazol-1-yl}, "-mercaptopolystyrene urea N-{3-(2-c-phenylethylamino)-4,5,6,7-tetra Hydrogen ratio. [4,3-c] D-pyrazol-1-yl}, Ν'-mercaptopolystyrene-ruthenium-{3-(1-cacoethylamino)-4,5,6,7-tetrahydro ° ratio ° [4,3-c] ratio. Sitting on the base, Ν '-methyl polystyrene Ν-{3-(4-phenylphenylguanidino)-4,5, 6,7-tetrahydroindole ° [4,3-〇 ] carbazole-1-ylindole, Ν'-methyl polystyrene uranium - { 3 - ( 2 -furanylamino)-4,5, 6, 7 -tetrahydropyridine [4,3 - c ] Pyrazolyl-based polyphenylethylene ring N-{3-(4-phenoxybenzamide)-4, 5, 6, 7-tetrahydroacridine [4, 3-c] pyrazole-l- }', Ν'-mercaptopolystyrene urea {{3-(3-phenoxybenzoguanamine)-4,5,6,7-tetrahydroacridine [4,3-indole] carbazole- 1-yl}, Ν'-mercaptopolystyrene-indole-{3-(4-t-butyl-benzoguanamine)-4,5,6,7-tetrahydropyridine [4,

C:\2D-C0DE\91-01\90119473.ptd 第283頁 1327569 五、發明說明（281) 3-c] °比唑-1-基}，N’-曱基聚苯乙烯脲 1^-{3-胡椒基羧醯胺基-4,5,6,7-四氫咄啶[4,3-<:]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 1'1-{3-(2-萘）丙醯胺基-4，5，6，7-四氫°比咬[4，3-<:]°比口坐 -l-基}，Ν’ -曱基聚苯乙烯脲 1^-{3-(6-甲氧-2-萘）丙醯胺基-4,5,6,7-四氫吡啶 [4，3-c] 〇比0坐_1_基}，1^’_甲基聚苯乙稀脈 N-{3-(2-乙基丁醯胺基）-4,5,6, 7-四氫吡啶[4,3-c] 0比唑-l-基}，Ν’ -甲基聚苯乙烯脲 N-{3-(4-Dtb略咬-1-基-苯基）丙蕴胺基-4，5，6，7 -四氫口比啶[4,3-c]吡唑-1-*}，N’ -曱基聚苯乙烯脲 1{3-(2-氧基-吼咯啶-1-基）苯基}丙醯胺基-4,5,6,7-四氫咄啶[4,3-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 ^{3-(雙環[4.2.0]辛-1，3,5-三烯-7-羧醯胺基）_ 4, 5, 6, 7-四氫咄啶[4, 3-c]咄唑-l-基}，Ν’ -曱基聚苯乙烯脲 ^{3-(2-氧基-吡咯啶-1-基）苯乙醯胺基-4,5,6,7-四氧 °比啶[4，3 - c ]吡唑-1 -基}，Ν ’ -甲基聚苯乙烯脲 ^{3-(4-吡咯啶-1-基）苯乙醯胺基-4,5,6,7-四氫吡啶 [4，3_c] 0比0坐_1_基}，1^’_曱基聚苯乙稀脈 1^-{3-(4-三氟甲基）苯乙醯胺基-4,5,6,7-四氫°比啶 [4,3-〇]吡唑-1-基}，1^’-曱基聚苯乙烯脲 1^-{3-(2-溴）苯乙醯胺基-4,5,6,7-四氫吡啶[4,3-〇]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲C:\2D-C0DE\91-01\90119473.ptd Page 283 1327569 V. INSTRUCTIONS (281) 3-c] °Bizozol-1-yl}, N'-mercaptopolystyrene urea 1^- {3-Chlorocarboylamino-4,5,6,7-tetrahydroacridine [4,3-<:]pyrazol-1-yl}, Ν'-mercaptopolystyrene urea 1' 1-{3-(2-naphthalene)propanolamine-4,5,6,7-tetrahydrogen ratio bite [4,3-<:]° than mouth-l-base}, Ν' - Mercapto-polystyrene urea 1^-{3-(6-methoxy-2-naphthalene)-propanylamino-4,5,6,7-tetrahydropyridine [4,3-c] 〇 is 0 _ 1_基}, 1^'_methyl polystyrene ring N-{3-(2-ethylbutylamido)-4,5,6,7-tetrahydropyridine [4,3-c] 0 azole-l-yl}, Ν'-methyl polystyrene urea N-{3-(4-Dtb singly-l-yl-phenyl) propylamino-4,5,6,7- Tetrahydroabipyridine [4,3-c]pyrazole-1-*}, N'-mercaptopolystyrene urea 1{3-(2-oxy-indolyl-1-yl)phenyl} Propylamine-4,5,6,7-tetrahydroacridine [4,3-c]pyrazol-1-yl}, N'-mercaptopolystyrene urea^{3-(bicyclo[4.2. 0] octyl-1,3,5-triene-7-carboxyguanidino)_ 4, 5, 6, 7-tetrahydroacridine [4,3-c]carbazole-l-yl}, Ν' - mercapto polystyrene urea {3-(2-oxy-pyrrolidin-1-yl)phenylethylamino group -4,5,6,7-tetraoxapyridinium [4,3 - c ]pyrazole-1-yl}, Ν '-methyl polystyrene urea^{3-(4-pyrrolidin-1- Phenylethylamino-4,5,6,7-tetrahydropyridine [4,3_c] 0 to 0 sitting on the _1_ base}, 1^'_曱-based polystyrene pulse 1^-{3 -(4-Trifluoromethyl)phenylethylamino-4,5,6,7-tetrahydropyridinium [4,3-indole]pyrazol-1-yl}, 1^'-fluorenyl Styrene urea 1^-{3-(2-bromo)phenethylamino-4,5,6,7-tetrahydropyridine[4,3-indolyl]pyrazole-1-yl},Ν'-曱Polystyrene

C:\2D-CODE\91-01\90119473.ptd 第284頁 1327569 五、發明說明（282) 1{3-[4-(吡咯啶-1-基_羰基曱氧基）]苯乙醯胺基-4,5, 6, 7-四氫吡啶[4, 3-c]吡唑-l-基}，Ν’ -甲基聚苯乙烯脲 1^-{3-[3-(胺基羰基曱氧）苯乙醯胺基]-4,5,6,7-四氫口比啶[4,3-c]吡唑-1-基}，1^’_曱基聚苯乙烯脲 1^1-{3-[4-(2-氧基-$唑啶-3-基）苯乙醯胺基]-4,5,6,7-四氫吡啶[4,3-c]吡唑-1-基}，1’_曱基聚苯乙烯脲 1{3-[4-(4-甲基哌畊基）苯乙醯胺基]-4,5,6,7-四氫口比啶[4,3-c]吡唑-1-基}，N’-曱基聚苯乙烯脲 1{3-(苯并[1，3]二氧伍圜-5-基）乙醯胺基-4.，5,6,7-四氫吡啶[4,3-c]咄唑-1-基},N’-曱基聚苯乙烯脲 !']-{3-[4-(2-氧基-''|唑啶-3-基）苯乙醯胺基]-4,5,6,7-四氫吼啶[4,3-c]吡唑曱基聚苯乙烯脲 N-{3-(2 -苯基_1，3 - σ塞0坐_4_基）乙酿胺基_4, 5，6，7_四氫吡啶[4,3-c]吡唑-1-基}，1^’-曱基聚苯乙烯脲 N-{3_[4_(1- 口比17各σ定_2_嗣）苯甲酿胺基]_4，5，6，7 -四氫吡啶[4,3-c]吡唑-1-基}，Ν’-曱基聚苯乙烯脲 1{3-[2-(3-氧基-3,4,48,8&-四氫-211-苯并[1，4]4口井 -6-'基）乙醢胺基]-4，5，6，7-四氫0比口定[4，3 — c] 0比0坐_1一基}， Ν’ -甲基聚苯乙烯脲 1^-{3-(1-曱基-吲哚-3-基）乙醯胺基-4,5,6,7-四氫吡啶 [4,3-(：]咄唑-1-基}^’-曱基聚苯乙烯脲 ^{3-(6-氧基-611-嗒畊-；1-基）乙醯胺基-4,5,6,7-四氫吡啶[4,3-c]吡唑-1-基}，Ν’-甲基聚苯乙烯脲 Ν_{3_(4_(嗎琳_1_基）_苯基）乙酿胺基_4，5，6,7_四氮口比C:\2D-CODE\91-01\90119473.ptd Page 284 1327569 V. INSTRUCTIONS (282) 1{3-[4-(Pyrrolidin-1-yl-carbonyloxy)oxy)benzamide 4-,5,6,7-tetrahydropyridine [4,3-c]pyrazole-l-yl}, Ν'-methyl polystyrene urea 1^-{3-[3-(aminocarbonyl)曱 ) ) ) 醯 ] ] ] ] ] ] ] -4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 1-{3-[4-(2-oxy-$oxazol-3-yl)phenylethylamino]-4,5,6,7-tetrahydropyridine [4,3-c]pyrazole- 1-yl},1'-mercaptopolystyrene urea {{3-[4-(4-methylpipedyl)phenylethylamino)-4,5,6,7-tetrahydropyridinium [4,3-c]pyrazol-1-yl}, N'-mercaptopolystyrene urea 1{3-(benzo[1,3]dioxoindol-5-yl)ethinylamino- 4.,5,6,7-tetrahydropyridine [4,3-c]oxazol-1-yl}, N'-mercaptopolystyrene urea!']-{3-[4-(2-oxygen -''|oxazolidine-3-yl)phenethylamino]-4,5,6,7-tetrahydroacridine [4,3-c]pyrazolyl polystyrene urea N-{3 -(2-phenyl_1,3 - σ plug 0 sits _4_yl) ethyl amide 4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl} , 1^'-decyl polystyrene urea N-{3_[4_(1-port ratio 17 σ 定 _2 嗣嗣) benzoylamino]_4,5 6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, Ν'-mercaptopolystyrene urea 1{3-[2-(3-oxy-3,4,48, 8&-tetrahydro-211-benzo[1,4] 4-well-6-'yl)acetamido]-4,5,6,7-tetrahydro 0 ratio [4,3 - c ] 0 to 0 sitting _1 yl}, Ν'-methyl polystyrene urea 1^-{3-(1-indolyl-indol-3-yl)acetamido-4,5,6, 7-tetrahydropyridine [4,3-(:]carbazol-1-yl}^'-mercaptopolystyrene urea {3-(6-oxy-611-嗒耕-; 1-yl) B Amidino-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-1-yl}, Ν'-methyl polystyrene Ν_{3_(4_(么琳_1_ Base) _phenyl) ethyl amide 4,5,6,7_tetrazine ratio

C:\2D-C0DE\91-01\90119473.ptd 第285頁 1327569 五、發明說明（283) 口比 c 啶[4,3-c]吡唑-1_基}，N，-甲基聚笨乙烯脲 ^{3-(4-吼咬基乙酿胺基）_4,5,67_四氫吼唑-卜基}，Ν’ -曱基聚苯乙烯脲定[4,3- N-{3-苯氧乙酿胺基-4, 5, 6, 7-四氫吡啶[ 基}，Ν’ -曱基聚苯乙烯脲 l ’ a c」 N-{3-(3-吼啶基乙醯胺基）_4,5, 6，？_四氫吡唑-卜基}，Ν’ -甲基聚苯乙烯脲幻4’ 3-c] C J °tb Ν-{3-[5-(4-氣苯基）呋喃_2_羧醯胺基卜4 5 吡啶[4,3_c]咄唑-1_基}，『_曱基聚苯乙烯脲，，-四氫 NM3-[喳啉-6-羧醯胺基卜4,5,6,7_四氫吡 _ 唑-1-基}，Ν’ -曱基聚苯乙烯脲 L4’ 3一四 N-{3-[2-曱基-5-苯基-呋喃一3_羧醯胺基]_4 5 氮吼咬[4,3-c]吼。坐-1-基}，N、甲基聚苯乙烯脲，，7 ^{3-[苯并呋喃-2-羧醯胺基卜4,5,6,7_四氫吡 [4, 3-c]吼唑-1-基}，N，-曱基聚苯乙烯脲定 N-{ 3-[6-氣菸鹼醯胺基]-4, 5, 6, 7-四氫吡啶「4 唑-1-基}，Ν’ -曱基聚苯乙烯脲 ’ N-{3-[5 -氯噻吩-2 -羧醯胺基]_4,5,6 7_四 ^4,3-c]吡唑-1-*}，N，-甲基聚苯乙稀脲 I D比喷實施例5 N-{3 -苯乙酿胺基-5 -苯乙醢基一4,5,6,?_四畫 [4,3-<:]吡唑-1-基}，『-曱基聚笨乙烯脲之製^比咬笨乙酸（0. 43毫莫耳’ 58. 5毫克）’ NMM( 0. 43毫呈 47.3微升）及？丫8(^(0.43毫莫耳，223 8臺#、；莫耳’ 宅兄）添加至C:\2D-C0DE\91-01\90119473.ptd Page 285 1327569 V. INSTRUCTIONS (283) Mouth ratio c pyridine [4,3-c]pyrazole-1 yl}, N,-methyl poly Stupid vinyl urea ^{3-(4-吼乙乙乙胺基)_4,5,67_tetrahydrocarbazole-buji},Ν'-mercaptopolystyrene urea [4,3- N- {3-phenoxyethylamino-4,5,6,7-tetrahydropyridine [yl}, Ν'-mercaptopolystyrene urea 1 'ac" N-{3-(3-acridinyl Amidino)_4,5, 6,? _tetrahydropyrazole-buji}, Ν'-methyl polystyrene urea 4' 3-c] CJ °tb Ν-{3-[5-(4-phenylphenyl)furan_2_carboxylate Aminobi 4 5 pyridine [4,3_c]carbazole-1_yl}, "_mercaptopolystyrene, -tetrahydro NM3-[porphyrin-6-carboxyguanamine 4,5,6 , 7_tetrahydropyrazole-1-yl}, Ν'-mercaptopolystyrene urea L4' 3 - four N-{3-[2-mercapto-5-phenyl-furan-3_carboxylate Amino]_4 5 Nitrogen bites [4,3-c]吼. Sodium-1-yl}, N, methyl polystyrene, 7 ^{3-[benzofuran-2-carboxyindoleyl 4,5,6,7-tetrahydropyrim [4, 3- c] oxazol-1-yl}, N,-mercaptopolystyrene, N-{ 3-[6-gasnicotinium amide]-4, 5, 6, 7-tetrahydropyridine "4 azole -1-yl}, Ν'-mercaptopolystyrene urea 'N-{3-[5-chlorothiophene-2-carboxyindoleamino]_4,5,6 7_tetra^4,3-c]pyridin Imidazole-1-*}, N,-methyl polystyrene urea ID ratio spray Example 5 N-{3 - phenylethylamino-5-phenethyl group-4,5,6,?_4 Draw [4,3-<:]pyrazol-1-yl}, "-- thiol-polystyrene-formaldehyde system ^^ bite acetic acid (0. 43 millimoles '58. 5 mg)' NMM (0 43 milligrams is 47.3 microliters) and ?丫8 (^ (0.43 millimoles, 223 8 sets #,; Moer 'home brothers) added to

C:\2D-G0DE\91-01\90119473.ptd 第286頁 1327569 五、發明說明（284) 笨乙醯胺基-4，5，6，7-四氫17比0定[4，3-〇]〇比0坐-1-基}，『_曱基5^本乙稀脈（0.086毫莫耳，1〇〇毫克），該服事先於4毫升無水N，N-二甲基曱醯胺溶脹。結果所得懸浮液於22。〇溫和攪拌2 4小時。然後樹脂經過濾，以n，N -二甲基甲醯胺、二氯曱烧、甲醇洗條及真空脫水。 f施例1 5 4, 5, 6, 7-四氫吡啶[4, 3-c]咄唑-3-基衍生物存庫之製備步驟a : 540克3 -胺基- 5- (第二丁醋基）—4，5，6,7 -四氫π比口定 [4，3 - c ] π比嗤係根據實施例4報告之程序製備。步驟b : 結果所得3 -胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫吼啶 [4，3 - c ]吡唑根據實施例5報告之程序支撐於甲基異氰酸酯聚苯乙烯樹脂（200-400 1帛目，2%DVB，負載1.49毫莫耳/ 克，9 0 0 克、步驟c : 結果所得N-{3 -胺基-5-(第三丁酯基）-4, 5, 6, 7-四氫0比啶[4,3-c]吡唑-1-*}，N’-曱基聚笨乙烯脲分成96個不同批次（各批1 5克）。各批次根據實施例1 3所述程序與適當醯基氣反應獲得實施例1 3列舉之產物。步驟d : 96批次N-{3 -醯基醢胺基- 5- (第三丁酯基）-4, 5, 6, 7-四氫吡啶[4, 3-c] °比唑-1-基}, Ν’ -甲基聚苯乙烯脲根據實施例1 4所述程序各別使用T F A 5 0 %於無水二氯曱燒溶液處C:\2D-G0DE\91-01\90119473.ptd Page 286 1327569 V. Description of the invention (284) Stupid amino-4,5,6,7-tetrahydro 17 to 0 [4,3- 〇]〇坐-1-基}, _曱基5^本乙稀脉 (0.086 mmol, 1〇〇mg), the service before 4 ml of anhydrous N,N-dimethyl The amine swells. The resulting suspension was at 22. 〇 Warm and stir for 24 hours. The resin was then filtered, washed with n,N-dimethylformamide, dichlorohydrazine, methanol, and vacuum dehydrated. f Example 1 5 4, 5, 6, 7-tetrahydropyridine [4, 3-c]oxazol-3-yl derivative library preparation step a: 540 g 3-amino- 5- (second Butyl vinegar) - 4,5,6,7-tetrahydropi 比[4,3 - c ] π ratio oxime was prepared according to the procedure reported in Example 4. Step b: The resulting 3-amino-5-(t-butyl ester)-4,5,6,7-tetrahydroacridine [4,3 - c ]pyrazole was supported according to the procedure reported in Example 5 Methyl isocyanate polystyrene resin (200-400 1 mesh, 2% DVB, load 1.49 mmol/g, 900 g, step c: result N-{3-amino-5-(third Butyl ester)-4, 5, 6, 7-tetrahydro 0-pyridine [4,3-c]pyrazole-1-*}, N'-fluorenyl polystyrene urea is divided into 96 different batches (each Batch 1 5 g). Each batch was reacted with an appropriate hydrazine gas according to the procedure described in Example 13 to obtain the product of Example 13. Step d: 96 batches of N-{3 -mercaptoamine- 5 - (t-butyl ester)-4,5,6,7-tetrahydropyridine [4,3-c] °biazol-1-yl}, Ν'-methyl polystyrene according to Example 1 4 The procedure uses TFA 50% each in an anhydrous dichlorohydrazine solution.

C: \2D-CX)DE\91 -〇] \90119473.ptd 第 287 頁 1327569 五、發明說明（285) 理’獲得實施例1 4列舉之產物。步驟e : 步驟d所得96批次中之一批次分成丨49批次（各5〇毫克）。 1 4 9批次各別與全部用於製備實施例8 ' 9、i 〇列舉的產物之叛酸、辱醯氯或異氰酸酯反應。步驟f : 步驟d所得96批次中之一批次分成丨49批次（各5〇毫克）。此1 4 9批次各別與實施例8使用的9 5種羧酸、實施例9使用的1 5種續酿氣及實施例丨〇使用的丨5種異氰酸酯反應。步驟g: 步驟d之其餘9 5批次各別進行步驟e及f。整體綜合化學製程共獲得96>< 149=143()4種4,5,67-四氯吡啶[4，3 - c ]吡唑-1 -基衍生物存庫。前述綜合存庫之代表性化合物為： Ν-{5 -笨續酿基-4, 5, 6, 7-四氫°比啶[4, 3-c] °比唾-3-基}-4_ 氟苯曱醯胺；ih-NMR (DMSO-d6) d ppm 2. 7(m); 3. 4(m) ; 4. 1 (s) ; 7. 25-8· 1 (m)。 N-[5-(曱基磺醯基）-4,5,6,7-四氫吡啶[4,3-c]吡峻-3_ 丨_基]苯曱醯胺；IH-NMR (DMSO-d6) d ppm 2. 78(m) ，2.89(s)，3.45(m)，4.15(s),7.4-8.0(m)。 N -異丙基-Ν’ - {3 -苯曱醯胺基-4, 5, 6, 7-四氫吡咬 [4,3-c]咣唑-5-基}脲；IH-NMR (DMS0-d6) d ppm l(d)，2.6(m)，3.57(m)，3.75(ni)，4.2(s)，7.4-8.0(m)。 N-異丙基-Ν’ - {3-苯乙醯胺基-4, 5, 6, 7 -四氫咄啶C: \2D-CX)DE\91 -〇] \90119473.ptd Page 287 1327569 V. Description of the Invention (285) The product obtained in Example 1 is obtained. Step e: One of the 96 batches obtained in step d was divided into 49 batches (5 mg each). 1 4 9 batches were each and all used to prepare the reaction of the products listed in Example 8 '9, i 〇, tart, abusive chlorine or isocyanate. Step f: One of the 96 batches obtained in step d is divided into 49 batches (5 mg each). The 194 batches were each reacted with the 9 carboxylic acids used in Example 8, the 15 contiguous granules used in Example 9, and the hydrazine 5 isocyanates used in the examples. Step g: The remaining 9.5 batches of step d are subjected to steps e and f, respectively. A total of 96 >< 149 = 143 () 4 4,5,67-tetrachloropyridine [4,3 - c ]pyrazole-1-yl derivative libraries were obtained. Representative compounds of the aforementioned comprehensive storage are: Ν-{5 - styrene-4, 5, 6, 7-tetrahydropyridinium [4, 3-c] ° than sial-3-yl}-4_ Fluoroquinone; ih-NMR (DMSO-d6) d ppm 2. 7 (m); 3. 4 (m); 4. 1 (s); 7. 25-8 · 1 (m). N-[5-(indolylsulfonyl)-4,5,6,7-tetrahydropyridine[4,3-c]pyridin-3-yl-phenyl]benzamide; IH-NMR (DMSO- D6) d ppm 2. 78(m), 2.89(s), 3.45(m), 4.15(s), 7.4-8.0(m). N-isopropyl-Ν'-{3-benzoguanamine-4, 5, 6, 7-tetrahydropyridin [4,3-c]oxazol-5-yl}urea; IH-NMR ( DMS0-d6) d ppm l(d), 2.6(m), 3.57(m), 3.75(ni), 4.2(s), 7.4-8.0(m). N-isopropyl-Ν' - {3-phenethylamino-4, 5, 6, 7-tetrahydroacridine

1327569 五、發明說明（286) [4, 3-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm 1(d)， 1.01(s，3H)，1.04(s，3H)，2.55(t，2H)，3.50(t，2H)，3.60(s ，2H)，3.62-3.80(m，lH),4.15(s，2H),6.15(d，lH)，7.20-7·40(m，5H)。" 1^-[5-(甲基磺醯基）-4,5,6,7-四氫吡啶[4,3-(：]吡唑-3-基]環丙烷羧醯胺；iH-NMR (DMS0-d6) d ppm 0.75(m)， 1.8(m)，2.7(m)，2.85(s)，3.4(m)，4.1(s)。 N-(5 -苯甲醯基-4, 5, 6, 7-四氫0比咬[4, 3-c] 0比峻-3 -基）環丙烧羧醯胺；(DMS0_d6) d PPm 〇. 75(m)， 1.8(m),2.7(m)，3.65(bs)，4.4(s)，7.3-7.5(m)。 N_[5_苯乙酿基-4, 5, 6, 7-四氫。比咬[4, 3-c] 〇比唾-3-基] 環丙烷羧醯胺(DMS0_d6) d PPm 〇.75(bs)， 1. 8(m)，2. 6(bs)，4. 2-4. 4(2s)，7. 1-7. 35(m)。 N—異丙基-Ν’ - {3 -環丙烧後醯胺基-4, 5, 6, 7-四氫吼0定 [4，3-。]°比°坐-5-基}脈；1H-NMR (DMSO-d6) d ppm 0. 75(bs)，1. 0(d)，1. 8(m)，2. 55(m)，3. 5(m)，3. 75(m)，4. 05 (s)。" 1[5-(曱基石黃醯基）_4,5,6,7-四氫0比咬[4,3-<:]0比唑-3-基]_4_ 苯氧苯甲酿胺；1H-NMR (DMS〇-d6) d ppm 2.8 (bs)，2.9(s)，3.5(m)，4.2(s)，7.0-8.0(m)。 N一（5 -苯甲醯基-4, 5, 6, 7-四氫吡啶[4, 3-c]咄唑-3-基） -4-苯氧苯甲醯胺；1H-NMR (DMSO-d6) d ppm 2.75 (bs)，3.7(bs)，4.5(bs)，7.0-8.0(m)。 N-[5 -苯乙醯基-4, 5, 6, 7-四氫0比啶[4, 3-c] 口比唑-3-基]1327569 V. INSTRUCTIONS (286) [4,3-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm 1(d), 1.01 (s, 3H), 1.04 (s, 3H), 2.55 (t, 2H), 3.50 (t, 2H), 3.60 (s, 2H), 3.62-3.80 (m, lH), 4.15 (s, 2H), 6.15 (d, lH), 7.20-7 · 40 (m, 5H). " 1^-[5-(methylsulfonyl)-4,5,6,7-tetrahydropyridine [4,3-(:]pyrazol-3-yl]cyclopropanecarboxamide; iH- NMR (DMS0-d6) d ppm 0.75 (m), 1.8 (m), 2.7 (m), 2.85 (s), 3.4 (m), 4.1 (s). N-(5-benzhydryl-4, 5, 6, 7-tetrahydro 0-bite [4, 3-c] 0-jun-3-yl) Cyclopropanol carboxamide; (DMS0_d6) d PPm 〇. 75(m), 1.8(m), 2.7 (m), 3.65 (bs), 4.4 (s), 7.3-7.5 (m). N_[5_phenylethyl 4, 5, 6, 7-tetrahydro. than bite [4, 3-c 〇唾唾基基基唾唾唾唾唾唾唾 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 75 , 7. 1-7. 35(m). N-Isopropyl-Ν' - {3 - Cyclopropanol amide amino-4, 5, 6, 7-tetrahydro hydrazine 0 [4,3- ..°°°°-5-base} pulse; 1H-NMR (DMSO-d6) d ppm 0. 75(bs), 1. 0(d), 1. 8(m), 2. 55(m) , 3. 5 (m), 3. 75 (m), 4. 05 (s). " 1[5-(曱基石黄醯基)_4,5,6,7-tetrahydro 0 ratio bite [4,3 -<:]0-pyrazol-3-yl]_4_phenoxybenzamide; 1H-NMR (DMS〇-d6) d ppm 2.8 (bs), 2.9(s), 3.5(m), 4.2(s ), 7.0-8.0 (m). N-(5-benzylidenyl-4,5,6,7-tetrahydropyridine[4,3-c]oxazol-3-yl)-4-phenoxybenzene Formamide ;1H-NMR (DMSO-d6) d ppm 2.75 (bs), 3.7 (bs), 4.5 (bs), 7.0-8.0 (m). N-[5-phenylethenyl-4, 5, 6, 7 - tetrahydro 0-pyridyl [4, 3-c] port-azol-3-yl]

C:\2D-CXBE\91-01\90119473.ptd 第289頁 1327569 五、發明說明（287) 苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.6(bs)， 3. 75(bs)，4.4(bs)，7. 0-8.0(m)。 N_異丙基-Ν’ - {3-(4-氟-苯曱醯胺基）-4，5, 6, 7-四氫吡 °定[4，3-(：]'>比°坐-5-基}脲；111-關1^(0^180-(16)(1??111 1.0(d);2.6(m);3.55(m);3.7(m);4.2(s);6.2(d);7.3-8. 1 (m) ° N-(5-(4-氣-苯甲 it基）一4, 5, 6, 7 —四氫0比0定[4, 3-c] 口比口坐 -3-基）-4-|1笨曱醯胺；111-麗1^(〇^150-(16)(1卩口1112.7 (bs);3.5-4.0(2bs);4.4(bs);7.1-8.2(m)。 N -異丙基-N’-{3-(4-第三丁基-苯曱醯胺基）-4,5,6,7-四氫0比。定[4，3-〇]°比°坐-5-基}脲；1H-NMR (DMSO-d6) d ppm l(d);l.3(s);2.6(m);3.6(m);3.7(m);4.15(s);7.45 -7. 95(m)。" N_[5_(曱基確酿基）_4，5，6，7-四氮π比咬[4，3-c]D比o坐_3-基卜4-氟苯曱醯胺；lH-NMR(DMSO-d6)dppm2·8(m); 2.9(s);3.5(m);4.2(s);7.2-8.l(m)。 N-{5-苯石黃酿基-4，5，6，7-四氫°比咬[4，3-c] D比0坐-3-基} -4-苯氧苯曱醯基；1H-NMR (DMS0-d6) d ppm 2· 7(m)， ⑩3. 4(m)，4. 05(s)，7. 0-8· 0(m)。 N-{5-辛基續酿基-4, 5，6，7-四氫°比°定[4，3-c] 0比°坐-3-基}-4 -苯氧苯曱醯基；1H-NMR (DMSO_d6) d ppm 2. 6(m)， 3. 4(m)，4. 2(s)，4· 4(s)，7. 0-8. 0(m)。 N-苯基-N’-{3-(4-苯氧-苯甲醯胺基）-4,5,6,7-四氫口比咬[4，3-。]°比峻-5-基}脲；111-題1^(0^180-(16)(1〇口111C:\2D-CXBE\91-01\90119473.ptd Page 289 1327569 V. INSTRUCTIONS (287) Phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm 2.6(bs), 3. 75 (bs), 4.4 (bs), 7. 0-8.0 (m). N_isopropyl-Ν' - {3-(4-fluoro-benzoguanamine)-4,5, 6, 7-tetrahydropyridin [4,3-(:]'>°° Sodium-5-urea; 111-off 1^(0^180-(16)(1??111 1.0(d); 2.6(m); 3.55(m); 3.7(m); 4.2(s) ;6.2(d);7.3-8. 1 (m) ° N-(5-(4-Gas-Benzyl)- 4, 5, 6, 7-Tetrahydrogen 0 to 0 [4, 3- c] mouth is more than -3- group)-4-|1 alum; amine 1; (〇^150-(16) (1 mouth 1112.7 (bs); 3.5-4.0 (2bs); 4.4(bs);7.1-8.2(m) N-isopropyl-N'-{3-(4-t-butyl-benzoguanamine)-4,5,6,7-tetrahydro 0 Ratio [4,3-〇]°°°-5-yl}urea; 1H-NMR (DMSO-d6) d ppm l(d); l.3(s); 2.6(m); 3.6( m); 3.7 (m); 4.15 (s); 7.45 -7. 95 (m). " N_[5_(曱基确酿)_4,5,6,7-tetrazine π ratio bite [4, 3-c]D ratio o sitting _3-kib 4-fluorophenylguanamine; lH-NMR (DMSO-d6) dppm2·8 (m); 2.9 (s); 3.5 (m); 4.2 (s) ; 7.2-8.l(m). N-{5-Phenyl yellow-branched-4,5,6,7-tetrahydrogen ratio [4,3-c] D is 0 to -3- base} -4-phenoxyphenyl fluorenyl; 1H-NMR (DMS0-d6) d ppm 2· 7(m), 103. 4(m), 4. 05(s), 7. 0-8· 0(m N-{5-octyl continuation base-4, 5,6,7-tetrahydrogen ratio °[4,3-c] 0 ratio ° sitting-3- }-4-phenoxybenzoin; 1H-NMR (DMSO_d6) d ppm 2. 6(m), 3. 4(m), 4. 2(s), 4·4(s), 7. 0 -8. 0(m). N-phenyl-N'-{3-(4-phenoxy-benzamide)-4,5,6,7-tetrahydro port ratio bite [4,3- .]°比峻-5-基}Urea; 111-question 1^(0^180-(16)(1〇口111

C:\2D-00DE\91-0U90119473.ptd 第290頁 1327569 五、發明說明（288) 2.7(m)，3.7(m)，4.35(s)，6.9-8.0(m)。，丨 N-[5-(°奎琳-8-石黃酿基）-4，5，6，7 -四氫〇比°定[4，3-c] σ比口坐 -3 -基]-4-苯氧苯曱醯基；1H-NMR (DMS0-d6) d ppm 2_6(m)，3.75(m)，4.3(s)，7.0-9.0(in)。 N-{5-(2-°塞吩）乙醯基-4，5，6，7-四氫°比咬[4, 3-c] 0比口坐 -3 -基}-4 -苯氧苯曱醯基；1H-NMR (DMS0-d6) d ppm 2.65(bs)，3.8(m)，3.9-4.1(2s)，4.4-4.5(2s)，6.8-8.0(m) ο ^[5-異丁醯基-4，5，6，7-四氫17比咬[4，3-(：]°比°坐-3-基] -4-氟苯曱醯胺；111-麗1^(〇1^〇-(16)(1??1111.0((1);2.5-2.7(2m);2.9(m);3.7(m);4.3-4.5(2s);7.3-8.1(m)。 N-(5 -苯曱醯基-4，5, 6, 7_四氫0比唆[4, 3-c] 口比〇坐—3-基） -4-第三丁基-苯甲醯基；1H-NMR (DMS0-d6) d ppm 1. 3 (s);2.7(m);3.7(m);4.45(s);7.3-7.9(m)。 1'1-{5-苯石黃醯基-4，5,6,7-四氫°比。定[4，3-(：]°比°坐-3-基} -4-第三丁基-苯曱醯基；1H-NMR (DMS0-d6) d ppm 1.3(s);2.7(m);3.4(m);4.1(s);7.45-7.95(m)。 N-異丙基-Ν’ - {3-(4-第三丁基-苯曱醯胺基）-4,5,6,7-四氫吡啶[4, 3-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm 1.3(s);2.7(m);3.7(m);4.35(s);6.8-8.0(m) ° " N-{5-(嗤琳-8-績醯基）-4, 5，6，7 -四氫°比咬[4，3-c] D比口坐 -3-基}-4-第三丁基-苯氧苯曱醯基；1H-NMR (DMS0-d6) d ppm 1.3(s);2.6(m);3.7(m);4.3(s);7.4-9.0(m) 〇 N-(5-苄基確醯基一4，5，6，7 -四氫0比咬[4，3-c] 〇比0坐-3—基C:\2D-00DE\91-0U90119473.ptd Page 290 1327569 V. INSTRUCTIONS (288) 2.7(m), 3.7(m), 4.35(s), 6.9-8.0(m). ,丨N-[5-(°奎琳-8-石黄牛)-4,5,6,7-tetrahydropyrene ratio °[4,3-c] σ than mouth sitting -3 - group] 4-phenoxyphenyl hydrazino; 1H-NMR (DMS0-d6) d ppm 2_6 (m), 3.75 (m), 4.3 (s), 7.0-9.0 (in). N-{5-(2-° phenophene)ethinyl-4,5,6,7-tetrahydrogen ratio bite [4, 3-c] 0 than mouth-spin-3-yl}-4-phenoxy Benzoyl; 1H-NMR (DMS0-d6) d ppm 2.65 (bs), 3.8 (m), 3.9-4.1 (2s), 4.4-4.5 (2s), 6.8-8.0 (m) ο ^[5- Isobutyl fluorenyl-4,5,6,7-tetrahydro 17 ratio bite [4,3-(:]° ratio ° sit-3-yl]-4-fluorophenylamine; 111-丽1^(〇1 ^〇-(16)(1??1111.0((1); 2.5-2.7(2m); 2.9(m); 3.7(m); 4.3-4.5(2s); 7.3-8.1(m). N-( 5-Benzyl phenyl-4,5, 6, 7_tetrahydro 0 唆[4, 3-c] 〇 — -3-yl)-4-t-butyl-benzylidene; 1H -NMR (DMS0-d6) d ppm 1. 3 (s); 2.7 (m); 3.7 (m); 4.45 (s); 7.3-7.9 (m). 1'1-{5-Phenylxanthyl-4 ,5,6,7-tetrahydrogen ratio. [4,3-(:]° ratio °-3-yl}-4-t-butyl-phenylhydrazine; 1H-NMR (DMS0-d6 d ppm 1.3(s); 2.7(m); 3.4(m); 4.1(s); 7.45-7.95(m). N-isopropyl-Ν' - {3-(4-t-butyl- Benzoguanamine)-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm 1.3(s); (m); 3.7 (m); 4.35 (s); 6.8-8.0 (m) ° " N-{5-(嗤琳-8-醯基基)-4, 5,6,7-tetrahydrogen Than the bite [4,3-c] D than the mouth -3- base}-4 -T-butyl-phenoxybenzoin; 1H-NMR (DMS0-d6) d ppm 1.3(s); 2.6 (m); 3.7 (m); 4.3 (s); 7.4-9.0 (m) 〇 N-(5-benzyl decyl- 4,5,6,7-tetrahydro 0-bit [4,3-c] 〇 is 0--3

C:\2D-00DE\91-01\90119473.ptd 第291頁 1327569 五、發明說明（289) )-環丙烷羧醯胺；1H-NMR (DMS0-d6) d ppm 0_75(m)， 1.8(m)，2.55(m)，3.35(m)，4.1(s)，4.4(s)，7.2-7.4(m)。 N -異丙基-N，- {3 -環丙烷羧醯胺基-4, 5, 6, 7-四氫吡啶 [4, 3-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm 0. 75 (m), 1. 8(m), 2. 6(m), 3. 7(m), 4. 3(s), 4. 3(s), 6. 8-7. 5(m) o " N-{5-(2-°塞吩基）乙蕴基_4，5，6, 7-四氫〇比°定[4，3-(：] B比唑-3 -基卜環丙烷羧醯胺基；1H-NMR (DMS0-d6) d ppm 〇.75(m)，1·8(π〇, 2.6(m)，3_7(m)，3.85-4.05(2s) ,4.3-4.5 灸(2s),6.8-7.4(m)。 N-{5-(嗜琳-8-確醯基）-4，5，6，7 -四氫°比°定[4，3-c]吼〇坐 -3-基}-環丙烷羧醯胺基；1H-NMR (DMS0-d6) d ppm 0. 75 (bs)，1.8(m)，2.5(m)，3.7(m)，4_25(s)，7.6-9.0(m)。 N-(5-乙酿基-4，5，6，7 -四氫0比咬[4，3-c] 〇比0坐-3-基）苯甲醯胺；111-關1^(0河5〇-(16)(1〇?1112.05(5)，2.6- 2.8(2m),3.6-3.7(2m)，4.3-4.4(2s)，7.4-8.0(m)。 N -（5 -苯曱醯基-4，5，6，7-四氫0比°定[4，3-c] 0比0坐-3-基）苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.75(m)，3.7(bs)， •4.5(s)，7.4_8,0(m)。 N-[5-(2-苯乙醯基）-4,5, 6, 7-四氫吼啶[4, 3-c]吼唑-3-基]苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2· 6(bs)， 3. 75(bs)，4. 5(bs), 7.卜8. 0(m)。 N-{5 -苯績醯基-4, 5, 6, 7-四氫"比咬[4, 3-c] °比0坐-3-基} 苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.7(m),4.05(s)，C:\2D-00DE\91-01\90119473.ptd Page 291 1327569 V. INSTRUCTIONS (289) )-Cyclopropane Carboxamide; 1H-NMR (DMS0-d6) d ppm 0_75(m), 1.8( m), 2.55 (m), 3.35 (m), 4.1 (s), 4.4 (s), 7.2-7.4 (m). N-isopropyl-N,-{3-cyclopropanecarboxamido-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-5-yl}urea; 1H-NMR ( DMS0-d6) d ppm 0. 75 (m), 1. 8(m), 2. 6(m), 3. 7(m), 4. 3(s), 4. 3(s), 6. 8-7. 5(m) o " N-{5-(2-°Sepyl) B-yl 4,5,6,7-tetrahydropyrene ratio [4,3-(:] B-pyridol-3-ylcyclopropanecarboxamide; 1H-NMR (DMS0-d6) d ppm 〇.75(m),1·8(π〇, 2.6(m), 3_7(m), 3.85 -4.05(2s), 4.3-4.5 moxibustion (2s), 6.8-7.4(m). N-{5-(嗜琳-8- 醯醯)-4,5,6,7-tetrahydrogen °° [4,3-c] 吼〇-3-yl}-cyclopropanecarboxamide; 1H-NMR (DMS0-d6) d ppm 0. 75 (bs), 1.8 (m), 2.5 (m) , 3.7 (m), 4_25 (s), 7.6-9.0 (m). N-(5-ethyl-branched-4,5,6,7-tetrahydro- 0 ratio bite [4,3-c] 〇 ratio 0 Sodium-3-yl)benzamide; 111- Guan 1^(0 River 5〇-(16)(1〇?1112.05(5), 2.6-2.8(2m), 3.6-3.7(2m),4.3- 4.4(2s), 7.4-8.0(m). N-(5-phenylhydrazino-4,5,6,7-tetrahydro- 0 ratio °[4,3-c] 0 to 0 sitting-3- Benzoamine; 1H-NMR (DMS0-d6) d ppm 2.75(m), 3.7(bs), •4.5(s), 7.4_8,0(m). N-[5-(2-Benzene Ethyl)-4,5, 6, 7-tetrahydroacridine [4, 3-c]oxazol-3-yl]benzamide; 1H-NMR (DMS0-d6) d ppm 2·6(bs), 3. 75(bs) , 4. 5 (bs), 7. Bu 8. 0 (m). N-{5 - Benzene -4 -4, 5, 6, 7-tetrahydro " than bite [4, 3-c] ° Benzene amide; 1H-NMR (DMS0-d6) d ppm 2.7 (m), 4.05 (s),

C:\2D-OODE\91-01\90119473.ptd 第292頁 1327569 五、發明說明（290) 7.4-8.0(m)。 N- 丁基-Ν’ - {3 -苯曱醯胺基-4, 5, 6, 7 -四氫吡啶[4, 3-c] η比0坐_5_基}脈；111_關1^(〇%3〇_(16)(10卩111〇.8(111)，1.2_ 1. 4(m), 2. 6(m), 3. 0(m), 3. 6(m), 4. 2(s), 7. 4-8. 0(m) ° " N-乙基-Ν’ - {3 -苯甲醯胺基-4, 5, 6, 7 -四氫吡啶[4, 3-c] 口比唑-5 -基丨脲；1H-NMR (DMSO-d6) d ppm l(m)，2. 6(m)， 3. 0(q)，4. 2(s)，7. 4-8. 0(m)。，， N-{5-(2 -口夫喃曱醯基）-4，5, 6, 7-四氫0比咬[4, 3-c]吼〇坐 -3-基}-4-第三丁基-苯曱醯胺；1H-NMR (DMSO-d6) d ppm 1.3(s);2.8(m);3.9(m);4.6(bs);6.5-8·0(m) 〇 N-{5-(2-°塞吩基乙醯基）-4, 5，6，7 -四氫0比0定[4，3-c] 0比唑-3 -基}-4-第三丁基-苯曱醯胺；1H-NMR (DMSO-d6) d ppm 1. 3(s);2. 6(m);3. 75(m);3. 9-4. l(2s);4. 3-4. 5(2s); 6·8-7.9(m)。 N-苯基- Ν’ - {3-乙醯胺基-4, 5，6，7 -四氫°比〇定[4，3-c] 口比唑-5 -基}脲；1H-NMR (DMSO-d6) d ppm 2. 0(s)，2. 7(m)， 3.7(m),4.35(s),6.8-7.5(m)。” N-[5-(2-苯基乙醯基）-4, 5，6，7-四氫0比0定[4，3-c]"比〇圭 -3 -基]乙醯胺；1}1-關1?(0讨30-46)(1??1112.0(5)，2.4-2.6(2m)，3.6-3.9(m)，4.3-4.5(2s)，7.15-7.35(m)。 N-{5 -苯續醢基-4，5，6, 7-四氫吼咬[4，3-c] 〇比°坐-3 -基}-乙酿胺；1H-NMR (DMS〇-d6) d ppm 2.0(s)，2.65(m)， 3. 4(m)，4. 0(s)，7. 5-7. 8(m)。 N-[5-(芊基石黃醯基）一4, 5, 6, 7-四氫口比咬[4, 3-c] 口比口坐-3-C:\2D-OODE\91-01\90119473.ptd Page 292 1327569 V. Description of invention (290) 7.4-8.0(m). N- butyl-Ν' - {3-benzoguanamine-4, 5, 6, 7-tetrahydropyridine [4, 3-c] η is 0 _5_ base} pulse; 111_off 1 ^(〇%3〇_(16)(10卩111〇.8(111),1.2_ 1. 4(m), 2. 6(m), 3. 0(m), 3. 6(m) , 4. 2(s), 7. 4-8. 0(m) ° " N-ethyl-Ν' - {3 -benzimidamide-4, 5, 6, 7-tetrahydropyridine [ 4, 3-c] oxazole-5-yl carbazide; 1H-NMR (DMSO-d6) d ppm l(m), 2. 6(m), 3. 0(q), 4. 2(s ), 7. 4-8. 0(m).,, N-{5-(2 - 口夫曱醯曱醯)-4,5, 6, 7-tetrahydro 0 ratio bite [4, 3-c吼〇-3-yl}-4-t-butyl-benzoguanamine; 1H-NMR (DMSO-d6) d ppm 1.3(s); 2.8 (m); 3.9 (m); 4.6 (bs ); 6.5-8·0(m) 〇N-{5-(2-°Sepretinyl)-4, 5,6,7-tetrahydro 0 to 0 [4,3-c] 0 Benzazole-3-yl}-4-t-butyl-benzoguanamine; 1H-NMR (DMSO-d6) d ppm 1. 3(s); 2. 6(m); 3.75(m) ;3. 9-4. l(2s); 4. 3-4. 5(2s); 6·8-7.9(m). N-phenyl- Ν' - {3-acetamido-4, 5,6,7-tetrahydrogen ratio [4,3-c] port-azol-5-yl}urea; 1H-NMR (DMSO-d6) d ppm 2. 0(s), 2. 7 ( m), 3.7 (m), 4.35 (s), 6.8-7.5 (m)." N-[5-(2-phenylethenyl)-4, 5,6,7-tetrahydro 0 Than 0 [4,3-c]"比〇圭-3-yl]acetamide; 1}1-off 1?(0 Discussion 30-46)(1??1112.0(5), 2.4-2.6 (2m), 3.6-3.9(m), 4.3-4.5(2s), 7.15-7.35(m). N-{5-Benzene fluorenyl-4,5,6,7-tetrahydrobite [4, 3-c] 〇 ratio ° sitting -3 -yl}-ethylamine; 1H-NMR (DMS〇-d6) d ppm 2.0(s), 2.65(m), 3. 4(m), 4. 0( s), 7. 5-7. 8(m). N-[5-(芊基石黄醯基)-4, 5, 6, 7-tetrahydro port ratio bite [4, 3-c] mouth than mouth - 3-

C:\2D-C0DE\91-01\90119473.ptd 第293頁 1327569 五、發明說明（291) 基]乙醯胺；1H-NMR (DMS0-d6) d ppm 2. 0(s)，2. 6(m)， 3.4(m)，4.15(s)，4.4(s)，7.35(s)。 N-(5 -苯曱醢基一4，5，6，7-四氫0比0定[4，3-c] 口比〇坐-3-基）乙醯胺；1H-NMR (DMS0-d6) d ppm 1.8-2.0(2bs)， 2.7(bs)，3.4-3.9(2bs)，4.1-4.5(2bs),7.4(bs)。 N-[5-(嗜啉-8-石黃酿基）-4, 5，6，7 -四氫°比°定[4，3-c] °比〇坐 -3 -基]乙醯胺；1H-NMR (DMS0-d6) d ppm 2. 0(s)， 2. 55(m)，3. 7(m), 4. 25(s)，7. 4-9. 0(m)。 N-{5-〇查琳-8-石黃醯基）-4, 5, 6, 7 -四氫°比°定[4，3-c] D比0坐 >3-基}-4-氟苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2. 6(m) ;3. 7(m) ; 4. 3(s) ; 7. 3-9. 0(m)。 N-[5 -苯乙酿基-4，5，6，7-四氫比咬[4，3_c] 〇比°坐-3_基] -4-第三丁基-苯甲醯胺；1H-NMR (DMS0-d6) d ppm 2. 5 -2·7(2m);3.65-3.8(m);4.3-4.5(2s);7.15-8.0(m)。 N_{5-辛基石黃酿基_4，5，6，7_四氫n比〇定[4，3-c] 0比坐-3 -基 }-4-第三丁基-苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.6 (m);3.4(m);4.2(s);4·4(s);7.3_7·9(m)。 N -異丙基-Ν’ - {3-乙醯胺基-4, 5, 6, 7-四氫咄啶[4, 3-c] •吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm 1. 0(d)，1. 95 P(s),2.55(m),3.55(m),3.7(m),4.15(s) N-[5-(曱基石黃醯基）-4, 5，6，7 -四氫0比。定[4，3-c] D比0坐- 3-基]6 醯胺；1H-NMR (DMSO-d6) d ppm 1.95(s)，2.7(m)， 2. 85(s)，3. 4(m)，4. 1 (s)。 N-(5-乙醯基-4, 5, 6,7-四氫0比咬[4,3-c] 0比。坐-3-基）乙C:\2D-C0DE\91-01\90119473.ptd Page 293 1327569 V. Description of the invention (291) Group] acetamamine; 1H-NMR (DMS0-d6) d ppm 2. 0(s), 2. 6(m), 3.4(m), 4.15(s), 4.4(s), 7.35(s). N-(5-phenylhydrazino-4,5,6,7-tetrahydro 0 to 0 [4,3-c] 〇 -3-yl) acetamide; 1H-NMR (DMS0- D6) d ppm 1.8-2.0 (2bs), 2.7 (bs), 3.4-3.9 (2bs), 4.1-4.5 (2bs), 7.4 (bs). N-[5-(Porphyrin-8-Aqueous)-4,5,6,7-tetrahydrogen ratio [4,3-c] ° 〇 -3 -3 -yl] acetamide 1H-NMR (DMS0-d6) d ppm 2. 0(s), 2. 55(m), 3. 7(m), 4. 25(s), 7. 4-9. 0(m). N-{5-〇查琳-8-石黄醯基)-4, 5, 6, 7 -tetrahydrogen ° ° [4,3-c] D ratio 0 sit > 3-based}-4-fluoro Benzoylamine; 1H-NMR (DMS0-d6) d ppm 2. 6 (m); 3. 7 (m); 4. 3 (s); 7. 3-9. 0 (m). N-[5-phenylethylidene-4,5,6,7-tetrahydrogen bite [4,3_c] 〇 ratio ° sitting -3_yl] -4-t-butyl-benzamide; 1H - NMR (DMS0-d6) d ppm 2. 5 -2·7 (2m); 3.65-3.8 (m); 4.3-4.5 (2s); 7.15-8.0 (m). N_{5-octyl sulphate _4,5,6,7_tetrahydron is more specific than [4,3-c] 0 than sitting -3 -yl}-4-t-butyl-benzoquinone Amine; 1H-NMR (DMS0-d6) d ppm 2.6 (m); 3.4 (m); 4.2 (s); 4·4 (s); 7.3_7·9 (m). N-isopropyl-Ν' - {3-acetamido-4, 5, 6, 7-tetrahydroacridine [4, 3-c] • pyrazol-5-yl} urea; 1H-NMR ( DMS0-d6) d ppm 1. 0(d), 1. 95 P(s), 2.55(m), 3.55(m), 3.7(m), 4.15(s) N-[5-(曱基石黄醯基) -4, 5, 6, 7 - tetrahydrogen 0 ratio. [4,3-c] D is 0-position - 3-yl]6 decylamine; 1H-NMR (DMSO-d6) d ppm 1.95 (s), 2.7 (m), 2. 85 (s), 3. 4(m), 4. 1 (s). N-(5-Ethylidene-4, 5, 6,7-tetrahydro 0 is more than bite [4,3-c] 0 ratio. Sit-3-yl) B

C:\2D-C0DE\91-01\90119473.ptd 第294頁 1327569 五、發明說明（292) 醯胺；111-題1^(〇1^〇-(16)(10?1111.9-2.1(25),2.5-2. 7(2m),4.25-4.35(2s)。 N-{5-(2-°塞吩基）乙醢基-4，5，6，7-四氫0比咬[4，3-c] σ坐-3-基}-乙醯胺；1H-NMR (DMS0-d6) d ppm 1.95(s)， 2.6(m),3.75(m),3.9-4.1(2s),4.3-4.5(2s),6.9-7.5(m) o N-(5-苯曱醯基-4，5, 6, 7-四氫0比0定[4，3-c] D比0坐-3-基） -4-氟苯曱醢胺；1H-NMR (DMS0-d6) d ppm 2(bs) ; 3. 3-3.9(2bs);4.3-4.6(2bs);7.2-8.1(m)。 N-[5-(曱基石黃醯基）-4，5，6，7-四氫σ比。定[4，3-c] 0比0坐- 3-基]-4 -第三丁基-苯甲醯胺；1H-NMR (DMS0-d6) d ppm 1.3(s);2.75(m);2.9(s);3.5(m);4.15(s);7.4-7.9(m)。 ^1-(5-(1-蔡魏基）-4，5，6，7-四氫°比〇定[4，3-(：]°比。坐-3-基）-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm 1.2-1.3(2s);2.45-2.9(2bs);3.35(bs);4.4-4.8(m);7.3-8 · 0 ( m) o 1'1-{5-:¥:基石黃醢基-4，5，6，7-四氫11比°定[4，3-(：]吼〇坐-3-基}-4-氟苯曱隨胺；1H-NMR (DMS0-d6) d ppm 2.6(m); 3.4(m);4.2(s);4.4(s);7.15-8.1(m)。 N-[5 -苯乙醯基-4，5，6，7-四氫n比咬[4，3-c] 〇比〇坐-3 -基] -4-氟苯曱醯胺；1H-NMR (DMS0-d6 ) d ppm 2· 5-2. 7(2m); 3.7-3.8(2m);3.85(s);4.35-4.5(2s);7.：l-8.1(m)。 N-[5-(曱基磺醯基）-4,5,6,7-四氫咄啶[4,3-c]吡唑-3-基]-4-苯氧-苯甲醯胺；lH-NMR(DMS0-d6)dppm2.75C:\2D-C0DE\91-01\90119473.ptd Page 294 1327569 V. Description of invention (292) Indoleamine; 111-title 1^(〇1^〇-(16)(10?1111.9-2.1(25) ), 2.5-2. 7(2m), 4.25-4.35(2s). N-{5-(2-°Septyl)ethinyl-4,5,6,7-tetrahydro 0-bit [4 ,3-c] σ--3-yl}-acetamide; 1H-NMR (DMS0-d6) d ppm 1.95(s), 2.6(m), 3.75(m), 3.9-4.1(2s), 4.3 -4.5 (2s), 6.9-7.5 (m) o N-(5-benzoinyl-4,5, 6, 7-tetrahydro 0 to 0 definite [4,3-c] D ratio 0 sitting-3 -yl)-4-fluorophenylguanamine; 1H-NMR (DMS0-d6) d ppm 2 (bs); 3. 3-3.9 (2bs); 4.3-4.6 (2bs); 7.2-8.1 (m). N-[5-(曱基石黄醯基)-4,5,6,7-tetrahydro-sigma ratio. [4,3-c] 0 to 0-spin-3-yl]-4-tert-butyl-benzene Methionine; 1H-NMR (DMS0-d6) d ppm 1.3(s); 2.75(m); 2.9(s); 3.5(m); 4.15(s); 7.4-7.9(m). 5-(1-Caiwei)-4,5,6,7-tetrahydrogen ratio [4,3-(:]° ratio. sit-3-yl)-4-t-butylbenzamide ;1H-NMR (DMS0-d6) d ppm 1.2-1.3 (2s); 2.45-2.9 (2bs); 3.35 (bs); 4.4-4.8 (m); 7.3-8 · 0 (m) o 1'1- {5-:¥: Cornerstone xanthine-4,5,6,7-tetrahydro 11 ratio [4,3-(:] 吼〇-3-yl}-4-fluorophenylhydrazine with amine; 1 H-NMR (DMS0-d6) d ppm 2.6 (m); 3.4 (m); 4.2 (s); 4.4 (s); 7.15-8.1 (m). N-[5-phenethinyl-4,5 ,6,7-tetrahydron ratio bite [4,3-c] 〇〇 -3 -3 -yl]-4-fluorobenzamine; 1H-NMR (DMS0-d6 ) d ppm 2· 5-2 7(2m); 3.7-3.8(2m); 3.85(s); 4.35-4.5(2s); 7.:l-8.1(m). N-[5-(indolylsulfonyl)-4, 5,6,7-tetrahydroacridine [4,3-c]pyrazol-3-yl]-4-phenoxy-benzamide; lH-NMR (DMS0-d6)dppm 2.75

C:\2D-00DE\91-01\90119473.ptd 第295頁 1327569 五、發明說明（293) (m);2.9(s);3.5(m);4.15(s);7.0-7.8(m)。 N-[5-(曱基讀酿基）_4, 5, 6, 7-四氫11比咬[4, 3-c] 口比嗅- 3-基]一3-曱氧-苯甲醯胺；1H-NMR (DMS0-d6) d ppm 2.75 (m);2.9(s);3.5(m);3.8(s);4.2(s);7.1-7.6(m) ° N_{5_( u奎琳-8-磺醯基）_4, 5, 6, 7 -四氫吡"定[4, 3-c] D比唑 _3-基}-4-苯氧-苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.6 (m);3_ 7(m);4.3(s);7.0-9.0(m)。 ?^-{5-(喳啉-8-磺醯基）-4,5,6,7-四氫吡啶[4,3-(：]吡唑 -3_ 基卜3_ 甲氧-苯曱醯胺；1H-NMR (DMS0-d6) d ppm j|^.6(m);3.7(m);3.8(s);4.3(s);7.0-9.0(m) » N -苯基-N，- {3 -苯甲醯胺基-4, 5, 6, 7-四氫吡啶[4, 3-c] 吡唑-5-基}脲；1H-NMR (DMS0-d6) d ppm 2.7(m)，3.7 (m )，4. 4 ( s )，6 · 9 - 8. 0 ( m )，8. 6 ( s ) o N-[5-(甲基石黃酿基）-4，5，6，7-四氫0比咬[4，3-c]°比0坐_3_ 基]-苯基乙醯胺；1H-NMR (DMS0-d6) d ppm 2.65(t，2H)， 2.85(s,3H),3.40(t,2H),3.80(s,2H),4.10(s,2H),7.20-7.40(m，5H)。 N_{5-[2-(2-°塞吩基）乙酿基]-4，5，6, 7-四氫0比唆 •[4, 3-c]吡唑-3 -基}苯曱醯胺；1H-NMR (DMSO-d6) d ppm 2.6(m)，3.77(m)，3.9-4.1(2s)，4.4-4.5(2s)，6.9-8.0(m) ο N-{5-( e奎琳-8-續醯基）-4，5，6，7 -四氫°比咬[4，3-c] p比口坐 _3-基}-苯甲酿胺；1H-NMR (DMS0-d6) d ppm 2.6(m)， 3. 75(m)，4. 35(s)，7·4-9.0(m)。C:\2D-00DE\91-01\90119473.ptd Page 295 1327569 V. Description of invention (293) (m); 2.9(s); 3.5(m); 4.15(s); 7.0-7.8(m) . N-[5-(曱-reading) _4, 5, 6, 7-tetrahydro 11 ratio bite [4, 3-c] than olfactory 3-yl]- 3-oxo-benzamide ;1H-NMR (DMS0-d6) d ppm 2.75 (m); 2.9(s); 3.5(m); 3.8(s); 4.2(s);7.1-7.6(m) ° N_{5_( u 奎琳-8-sulfonyl)_4, 5, 6, 7-tetrahydropyridyl "[4,3-c] D-pyrazole-3-yl}-4-phenoxy-benzoguanamine; 1H-NMR (DMS0-d6) d ppm 2.6 (m); 3-7 (m); 4.3 (s); 7.0-9.0 (m). ?^-{5-(Porphyrin-8-sulfonyl)-4,5,6,7-tetrahydropyridine [4,3-(:]pyrazole-3_ylbu-3_methoxy-benzoguanamine ;1H-NMR (DMS0-d6) d ppm j|^.6(m); 3.7(m); 3.8(s); 4.3(s); 7.0-9.0(m) » N-phenyl-N,- {3-Benzylamino-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-5-yl}urea; 1H-NMR (DMS0-d6) d ppm 2.7(m) , 3.7 (m ), 4. 4 ( s ), 6 · 9 - 8. 0 ( m ), 8. 6 ( s ) o N-[5-(methyl scutellaria)-4,5,6 , 7-tetrahydro 0 ratio bite [4,3-c] ° ratio 0 sitting _3_ ki]-phenyl acetamidine; 1H-NMR (DMS0-d6) d ppm 2.65 (t, 2H), 2.85 (s , 3H), 3.40 (t, 2H), 3.80 (s, 2H), 4.10 (s, 2H), 7.20-7.40 (m, 5H). N_{5-[2-(2-°Septyl)B -4,5,6,7-tetrahydro 0 唆•[4,3-c]pyrazol-3-yl}benzoguanamine; 1H-NMR (DMSO-d6) d ppm 2.6 (m ), 3.77 (m), 3.9-4.1 (2s), 4.4-4.5 (2s), 6.9-8.0 (m) ο N-{5-( e 奎琳-8- continued 醯)-4,5,6 , 7-tetrahydrogen ratio bite [4,3-c] p than mouth _3-yl}-benzamide; 1H-NMR (DMS0-d6) d ppm 2.6(m), 3. 75(m ), 4. 35(s), 7·4-9.0(m).

C:\2D-00DE\91-01\90119473_ptd 第 296 頁 1327569 五、發明說明（294) N-[5-(曱基石黃酿基）- 4，5，6，7_四氫0比口定[4，3-c]d比〇坐-3-基]-3-氟-苯甲醯胺；1H-NMR (DMS0-d6) d ppm 2.8(m)， 2.9(s)，3.45(m)，4.2(s)，7.35-7.9(m)。 1'}-[5-(:¥:基石黃醯基）_4，5，6，7-四氫0比咬[4，3-(：]0比〇坐-3-基]-3-氟苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.6(m)， 3. 4(m)，4. 2(s)，4. 4(s)，7. 3-7. 9(m)。 N-[5 -苯乙酿基-4，5，6，7-四氫D比咬[4，3-c] °比。坐-3_基] -3-氟苯甲醯胺；1H-NMR (DMS0-d6) d ppm 2.5-2.65(2m) ，3.75-3.85(2m)，4.35-4.6(2s)，7.15-7.95(m)。 N_(5-乙醯基-4，5，6，7 -四氫 °比口定[4，3_c] 口比〇坐 _3_ 基）_3 — 氟苯甲醯胺；1H-NMR (DMS0-d6) d ppm 2.0-2. l(2s)， 2.6-2.8(2m)，3.6-3.8(2m)，4.3-4.4(2s)，7.4-7.9(m)。 -3-氟苯甲醯胺；1H-NMR (DMSO-d6) d ppm 2.75(bs)， 3.5-3.9(2bs)，4.3-4.6(2bs)，7.3-7.9(m)。 N-{5 -苯續醯基-4，5，6, 7 -四氫D比咬[4, 3-c] n比。坐-3-基} -3-氟苯曱醯胺；1H-NMR (DMSO-d6) d ppm 2. 65(m)， 3. 4(m)，4· 1 (s)，7. 4-7· 9(m)。 N-異丙基-Ν’ - {3-(3-氟苯曱醯胺基）-4,5，6, 7-四氫咄啶 [4, 3-c]ub 唑-5 -基丨脲；1H-NMR (DMSO-d6) d ppm 1. 0(d) ，2.6(m)，3.6(m)，3.7(m)，4.2(s)，6.2(d)，7_4_7.9(m) 〇，， N-{5-苯乙醯基-4，5，6，7-四氫D比咬[4，3-c] 0比0坐-3-基} -3 -苯氧苯曱醯胺；1H-NMR (DMSO-d6) d ppm 2· 6(m); 3.4(m);4. 0(s) ; 7. 0-7.8(m)。C:\2D-00DE\91-01\90119473_ptd Page 296 1327569 V. INSTRUCTIONS (294) N-[5-(曱基石黄酒)-4,5,6,7_tetrahydro 0 ratio [4,3-c]d is more than -3-yl]-3-fluoro-benzamide; 1H-NMR (DMS0-d6) d ppm 2.8 (m), 2.9 (s), 3.45 (m) , 4.2 (s), 7.35-7.9 (m). 1'}-[5-(:¥:基石黄醯基)_4,5,6,7-tetrahydro 0 ratio bite [4,3-(:]0 than 〇-3-yl]-3-fluorophenylhydrazine ( ;; 1H-NMR (DMS0-d6) d ppm 2.6 (m), 3. 4 (m), 4. 2 (s), 4. 4 (s), 7. 3-7. 9 (m). N-[5-phenylethylidene-4,5,6,7-tetrahydro D ratio bite [4,3-c] °. sit -3_yl]-3-fluorobenzamide; 1H- NMR (DMS0-d6) d ppm 2.5-2.65 (2m), 3.75-3.85 (2m), 4.35-4.6 (2s), 7.15-7.95(m). N_(5-Ethyl-4,5,6, 7-tetrahydrogen ratio [4,3_c] 〇 _3_ base)_3 — fluorobenzamide; 1H-NMR (DMS0-d6) d ppm 2.0-2. l(2s), 2.6- 2.8 (2m), 3.6-3.8 (2m), 4.3-4.4 (2s), 7.4-7.9 (m). 3-fluorobenzamide; 1H-NMR (DMSO-d6) d ppm 2.75 (bs), 3.5-3.9(2bs), 4.3-4.6(2bs), 7.3-7.9(m). N-{5-Benzene fluorenyl-4,5,6,7-tetrahydro D ratio bite [4, 3-c n ratio. sit-3-yl}-3-fluorobenzamide; 1H-NMR (DMSO-d6) d ppm 2. 65(m), 3. 4(m), 4· 1 (s), 7. 4-7· 9(m). N-Isopropyl-Ν' - {3-(3-fluorophenylguanidino)-4,5,6,7-tetrahydroacridine [4, 3 -c]ubazol-5-yl carbazide; 1H-NMR (DMSO-d6) d ppm 1. 0(d), 2.6(m), 3.6(m), 3.7(m) 4.2(s), 6.2(d), 7_4_7.9(m) 〇,, N-{5-phenethyl fluorenyl-4,5,6,7-tetrahydro D ratio bite [4,3-c] 0 0-0 phenoxybenzamine; 1H-NMR (DMSO-d6) d ppm 2·6(m); 3.4(m); 4. 0(s) ; 7. 0 -7.8 (m).

C:\2D-G0DE\91-01\90119473.ptd 第297頁 1327569 五、發明說明（295) N-(5 -苯曱醢基-4，5, 6，7 -四氫0比咬[4，3-c] 口比0坐-3-基） -3-苯氧苯甲醯胺；1H-NMR (DMS0-d6) d ppm 2.7(bs); 3.5(bs);4·15-4.25(2bs);7.0-7.9(m)。 N-{ 5-辛基磺醯基-4, 5, 6, 7 -四氫吡啶[4, 3-c]吡唑-3-基}-3 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.6(m); 3.4(m);4.l(s);4.4(s);7.0-7·8(m)。卜（5-(1-萘羰基）-4,5,6,7-四氫吡啶[4,3-〇]吼唑-3-基）-3 -苯氧苯曱醯胺；111-關1?(0^150-(16)(1??11]2.5-2.9(2bs);4.0-4.2(2bs);4.5-4.9(2bs);6.9-8.0(m)。 N-[5-苯乙醯基-4，5，6，7-四氫0比。定[4，3-c] 〇比0坐-3-基] -3-苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.4-2.7(2n〇;3.6-3.8(2m);4.3-4.5(2s);7.0-7.8(m)。 ^{5-(2-°塞吩基）乙醢基-4，5，6，7-四氫11比。定[4，3-(：] 唑-3-基}-3 -苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2.6(m);3.75(m);3.9-4.1(2s);4.3-4.5(2s);6.8-7.8(in)C:\2D-G0DE\91-01\90119473.ptd Page 297 1327569 V. INSTRUCTIONS (295) N-(5-Benzenzyl-4,5, 6,7-tetrahydro 0-bit [4] , 3-c] -3-yloxy-3-mercaptoamine; 1H-NMR (DMS0-d6) d ppm 2.7(bs); 3.5(bs);4·15-4.25( 2bs); 7.0-7.9(m). N-{ 5-octylsulfonyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-3-phenoxybenzamine; 1H-NMR ( DMS0-d6) d ppm 2.6(m); 3.4(m); 4.l(s); 4.4(s); 7.0-7·8(m). Bu(5-(1-naphthalenecarbonyl)-4,5,6,7-tetrahydropyridine[4,3-indolyl]oxazol-3-yl)-3-phenoxybenzamide; 111-off 1 (0^150-(16)(1??11)2.5-2.9(2bs); 4.0-4.2(2bs); 4.5-4.9(2bs);6.9-8.0(m). N-[5-phenylethyl醯-4,5,6,7-tetrahydro 0 ratio. [4,3-c] 〇 is 0 -3-yl] -3-phenoxybenzamine; 1H-NMR (DMS0-d6 d ppm 2.4-2.7 (2n〇; 3.6-3.8 (2m); 4.3-4.5(2s); 7.0-7.8(m). ^{5-(2-°Septyl)ethinyl-4,5 ,6,7-tetrahydro-11 ratio. [4,3-(:]oxazol-3-yl}-3-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm 2.6 (m); 3.75(m); 3.9-4.1(2s); 4.3-4.5(2s); 6.8-7.8(in)

O N-{5-( 0 奎 pf 琳-2-獄基）-4, 5, 6, 7 -四氫0比0定[4, 3-c] 0 比0坐 -3-基}-4-第三丁基苯曱醯胺；1H-NMR (DMS0-d6) d ppm N-{5-( °奎 1 琳-2 -幾基）-4，5，6，7 -四氫 D比咬[4，3-c] °比〇坐 -3-基}-3-苯氧苯曱醯胺；1H-NMR (DMS0-d6) d ppm 2. 8 (m);3.7-4.05(2m);4.5-4.7(2s);6.9-8.2(m)。 N -苯基-Ν’ - {3-(3 -苯氧-苯曱醯胺）基-4, 5, 6, 7-四氫口比口定[4，3-。]°比°坐-5-基}脲；111-關1^(0材80-(16)(1卩口111O N-{5-( 0 奎 pf 琳-2- prison)-4, 5, 6, 7 -tetrahydro 0 to 0 determinate [4, 3-c] 0 to 0 -3-yl}-4 - tert-butylbenzamide; 1H-NMR (DMS0-d6) d ppm N-{5-( ° Kui 1 Lin-2 -methyl)-4,5,6,7-tetrahydro D ratio bite [4,3-c] ° 〇-3-yl}-3-phenoxybenzamine; 1H-NMR (DMS0-d6) d ppm 2. 8 (m); 3.7-4.05 (2m); 4.5-4.7 (2s); 6.9-8.2 (m). N-phenyl-indole-{3-(3-phenoxy-benzoguanamine)--4, 5, 6, 7-tetrahydro port ratio [4,3-. ]°°°S-5-based urea; 111-off 1^(0 material 80-(16)(1卩口111

C:\2D-00DE\91-01\90119473.ptd 第298頁 1327569 五、發明說明（296) 2.7(m)；3.7(m);4.35(s)；6.8-7.8(m) N-(5 -苯曱酿基-4, 5, 6, 7 -四氫0比〇定[4, 3-c] π比0坐-3-基）_ 苯乙醯胺；1H-NMR (DMS0-d6) d ppm 2.70(t，2H)，3.58 (s，2H)，3.60(t，2H)，4.20(s，2H)，7.20-7.50(m，10H)。 N_(5 -苯乙 Si 基-4，5，6, 7 -四氫0比咬[4，3-c] 0比0坐-3 -基）_ 苯乙醯胺；1H-NMR (DMS0-d6) d ppm 2.60(t，2H)，3.60 (s,2H),3.70(t,2H),3.80(s,2H),4.30(s,2H),7.08-7.40( m， 10H)。 1(5-胺基幾基-4,5，6，7-四氫"比咬[4，3-(：]'1比°坐-3-基）-苯乙醯胺；1H-NMR (DMS0-d6) d ppm 2.58(t，2H)，3.50 (t，2H)，3.60(s，2H)，4.15(s，2H)，5.90(s，2H)，7.15-7.35( m，5H)，10_15(bs，lH)，12.10(bs，lH)。 N- 丁基-Ν’ - {3 -苯乙醯胺基-4, 5, 6, 7-四氫咄啶[4,3-c] n比0坐-5 -基}脈； 0.80(t，3H), 1.18-1. 28(m，2H)，1.30-1.4〇(m，2H)，2.55( t,2H),3.00(t,2H),3.50(t,2H),3.60(s,2H),4.15(s,2H), 6.45(bs，lH)，7.20-7.45(m，5H)，10.22(bs，lH) ο11 Ν-乙基- Ν’ - {3 -苯乙醢胺基-4, 5, 6, 7-四氫咄啶[4, 3-c] 口比0坐-5-基}脲；1H-NMR (DMS0-d6) d ppm l(d)，1.00 (t,3H),2.80(t,2H),2.95-3.05(m,2H),3.50(t,2H),3.60( sJ2H),4.20(s,2H),6.50(bs,lH),7.20-7.35(m,5H),10.35 (s，lH)〇 " N-苯基- Ν’ - {3 -苯乙酿胺基-4，5，6，7-四氫"比咬[4，3-c] 〇比0坐-5 -基}脈；C:\2D-00DE\91-01\90119473.ptd Page 298 1327569 V. INSTRUCTIONS (296) 2.7(m); 3.7(m); 4.35(s); 6.8-7.8(m) N-(5 -Benzene-based 4-, 5, 6, 7-tetrahydro 0-pyrene [4, 3-c] π ratio 0--3-yl) phenethylamine; 1H-NMR (DMS0-d6) d ppm 2.70 (t, 2H), 3.58 (s, 2H), 3.60 (t, 2H), 4.20 (s, 2H), 7.20-7.50 (m, 10H). N_(5-phenethyl Si-4,5,6,7-tetrahydro 0-bite [4,3-c] 0 to 0-spin-3-yl)_ phenethylamine; 1H-NMR (DMS0- D6) d ppm 2.60 (t, 2H), 3.60 (s, 2H), 3.70 (t, 2H), 3.80 (s, 2H), 4.30 (s, 2H), 7.08-7.40 (m, 10H). 1(5-Amino-based-4,5,6,7-tetrahydro" than biting [4,3-(:]'1°°-3-yl)-phenethylamine; 1H-NMR (DMS0-d6) d ppm 2.58(t,2H), 3.50 (t,2H), 3.60(s,2H), 4.15(s,2H), 5.90(s,2H),7.15-7.35( m,5H) , 10_15(bs, lH), 12.10(bs, lH). N- butyl-Ν' - {3 - phenethylamino-4, 5, 6, 7-tetrahydroacridine [4,3-c n is 0 to 0 - base} pulse; 0.80 (t, 3H), 1.18-1. 28 (m, 2H), 1.30 - 10.4 〇 (m, 2H), 2.55 (t, 2H), 3.00 (t , 2H), 3.50 (t, 2H), 3.60 (s, 2H), 4.15 (s, 2H), 6.45 (bs, lH), 7.20-7.45 (m, 5H), 10.22 (bs, lH) ο11 Ν- Ethyl- Ν' - {3 - phenethylamino-4, 5, 6, 7-tetrahydroacridine [4, 3-c] valence ratio 0--5-yl} urea; 1H-NMR (DMS0 -d6) d ppm l(d), 1.00 (t, 3H), 2.80 (t, 2H), 2.95-3.05 (m, 2H), 3.50 (t, 2H), 3.60 (sJ2H), 4.20 (s, 2H) ), 6.50 (bs, lH), 7.20-7.35 (m, 5H), 10.35 (s, lH) 〇 " N-phenyl- Ν' - {3 - phenylethylamino-4, 5, 6, 7-tetrahydro" than bite [4,3-c] 〇 is more than 0 sitting -5 - base} pulse;

C: \2D-00DE\91-01\90119473.ptd 第299頁 1327569 五、發明說明（297) 2.65(t,2H),3.60(s,2H),3.65(t,2H),4.35(s,2H),6.90 (t，lH)，7.15-7.40(m，9H)，8.60(s,lH)，10.25(s，lH)。" N -苄基-Ν’ -{3 -苯乙醯胺基-4, 5, 6, 7-四氫吡啶[4, 3-c] 吡唑-5 -基}脲；1H-NMR (DMS0-d6) d ppm 1(d)，2. 60 (t, 2H), 3. 60(t, 2H), 3. 70(s, 2H), 4. 18-4. 2 2(m, 4H), 7. 10( bs, 1H)，7. 15-7. 25(m，10H)，10. 20(bs, 1H)。" N-乙基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7 -四氫吡啶 [4, 3-c]吡唑-5-基}脲； 0.95(t,3H),2.65(t,2H),2.95-3.05(m,2H),3.50(t,2H) #, 3.80(s,2H),4.15(s,2H),6.45(t,lH),7.40-7.50(m,3H), 7.80-7· 90(m，4H)。" N —(5-(2-曱氧苯曱醢基）一4, 5, 6, 7-四氫口比咬[4, 3-c]"比唑-3-基）-(2 -萘）乙醯胺 2.55-2.65(m，2H)，3.40(t，2H)， 3.50-3.60(m，2H)，3.75(s’2H),4.00-4.45(m，2H)，6.80-7. 20(m，3H)，7. 25-7. 55(m，4H),7.65-7. 90(m，4H)。 N -苯基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7-四氫吡啶 [4，3-。]°比°坐-5-基}服；1H-NMR (DMS0-d6) d ppml(d) 2_68(t，2H)，3.65(t，2H)，3.80(s，2H)，4.35(s，2H)，6.90(t (^lH),7.25-7.32(m,2H)>7.35-7.50(m,5H),7.80(s,lH), 7. 85-7. 90 (m，4H), 8. 60(s, 1H)。" N-[5-苯甲酿基-4, 5，6，7-四氫0比咬[4，3_c] 0比0坐-3 -基] -(2-萘）乙醯胺 2.65(t，2H)，3.65(bs，2H ),3.75( bs，2H)， 7.30-7.50(m，8H)，7.7〇-7.90(in，4H)。 N-(5_苯乙酿基-4，5，6，7-四氫”比〇定[4，3-c] 0比°坐-3 -基）C: \2D-00DE\91-01\90119473.ptd Page 299 1327569 V. Description of invention (297) 2.65(t, 2H), 3.60(s, 2H), 3.65(t, 2H), 4.35(s, 2H), 6.90 (t, lH), 7.15-7.40 (m, 9H), 8.60 (s, lH), 10.25 (s, lH). "N-benzyl-Ν'-{3-phenethylamino-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-5-yl}urea; 1H-NMR ( DMS0-d6) d ppm 1(d), 2. 60 (t, 2H), 3. 60(t, 2H), 3. 70(s, 2H), 4. 18-4. 2 2(m, 4H ), 7. 10( bs, 1H), 7. 15-7. 25(m,10H), 10. 20(bs, 1H). " N-ethyl-Ν' - {3-(2-naphthyl)acetamido-4,5,6,7-tetrahydropyridine [4,3-c]pyrazol-5-yl}urea; 0.95(t,3H), 2.65(t,2H), 2.95-3.05(m,2H),3.50(t,2H) #, 3.80(s,2H),4.15(s,2H),6.45(t,lH ), 7.40-7.50 (m, 3H), 7.80-7·90 (m, 4H). " N —(5-(2-曱-Phenoxyphenyl)- 4, 5, 6, 7-tetrahydro-port ratio [4, 3-c]"Bizozol-3-yl)-(2 -naphthalene) acetamamine 2.55-2.65 (m, 2H), 3.40 (t, 2H), 3.50-3.60 (m, 2H), 3.75 (s'2H), 4.00-4.45 (m, 2H), 6.80-7 20 (m, 3H), 7. 25-7. 55 (m, 4H), 7.65-7. 90 (m, 4H). N-phenyl-indole-{3-(2-naphthyl)acetamido-4,5,6,7-tetrahydropyridine [4,3-. ° ° ° ° -5 - base} service; 1H-NMR (DMS0-d6) d ppml (d) 2_68 (t, 2H), 3.65 (t, 2H), 3.80 (s, 2H), 4.35 (s, 2H), 6.90 (t (^lH), 7.25-7.32 (m, 2H)> 7.35-7.50 (m, 5H), 7.80 (s, lH), 7. 85-7. 90 (m, 4H), 8. 60(s, 1H)." N-[5-Benzyl alcohol-4, 5,6,7-tetrahydro 0 ratio bite [4,3_c] 0 to 0 sitting -3 - base] -( 2-naphthyl)acetamide 2.65 (t, 2H), 3.65 (bs, 2H), 3.75 (bs, 2H), 7.30-7.50 (m, 8H), 7.7 〇 - 7.90 (in, 4H). 5_phenylethyl 4,5,6,7-tetrahydro" is more than [4,3-c] 0 ratio ° sitting -3 - base)

C:\2D-C0DE\91-01\90119473.ptd 第300頁 1327569 五 '發明說明（298) -(2-萘）乙醯胺 2.58(t，2H)，3.65(t，2H)，3.70-3.80 (m,4H),4.30-4.40(m,2H),7.02-7. 30(m,5H),7.40-7.52 (m, 3H)，7. 80-7. 90(m，4H)。 N-(5-乙酿基-4，5，6, 7-四氫〇比咬[4，3-c] 〇比口坐-3 -基） -（2-萘）乙醯胺2.05(8,31〇,2.55-2.70(111，211)，3.60-3.70 (m，2H)，3.80(s，2H)，4.25-4.35(m，2H)，7.40-7.5〇(m，3H)， 7· 80 -7. 9 0 (m，4H)。 N- 丁基-Ν’- {3-(2 -萘）乙醯胺基-4, 5, 6, 7-四氫《比啶 [4，3-c].Bite坐-5-基}脈；1H-NMR (DMS〇-d6) d.ppml(d) 0· 83 (t，3H)，1.18-1. 28(m，2H)，1. 30-1. 40(m，2H)，2. 55(t， 2H)，2.90-3.00(m，2H)，3.50(t，2H)，3.78(s，2H)，4.15(s，2 H)，6.40(t，lH)，7.40_7.50(m，3H)，7.80-7-90(m，4H)。" N-苄基-Ν’-{3-(2 -萘）乙醯胺基-4, 5, 6, 7-四氫吡啶 [4, 3-c] »比唑-5 -基}脲；1H-NMR (DMSO-d6) d ppml(d) 2.60(t，2H)，3.55(t，2H)，3.75(s，2H)，4.15-4.25(m，4H)， 7.08(t，lH)，7.12-7.28(m，5H),7.40-7.50(m，3H)，7.80-7· 90(m，4H)。" 1'1-(5-(2-〇夫喃曱酿基）-4,5,6,7-四氫0比咬[4,3_〇]'»比口坐 -3 -基）-(2 -萘）乙醯胺 2.75(bs，2H)，3.75(bs，2H)，3.80 (bs，2H)，4.50(bs，2H)，6.55(bs，lH)，6.95(bs，lH),7.40-7. 55(m，3H ),7.70( bs,lH), 7.80-7.90( m, 4H )。 N-(5-乙醢基-4，5，6，7-四氫口比咬[4，3-c] 0 比。坐-3-基）-3-甲基丁醯胺 0· 88 (s，3H)，0.90(s，3H)，2.00-2.10( m,4H)， 2.15(d,2H),2.60-2.70(m,2H),3.60-3.70(m,2H),4.25-C:\2D-C0DE\91-01\90119473.ptd Page 300 1327569 V' invention description (298) -(2-naphthalene)acetamide 2.58(t,2H), 3.65(t,2H), 3.70- 3.80 (m, 4H), 4.30-4.40 (m, 2H), 7.02-7. 30 (m, 5H), 7.40-7.52 (m, 3H), 7. 80-7. 90 (m, 4H). N-(5-ethyl-branched-4,5,6,7-tetrahydroindole ratio bite [4,3-c] 〇 is more than -3 -yl) -(2-naphthalene)acetamidamine 2.05 (8 , 31〇, 2.55-2.70(111,211), 3.60-3.70 (m,2H), 3.80(s,2H), 4.25-4.35(m,2H), 7.40-7.5〇(m,3H), 7· 80 -7. 9 0 (m, 4H). N- butyl-Ν'- {3-(2-naphthyl)acetamido-4, 5, 6, 7-tetrahydro"pyridyl[4,3 -c].Bite sits -5-base} pulse; 1H-NMR (DMS〇-d6) d.ppml(d) 0· 83 (t,3H), 1.18-1. 28(m,2H),1. 30-1. 40 (m, 2H), 2. 55 (t, 2H), 2.90-3.00 (m, 2H), 3.50 (t, 2H), 3.78 (s, 2H), 4.15 (s, 2 H) , 6.40 (t, lH), 7.40_7.50 (m, 3H), 7.80-7-90 (m, 4H). " N-benzyl-Ν'-{3-(2-naphthyl)acetamide 4-, 5, 6, 7-tetrahydropyridine [4, 3-c] » bisazol-5-yl} urea; 1H-NMR (DMSO-d6) d ppml (d) 2.60 (t, 2H), 3.55(t,2H), 3.75(s,2H), 4.15-4.25(m,4H), 7.08(t,lH),7.12-7.28(m,5H), 7.40-7.50(m,3H), 7.80- 7·90(m,4H)." 1'1-(5-(2-〇夫喃曱基)-4,5,6,7-tetrahydro 0 ratio bite [4,3_〇]' »The ratio of -3 -yl)-(2-naphthyl)acetamide 2.75 (bs, 2H), 3.75 (bs, 2H), 3.80 (bs, 2H), 4.50 (bs, 2H), 6.55 (bs, lH), 6.95 (bs, lH), 7.40-7. 55 (m, 3H), 7.70 (bs, lH), 7.80-7.90 (m, 4H). (5-Ethyl-4,5,6,7-tetrahydrol port ratio bite [4,3-c] 0 ratio. Sodium-3-yl)-3-methylbutyramine 0·88 (s, 3H), 0.90 (s, 3H), 2.00-2.10 (m, 4H), 2.15 (d, 2H), 2.60-2.70 (m, 2H), 3.60-3.70 (m, 2H), 4.25-

C:\2D-CDDE\91-01\901l9473.ptd 第301頁 1327569 五、發明說明（299) 4. 35(m，2H)。 N_(5 -苯曱酿基-4，5，6，7-四氫0比0定[4，3_c] 〇比0坐-3_基） _3_ 甲基丁酿胺0. 90_0. 95(m，6H)，2. 00_2. 20(m，3H)， 2.70(bs，2H)，3.50-3.90(m，2H)，4.20-4.50(m，2H)，7.30-7. 50(m，5H)。 N-(5-苯乙酿基-4，5，6，7-四氮π比咬[4，3_c] π比0坐_3 -基） -3-甲基丁醯胺0.85-0.95(m，6H)，1.9 5-2.10(m，lH)， 2.15(d,2H),2.85(t,2H),3.70(t,2H),3.80(s,2H),4.35 (s’ 2H),7. 15-7.30(m,5H)。 • N-(5-(2-0夫0南曱酿基）-4, 5, 6, 7-四氫口比咬[4, 3-c] 口比口坐 -3 -基）-3-曱基丁醯胺 0.85-0.95(m，6H)，1.95-2. 05 (m，lH)，2.15(d，2H)，2.75(bs，2H)，3.80(t，2H)，4.50(bs，2 H)，6.58-6.62(m，lH)，6.98(bs，lH)，7.80(bs，lH)。 N -異丙基-Ν’ - {3-(3-曱基-丁醯胺基）-4,5,6,7-四氫吡咬[4,3-c]°比。坐-5-基}脈； 1H-NMR (DMSO-d6) d ppm 1(d) 0.90(s,3H),0.95 (s，3H)，1.02(s，3H)，1.04(s，3H)，2.00-2.10(m，lH)， 2. 15(d, 2H), 2. 65(t, 2H), 3. 6 0(t, 2H), 3. 6 2-3. 7 5(m, 1H), 4. 15(s, 2H), 6. 15(d，1H)。·· _ N-苄基-Ν’ - {3-(3-曱基-丁醯胺基）-4,5,6,7 -四氫吡啶 [4，3 - c ]"比峻-5 -基}脲； 1H-NMR (DMSO-d6) d ppml(d) 0.88(s,3H ) , 0. 90 (s, 3H), 1. 95-2. 10(m, 1H), 2. 15(d, 2H), 2. 60(t, 2H), 3.60(t,2H),4.20-4.28(m,4H),7.10(t,lH),7.15-7.30(m,C:\2D-CDDE\91-01\901l9473.ptd Page 301 1327569 V. Description of invention (299) 4. 35 (m, 2H). N_(5-benzoquinone-4,5,6,7-tetrahydro 0 to 0 is determined [4,3_c] 〇 is 0--3 yl) _3_ methyl butylamine 0. 90_0. 95(m , 6H), 2. 00_2. 20 (m, 3H), 2.70 (bs, 2H), 3.50-3.90 (m, 2H), 4.20-4.50 (m, 2H), 7.30-7. 50 (m, 5H) . N-(5-phenylethyl 4,5,6,7-tetrazine π ratio [4,3_c] π ratio 0 sitting _3 -yl) -3-methylbutanamine 0.85-0.95 (m , 6H), 1.9 5-2.10 (m, lH), 2.15 (d, 2H), 2.85 (t, 2H), 3.70 (t, 2H), 3.80 (s, 2H), 4.35 (s' 2H), 7 15-7.30 (m, 5H). • N-(5-(2-0) 0, 5, 6, 7-tetrahydrogen port bite [4, 3-c] mouth than mouth -3 - base)-3- Indolinamide 0.85-0.95 (m, 6H), 1.95-2. 05 (m, lH), 2.15 (d, 2H), 2.75 (bs, 2H), 3.80 (t, 2H), 4.50 (bs, 2 H), 6.58-6.62 (m, lH), 6.98 (bs, lH), 7.80 (bs, lH). N-isopropyl-indole-{3-(3-mercapto-butylammonium)-4,5,6,7-tetrahydropyridyl [4,3-c]° ratio. Sit-5-based pulse; 1H-NMR (DMSO-d6) d ppm 1(d) 0.90 (s, 3H), 0.95 (s, 3H), 1.02 (s, 3H), 1.04 (s, 3H), 2.00-2.10(m,lH), 2. 15(d, 2H), 2. 65(t, 2H), 3. 6 0(t, 2H), 3. 6 2-3. 7 5(m, 1H ), 4. 15(s, 2H), 6. 15(d, 1H). ··_ N-Benzyl-Ν' - {3-(3-indolyl-butyrylamino)-4,5,6,7-tetrahydropyridine [4,3 - c ]"比峻-5 -1) urea; 1H-NMR (DMSO-d6) d ppml(d) 0.88(s,3H), 0. 90 (s, 3H), 1. 95-2. 10(m, 1H), 2. 15 (d, 2H), 2. 60(t, 2H), 3.60(t, 2H), 4.20-4.28(m, 4H), 7.10(t, lH), 7.15-7.30(m,

C:\2D-CODE\91-01\90119473.ptd 第 302 頁 1327569 五、發明說明（300) 5H)。" N- 丁基-Ν’ - {3-(3-曱基-丁醯胺基）-4, 5, 6, 7-四氫咄啶 [4，3 - c ]"比 °坐-5 -基}脲； 0.85(t,3H),0.88(s,3H),0.90(s,3H),1.20-1.30(m,2H) ,1.32-1.40(m,2H),1.95-2.10(m,lH),2.15(d,2H),2.55(t ,2H),2.95-3.02(m,2H),3.55(t,2H),4.15(s,2H),6.45(t, 1 Η" Ν-苯基-Ν’ - {3-(3-曱基-丁醯胺基）-4,5, 6, 7-四氫吡啶 [4，3-〇]°比°坐-5-基}脈； 0.90-0.95(m，6H)，2.00_2.10(m，lH)，2.15(d，2H)，2.65( t，2H)，3.65(t，2H)，4.25(s，2H)，6.85(t，lH)，7.15-7.22(m ，2H)，7.28-7.32(m，2H),8.60(s，lH)。" N-乙基-N’-{3-(3-曱基-丁醯胺基）-4,5,6,7-四氫吡啶 [4，3 - c ] β 比 °坐-5 -基}脲； 0.88-0.90(m,6H),1.00(t,3H),1.95-2.10(m,lH),2.15( d,2H),2.58(t,2H),2.95-3.08(m,2H),3.55(t,2H),4.15(s ，2H), 6. 45(t，1H)。" N-乙基-N’-{3-(4-苯基）苯乙醯胺基）-4,5,6,7-四氫吡 ? [4,3-c]吼唑-5-基}脲； 0.95(t,3H),2.58(t,2H),2.95-3.05(m,2H),3.50(t,2H) ,3.65(s,2H),4.15(s,2H),6.45(t,lH),7.30-7.50(m,4H), 7. 55-7. 65 (m, 3H) » " N-異丙基-Ν’ - {3-(4 -苯基）苯乙醯胺基）-4,5，6, 7 -四氫 D比咬[4,3-c]e比峻-5-基}脲；C:\2D-CODE\91-01\90119473.ptd Page 302 1327569 V. Description of invention (300) 5H). " N- butyl-Ν' - {3-(3-mercapto-butylamino)-4, 5, 6, 7-tetrahydroacridine [4,3 - c ]" 5-based urea; 0.85 (t, 3H), 0.88 (s, 3H), 0.90 (s, 3H), 1.20-1.30 (m, 2H), 1.32-1.40 (m, 2H), 1.95-2.10 (m , lH), 2.15 (d, 2H), 2.55 (t, 2H), 2.95-3.02 (m, 2H), 3.55 (t, 2H), 4.15 (s, 2H), 6.45 (t, 1 Η " Ν- Phenyl-fluorene-{3-(3-mercapto-butylamino)-4,5,6,7-tetrahydropyridine [4,3-〇]°°°-5-yl} vein; 0.90-0.95 (m, 6H), 2.00_2.10 (m, lH), 2.15 (d, 2H), 2.65 (t, 2H), 3.65 (t, 2H), 4.25 (s, 2H), 6.85 (t , lH), 7.15-7.22 (m , 2H), 7.28-7.32 (m, 2H), 8.60 (s, lH). " N-ethyl-N'-{3-(3-indolyl-butyrene) Amino)-4,5,6,7-tetrahydropyridine [4,3 - c ] β ratio ° sit-5-yl}urea; 0.88-0.90 (m, 6H), 1.00 (t, 3H), 1.95 -2.10 (m, lH), 2.15 (d, 2H), 2.58 (t, 2H), 2.95-3.08 (m, 2H), 3.55 (t, 2H), 4.15 (s, 2H), 6. 45 (t ,1H)." N-Ethyl-N'-{3-(4-phenyl)phenylethylamino)-4,5,6,7-tetrahydropyrrole [4,3-c]吼Oxazol-5-yl}urea; 0.95 (t, 3H), 2.58 (t, 2H), 2.95-3.05 (m, 2H), 3.50 (t, 2H), 3.65 (s, 2H), 4.15 (s, 2H) ), 6.45 (t, lH), 7.30-7.50 (m, 4H), 7. 55- 7. 65 (m, 3H) » " N-isopropyl-Ν' - {3-(4-phenyl)phenethylamino)-4,5,6,7-tetrahydro D ratio bite [ 4,3-c]e than quaternary-5-yl}urea;

C:\2D-00DE\91-01\90119473.ptd 第303頁『1327569 五、發明說明（301) 1.00-1.05(ra,6H),2.55(tJ2H),3.40(t,2H),3.65(sJ2H) ,3.70-3.80(m,lH),4.15(s,2H),6.15(d,lH),7.30-7.45(ni ,5H), 7. 55-7. 65 (m, 4H) ° n 1^-(5-’苯甲酿基）-4,5,6,7-四氫|1比咬[4，3-〇]〇比〇坐-3-基） -(4-苯基）苯乙醯胺 2.70(t，2H),3.6〇-3.70(m,4H)， 4.40(bs，2H)，7.30-7.62(m，14H)。 ?'1-(5-(2-口夫喊甲酿基）-4,5,6,7-四氫11比〇定[4,3-(：]0比〇坐 -3 -基）-(4 -苯基）苯乙醯胺 2_75(bs，2H0,3.65(bs，2H)， 3.80(bs，2H)，4.50(bs，2H)，6.60(bs，lH)，6.95(bs，lH)， ^7.30-7.50(m，5H)，7.55-7.65(m,4H)，7.80(bs，lH)。 N-丙基-N’-{3-(4-苯基）苯乙醯胺基）-4,5,6,7-四氫口比啶[4, 3-c]吡唑-5-基}脲； 0.85(t,3H),l.20-1.30(m,2H),l.35-1.40(m,2H),2.55( t,2H),2.95-3.00(m,2H),3.50(t,2H),3.62(s,2H),4.15(s ,2H), 6. 42(t, 1H), 7. 30-7. 5 0 (m, 5H), 7. 55-7. 65(m, 4H) » " N-(5-(2-曱氧苯基）-4, 5, 6, 7-四氫咄啶[4, 3-c]咄唑-3-基）-(4-苯基）苯乙醯胺 2.50-2.65(m，2H) ,3.40-3.70 (m，2H)，3.75(s，3H)，4.00-4.45(m，2H)，6.85-7-25(in，4H)， •7.30-7.55(m，5H)，7.57-7.64(m，4H)。 P N-苄基-Ν’- {3-( 4-苯基）苯乙醯胺基）-4,5,6，7-四氫吡啶[4, 3-c]吡唑-5-基}脲； 2.60(t,2H)，3.55(t，2H)，3.62(s，2H),4.20-4.30(m，4H) ，7. 10(t, 1H), 7. 15-7. 65(m，14H)。" 卜苯基4，-{3-(4-苯基）苯乙醯胺基）-4,5,6,7-四氫口比C:\2D-00DE\91-01\90119473.ptd p. 303 “1327569 V. Inventions (301) 1.00-1.05 (ra, 6H), 2.55 (tJ2H), 3.40 (t, 2H), 3.65 (sJ2H) ), 3.70-3.80 (m, lH), 4.15 (s, 2H), 6.15 (d, lH), 7.30-7.45 (ni, 5H), 7. 55-7. 65 (m, 4H) ° n 1^ -(5-'Benzene-based)-4,5,6,7-tetrahydro-[1 bite [4,3-〇]〇 than 〇-3-yl)-(4-phenyl)benzene Indole 2.70 (t, 2H), 3.6 〇 - 3.70 (m, 4H), 4.40 (bs, 2H), 7.30-7.62 (m, 14H). ?'1-(5-(2- 口夫叫甲基)-4,5,6,7-tetrahydro 11 ratio [4,3-(:]0 is more than -3 - base) - (4-phenyl) phenethylamine 2_75 (bs, 2H0, 3.65 (bs, 2H), 3.80 (bs, 2H), 4.50 (bs, 2H), 6.60 (bs, lH), 6.95 (bs, lH) , ^7.30-7.50 (m, 5H), 7.55-7.65 (m, 4H), 7.80 (bs, lH). N-propyl-N'-{3-(4-phenyl)phenylethylamino) -4,5,6,7-tetrahydropyridinium [4,3-c]pyrazol-5-yl}urea; 0.85 (t, 3H), 1.20-1.30 (m, 2H), l. 35-1.40 (m, 2H), 2.55 (t, 2H), 2.95-3.00 (m, 2H), 3.50 (t, 2H), 3.62 (s, 2H), 4.15 (s, 2H), 6. 42 ( t, 1H), 7. 30-7. 5 0 (m, 5H), 7. 55-7. 65(m, 4H) » " N-(5-(2-indolylphenyl)-4, 5, 6, 7-tetrahydroacridine [4,3-c]oxazol-3-yl)-(4-phenyl)phenylacetamide 2.50-2.65 (m, 2H), 3.40-3.70 (m, 2H), 3.75 (s, 3H), 4.00-4.45 (m, 2H), 6.85-7-25 (in, 4H), • 7.30-7.55 (m, 5H), 7.57-7.64 (m, 4H). N-benzyl-Ν'- {3-(4-phenyl)phenylethylamino)-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-5-yl}urea ; 2.60(t,2H), 3.55(t,2H), 3.62(s,2H), 4.20-4.30(m,4H), 7.10(t, 1H), 7. 15-7. 65(m, 14H). " Phenyl 4,-{3-(4-phenyl)phenylethylamino)-4,5,6,7-tetrahydroport ratio

C:\2D-OODE\91-01\90119473.ptd 第304頁 1327569 五 '發明說明（302) 。定[4,3-c]Btb°坐-5-基}脲； 2.65(t，2H)，3.60-3.70(m，4H)，4.35(s，2H)，6.90(t，lH) ,7.15-7. 20(m，2H)，7. 30-7. 50(m，8H)，7. 55-7. 65(m，3H)， 8· 60(s， 1H)。 ” N-異丙基-Ν，-{3-[4-(1-吡啶啶-2 -酮）]苯乙醢胺基 -4,5, 6, 7-四氫吡咬[4, 3-c] D比唑-5-基}脲； 1.02-1.07(m,6H),2.00-2.10(m,2H),2.45(t,2H),2.55( t，2H)，3.50(t，2H)，3.55(s，2H)，3.62-3.75(m,lH)，3.80(t ，2H)，4.15(s,2H)，6.15(d，lH)，7.25-7.35(m，2H)，7.55-7. 60(m，2H) 〇 ·， N-乙基-N，- (3-(2-(2 -萘）苯醯胺基）-4,5, 6, 7 -四氫吡啶 [4，3 - c ]吡唑-5 -基}脲； 0.98(t，3H)，1.48(d，3H)，2.55(t，2H)，2.95-3.05 (m,2H), 3.55(t,2H), 4.00(m,lH), 4. 1 0-4. 2 2 (m, 2H), 6.42(t,lH), 7. 40-7. 58(m, 3H), 7 . 80-7. 90 (m, 4H) 〇 " N-異丙基-Ν’ - {3-(2-(2 -萘）苯醯胺基）-4, 5，6，7-四氫口比啶[4,3-c]吡唑-5-基}脲； 1.00-1.05(m,6H),1.50(d,3H),2.55(t,2H),3.45-3.55( m，2H), 3. 62-3. 75 (m，lH)，4.00(m，lH)，4.10-4.25 (m，2H)，6.15(d，lH)，7.40-7.55(m，3H)， 7. 80-7.90 (m，4H)。" N- 丁基- Ν’ - {3-(2-(2 -萘）苯酿胺基）-4, 5, 6，7-四氫°比口定 [4,3-〇]»比°坐-5-基}脲； 0.80(t,3H), 1. 18-1. 27(ιη, 2H), 1. 30-1. 40 (m, 2H), 1.C:\2D-OODE\91-01\90119473.ptd Page 304 1327569 Five 'Inventions (302). [4,3-c]Btb° sit-5-yl}urea; 2.65(t,2H), 3.60-3.70(m,4H), 4.35(s,2H), 6.90(t,lH),7.15- 7. 20 (m, 2H), 7. 30-7. 50 (m, 8H), 7. 55-7. 65 (m, 3H), 8 · 60 (s, 1H). N-isopropyl-indole, -{3-[4-(1-pyridin-2-one)]phenylethylamino-4,5,6,7-tetrahydropyridyl [4, 3- c] D-biazole-5-yl}urea; 1.02-1.07 (m, 6H), 2.00-2.10 (m, 2H), 2.45 (t, 2H), 2.55 (t, 2H), 3.50 (t, 2H) , 3.55 (s, 2H), 3.62-3.75 (m, lH), 3.80 (t, 2H), 4.15 (s, 2H), 6.15 (d, lH), 7.25-7.35 (m, 2H), 7.55-7 60(m,2H) 〇·, N-ethyl-N,-(3-(2-(2-naphthyl)phenylhydrazino)-4,5, 6, 7-tetrahydropyridine [4,3 - c ] pyrazol-5 -yl}urea; 0.98 (t, 3H), 1.48 (d, 3H), 2.55 (t, 2H), 2.95-3.05 (m, 2H), 3.55 (t, 2H), 4.00 (m,lH), 4. 1 0-4. 2 2 (m, 2H), 6.42(t,lH), 7. 40-7. 58(m, 3H), 7. 80-7. 90 (m , 4H) 〇" N-isopropyl-Ν' - {3-(2-(2-naphthyl)phenylhydrazino)-4, 5,6,7-tetrahydropyrazine [4,3- c]pyrazole-5-yl}urea; 1.00-1.05 (m, 6H), 1.50 (d, 3H), 2.55 (t, 2H), 3.45-3.55 (m, 2H), 3. 62-3. (m, lH), 4.00 (m, lH), 4.10-4.25 (m, 2H), 6.15 (d, lH), 7.40-7.55 (m, 3H), 7. 80-7.90 (m, 4H). ; N- butyl- Ν' - {3-(2-(2-naphthalene)phenyl arylamino)-4, 5, 6,7-tetrahydrogen ratio [4,3-〇]» ratio ° Sodium-5-urea 0.80 (t, 3H), 1. 18-1. 27 (ιη, 2H), 1. 30-1. 40 (m, 2H), 1.

C:\2D-C0DE\91-01\90119473.ptd 第305頁 1327569 五、發明說明（303) 48(d,3H), 2.55(t,2H), 2. 9 5 - 3. 0 2 (m, 2 Η ) , 3.40-3.60 (m,2H), 4.00(m,lH), 4. 08-4. 22 ( m, 2H) , 6.40(t,lH), 7. 40-7. 55(m, 3H), 7. 80-7. 9 0 (m, 4H) ° " N-苄基-Ν’ - {3-(2-(2-萘）苯醯胺基）-4,5,6,7 -四氫吼啶 [4,3-〇]°比°坐-5-基}脈； 1.45(d，3H)，2. 60(t，2H)，3.50 -3.62 (m，2H)，4.00 (m，lH)，4.20(s，2H)，4.25(d，2H)，7·08(ΐ，1Η), 7.15-7.30(m,5H), 7.40-7.55(m,4H), 7.80-7.90(m,3H), 10. 10(s，1H), 12· 10(s，1H)。” |||^1-(5-(2-〇夫味甲酿基）-4,5,6,7-四氫口比0定[4,3-〇〇口比口坐 -3 -基）丙醯胺 1.50(d，3H)，2.70(bs，2H), 3.80(bs，2H)， 4.00(m,lH), 4. 30-4. 55(m, 2H), 6.50(bs,lH), 6.90(bs, 1H), 7. 40-7. 58 (m, 4H), 7.70(bs,lH), 7.80-7.90 (m，3H)，10. 18(s, 1H)，12· 18(s, 1H)。 1^-(5-(2-曱氧-苯曱醯基）-4,5,6,7-四氫吡啶[4,3-(：]吡唑-3 -基）-[4-(l -咄咯啶-2 -酮）]苯乙醯胺 2.00-2.10(ra,2H), 2.45(t,2H), 2.55-2.65(m,2H), 3. 30-3. 45(m, 2H), 3.60(s,2H), 3.80(t,2H), 4.00-4.45 ^(ra,2H), 6.90-7. 15(m,4H), 7.30-7.40(m,2H), 7.50-’7. 60(m，2H)。 N-乙基-Ν’ - {3-[2-(4-苯基-3-氟-苯基）丙醯胺基]-4, 5，6，7-四氫π比咬[4，3-c] β比0坐-5-基}脈； 0.95 (t,3H), 1.42(d,3H), 2.55(t,2H), 2.95-3.05 (m,2H), 3.40-3.60(m,2H), 3.95(m,lH), 4.10-4.22C:\2D-C0DE\91-01\90119473.ptd Page 305 1327569 V. INSTRUCTIONS (303) 48(d,3H), 2.55(t,2H), 2. 9 5 - 3. 0 2 (m , 2 Η ) , 3.40-3.60 (m, 2H), 4.00 (m, lH), 4. 08-4. 22 ( m, 2H) , 6.40 (t, lH), 7. 40-7. 55 (m , 3H), 7. 80-7. 9 0 (m, 4H) ° " N-benzyl-Ν' - {3-(2-(2-naphthalene)phenylhydrazino)-4,5,6 ,7-tetrahydroacridine [4,3-〇]°°°-5-base} vein; 1.45(d,3H), 2.60(t,2H),3.50 -3.62 (m,2H), 4.00 (m, lH), 4.20 (s, 2H), 4.25 (d, 2H), 7·08 (ΐ, 1Η), 7.15-7.30 (m, 5H), 7.40-7.55 (m, 4H), 7.80- 7.90 (m, 3H), 10. 10 (s, 1H), 12·10 (s, 1H). ”|||^1-(5-(2-〇夫味甲基)-4,5,6,7-tetrahydroport ratio 0 [4,3-〇〇口比口-3 -基Propylamine 1.50 (d, 3H), 2.70 (bs, 2H), 3.80 (bs, 2H), 4.00 (m, lH), 4. 30-4. 55 (m, 2H), 6.50 (bs, lH) ), 6.90(bs, 1H), 7. 40-7. 58 (m, 4H), 7.70 (bs, lH), 7.80-7.90 (m, 3H), 10. 18(s, 1H), 12· 18 (s, 1H). 1^-(5-(2-oxime-benzoyl)-4,5,6,7-tetrahydropyridine [4,3-(:]pyrazol-3-yl) -[4-(l-Pyrrolidin-2-one)]phenethylamine 2.00-2.10 (ra, 2H), 2.45 (t, 2H), 2.55-2.65 (m, 2H), 3. 30-3 45(m, 2H), 3.60(s,2H), 3.80(t,2H), 4.00-4.45 ^(ra,2H), 6.90-7. 15(m,4H), 7.30-7.40(m,2H ), 7.50-'7. 60(m, 2H). N-Ethyl-Ν' - {3-[2-(4-phenyl-3-fluoro-phenyl)propanylamino]-4, 5 ,6,7-tetrahydropyrene ratio bite [4,3-c] β is 0-5-base} pulse; 0.95 (t,3H), 1.42 (d,3H), 2.55(t,2H), 2.95 -3.05 (m, 2H), 3.40-3.60 (m, 2H), 3.95 (m, lH), 4.10-4.22

C:\2D.C0DE\91-01\90119473.ptd 第306頁 1327569 五、發明說明（304) (m，2H)，6.45(t，lH)，7.25-7.55 (m，8H)。" N_異丙基-Ν’ - {3-[2-(4 -苯基-3-氟-苯基）丙醯胺基]-4,5,6,7-四氫°比咬[4,3-〇]11比°坐-5-基}腺； 1.00-1.05(m，6H)，1.42(d，3H)，2.55(t，2H)，3.40-3. 60(m, 2H), 3. 70(m, 1H), 4. 08-4 . 22 (m, 2H), 6. 15(t, 1H)，7. 22-7. 57(m，8H)。n N- 丁基- Ν’ - {3-[2-(4_苯基-3-氟-苯基）丙酿胺基]-4，5, 6,7-四氫D比咬[4, 3-c] n比。坐-5-基}脈； 0.82(t，3H)，1.18-1.28(m，2H)，l,30- 1.38 (m，2H)，l· 42(d，3H)，2. 55(t,2H)，2.95-3. 02(m，2H)，3.40-3.60 (m,2H), 3.90(m,lH), 4. 1 0-4. 20 (m, 2H), 6.42(t,lH), 7. 25-7. 58 (m, 8H) ° " 1'1-(5_(2-〇夫喃曱醯基）-4，5，6，7-四氫口比〇定[4，3-(：]1>比〇坐 -3-基）-2-(3-氣-4-苯基-苯基）丙酿胺 1.40 (d，3H)，2.75 (bs,2H), 3.80(bs,2H), 3.90(m,lH), 4. 4 0-4. 6 0 (m, 2H ), 6.60(bs,lH), 6.95(bs,lH), 7.25-7.55(m,8H), 7.80(bs， 1H)。 N-異丙基- Ν’ _{3-(l -甲基-叫丨喃-3 -基）乙醯胺基-4，5，6, 7 -四氫°比咬[4，3 - c ]吡唑-5 -基}脲； 1.0〇-1.05(m，6H)，2.55(t，2H)，3.50(t，2H)，3.65-3.75(m,6H),4.15(s,2H), 6.12(d,lH), 7.00 (t,lH), 7.12(t,lH), 7.20(s,lH), 7.35(d,lH), 7.60 (d，1H)。" N，N-異丙基-Ν’ - {3-(苯并[1，3]二氧伍圜-5-基）乙醯胺C:\2D.C0DE\91-01\90119473.ptd Page 306 1327569 V. INSTRUCTIONS (304) (m, 2H), 6.45 (t, lH), 7.25-7.55 (m, 8H). " N_isopropyl-Ν' - {3-[2-(4-phenyl-3-fluoro-phenyl)propanylamino]-4,5,6,7-tetrahydrogen ratio bite [ 4,3-〇]11 than ° sitting -5-base} gland; 1.00-1.05 (m, 6H), 1.42 (d, 3H), 2.55 (t, 2H), 3.40-3. 60 (m, 2H) , 3. 70 (m, 1H), 4. 08-4 . 22 (m, 2H), 6. 15 (t, 1H), 7. 22-7. 57 (m, 8H). n N- butyl- Ν' - {3-[2-(4-phenyl-4-fluoro-phenyl) propylamino]-4,5, 6,7-tetrahydro D ratio bite [4, 3-c] n ratio. Sit on the -5-base}; 0.82 (t, 3H), 1.18-1.28 (m, 2H), l, 30- 1.38 (m, 2H), l · 42 (d, 3H), 2. 55 (t, 2H), 2.95-3. 02(m, 2H), 3.40-3.60 (m, 2H), 3.90 (m, lH), 4. 1 0-4. 20 (m, 2H), 6.42 (t, lH) , 7. 25-7. 58 (m, 8H) ° " 1'1-(5_(2-〇夫曱醯曱醯)-4,5,6,7-tetrahydro port ratio [4, 3-(:]1> 〇-3-yl)-2-(3- ace-4-phenyl-phenyl) propylamine 1.40 (d, 3H), 2.75 (bs, 2H), 3.80 ( Bs, 2H), 3.90 (m, lH), 4. 4 0-4. 6 0 (m, 2H ), 6.60 (bs, lH), 6.95 (bs, lH), 7.25-7.55 (m, 8H), 7.80(bs, 1H). N-isopropyl- Ν' _{3-(l-methyl-called 丨-anthracen-3-yl)acetamido-4,5,6,7-tetrahydrogen ratio Biting [4,3 - c ]pyrazol-5-yl}urea; 1.0〇-1.05 (m, 6H), 2.55 (t, 2H), 3.50 (t, 2H), 3.65-3.75 (m, 6H), 4.15(s,2H), 6.12(d,lH), 7.00 (t,lH), 7.12(t,lH), 7.20(s,lH), 7.35(d,lH), 7.60 (d,1H).&quot ; N,N-isopropyl-Ν' - {3-(benzo[1,3]dioxos-5-yl)acetamide

C:\2D-CDDE\91-01\90119473.ptd 第307頁 1327569 五、發明說明（305) 基-4, 5, 6, 7 -四氫吡啶[4, 3-c] °比唑-5-基}脲； 1. 00- 1. 0 5 (m, 6H), 2.55(t,2H), 3. 45-3. 55(m, 4H), 3. 6 5-3. 75 (m, 1H), 4.15(s,2H), 5.95(s,2H), 6.15 (d，lH), 6. 75(d,lH)，6.80-6.88(m，3H)。" N，N-二曱基-N’-{3-(苯并[1，3]二氧伍園-5-基）乙酿胺基-4，5，6，7 -四氫°比咬[4，3-c]吼"坐-5-基}脈； 2.65(t,2H), 2.70(s,6H), 3.48(s,2H), 4.00(s,2H), 5.95(s,2H), 6.75(d,lH), 6. 80-6.88 (m,3H) ° " N-乙基-Ν’ - (3-(2-(6-曱氧-2 -萘）丙酿胺基）-4, 5, 6, 7-•四氫"比咬[4, 3-c] °比〇坐-5-基}脲； 0.95(t,3H), 1.42((1,3H), 2.55(t,2H), 2.95-3.05 (m,2H), 3. 40-3. 60 (m, 2H), 3.82(s,3H), 3.95(m,lH), 4.10-4.22(ra,2H), 6.42(t,lH),7.10(d,lH),7.25(s,lH), 7. 45(d, 1H)，7. 65-7· 82(m，3H)。 N -異丙基_N’ - {3-(2-(6-曱氧-2-萘）丙醯胺基）-4，5，6，7 -四氫°比。定[4，3 - c ] °比°坐-5 -基}服； 1.00-1. 05(m,6H), 1.45(d,3H), 2.53(t,2H), 3.40-3. 60(m, 2H), 3. 6 5 - 3. 7 5 (m, 1 Η ) , 3.85(s,3H), 3.95 4. 05-4. 22(m, 2H), 6.15(d,lH), 7.12(d,lH), ’7.25(s，lH)，7.45(d，lH), 7.70-7.81(m，3H)。" N- 丁基-Ν’ -(3-(2-(6-甲氧-2-萘）丙醯胺基）-4,5，6,7-四氫"比咬[4, 3-c]"比唑-5-基}脲； 0.82(t，3H), 1.18-1.28(m，2H)，1.30-1.40 (m,2H)，1. 45(d，3H)，2. 55(t，2H)，2.90-3.0 0 (m，2H)，3.40-3.60C:\2D-CDDE\91-01\90119473.ptd Page 307 1327569 V. INSTRUCTIONS (305) Base-4, 5, 6, 7-tetrahydropyridine [4, 3-c] °Biazole-5 - ki) urea; 1. 00- 1. 0 5 (m, 6H), 2.55 (t, 2H), 3. 45-3. 55(m, 4H), 3. 6 5-3. 75 (m, 1H), 4.15 (s, 2H), 5.95 (s, 2H), 6.15 (d, lH), 6. 75 (d, lH), 6.80-6.88 (m, 3H). " N,N-Dimercapto-N'-{3-(benzo[1,3]dioxoin-5-yl)ethanoyl-4,5,6,7-tetrahydrogen ratio Bite [4,3-c]吼"Sit-5-base} pulse; 2.65(t,2H), 2.70(s,6H), 3.48(s,2H), 4.00(s,2H), 5.95(s , 2H), 6.75(d,lH), 6. 80-6.88 (m,3H) ° " N-ethyl-Ν' - (3-(2-(6-曱o-2-ene)) Amino)-4, 5, 6, 7-•tetrahydro" than bite [4, 3-c] ° 〇 -5 -5-} urea; 0.95 (t, 3H), 1.42 ((1,3H ), 2.55(t,2H), 2.95-3.05 (m,2H), 3. 40-3. 60 (m, 2H), 3.82(s,3H), 3.95(m,lH), 4.10-4.22(ra , 2H), 6.42 (t, lH), 7.10 (d, lH), 7.25 (s, lH), 7. 45 (d, 1H), 7. 65-7 · 82 (m, 3H). propyl_N' - {3-(2-(6-oxime-2-naphthalene)propylamino)-4,5,6,7-tetrahydrogen ratio. [4,3 - c ] °坐-5-5 base service; 1.00-1. 05(m,6H), 1.45(d,3H), 2.53(t,2H), 3.40-3. 60(m, 2H), 3. 6 5 - 3. 7 5 (m, 1 Η ) , 3.85(s,3H), 3.95 4. 05-4. 22(m, 2H), 6.15(d,lH), 7.12(d,lH), '7.25( s,lH), 7.45(d,lH), 7.70-7.81(m,3H)." N- butyl-Ν'-(3-(2-(6-methoxy-2-naphthalene)propanamide Base)-4,5,6,7-tetrahydro" than bite [4, 3-c]"Oxazol-5-yl}urea; 0.82 (t, 3H), 1.18-1.28 (m, 2H), 1.30-1.40 (m, 2H), 1.45 (d, 3H), 2. 55 (t, 2H) , 2.90-3.0 0 (m, 2H), 3.40-3.60

C:\2D-OODE\91-Ol\90119473.ptd 第308頁 1327569 五、發明說明（306) (m,2H), 3.85(s,3H), 3.95(m,lH), 4. 08-4. 22(m, 2H), 6.41(t,lH), 7.12(d,lH), 7.25(s,lH), 7.45(d,lH), 7. 70-7. 80 (m, 3H) ° " N-苄基-Ν’ - {3-(2-（6-曱氧-2 -萘）丙醯胺基）-4, 5,6, 7-四氩°比°定[4，3 - c ] °比°坐-5 -基}脲； 1.42(d,3H), 2.58(t,2H), 3. 45-3. 65(m, 2H), 3.82 (s,3H), 3.95(m,lH), 4. 1 0-4. 30 ( m, 2H) , 7.10(t,lH), 7.15-7.30(m，7H), 7.45(d，lH), 7.70-7.80(m，3H)。 N-苯基-Ν’ - {3_(3 -氟苯曱醯胺基）-4,5,6, 7-四氫吡啶 [4,3-(：]吼嗤-5-基}脲； 1H-NMR (DMSO-d6) d ppm 2.7(m), 3.7(m), 4.4(s), 6_ 9-8. 6(m)。 ” N-{5 -苯石黃酿基-4，5，6, 7-四氫0比咬[4，3-c] D比0坐-3-基}_ 環丙烷羧醯胺 1H-NMR (DMSO-d6) d ppm 0.7(m)，1.8(m)， 2. 6(m)，3. 4(m)，4. 0(s)，7· 5-7. 8(m)。 N-{5-( °奎琳-8-確醢基）-4, 5，6，7 -四氫p比咬[4,3-c] °比°坐 -3-基卜3-氟苯曱醯胺 1H-NMR (DMSO-d6) d ppm 2·6(ιη), 3.75(m), 4. 35(s)， 7.35-9.0(m)。 N-[5-(苄基續醢基）-4, 5，6, 7-四氫0比0定[4, 3-c]吼0坐- 3-基]-苯甲醯胺 1H-NMR (DMSO-d6) d ppm 2.6(m)，3.4(m)， 4. 2(s)，4. 4(s)，7. 3-8. 0(m)。 N-{5 -苯績酿基-4，5，6，7-四氫°比0定[4，3-c] D比0坐-3-基} -3-溴苯甲醯胺 1H-NMR (DMSO-d6) d ppm 2.65(m)， 4. 05(s)，7. 4-8. 0(m)。C:\2D-OODE\91-Ol\90119473.ptd Page 308 1327569 V. Description of invention (306) (m, 2H), 3.85 (s, 3H), 3.95 (m, lH), 4. 08-4 .22(m, 2H), 6.41(t,lH), 7.12(d,lH), 7.25(s,lH), 7.45(d,lH), 7. 70-7. 80 (m, 3H) ° &quot ; N-benzyl-Ν' - {3-(2-(6-oxime-2-naphthalene)propanylamino)-4, 5,6, 7-tetra-argon ° ratio [4,3 - c ] ° ratio ° sitting -5 - base urea; 1.42 (d, 3H), 2.58 (t, 2H), 3. 45-3. 65 (m, 2H), 3.82 (s, 3H), 3.95 (m , 1H-4, 30 (m, 2H) N-phenyl-Ν'-{3_(3-fluorophenylguanidino)-4,5,6,7-tetrahydropyridine [4,3-(:]吼嗤-5-yl}urea; 1H -NMR (DMSO-d6) d ppm 2.7 (m), 3.7 (m), 4.4 (s), 6_ 9-8. 6 (m). "N-{5 - benzophenanthrene-4,5, 6, 7-tetrahydro 0 ratio bite [4,3-c] D to 0 -3-yl}_cyclopropanecarboxamide 1H-NMR (DMSO-d6) d ppm 0.7 (m), 1.8 (m) , 2. 6(m), 3. 4(m), 4. 0(s), 7· 5-7. 8(m). N-{5-(°奎琳-8-确醢基)- 4, 5,6,7-tetrahydrop ratio bite [4,3-c] ° ratio -3--3-b 3-fluorobenzamide 1H-NMR (DMSO-d6) d ppm 2·6 ( Imη), 3.75(m), 4. 35(s), 7.35-9.0(m). N-[5-(Benzyl fluorenyl)-4, 5,6, 7-tetrahydro 0 to 0. 4, 3-c] 吼 0 - - 3-yl]-benzamide 1H-NMR (DMSO-d6) d ppm 2.6 (m), 3.4 (m), 4. 2 (s), 4. 4 ( s), 7. 3-8. 0(m). N-{5 - benzene-flavoring base-4,5,6,7-tetrahydrogen ratio 0 [4,3-c] D ratio 0 sitting- 3-(1)- bromobenzamide 1H-NMR (DMSO-d6) d ppm 2.65 (m), 4. 05 (s), 7. 4-8. 0 (m).

C:\2D-00DE\91-01\90119473.ptd 第309頁 1327569 五、發明說明（307) N-[5-( ¥基磺醯基）_4,5,6,7 -四氫吡啶[4,3-c]吡唑-3-基]-3-溴苯曱醯胺 1H-NMR (DMS0-d6) d ppm 2.6(m)， 4. 15(s)，4. 4(s)，7. 3-8. 0(m)。 N-{ 5-(4-氟苯）磺醯基-4, 5, 6, 7-四氫吡啶[4, 3-c]吡唑 -3-基}-3-溴苯甲醯胺 1H-NMR (DMSO-d6) d ppm 2.7(m)， 3. 4(m)，4. l(s)，7. 4-8. 2(m)。 N-{5 -（3 -三氟曱基苯）磺醯基-4, 5,6, 7 -四氫》比啶 [4,3-c] 口比唑-3-基}-3-溴苯曱醯胺 1H-NMR (DMSO-d6) d ppm 2. 6(m)，3.5(m), 4.2( s)，7.4-8. 2(m)。费1'1-{5-(4-甲苯確酿基）-4,5，6，7-四氫〇比。定[4,3-0：]〇比〇坐 -3-基}-3-漠苯甲醢胺 1H-NMR (DMSO-d6) d ppm 2.4(s)， 2. 7(m)，3. 3(m)，4. 0(s)，7. 4-8. 2(m)。 ?^-{5-(4-甲氧苯）確醯基-4,5，6，7-四氫0比〇定[4,3-(：]0比 0坐-3-基}_3-溴苯曱醯胺 1H-NMR (DMSO-d6) d ppm 2.7 (m), 3.3(m), 3.8(s), 4.0(s), 7.1-8.2(m) e N-{5-(4-第三丁基苯）磺醯基-4, 5, 6, 7-四氫吡啶 [4,3-c]吡唑-3-基}-3-溴苯曱醯胺 1H-NMR (DMSO-d6) d ppm 1.3(s)，2.7(m)，3.3(m)，4.1(s)，7.4-8.2(m)。 _!^-{5-(4-氣苯）磺醯基-4,5,6,7-四氫"比啶[4,3-(：]吼唑 _3_基}-3_ 漠苯曱酿胺 1H_NMR (DMSO_d6) d ppm 2. 7(m)， 3.4(m)，4.1(s)，7.4_8.2(m)。 N-{5-(2 -萘）續醯基_4, 5, 6, 7-四氫B比咬[4, 3-c]吡唑- 3-基}-3-溴苯曱酿胺 1H-NMR (DMSO-d6) d ppm 2.7(m)， 3.6(m)，4.3(s)， 7.4-8.6(m)。C:\2D-00DE\91-01\90119473.ptd Page 309 1327569 V. INSTRUCTIONS (307) N-[5-(¥ sulfamoyl)_4,5,6,7-tetrahydropyridine [4 ,3-c]pyrazol-3-yl]-3-bromophenylguanamine 1H-NMR (DMS0-d6) d ppm 2.6(m), 4. 15(s),4. 4(s),7 3-8. 0(m). N-{ 5-(4-fluorophenyl)sulfonyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-3-bromobenzamide 1H- NMR (DMSO-d6) d ppm 2.7 (m), 3. 4 (m), 4. l (s), 7. 4-8. 2 (m). N-{5-(3-trifluorodecylbenzene)sulfonyl-4,5,6,7-tetrahydro"pyridyl[4,3-c]-portoxazol-3-yl}-3-bromo Benzoylamine 1H-NMR (DMSO-d6) d ppm 2. 6 (m), 3.5 (m), 4.2 (s), 7.4-8. 2 (m). It is a 1'1-{5-(4-toluene)-4,5,6,7-tetrahydroanthracene ratio. Ding [4,3-0:] 〇〇 -3- yl} -3- benzoic acid amide 1H-NMR (DMSO-d6) d ppm 2.4 (s), 2. 7 (m), 3. 3(m), 4. 0(s), 7. 4-8. 2(m). ?^-{5-(4-methoxybenzene) is a thiol-4,5,6,7-tetrahydro 0 ratio [4,3-(:]0 is 0 to -3-yl}_3- Bromide 1H-NMR (DMSO-d6) d ppm 2.7 (m), 3.3 (m), 3.8 (s), 4.0 (s), 7.1-8.2 (m) e N-{5-(4- Tert-butylbenzene)sulfonyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-3-bromophenylamine 1H-NMR (DMSO-d6 d ppm 1.3(s), 2.7(m), 3.3(m), 4.1(s), 7.4-8.2(m). _!^-{5-(4-Phenylbenzene)sulfonyl-4,5 ,6,7-tetrahydro"bipyridine[4,3-(:]carbazole_3_yl}-3_ benzoquinone 1H_NMR (DMSO_d6) d ppm 2. 7(m), 3.4(m) , 4.1(s), 7.4_8.2(m). N-{5-(2-naphthalene) continued fluorenyl _4, 5, 6, 7-tetrahydro B ratio bite [4, 3-c]pyrazole - 3-yl}-3-bromophenylamine 1H-NMR (DMSO-d6) d ppm 2.7 (m), 3.6 (m), 4.3 (s), 7.4 - 8.6 (m).

C: \2D-OODE\91 -01 \90119473.ptd 第 310 頁 1327569 五、發明說明（308) N-{5-(2-°塞吩基）乙醯基-4，5，6，7 -四氫"比。定[4，3-c] 口比 °坐-3-基}-4-氟苯甲醯胺 1H-NMR (DMSO-d6) d ppm 2.6 (m), 3.75(m), 3.9-4.1(2s), 4. 3 5-4. 5 ( 2s ), 6.8-8 · 1 ( m ) o N-{5-(2-°塞吩基）乙醯基-4，5，6，7 -四氫0比咬[4，3-c] 口比唑-3-基}-3-曱氧苯曱醯胺 1H-NMR (DMSO-d6) d ppm 2.6 (m), 3.75(m), 3. 8 ( s ) , 3. 9 - 4. 1 ( 2 s ), 4. 3 5-4. 5 ( 2 s ), 6,8-7_6(m)。 N-[5_(l, 3 -苯并二氧伍圜_5_基幾基）乙酿基-4，5，6, 7-四氫咄啶[4, 3-c]咄唑-3 -基]-4-第三丁基-苯甲醯胺 1H-NMR (DMSO-d6) d ppm 1.3(s), 2.75(m), 4.4(s), 6.0(s)，6.9-7.6(m)。 1^-[5-(1，3-苯并二氧伍圜-5-基羰基）乙醯基-4,5,6,7-四氫吡啶[4, 3-c]吡唑-3 -基]-3-曱氧苯曱醯胺1H-NMR (DMSO-d6) d ppm 2.75(m), 3.6(m), 3.8(s), 4.4(s), 6. 0(s), 6. 9-7. 6(m)。 N-[5-(l, 3 -苯并二氧伍圜_5_基幾基）乙酿基-4, 5，6, 7-四氮D比咬[4，3_c] n比〇坐_3_基]_3_苯氧苯甲酿胺1H-NMR (DMSO-d6) d ppm 2.7(m), 4.4(s), 6.0(s), 6.9-7.8 (m)。 N-[5-(l, 3 -苯并二氧伍圜_5_基裁基）乙酿基-4，5，6，7-四.氫D比咬[4，3_c] °比〇坐_3_基]_3-苯氧苯甲酿胺1H-NMR (DMSO-d6) d ppm 1. 95-2. 05 ( 2s), 2. 55-2. 65 ( 2m), 3. 55-3. 75 ( 2m)，4.3-4.4(2s)，7.0-7.8(m)。C: \2D-OODE\91 -01 \90119473.ptd Page 310 1327569 V. INSTRUCTIONS (308) N-{5-(2-°Septyl)ethenyl-4,5,6,7 - Tetrahydrogen" Determination of [4,3-c] °-3-yl}-4-fluorobenzamide 1H-NMR (DMSO-d6) d ppm 2.6 (m), 3.75(m), 3.9-4.1 (2s ), 4. 3 5-4. 5 ( 2s ), 6.8-8 · 1 ( m ) o N-{5-(2-°Sepyl)ethinyl-4,5,6,7-tetrahydro 0 to bite [4,3-c] bisazol-3-yl}-3-oxobenzoquinone 1H-NMR (DMSO-d6) d ppm 2.6 (m), 3.75 (m), 3. 8 ( s ) , 3. 9 - 4. 1 ( 2 s ), 4. 3 5-4. 5 ( 2 s ), 6,8-7_6(m). N-[5_(l, 3 -benzodioxanthene-5-yl)yl-bromo-4,5,6,7-tetrahydroacridine [4,3-c]carbazole-3 - 1-4-t-butyl-benzamide 1H-NMR (DMSO-d6) d ppm 1.3(s), 2.75(m), 4.4(s), 6.0(s), 6.9-7.6(m) . 1^-[5-(1,3-benzodioxoindol-5-ylcarbonyl)ethinyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-3 1H-NMR (DMSO-d6) d ppm 2.75 (m), 3.6 (m), 3.8 (s), 4.4 (s), 6. 0 (s), 6. 9-7. 6(m). N-[5-(l, 3 -benzodioxanthene-5_yl)yl-bristyl-4, 5,6,7-tetrazide D ratio bite [4,3_c] n ratio 〇 sitting_ 3_基]_3_phenoxybenzamide 1H-NMR (DMSO-d6) d ppm 2.7 (m), 4.4 (s), 6.0 (s), 6.9-7.8 (m). N-[5-(l, 3 -benzodioxanthene _5_ yl base) ethyl ketone-4,5,6,7-tetra. Hydrogen D ratio bite [4,3_c] ° _3_基]_3-phenoxybenzamide 1H-NMR (DMSO-d6) d ppm 1. 95-2. 05 ( 2s), 2. 55-2. 65 ( 2m), 3. 55-3 75 (2m), 4.3-4.4 (2s), 7.0-7.8 (m).

C:\2D-G0DE\91-01\90119473.ptd 第311頁 1327569 五、發明說明（309) N-[5-苯乙酿基-4，5，6，7-四氫0比咬[4，3-c] °比0坐-3-基] -3- 甲氧苯曱醯胺 1H-NMR (DMS0-d6) d ppm 2.5-2.65 (2m);3.5-3.7(2m);3.8(s);4.35-4.5(2s);7」-7.6(m)。 N-芊基-N’-{3-(3-甲氧-苯曱醯胺基）-4,5,6,7-四氫口比 0定[4,3-c] °比"坐-5-基}服； 1H-NMR (DMS0-d6) d ppm 2.65(m);3. 65(m);3.8(s); 4. 15-4. 3(m);7.卜7. 6(m)。" 1^-{5-苄基磺醯基-4,5,6,7-四氫吡啶[4,3-(：]"比唑-3-基}-3-曱氧苯甲醯胺 1H-NMR (DMSO-d6) d ppm 2.6(m); #3.4(m);3.8(s);4.2(s);4.4(s);7. 1-7. 6(m) N-異丙基-Ν’ - {3-(3-甲氧-苯甲醯胺基）-4,5,6, 7-四氫 0比咬[4，3-c]0比0坐-5_基}脲 » 1 H-NMR (DMS0-d6) d ppm 1.0(d);2.6(m);3.55(m);4.2(s);7.1-7.6(ni)。" 1^，^'}-二曱基-^'1’-{3-(2-苯基-〇比〇坐-4-基）乙酿胺基-4，5, 6，7-四氫〇比。定[4，3-c] D比0坐-5-基}脲； 2.60-2.75(m，6H)，3.30(t，2H)，3.82(s，2H)，4.10(s，2H)，7 .40-7.55(m，4H)，7.85-7.95(m，2H)。 N-異丙基-Ν’ - {3-(2 -苯基-1，3 - °比。坐-4-基）乙醯胺基-4, Λ5, 6, 7-四氫"比啶[4, 3-c]吡唑-5 -基}脲；1. 02(s，3Η)，1. '04(s,3H),2.55(t,2H),3.55(t,2H),3.65-3.88(m,lH),3.9 5(s，2H)，4.20(s,2H)，6.15(d，lH)，7.4〇-7.55(m，4H) ,7.88 -7.98(m，2H)。 N-乙基-Ν’ - {3-(4-氟苯甲醯胺基）-4,5, 6,7-四氫吼啶 [4, 3-c]吡唑-5-基}脲；C:\2D-G0DE\91-01\90119473.ptd Page 311 1327569 V. INSTRUCTIONS (309) N-[5-Phenylethyl 4,5,6,7-tetrahydro 0-bit [4] , 3-c] ° is 0 -3-yl] -3- methoxybenzamine 1H-NMR (DMS0-d6) d ppm 2.5-2.65 (2m); 3.5-3.7 (2m); 3.8 (s ); 4.35-4.5 (2s); 7"-7.6 (m). N-mercapto-N'-{3-(3-methoxy-benzoguanamine)-4,5,6,7-tetrahydro port ratio 0 [4,3-c] ° ratio "sit -5-基} service; 1H-NMR (DMS0-d6) d ppm 2.65 (m); 3.65 (m); 3.8 (s); 4. 15-4. 3 (m); 7. 6 (m). " 1^-{5-Benzylsulfonyl-4,5,6,7-tetrahydropyridine [4,3-(:]"Bizozol-3-yl}-3-indolylbenzoquinone 1H-NMR (DMSO-d6) d ppm 2.6 (m); #3.4 (m); 3.8 (s); 4.2 (s); 4.4 (s); 7. 1-7. 6 (m) N- Propyl-Ν' - {3-(3-methoxy-benzamide)-4,5,6,7-tetrahydro 0 ratio bite [4,3-c]0 to 0--5-based Urea » 1 H-NMR (DMS0-d6) d ppm 1.0 (d); 2.6 (m); 3.55 (m); 4.2 (s); 7.1-7.6 (ni). " 1^,^'}- Dimercapto-^'1'-{3-(2-phenyl-indole 〇-4-yl)ethanoyl-4,5,6,7-tetrahydroindole ratio. [4,3 -c] D is 0 to 5-base urea; 2.60-2.75 (m, 6H), 3.30 (t, 2H), 3.82 (s, 2H), 4.10 (s, 2H), 7.40-7.55 ( m,4H), 7.85-7.95 (m, 2H). N-isopropyl-Ν' - {3-(2-phenyl-1,3 - ° ratio. sit-4-yl)acetamido- 4, Λ5, 6, 7-tetrahydro"bipyridine[4,3-c]pyrazol-5-yl}urea; 1. 02(s,3Η), 1. '04(s,3H),2.55 (t, 2H), 3.55 (t, 2H), 3.65-3.88 (m, lH), 3.9 5 (s, 2H), 4.20 (s, 2H), 6.15 (d, lH), 7.4 〇 - 7.55 (m , 4H), 7.88 -7.98 (m, 2H). N-ethyl-Ν' - {3-(4-fluorobenzamide)-4,5,6,7-tetrahydroacridine [4, 3-c]pyrazole-5-yl}urea;

C:\2D-00DE\91-01\90119473.ptd 第 312 頁 1327569 五、發明說明（310) 1H-NMR (DMSO-d6) d ppm :8.08-7. 34(m,4H),4.17 (s，2H),3.58-2.7(6H)，l.〇〇(m，3H)。實施例1 6 N-{3-苯乙醯胺基-5-(第三丁酯基）-6，6 -二曱基-4, 6 -二氫吡咯并[3, 4-c]吼唑-1-基}，N，-甲基聚苯乙烯脲之製備笨乙醯氯（24.08毫莫耳，3. 18毫升）於1〇毫升無水二氣甲烷之溶液逐滴添加至先前於90毫升無水二氣曱烷及16. 5 毫升DIEA(96.32毫莫耳）溶脹的n-{3 -胺基-5-(第三丁醋基）-6，6 - 一甲基 _4，6 -—氫 0比 p各并[3，4-c] d 比。坐-1-基}，1^’ -甲基聚苯乙稀脲（3. 01毫莫耳’3.5克）。結果所得懸浮液於2 2 °C溫和攪拌1 8小時。然後樹脂經過濾，以二氯曱烧、甲醇洗滌及真空脫水。以類似方式，使用適當酿基氣可製備下列化合物： N-{3-(2 -萘）乙酿胺基-5-(第三丁酯基6_二曱其_4 6-二氮吼略并[3,4_c]吼啥一 i-基}，N，-甲基聚苯^烯^ ’ N-{3-(3 -溴）苯甲醯胺基-5-(第三丁酯基）_6 6一二甲基 -4, 6-二氯吼洛并[3, 4-c]%。坐μ-基}，N，—甲基聚苯-乙稀"脏 N-{3 -環丙烧羧醯胺基-5-(第三丁酯基）一6 6_二曱其_4 6-二氫。比略并[3,4_c]吼唾-i-基}，N，_甲基聚苯I烯^ ’ N-丨3-(4-氟）苯曱醯胺基-5-(第三丁酯基）_6,卜二甲基 -4, 6-二氯吼哈并[3, 4-c] D比唾-】-基}，N、甲基聚苯乙稀^脏 N-{3-(4-第三丁基）苯甲醯胺基-5-(第三丁酿基）_66_ 二甲基-4, 6 -二氫11比哈并[3,4-c] D比"坐-1-基}，n，_曱基聚苯C:\2D-00DE\91-01\90119473.ptd Page 312 1327569 V. INSTRUCTIONS (310) 1H-NMR (DMSO-d6) d ppm : 8.08-7. 34(m, 4H), 4.17 (s , 2H), 3.58-2.7 (6H), l. 〇〇 (m, 3H). Example 1 6 N-{3-Phenylethylamino-5-(t-butylester)-6,6-dimercapto-4,6-dihydropyrrolo[3,4-c]carbazole Preparation of -1-yl},N,-methylpolystyrene Urea (5. Anhydrous dioxane and 16.5 ml of DIEA (96.32 mmol) swollen n-{3-amino-5-(t-butyl acetophenate)-6,6-monomethyl-4,6-- Hydrogen 0 is greater than p and [3,4-c] d ratio. Sodium-1-yl}, 1^'-methylpolystyrene (3.01 mmol) 3.5 g. As a result, the resulting suspension was gently stirred at 22 ° C for 18 hours. The resin was then filtered, washed with dichlorohydrazine, methanol and vacuum dehydrated. In a similar manner, the following compounds can be prepared using a suitable basal gas: N-{3-(2-naphthalene)ethanoyl-5-(t-butyl ester 6-dioxime _4 6-diaza ruthenium And [3,4_c]吼啥-i-yl},N,-methylpolyphenyleneene^ 'N-{3-(3-bromo)benzimidamide-5-(t-butyl ester) _6 6-Dimethyl-4,6-dichloroindolo[3, 4-c]%. Sitting μ-based}, N,-methyl polyphenyl-ethylene "dirty N-{3 - ring Propylcarboylamino-5-(t-butyl ester)-6 6_diindole _4 6-dihydro. Ratio slightly [3,4_c]吼s-i-yl}, N, _ A Polyphenylene olefins ' N-丨3-(4-fluoro)phenylhydrazinyl-5-(t-butyl ester)-6, bis-dimethyl-4,6-dichloro-haha-[3 , 4-c] D than saliva-]-yl}, N, methyl polystyrene^dirty N-{3-(4-t-butyl)benzamide-5- (third distillation Base)_66_ dimethyl-4,6-dihydrogen 11 than haha[3,4-c] D ratio "sitting-1-yl}, n, _ mercapto polyphenylene

乙烯脲 ’ A FIT；.·Ethylene urea ‘ A FIT;.·

illIl

C:\2D-OODE\91-Ol\90119473.ptd 第313頁 1327569C:\2D-OODE\91-Ol\90119473.ptd Page 313 1327569

^{3-經取代之-6,6-二曱基-46__好唑-1-基}，N’_甲基聚苯乙烯脲之製備'虱咣咯并[3,4~c]Dfcb 經由如實施例7所述使用三氟乙醆處理物，獲得下列化合物：貫施例1 6化合 N-{3 -笨乙醯基- 6 6 -二曱基-4 唑-1-基I，Ν’ -甲基聚苯乙烯脲升L3,4-c]nt N-{3-(2-萘）乙醯胺基-6,6-二甲基_4 6 _ — 4_c]吡唑Μ-基}，N’_甲基聚笨乙烯脲’ 一氣°比哈并[3, |§[{3-(3-溴）苯甲醯胺基-6,6-二曱基一46__* [3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲’ 一氫π比咯并 Ν-{3 -環丙炫缓醯胺基- 5- (第三丁 |旨基）_6 6 6-二氫咄咯并[3, 4-c]"比唑-1-基}，N，-曱基聚二二甲基一4, N-{3-(4-氟）苯甲醯胺基-6, 6-二曱基6— = ^締服 [3,4-c]咄唑-1-基}，N，-甲基聚苯乙$脲’ 一風D比洛并 N-{3-(4-第三丁基）苯曱醯胺基-6, 6-二曱基_4 卜 0比咯并[3,4-c]咄唑-卜基}，N’-甲基聚苯乙烯^脲’6 一風實施例1 8 ^{3,5-經取代之-6,6-二曱基-4,6-二氫吡咯并[34_ 吡唑-1-基}, Ν’-甲基聚苯乙烯脲之製備 ’ 經由根據實施例8、9、1 0所述程序使用適當叛酸、異氛酸酯或磺醯氣處理實施例1 7化合物，可獲得下列化合物. Ν-{3 -苯乙醯基-5-乙醯基-6, 6 -二甲基-4，6 -二氫各并 [3,4-c] °比°坐-1-基}，1^’-甲基聚苯乙稀脲^{3-Substituted -6,6-dimercapto-46__oxazol-1-yl}, Preparation of N'-methyl polystyrene urea '虱咣并 [3,4~c] Dfcb The following compounds were obtained via treatment with trifluoroacetamidine as described in Example 7: Example 1 6 N-{3-stupyl- 6 6 -dimercapto-4 azole-1-yl I, Ν'-methyl polystyrene urea L3,4-c]nt N-{3-(2-naphthalene)acetamido-6,6-dimethyl-4 4 _-4_c]pyrazolium- Base}, N'_methyl polystyrene urea urea' one gas ° than haha [3, | § [{3-(3-bromo) benzalkonium-6,6-dimercapto-46__* [3 , 4-c]pyrazol-1-yl}, Ν'-methylpolystyreneurea'-hydrogen π-pyrrolo-{3-cyclopropanthene-amino- 5- (third butyl | Base)_6 6 6-dihydroindolo[3,4-c]"pyrazol-1-yl},N,-mercaptopolydimethyl- 4, N-{3-(4-fluoro Benzylguanidinyl-6,6-dimercapto 6- = ^Contains [3,4-c]oxazol-1-yl},N,-methylpolyphenylene bureide N-{3-(4-t-butyl)benzoguanamine-6,6-diindenyl-4, 0-pyrrolo[3,4-c]carbazole-buji}, N '-Methylpolystyrene^urea'6 wind example 1 8 ^{3,5-substituted-6,6-dimercapto-4, 6-Dihydropyrrolo[34_pyrazol-1-yl}, Preparation of Ν'-methyl polystyrene urea' via the procedures described in Examples 8, 9, 10 using appropriate tick, isomeric acid esters Alternatively, the compound of Example 17 can be treated with sulfonium gas to obtain the following compound: Ν-{3-phenethyl fluorenyl-5-ethenyl-6,6-dimethyl-4,6-dihydrogen[3 ,4-c] °°°-1-yl},1^'-methylpolystyrene

C:\2D-C0DE\91-01\90119473.ptd 第314頁 1327569 五、發明說明（312) N_{3_(2 -蔡）乙酿胺基_5_乙酿基_6，6_二甲基_4，6_二氫吡咯并[3,4-c]吡唑-1-基}，N’_甲基聚苯乙烯脲 N-{ 3-(3 -溴）苯甲醯胺基-5-乙醯基-6,6 -二曱基-4, 6 -二氫吡咯并[3,4-c]吼唑-1-*}，N’ -曱基聚苯乙烯脲 N_{3_環丙烧叛酿胺基_5_(第三丁 S旨基）-5_乙酿基_6，6_ 二曱基-4, 6 -二氫咄咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙稀服 Ν-{3-(4-氟）苯曱醯胺基-5-乙醢基-6, 6 -二曱基一4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-（4-第三丁基）苯曱醯胺基-5-乙醢基-6, 6-二曱基 -4，6-二氫吼11各并[3，4-〇]吼〇坐-1-基}^’-曱基聚苯乙烯脲 Ν-{3 -苯乙酿基- 5- (2-°塞吩基_乙酿基）-6, 6-二甲基 -4，6-二氫°比11各并[3，4-(：]〇比°坐-1-基}，1'1’-甲基聚苯乙稀脲 N-{3-(2 -萘）乙醯胺基-5-(2 -噻吩基-乙醯基）-6,6 -二曱基-4, 6 -二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(3 -溴）苯甲醯胺基-5-(2-噻吩基-乙醯基）-6,6 -二甲基-4, 6 -二氫吡咯并[3, 4-c]吡唑-l-基},Ν’ -甲基聚苯乙稀脲 Ν-{3 -環丙烷羧醯胺基-5-( 丁三丁酯基）-5-(2 -噻吩基-乙酿基）-6,6-二甲基-4,6-二氫D比^J各并[3,4-c]n比o坐-l-基}, Ν’ -甲基聚苯乙烯脲 Ν-{3-(4-氟）苯曱醯胺基-5-(2 -噻吩基-乙醯基）-6,6 -二曱基-4,6 -二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙C:\2D-C0DE\91-01\90119473.ptd Page 314 1327569 V. Description of invention (312) N_{3_(2 -Cai) Ethylamine _5_Ethyl _6,6_Dimethyl Base 4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-methyl polystyrene urea N-{ 3-(3-bromo)benzimidamide- 5-ethenyl-6,6-dimercapto-4,6-dihydropyrrolo[3,4-c]carbazole-1-*}, N'-mercaptopolystyrene urea N_{3_ Cyclopropyl burnt amine Amino 5-(_三丁 S基基)-5_乙牛基_6,6_ Dimercapto-4,6-dihydroindolo[3,4-c]pyrazole- 1-yl}, Ν'-methylpolystyrene-Ν-{3-(4-fluoro)benzoguanamine-5-ethenyl-6,6-dimercapto-4,6-di Hydropyrrolo[3,4-c]pyrazol-1-yl},Ν'-methylpolystyrene-indole-{3-(4-t-butyl)benzoguanamine-5-acetamidine 6,6-dimercapto-4,6-dihydroindole 11 and [3,4-〇]吼〇-1-yl}^'-mercaptopolystyrene-ruthenium-{3-benzene Ethyl-based 5-(2-°Septyl-ethyl)-6,6-dimethyl-4,6-dihydrogen ratio 11 and [3,4-(:]〇 ratio ° sitting -1-yl},1'1'-methyl polystyrene urea N-{3-(2-naphthyl)acetamido-5-(2-thienyl-ethenyl)-6,6- Dimethyl-4, 6-dihydropyrrolo[3,4-c]pyrazole-1-yl}, Ν'-mercaptopolystyrene uranyl-{3-(3-bromo)benzamide-5-(2 -thienyl-ethenyl)-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-l-yl},Ν'-methylpolystyrene Ν-{3-cyclopropanecarboguanamine-5-(butyltributyl)-5-(2-thienyl-ethenyl)-6,6-dimethyl-4,6-dihydrogen D The ratio of [3,4-c]n to o-l-yl}, Ν'-methylpolystyrene-hydrazone-{3-(4-fluoro)benzoguanamine-5-( 2-thiophenyl-ethenyl)-6,6-dimercapto-4,6-dihydropyrrolo[3,4-c]pyrazole-l-yl},Ν'-mercaptopolyphenylene

C: \2D-OODE\91-01\90119473.ptd 第315頁 1327569 五、發明說明（313) 烯脲 N-{3-(4-第三丁基）苯甲醯胺基-5-(2 -噻吩基-乙醯基） -6，6-二曱基-4，6-二氫口比17各并[3,4-〇]0比〇坐-1-基}，1'}’-曱基聚苯乙烯脲 N_{3 -苯乙酿基_5_乙基胺基|炭基-6，6_二曱基-4，6 -二氫吡咯并[3,4-c]吡唑-1-基},『-曱基聚苯乙烯脲 N_{3-(2_蔡）乙酿胺基-5-乙基胺基幾基-6，6_二曱基-4, 6 -二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯脲 ^^-{3-(3-溴）苯曱醯胺基-5-乙基胺基羰基-6,6-二曱基 -二氫吡咯并[3,4-c]咄唑-1-基}，Ν’-曱基聚苯乙烯脲 Ν - {3 -環丙烷羧醯胺基-5-(第三丁酯基）-5-乙基胺基羰基-6，6-二甲基-4，6-二氮〇比〇各弁[3，4_(3]11比〇坐-1-基}，1^’-甲基聚苯乙烯脲 N-{3-（4-氟）苯甲醯胺基-5-乙基胺基羰基_6, 6-二曱基 -4,6_二氫吡咯并[3,4-c]吡唑-1-基}，N’-甲基聚苯乙烯脲 N-{3-(4-第三丁基）苯曱醯胺基-5-乙基胺基羰基-6,6-二甲基-4, 6 -二氫吡咯并[3, 4-c]吡唑-l-基},Ν’ -曱基聚苯乙稀服苯乙酿基-5_乙基胺基幾基-6，6_二甲基-4，6 -二氣吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙烯脲 \-{3-(2_萘）乙醯胺基-5-乙基胺基羰基-6,6-二甲基-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 ^{3-(3-溴）苯甲醯胺基-5-乙基胺基羰基-6,6-二曱基 _4，6-二氫0比0各并[3，4-(：]0比〇坐-1-基}，1^’-曱基聚苯乙稀脈C: \2D-OODE\91-01\90119473.ptd Page 315 1327569 V. INSTRUCTIONS (313) Enurea N-{3-(4-t-butyl)benzimidamide-5-(2 -Thienyl-ethenyl) -6,6-dimercapto-4,6-dihydrogen port ratio 17 and [3,4-〇]0 is more than -1-yl}, 1'}'- Mercapto-polystyrene urea N_{3-phenylethyl ketone_5-ethylamino group|Carbonyl-6,6-dimercapto-4,6-dihydropyrrolo[3,4-c]pyrazole -1-yl}, "-mercaptopolystyrene urea N_{3-(2_Cai) Ethylamino-5-ethylaminomethyl-6,6-diindolyl-4,6-di Hydropyrrolo[3,4-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene urea^^-{3-(3-bromo)phenylhydrazinyl-5-ethylamino Carbonyl-6,6-dimercapto-dihydropyrrolo[3,4-c]oxazol-1-yl}, Ν'-mercaptopolystyrene uranium - {3-cyclopropanecarboxamide- 5-(T-butyl ester)-5-ethylaminocarbonyl-6,6-dimethyl-4,6-diazepine 〇[3,4_(3]11 than 〇-1 -yl},1^'-methylpolystyrene urea N-{3-(4-fluoro)benzimidamide-5-ethylaminocarbonyl-6,6-dimercapto-4,6_ Dihydropyrrolo[3,4-c]pyrazol-1-yl}, N'-methylpolystyrene urea N-{3-(4-t-butyl)benzoquinone 5-ethylaminocarbonyl-6,6-dimethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene Benzyl bromide-5-ethylamino benzyl-6,6-dimethyl-4,6-dioxapyrrolo[3,4-c]pyrazol-1-yl}, Ν'-曱Polystyrene urea\-{3-(2_naphthalene)acetamido-5-ethylaminocarbonyl-6,6-dimethyl-4,6-dihydropyrrolo[3, 4-c Pyrazol-1-yl}, Ν'-methyl polystyrene urea {3-(3-bromo)benzimidamide-5-ethylaminocarbonyl-6,6-diindenyl-4 , 6-dihydrogen 0 to 0 each and [3,4-(:]0 is more than -1-yl}, 1^'-mercaptopolystyrene

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N-{3 -環丙烷羧醯胺基-5-(第三丁酯基）-5-乙基胺基夢炭基-6,6-二曱基-4,6-二氫吡咯并[3,4-〇]吡唑-1-基}，~，、曱基聚苯乙烯脲五、發明說明（314) 1{3-(4-氟）苯甲醯胺基-5-乙基胺基羰基-6,6-二曱基 - 4, 6 -二氫咄咯并[3, 4-c]吡唑-l-基}，Ν’ -曱基聚苯乙烯服 Ν-{3-(4-第三丁基）苯曱醯胺基-5-乙基胺基羰基_6,6〜二曱基-4，6-二氫。比《1各并[3,4-(：]0比〇坐-1-基}，1^，-甲基聚笨乙烯脲 Ν-{3-苯乙醯基-5-乙基胺基羰基-6,6 -二曱基-4, 6 -二氣 °比咯并[3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲 Ν-{3-(2 -萘）乙酿胺基-5-乙基胺基叛基-6，6 -二甲基 6 -二氫呲咯并[3, 4-c]吡唑-l-基}，Ν’ -甲基聚苯乙歸脲 ’ 1{3-(3-溴）苯甲醯胺基-5-乙基胺基羰基-6,6-二甲基 -4,6-二氫吡咯并[3,4-(：]吡唑-1-基}，『-甲基聚苯乙烯服 Ν-{3 -環丙烷羧醯胺基-5-(第三丁酯基）-5-乙基胺基罗炭基_6，6 -二甲基一4,6_ 二氮0比略弁[3，4-c]0比0坐-1-基}，]\|，__ 曱基聚苯乙烯脲 N-{3-(4-氟）苯甲醯胺基-5-乙基胺基羰基-6, 6 -二甲基 -4’6 -二氫吡咯并[3, 4-c]吡唑-l-基}，Ν’ -甲基聚笨乙烯服 Ν-{3-(4-第三丁基）苯曱醯胺基-5-乙基胺基羰基_6,6_ 二甲基-4,6-二氫》比〇各并[3,4-(：]〇比"坐-1-基}^’-甲基聚笨乙缔服 Ν-{3 -苯乙醯基_5 -丁基胺基羰基-6, 6 -二曱基-4, 6 -二 0比咯并[3,4-c]咄唑-1-基}，1^ -甲基聚苯乙烯脲N-{3-cyclopropanecarboxamido-5-(t-butylester)-5-ethylaminomethane-6,6-dimercapto-4,6-dihydropyrrolo[3 , 4-〇]pyrazol-1-yl},~,, fluorenyl polystyrene urea, invention description (314) 1{3-(4-fluoro)benzimidamide-5-ethylamino Carbonyl-6,6-dimercapto-4,6-dihydroindolo[3,4-c]pyrazole-l-yl}, Ν'-mercaptopolystyrene clothing-{3-(4 -Tertibutyl) benzoguanamine-5-ethylaminocarbonyl-6,6~dimercapto-4,6-dihydro. Than 1 "[3,4-(:]0 is more than -1-yl}, 1^,-methyl polystyrene) - {3-phenethyl-5-ethylaminocarbonyl -6,6-dimercapto-4,6-diox-pyrolo[3,4-c]pyrazol-1-yl},Ν'-methylpolystyrene-ruthenium-{3-(2 -naphthyl)ethinyl-5-ethylamino-based t--6,6-dimethyl 6-dihydroindolo[3,4-c]pyrazole-l-yl}, Ν'- Poly(phenylene)-urea ' 1{3-(3-bromo)benzylidinium-5-ethylaminocarbonyl-6,6-dimethyl-4,6-dihydropyrrolo[3,4 -(:]pyrazol-1-yl},"-methylpolystyrene-{3-cyclopropanecarboxyguanamine-5-(t-butylester)-5-ethylamine-based charcoal Base _6,6-dimethyl- 4,6-dinitrogen 0 ratio slightly [3,4-c]0 to 0-spin-1-yl},]\|,__ decyl polystyrene urea N-{ 3-(4-fluoro)benzylidinium-5-ethylaminocarbonyl-6,6-dimethyl-4'6-dihydropyrrolo[3,4-c]pyrazole-l-yl },Ν'-Methyl polystyrene service-{3-(4-t-butyl)phenylhydrazinyl-5-ethylaminocarbonyl-6,6-dimethyl-4,6-di Hydrogen is more than 〇[3,4-(:]〇 ratio"sitting-1-yl}^'-methyl poly phenyl bromide-{3-phenethyl fluorenyl-5-butylamino carbonyl -6, 6 - two Yue-4, 6 - 20 than pyrrolo [3,4-c] Duo-1-yl}, 1 ^ - methyl polystyrene urea

1327569 五、發明說明（315) N-{3-(2 -萘）乙酿胺基-5 - 丁基胺基幾基-6,6_二曱基_4, 6 -二氫吡咯并[3,4-c]咄唑-1-*}，N’ -甲基聚苯乙烯脲 N-{ 3-(3 -溴）苯曱醯胺基-5 - 丁基胺基羰基-6, 6 -二曱基 -4,6-二氫。比咯并[3,4-(：]咄唑-1-基}，1')’-甲基聚苯乙烯脲 N_{3 -環丙烧缓酿胺基-5_(第三丁 S旨基）-5 - 丁基胺基罗炭基-6，6 -二曱基-4，6 -二氫 π比 11 各并[3,4-c] 0比。坐-1-基}，1^’ -曱基聚苯乙烯脲 N - {3_(4_敗）苯曱酿胺基_5_ 丁基胺基魏基-6，6_二曱基 -4，6-二氫0比°各并[3,4-(：]11比〇坐-1-基},1^’-甲基聚苯乙稀脲 N-{3-(4-第三丁基）苯曱酿胺基_5_ 丁基胺基幾基-6，6_ 二曱基-4, 6 -二氫吡咯并[3, 4-c]吡唑-1-基}，Ν’ -曱基聚苯乙稀脲實施例1 9 6，6 -二甲基-4，6 -二氫σ比ρ各并[3, 4 - c ] °比。坐衍生物之製備經由根據實施例1 1程序對實施例1 8化合物進行強鹼性水解，獲得下列化合物： 1^-{5-苯乙醯基-6,6-二甲基-4,6-二氫咄啶[3,4-〇]吡唑 -3-基}-(2_蔡）乙酿胺； Ν-{5 -苯乙醯基-6, 6 -二曱基-4, 6 -二氫吡啶[3, 4-c]咄唑 1 -基} - ( 3 -溴）苯曱醯胺； Ν-{5 -苯乙醯基-6,6-二甲基-4,6-二氫吡啶[3,4-(：]吼唑 -3-基}環丙烷羧醯胺； ^{5-苯乙醯基-6,6-二甲基-4,6-二氫吼啶[3,4-<:]吡唑 -3-基}-(4-氟）苯甲酿胺；1327569 V. INSTRUCTIONS (315) N-{3-(2-Naphthalene)ethanoyl-5-butylaminomethyl-6,6-didecyl-4,6-dihydropyrrolo[3] , 4-c]carbazole-1-*}, N'-methyl polystyrene urea N-{ 3-(3-bromo)benzoguanamine-5-butylaminocarbonyl-6,6- Dimercapto-4,6-dihydrogen. Bis-[3,4-(:]carbazol-1-yl},1')'-methylpolystyrene urea N_{3-cyclopropanol-supplementyl-5-(third-butyr )-5-butylaminocarboyl-6,6-dimercapto-4,6-dihydroπ ratio 11 each [3,4-c] 0 ratio. -1--1-yl}, 1^'-mercaptopolystyrene urea N - {3_(4_) phenyl hydrazone _5_ butylaminoweiyl-6,6-dimercapto-4, 6-Dihydrogen 0°°[3,4-(:]11 than 〇-1-yl}, 1^'-methylpolystyrene U-N-{3-(4-t-butyl Benzoquinone-based amine-5-butylaminomethyl-6,6-dimercapto-4,6-dihydropyrrolo[3,4-c]pyrazol-1-yl}, Ν'-fluorenyl Polystyrene urea Example 1 9 6,6-Dimethyl-4,6-dihydroσ ratio ρ and [3, 4 - c ] ° ratio. Preparation of the sitting derivative via the procedure according to Example 1 1 Strong alkaline hydrolysis of the compound of Example 18 gave the following compound: 1^-{5-phenethylamino-6,6-dimethyl-4,6-dihydroacridine [3,4-〇] Pyrazol-3-yl}-(2_cai)ethene; Ν-{5-phenethyl fluorenyl-6,6-dimercapto-4,6-dihydropyridine [3, 4-c]indole Iridazole 1-yl}-(3-bromo)phenylhydrazine; Ν-{5-phenethyl fluorenyl-6,6-dimethyl-4,6-dihydropyridine [3,4-(:]吼Zyridin-3-yl}cyclopropanecarboxamide; ^{5-phenethylamino-6,6-dimethyl-4,6-dihydroacridine [3,4-<:]pyrazole-3 -yl}-(4-fluoro)benzamide;

C:\2D-CODE\91-01\90119473.ptd 第318頁 1327569 五、發明說明（316) N-{5 -苯乙醯基-6,6-二曱基-4,6-二氫吡啶[3,4-(：]吡唑 _3_基}_(4_第三丁基）苯曱酿胺， !^-{5-乙醯基-6,6-二曱基-4,6-二氫0比咬[3,4-。]0比口坐 -3-基}苯乙醯胺； N-{5-乙醯基-6,6-二曱基-4,6-二氫吡啶[3,4-(：]吡唑 -3-基}-(2-萘）乙醯胺； _1_基}_(3_漠）苯曱酿胺 1H-NMR (DMS0-d6) d ppm: 8.2(t), 7.7-8.0(m), 4. 6(s), 2. 0(s), 1. 6(s)。 N-{5-乙醯基-6,6-二曱基-4,6-二氫11比咬[3,4-〇]0比〇坐 -3-基}環丙烷羧醢胺； 1^-{5-乙醢基-6，6-二曱基-4，6-二氫0比咬[3，4-(：]°比〇坐 _3_基}_(4_氣）苯曱酿胺； N-{5-乙醯基-6，6 -二曱基-4，6 -二氫0比咬[3，4-c] 0比0坐 -3-基}-(4-第三丁基）苯甲醯胺； Ν_{5-(2-°塞吩基-乙酿基）_6，6 -二甲基-4，6_二氫〇比°定 [3,4-c]吡唑-3 -基丨苯乙醯胺 N-{5-(2 -噻吩基-乙醯基）-6, 6 -二曱基-4, 6 -二氫咄啶 [3,4-c]吼唑-3-基}-(2 -萘）乙醢胺 1H-NMR (DMS0-d6) d ppm: 7.8-8(m), 7.4-7.6(m), 7. 2-7. 3(m)，4. 6(s), 1. 6(s)。 N-{5-(2 -噻吩基-乙醯基）-6, 6 -二甲基-4, 6 -二氳吡啶 [3, 4-c]吡唑-1-基}-(3 -溴）苯曱醯胺C:\2D-CODE\91-01\90119473.ptd Page 318 1327569 V. INSTRUCTIONS (316) N-{5-Phenylethenyl-6,6-dimercapto-4,6-dihydropyridine [3,4-(:]pyrazole_3_yl}_(4_t-butyl)benzoquinone, !^-{5-ethenyl-6,6-dimercapto-4,6 - Dihydrogen 0 to bite [3,4-.]0 is -3-yl}phenethylamine; N-{5-ethenyl-6,6-dimercapto-4,6-dihydrol Pyridine [3,4-(:]pyrazol-3-yl}-(2-naphthalene)acetamide; _1_yl}_(3_) benzoquinone 1H-NMR (DMS0-d6) d ppm : 8.2(t), 7.7-8.0(m), 4. 6(s), 2. 0(s), 1. 6(s). N-{5-Ethyl-6,6-didecyl -4,6-dihydrogen 11 than biting [3,4-〇]0 is more than -3-yl}cyclopropanecarboxamide; 1^-{5-ethenyl-6,6-dimercapto- 4,6-dihydrogen 0 ratio bite [3,4-(:]° than 〇3_base}_(4_gas) benzoquinone; N-{5-ethenyl-6,6- Dimercapto-4,6-dihydrogen 0 to bite [3,4-c] 0 to 0--3-yl}-(4-t-butyl)benzamide; Ν_{5-(2- °Cenyl-ethyl ketone)_6,6-Dimethyl-4,6-dihydroindole ratio [3,4-c]pyrazole-3-ylindoleacetamide N-{5- (2-thiophenyl-ethenyl)-6,6-dimercapto-4,6-dihydroacridine[3,4-c]oxazol-3-yl}-(2-naphthyl)acetamidine 1H-NMR (DMS0-d6) d ppm: 7.8-8 (m), 7.4-7.6 (m), 7. 2-7. 3 (m), 4.6 (s), 1. 6 (s). N-{5-(2-thiophenyl-ethenyl)-6,6-dimethyl-4,6-dipyridinyl[3,4-c]pyrazol-1-yl}-(3-bromo Benzoylamine

C:\2D-C0DE\91-01\90119473_ptd 第319頁 1327569 五、發明說明（317) ^{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶 [3, 4-c]吼唑-3 -基}環丙烷羧醯胺 1H-NMR (DMS0-d6) d ppm: 7.4-7.6(m), 6.8-7.0(m), 4.6(s)， 3.9(s), 0.8(m)。 ^}-{5-(2-°塞吩基-乙醯基）-6,6-二甲基-4,6-二氫0比〇定 [3,4-(：]"比唑-3-基}-(4-氟）苯曱醯胺 ^{5-(2-噻吩基-乙醯基）-6,6-二甲基-4,6-二氫吼啶 [3,4-c] 口比唑-3-基}-(4-第三丁基）苯曱醯胺 1^-{5-(4-氟苯甲醯基）-6,6-二甲基-4,6-二氫吼啶 |_3,4-(：]吡唑-3-基}苯乙醯胺 1^-{5-(4-氟苯甲醯基）-6,6-二曱基-4,6-二氫吡啶 [3,4-c]咄唑-3-基}-(2 -萘）乙醯胺 1^-{5-(4-氟苯曱醯基）-6,6-二甲基-4,6-二氫吡啶 [3, 4-c]吡唑-1-基}-(3 -溴）苯曱醯胺 1^-{5-(4-氟苯甲醯基）-6,6-二曱基-4,6-二氫》比啶 [3,4-c]吡唑-3-基}環丙烷羧醯胺 ^{5-(4-氟苯甲醯基）-6,6-二甲基-4,6-二氫咄啶 [3,4-c]吼唑-1-基}-(4-氟）苯曱醯胺 N-{5-(4-氟苯曱醯基）-6,6 -二曱基_4,6_二氫吡啶 [3，4_c] 0比0坐_3-基}_(4-第三丁基）苯甲酿胺 N_乙基-Ν’ _{3_苯乙酿胺基_6，6_二曱基-4，6 -二氣0比洛并[3, 4-c] Β比。坐-5-基}脲 Ν-乙基-Ν’ - {3-(2-萘）乙醯胺基-6,6-二曱基-4,6 -二氫 0比ρ各并[3，4 - c ] °比°坐-1 -基}脲C:\2D-C0DE\91-01\90119473_ptd Page 319 1327569 V. INSTRUCTIONS (317) ^{5-(2-Thienyl-ethenyl)-6,6-dimercapto-4,6- Dihydropyridine [3, 4-c]oxazol-3 -yl}cyclopropanecarboxamide 1H-NMR (DMS0-d6) d ppm: 7.4-7.6 (m), 6.8-7.0 (m), 4.6 (s ), 3.9(s), 0.8(m). ^}-{5-(2-°Shenyl-ethenyl)-6,6-dimethyl-4,6-dihydro 0-pyridin [3,4-(:]"Biazole- 3-yl}-(4-fluoro)benzoguanamine^{5-(2-thienyl-ethenyl)-6,6-dimethyl-4,6-dihydroacridine [3,4- c] Oroxazol-3-yl}-(4-t-butyl)benzamide 1^-{5-(4-fluorobenzhydryl)-6,6-dimethyl-4,6 - dihydroacridine|_3,4-(:]pyrazol-3-yl}phenethylamine 1^-{5-(4-fluorobenzhydryl)-6,6-dimercapto-4, 6-dihydropyridine [3,4-c]oxazol-3-yl}-(2-naphthyl)acetamide 1^-{5-(4-fluorophenylindenyl)-6,6-dimethyl 4-,6-dihydropyridine[3,4-c]pyrazol-1-yl}-(3-bromo)benzoquinone 1^-{5-(4-fluorobenzhydryl)-6 ,6-diamidino-4,6-dihydro"pyridinium[3,4-c]pyrazol-3-yl}cyclopropanecarboxamide^{5-(4-fluorobenzhydryl)-6 ,6-Dimethyl-4,6-dihydroacridine [3,4-c]oxazol-1-yl}-(4-fluoro)benzoguanamine N-{5-(4-fluorophenylhydrazine Indenyl)-6,6-dimercapto_4,6-dihydropyridine [3,4_c] 0 to 0 sitting _3-yl}_(4-t-butyl)benzamide N_ethyl -Ν' _{3_phenylethylamino-6,6-dimercapto-4,6-dialdehyde 0 piroxi[3,4-c] Β. sit-5-yl}urea- Ethyl-Ν' - {3-(2-naphthalene)acetamide Base-6,6-dimercapto-4,6-dihydrogen 0 ratio ρ and [3,4 - c ] ° ratio ° sit-1 -yl}urea

C:\2D-C0DE\91-01\90119473.ptd 第320頁 1327569 五、發明說明（318) lH-NMR(DMS0-d6)dppm:7.8-8(m),7.4-7.6(m),4· 3(s)，1. 6(s)，1. 0(t)。 N-乙基-Ν’ - {3-(3 -溴）苯曱醯胺基-6, 6 -二甲基-4, 6 -二氫吼p各并[3，4 - c ] D比。坐-1 -基}脲 N-乙基-Ν’ - {3 -環丙烷羧醯胺基-6, 6 -二曱基-4,6 -二氫 °比π各并[3，4 - c ] °比。坐-1 -基}脲 1H-NMR (DMS0-d6) d ppm: 4.6(s), 1. 75 - 7. 85 (m), 1. 6(s ) , l.O(t) o N-乙基-Ν’ - {3-(4-氟）苯甲醯胺基-6, 6 -二曱基-4, 6 -二氫π比p各并[3，4 - c ] D比。坐-1 -基}脲 1H-NMR (DMS0-d6) d ppm:8. 0 - 8. 2(m ) , 7.2-7.4(m), 4· 5(s), 3. 0-3. 2(m)，1· 6(s)，1. l(t)。 N_乙基- Ν’ - {3-(4-第三丁基）苯曱酿胺基-6，6-二曱基 -4,6-二氫°比11各并[3,4-(：]'1比°坐-1-基}脲 1H-NMR (DMS0-d6) d ppm: 8.0(d), 7.8(d), 4.6(s), 3. 0-3. 2(m), 1. 6(s)，0. 9(t)。 N- 丁基-Ν’ - {3 -苯乙醯胺基-6, 6 -二曱基_4, 6 -二氫吼咯并[3,4-c] °比。坐-5-基}脲 N- 丁基-Ν’ - {3-(2 -萘）乙醯胺基-6 ,6 -二曱基-4, 6 -二氫 0比ρ各并[3，4 - c ]吼°坐-1 -基}脲 1H-NMR (DMS0-d6) d ppm: 7.8-8(m), 7.4-7.6(m), 4. 3(s), 1.6(s), 0·9(t)。 N- 丁基-Ν’ - {3-(3 -溴）苯曱醯胺基-6, 6 -二甲基-4,6 -二氫吼略并[3，4 - c ] °比°坐-1 -基}脲C:\2D-C0DE\91-01\90119473.ptd Page 320 1327569 V. Description of Invention (318) lH-NMR (DMS0-d6) dppm: 7.8-8 (m), 7.4-7.6 (m), 4 · 3(s), 1. 6(s), 1. 0(t). N-ethyl-Ν' - {3-(3-bromo)benzoguanamine-6,6-dimethyl-4,6-dihydroindole p each [3,4 - c ] D ratio. Sodium-1 -yl}urea N-ethyl-Ν'-{3-cyclopropanecarbamoylamino-6,6-dimercapto-4,6-dihydrogen ratio π[3,4 - c ° ° ratio. 1 -H-NMR (DMS0-d6) d ppm: 4.6(s), 1. 75 - 7. 85 (m), 1. 6(s ) , lO(t) o N-ethyl -Ν' - {3-(4-fluoro)benzimidamide-6,6-dimercapto-4,6-dihydroπ ratio p and [3,4 - c ] D ratio. 1 -H-NMR (DMS0-d6) d ppm: 8. 0 - 8. 2 (m ) , 7.2-7.4 (m), 4 · 5 (s), 3. 0-3. (m), 1·6(s), 1. l(t). N_ethyl-Ν'-{3-(4-t-butyl)benzoquinone-amine-6,6-dimercapto-4,6-dihydrogen ratio 11 and [3,4-( :]'1°°-1-yl}urea 1H-NMR (DMS0-d6) d ppm: 8.0(d), 7.8(d), 4.6(s), 3. 0-3. 2(m), 1. 6(s),0. 9(t). N- butyl-Ν' - {3-phenylethylamino-6,6-dimercapto-4,6-dihydroindole[3 , 4-c] ° ratio. sit-5-yl}urea N-butyl-Ν' - {3-(2-naphthyl)acetamido-6,6-dimercapto-4,6-dihydrogen 0 ρ 并 [3,4 - c ] 吼 ° -1 - yl} urea 1H-NMR (DMS0-d6) d ppm: 7.8-8 (m), 7.4-7.6 (m), 4. 3 ( s), 1.6(s), 0·9(t). N-Butyl-Ν' - {3-(3-bromo)phenylhydrazinyl-6,6-dimethyl-4,6-di Hydrogen oxime and [3,4 - c ] ° ratio ° sit-1 -yl}urea

C:\2D-OODE\91-Ol\90119473.ptd 第321頁 1327569 五、發明說明（319) N - 丁基-Ν’ - {3 -環丙烷羧醯胺基-6, 6 -二曱基-4, 6 -二氫 °比°各并[3，4 - c ]"比°坐-1 -基}脲 1H-NMR (DMS0-d6) d ppm:4.6 (s), 3.0(t), 1.6(s), 0. 9(t)。 N -丁基—N，一 {3-(4-氟）苯甲醯胺基-6, 6 -二曱基一 4, 6 -二氫。比σ各并[3，4 - c ] °比β坐-1 -基}脲 1H-NMR (DMSO-d6) d ppm: 8.0-8.2(m), 7.2-7.4(m), 4.5(s), 3.0-3.2(m), 1.6(s), 1.2-1.3(m)，0.9(t)。 N - 丁基-Ν’ - {3-(4-第三丁基）苯曱醯胺基-6, 6-二甲基 4，6 -二氫吼p各并[3，4 - c ] p比嗤-1 -基}脲 1H-NMR (DMS0-d6) d ppm: 8.0(d), 7.8(d), 4.5(s), 3. 0-3. 2(πι)，1. 6(s), 0. 9(t)。實施例2 0 N-{3-(第三丁基-苯曱酿胺基）-6-(第三丁醋基）- 4, 5, 6, 7-四氫吡啶[3, 4-c]吡唑-1-基},Ν’ -甲基聚苯乙烯脲之製備第三丁基氯（24. 08毫莫耳，4. 5毫升）於10毫升無水二氯曱烷之溶液逐滴添加至先前於90毫升無水二氯曱烷及16. 5 毫升DIEA ( 96. 32毫莫耳）溶脹的Ν-{3-胺基-6-(第三丁酯 I基）-4,5,6,7_四氫吡啶[3,4-c]吡唑甲基聚苯乙烯脲（3. 0 1毫莫耳，3. 5克）。結果所得懸浮液於2 2 °C溫和攪拌1 8小時。然後樹脂經過濾，以二氯曱烷、甲醇洗滌及真空脫水。實施例2 1C:\2D-OODE\91-Ol\90119473.ptd Page 321 1327569 V. INSTRUCTIONS (319) N-Butyl-Ν'-{3-cyclopropanecarboxamido-6,6-didecyl -4,6-dihydrogen ratio °[3,4 - c ]" ratio °-1 -yl}urea 1H-NMR (DMS0-d6) d ppm:4.6 (s), 3.0(t) , 1.6(s), 0. 9(t). N-butyl-N,-{3-(4-fluoro)benzimidamide-6,6-dimercapto-4,6-dihydrogen. Ratio σ[3,4 - c ] ° ratio β sit-1 -yl}urea 1H-NMR (DMSO-d6) d ppm: 8.0-8.2(m), 7.2-7.4(m), 4.5(s) , 3.0-3.2 (m), 1.6 (s), 1.2-1.3 (m), 0.9 (t). N-butyl-Ν'-{3-(4-t-butyl)benzoguanamine-6,6-dimethyl 4,6-dihydroindole p and [3,4 - c ] p Specific 嗤-1 -yl}urea 1H-NMR (DMS0-d6) d ppm: 8.0(d), 7.8(d), 4.5(s), 3. 0-3. 2(πι), 1. 6(s ), 0. 9(t). Example 2 0 N-{3-(Third butyl-benzoinylamino)-6-(tributyl acetophenate)-4,5,6,7-tetrahydropyridine [3, 4-c] Preparation of pyrazol-1-yl}, Ν'-methyl polystyrene urea, third butyl chloride (24. 08 mmol, 4.5 ml) was added dropwise in 10 ml of anhydrous dichloromethane. To Ν-{3-amino-6-(t-butyl ester I-based)-4,5,6 previously swelled in 90 ml of anhydrous dichloromethane and 16.5 ml of DIEA (96.32 mmol) 7_tetrahydropyridine [3,4-c]pyrazole methyl polystyrene urea (3.01 mmol, 3.5 g). As a result, the resulting suspension was gently stirred at 22 ° C for 18 hours. The resin was then filtered, washed with dichloromethane, methanol and vacuum dried. Example 2 1

C:\2D-00DE\91-01\90119473.ptd 第322頁 1327569 五、發明說明（320) N-{3-(第三丁基-苯曱醯胺基）-4,5,6,7_四氫0比啶 [3, 4-c]吡唑-1-基}，Ν’ -甲基聚苯乙烯脲之製備如實施例7所述，經由使用三氟乙酸處理Ν-{3-(第三丁基-苯曱醯胺基）-6-(第三丁 S旨基）-4, 5, 6, 7 -四氫吼啶 [3,4-〇]"比唑-1-基}^’-曱基聚苯乙烯脲，獲得1{3-(第三丁基-苯曱醯胺基）-4,5,6,7 -四氫吼啶[3,4-c]咄唑-1-基}，Ν’ -甲基聚苯乙烯脲。實施例2 2 Ν-{3-(第三丁基-苯甲酿胺基）_6 -取代之_4，5，6，7 -四氫吼啶[3, 4-c]吼唑-1-基}, Ν’ -曱基聚苯乙烯脲之製備根據實施例8、9、1 0所述程序，經由使用適當羧酸、異氰酸酯、或磺醯氯處理Ν-{3-(第三丁基-苯甲醯胺基） -4,5,6,7-四氫吡啶[3,4-(：]吡唑-1-基},1^-曱基聚苯乙烯脲，獲得下列化合物： N-{ 3-(4-第三丁基-苯曱醯胺基）-6 -異丙基胺基羰基-4, 5,6,7-四氫吡啶[3,4-c]吡唑-6-基}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-第三丁基-苯曱醯胺基）-6-(2 -噻吩基）乙醯基 -4, 5, 6, 7-四氫咄啶[3, 4-c]咄唑-3-基}，Ν’ -曱基聚苯乙烯脲 1^-{3-(4-第三丁基-苯曱醯胺基）-6_乙醯基-4,5,6,7-四氫吡啶[3, 4-c]咄唑-3 -基}，Ν’ -曱基聚苯乙烯脲 Ν-{3_(4_第三丁基-苯曱酿胺基）_6-曱烧石黃酿基_4，5，6， 7-四氫吡啶[3,4-c]吡唑-3-*}，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-第三丁基-苯曱醯胺基）-6-乙基胺基羰基-4, 5,C:\2D-00DE\91-01\90119473.ptd Page 322 1327569 V. INSTRUCTIONS (320) N-{3-(Tertiary butyl-benzoguanamine)-4,5,6,7 Preparation of tetrahydro 0-pyridine [3, 4-c]pyrazol-1-yl}, Ν'-methyl polystyrene urea, as described in Example 7, treatment of hydrazine-{3- via trifluoroacetic acid (t-butyl-benzoguanamine)-6-(t-butylene)-4, 5, 6, 7-tetrahydroacridine [3,4-〇]" }}^'-mercaptopolystyrene, obtaining 1{3-(t-butyl-benzoguanamine)-4,5,6,7-tetrahydroacridine [3,4-c]咄Zin-1-yl}, Ν'-methyl polystyrene. Example 2 2 Ν-{3-(Third butyl-benzylamino)-6-substituted _4,5,6,7-tetrahydroacridine [3,4-c]carbazole-1- Preparation of Ν'-mercaptopolystyrene urea According to the procedure described in Examples 8, 9, 10, treatment of Ν-{3-(Third butyl via the use of a suitable carboxylic acid, isocyanate, or sulfonium chloride -benzimidamide) -4,5,6,7-tetrahydropyridine [3,4-(:]pyrazol-1-yl}, 1 - mercaptopolystyrene, the following compound was obtained: N -{ 3-(4-t-butyl-benzoguanamine)-6-isopropylaminocarbonyl-4,5,6,7-tetrahydropyridine[3,4-c]pyrazole-6 -yl},Ν'-mercaptopolystyrene-indole-{3-(4-t-butyl-benzoguanamine)-6-(2-thiophenyl)ethenyl-4, 5, 6 , 7-tetrahydroacridine [3, 4-c]oxazol-3-yl}, Ν'-mercaptopolystyrene urea 1^-{3-(4-t-butyl-benzoguanamine -6_Ethyl-4,5,6,7-tetrahydropyridine [3,4-c]carbazole-3-yl}, Ν'-mercaptopolystyrene uranium-{3_(4_ Tert-butyl-benzoquinone-based amine)_6-曱石石石黄基_4,5,6,7-tetrahydropyridine [3,4-c]pyrazole-3-*},Ν' -曱Polystyrene uranyl-{3-(4-t-butyl-benzoguanamine)-6-ethylamine Carbonyl-4, 5,

C:\2D-OODE\91-Ol\90119473.ptd 第323頁 1327569 五、發明說明（321) 6.7- 四氫吡啶[3,4<]°比°坐-6-基}，^-甲基聚苯乙烯脲 N-{3-(4-第三丁恭-苯曱酿胺基）_6_(3_曱基）丁酿基-4, 5, 6, 7 -四氫吡啶[3, 4-c]吼唑-3-基丨，Ν’ -曱基聚苯乙烯脲 Ν-{3-(4-第三丁基-苯曱醯胺基）-6-(2 -呋喃甲醯基）-4, 5.6.7- 四氫吡啶[3,4-〇]吼唑-3-基}，『-甲基聚苯乙烯脲 Ν-{3-(4-第三丁基"苯曱醯胺基）-6_笨乙醯基-4,5, 6, 7- 四氫咄啶[3,4-c]吡°坐-3-基}，『_甲基聚苯乙烯脲 1^-{3-(4-第三丁基_苯曱醯胺基）-6-甲基磺醯基-4,5,6, 7-四氫吡啶[3,4-c]"比°坐一3-基}，『-甲基聚苯乙烯脲 4 N-{3-(4-第三丁基-笨曱醯胺基）-4,5,6,7-四氫吡啶[3, 4-c]吡唑-3-基}-4-第三丁基-苯甲醯胺，N，-曱基聚苯乙烯脲實施例2 3 3-(第三丁基-笨甲醢胺基）_4，5，6，7-四氫0比0定[3，4-c] 吼°坐-6 -基衍生物之I備根據實施例11所述程序藉由實施例2 0化合物進行強驗性水解，獲得下列化合物： N -異丙基-N，-{3-（4-第三丁基-苯曱醯胺基）-4,5,6,7_ 四氫吼咬[3，4-〇]11比°坐-6-基}脲，111-關尺（01480-(16)(1 ppm: 7.90-7.47(m,4H), 4.41(s,2 Η ) ,3.75(m, 1 Η ), 3.47 (m，2H)，2.39(m，2H)，1.3(s，9H), 1.04(6Η)。 Ν-{6-(2-σ塞吩基）乙酿基-4，5，6，7-四氫0比咬[3，4-c] 〇比唑-3-基}-4-第三丁基-苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7. 9-7. 47(m, 4H), 4.58(m,2H), 4.04(s,2H), 3.71C:\2D-OODE\91-Ol\90119473.ptd Page 323 1327569 V. Description of invention (321) 6.7- Tetrahydropyridine [3,4<]°°°-6-yl},^-methyl Polystyrene urea N-{3-(4-Thirding-Benzene Benzylamino)_6_(3-fluorenyl) butyl- 4, 5, 6, 7-tetrahydropyridine [3, 4- c] carbazole-3-ylindole, Ν'-mercaptopolystyrene uranyl-{3-(4-t-butyl-benzoguanidino)-6-(2-furanylmethyl)- 4, 5.6.7-tetrahydropyridine [3,4-indolyl]oxazol-3-yl}, "-methyl polystyrene uranium-{3-(4-tert-butyl" benzoguanamine Base)-6_ 笨乙醯基-4,5, 6, 7-tetrahydroacridine [3,4-c]pyridin-3-yl}, "_methyl polystyrene urea 1^-{ 3-(4-t-butyl-benzoguanamine)-6-methylsulfonyl-4,5,6,7-tetrahydropyridine [3,4-c]" -yl}, "-methyl polystyrene urea 4 N-{3-(4-t-butyl-crackamine)-4,5,6,7-tetrahydropyridine [3, 4-c Pyrazol-3-yl}-4-tert-butyl-benzamide, N,-mercaptopolystyrene urea Example 2 3 3-(t-butyl-coomylamino)-4 5,6,7-tetrahydro 0 to 0 determines [3,4-c] 吼° sits -6-based derivative I prepared according to the procedure described in Example 11 Example 20 Compound was subjected to a vigorous hydrolysis to obtain the following compound: N-isopropyl-N,-{3-(4-t-butyl-benzoguanamine)-4,5,6,7-tetrahydrogen Bite [3,4-〇]11 than °S-6-base urea, 111-closed ruler (01480-(16) (1 ppm: 7.90-7.47 (m, 4H), 4.41 (s, 2 Η) , 3.75 (m, 1 Η ), 3.47 (m, 2H), 2.39 (m, 2H), 1.3 (s, 9H), 1.04 (6 Η). Ν-{6-(2-σsecenyl) Base-4,5,6,7-tetrahydro 0-bite [3,4-c]indazol-3-yl}-4-t-butyl-benzoguanamine; 1H-NMR (DMS0-d6 ) d ppm: 7. 9-7. 47(m, 4H), 4.58(m, 2H), 4.04(s, 2H), 3.71

C:\2D-00DE\91-01\90119473.ptd 第 324 頁 1327569 五、發明說明（322) (m，2H)，2. 44(m，2H), 1. 3(s，9H)。 N-{6-乙酿基_4，5，6，7-四氫0比咬[3，4-c] 〇比0坐-3-基}-4-第三丁基-苯曱醯胺； N-{6-曱烷磺醯基-4, 5, 6, 7-四氫吡啶[3, 4-c]吡唑-3 -基 }-4-第三丁基-苯曱醯胺；1H-NMR (DMS0-d6) d ppm: 7. 9 -7.47(m，4H)，4.3(s，2H)，3.40(m，2H)，3.94(s，3H), 2. 52(m, 2H)，1. 30(s, 9H)。 N-乙基-Ν’- {3-(4-第三丁基-苯甲醯胺基）-4，5,6, 7-四氫〇比咬[3，4-。]吼°坐-6-基}脲；1!1-關1^(1)^180-(16)(1??111: 7.90-7.47C4H), 4.41(s,2H), 3.49-3.04(m,4H), 2.38(m，2H), 1.30(s，9H)，1.01(t，3H)。 ~-{6-(3-甲基）丁酿基-4,5，6,7-四氫〇比咬[3,4-(：]口比〇坐 -3-基}-4-第三丁基-苯甲醯胺；1H-NMR (DMS0-d6) d p p m : 7. 9 1 - 7. 4 7 (m，4 Η)，4. 5 6 ( s，2 Η )，3. 6 2 - 2. 2 7 ( m，6 Η )， 1. 30(s，9H)，0· 88(m，6H)。 1{6-(2_0夫〇南甲醯基）-4,5,6,7-四氫0比0定[3,4-c]0比0坐 -3-基}-4-第三丁基-苯甲醯胺；1H-NMR (DMS0-d6) d ppm :7. 91-6. 62(m,7H), 3.82(m,2H), 2.56(m,2H), 1. 30(s，9H)。 N-{6-苯乙酿基_4, 5，6，7-四氮〇比咬[3，4-c] e比0坐_3-基} -4 -第三丁基-苯曱醯胺；1H-NMR (DMS0-d6) d ppm:7· 9 0 -7.29(m，9H)，4.6(2Η)，3.8(s，2H)，3.68(m，2H), 2.4(m，2H)，1.30(s，9H)。 N-{6-苯基石黃醯基_4，5，6，7-四氫n比咬[3，4-c] °比°坐_3_C:\2D-00DE\91-01\90119473.ptd Page 324 1327569 V. INSTRUCTIONS (322) (m, 2H), 2. 44 (m, 2H), 1. 3 (s, 9H). N-{6-ethyl-branched- 4,5,6,7-tetrahydro- 0 ratio bite [3,4-c] 〇 than 0--3-yl}-4-t-butyl-benzoguanamine N-{6-nonanesulfonyl-4,5,6,7-tetrahydropyridine[3,4-c]pyrazol-3-yl}-4-t-butyl-benzoguanamine; 1H-NMR (DMS0-d6) d ppm: 7. 9 -7.47 (m, 4H), 4.3 (s, 2H), 3.40 (m, 2H), 3.94 (s, 3H), 2. 52 (m, 2H) ), 1. 30 (s, 9H). N-ethyl-Ν'- {3-(4-t-butyl-benzylamino)-4,5,6,7-tetrahydroindole ratio [3,4-. ]吼°Sit-6-base}urea; 1!1-off 1^(1)^180-(16)(1??111: 7.90-7.47C4H), 4.41(s,2H), 3.49-3.04( m, 4H), 2.38 (m, 2H), 1.30 (s, 9H), 1.01 (t, 3H). ~-{6-(3-Methyl)-butanyl-4,5,6,7-tetrahydroindole ratio bite [3,4-(:] mouth 〇 -3--3-yl}-4-third Butyl-benzamide; 1H-NMR (DMS0-d6) dppm: 7. 9 1 - 7. 4 7 (m, 4 Η), 4. 5 6 (s, 2 Η ), 3. 6 2 - 2. 2 7 ( m,6 Η ), 1. 30(s,9H),0· 88(m,6H). 1{6-(2_0夫〇南甲醯基)-4,5,6,7 - tetrahydro 0 to 0 definite [3,4-c] 0 to 0 -3-yl}-4-t-butyl-benzamide; 1H-NMR (DMS0-d6) d ppm : 7.91 -6. 62(m,7H), 3.82(m,2H), 2.56(m,2H), 1. 30(s,9H). N-{6-phenylethylidene_4, 5,6,7 - tetraziridine ratio bite [3,4-c] e is 0 to _3-yl} -4 -t-butyl-benzoguanamine; 1H-NMR (DMS0-d6) d ppm:7· 9 0 -7.29 (m, 9H), 4.6 (2 Η), 3.8 (s, 2H), 3.68 (m, 2H), 2.4 (m, 2H), 1.30 (s, 9H). N-{6-phenyl sulphate _ 4,5,6,7-tetrahydron ratio bite [3,4-c] ° ratio ° sitting_3_

C:\2D-OODE\91-01\90119473.ptd 第325頁 1327569 五、發明說明（323) 基}-4_第三丁基-苯甲酿胺； N-{6-(嗜琳-8-績醯基）-4, 5，6，7 -四氫吼°定[3，4-c]吼〇坐 -3-基}-4-第三丁基-笨曱醯胺；1}1-關1?(0乂30-(16)(1??111 :8. 9-7. 47(m, 1 OH), 4.6(2H), 3.56(m,2H), 2.26(m,2H), 1. 30(s, 9H)。實施例24 N-{ 3-(4-第三丁基）苯甲醯胺基-5-( 3-曱基丁基）-4, 6-二氫吡咯并[3,4-c]吡唑-i-*}，N，-甲基聚苯乙烯脲之製備 _!^-{3-(4-第三丁基）笨曱酿胺基-4,6-二氫吼11各并 [3,4-<:]〇比唑_1-基}，1\1’-曱基聚苯乙烯脲（0.086毫莫耳， 100毫克）於4毫升無水DMF/乙醇（3:1)溶脹及使用異戊醛 (0. 86毫莫耳，74· 1毫克）及硼烷-吡啶錯合物（BAP)(〇. 86 毫莫耳，79.9毫克）處理。混合物於22°C於氬氣氣氛下溫和震搖4日。然後樹脂經過濾，以DMF/乙醇、DCM及MeOH洗滌及真空脫水。以類似方式可製備下列化合物： N - {3-(4-第三丁基）苯甲酿胺基-5-(2-苯基乙基）-4，6_ _二氫吼11 各并[3，4-c] °比》坐-1-基}，1^’ -曱基聚苯乙烯脲 N-{3-(4-第三丁基）苯曱醯胺基-5-[2-(2 -噻吩基）乙基] _4，6 -二氫p比略并[3，4-c] °比°坐基丨，Ν’ -曱基聚苯乙稀脲實施例25 3-(第三丁基-苯曱醯胺基）-4,6 -二氩咄咯并[3,4-c]吡唑-5 -烷基衍生物之製備C:\2D-OODE\91-01\90119473.ptd Page 325 1327569 V. Description of the invention (323) base}-4_t-butyl-benzamide; N-{6-(嗜琳-8 - 醯基基)-4, 5,6,7-tetrahydroindole ° [3,4-c] -3--3-yl}-4-tert-butyl-crackamine; 1}1 -Off 1?(0乂30-(16)(1??111:8. 9-7.47(m, 1 OH), 4.6(2H), 3.56(m,2H), 2.26(m,2H) , 1. 30(s, 9H). Example 24 N-{ 3-(4-Terbutyl)benzimidamide-5-(3-mercaptobutyl)-4,6-dihydropyrrole And [3,4-c]pyrazole-i-*}, preparation of N,-methyl polystyrene urea _!^-{3-(4-t-butyl) awkward amine-4 6-Dihydroindole 11 each [3,4-<:]pyrazole-1 -yl},1\1'-mercaptopolystyrene (0.086 mmol, 100 mg) in 4 ml of anhydrous DMF/ethanol (3:1) swell and treated with isovaleraldehyde (0.86 mmol, 74. 1 mg) and borane-pyridine complex (BAP) (〇. 86 mM, 79.9 mg) The mixture was gently shaken at 22 ° C for 4 days under an argon atmosphere. The resin was then filtered, washed with DMF / ethanol, DCM and MeOH and vacuum dried. The following compound was prepared in a similar manner: N - {3-(4 - tert-butyl) benzene Acrylamino-5-(2-phenylethyl)-4,6_-dihydroindole 11 each [3,4-c] ° ratio -1-yl}, 1^'-fluorenyl polyphenylene Ethylene urea N-{3-(4-t-butyl)phenylhydrazino-5-[2-(2-thiophenyl)ethyl] _4,6-dihydrop ratio is slightly [3,4- c] ° ratio 坐丨, Ν '-mercapto polystyrene urea Example 25 3-(t-butyl-benzoguanidino)-4,6-diarhydronium [3,4 -c]Preparation of pyrazole-5-alkyl derivative

Ο:\2ϋ-ΟΟΟΕ\91-Ο1\90119473.ptd 第 326 頁 1327569 五、發明說明（324) 根據貫施例1 1所述程序，藉由實施例2 2化合物之強鹼處理，獲得下列化合物： N-{5-異戊基-4,6-二氫咄咯并[3,4_c]吡唑_3_基卜4_第三丁基-苯曱醯胺 1H-NMR (DMS0-d6) d ppm：7.9-7 8(m)1 27 5-7 4(m) ;4.〇-3.8(m);1.7-1.6(m);1.5-l.4(m);1：3〇(s)；〇i9〇(d) 氫0比D各并[3, 4-c]"比唑-3-基}-4-第 N- { 5-苯乙基-4, 6- 三丁基-苯甲醯胺 1H-NMR (DMS0-d6) d PPm：7.9-?.8(m);7. 5-7.4(m) M m);4.0-3.8(m);3·卜2.8⑷;1.3〇(s)。 1其__楚嘆吩—2_基乙基）—4,6~二氫"比略并[3,4-c]吼峻 1 Q9 R。二丁基_ 苯甲醯胺；1H~NMR (DMS〇_d6) d PP«n:7.92-6.92 (m，7I〇, 32 實施例26 Λ 1·«Η9Η;Ο:\2ϋ-ΟΟΟΕ\91-Ο1\90119473.ptd Page 326 1327569 V. INSTRUCTIONS (324) According to the procedure described in Example 1 1 , the following compound was obtained by treatment with a strong base of the compound of Example 2 2 : N-{5-Isoamyl-4,6-dihydroindolo[3,4_c]pyrazole_3_ylbu-4_t-butyl-benzoguanamine 1H-NMR (DMS0-d6) d ppm: 7.9-7 8 (m) 1 27 5-7 4 (m); 4. 〇-3.8 (m); 1.7-1.6 (m); 1.5-l.4 (m); 1:3 〇 ( s); 〇i9〇(d) Hydrogen 0 to D and [3, 4-c]"Bizozol-3-yl}-4-N-{ 5-phenethyl-4,6-tributyl 1 - benzylamine 1H-NMR (DMS0-d6) d PPm: 7.9-?.8 (m); 7. 5-7.4 (m) M m); 4.0-3.8 (m); 3 · 2.8 (4) ; 1.3〇(s). 1 its __ Chu sings - 2_ yl ethyl) - 4,6 ~ dihydro " ratio slightly [3,4-c] 吼 1 1 Q9 R. Dibutyl-benzamide; 1H~NMR (DMS〇_d6) d PP«n: 7.92-6.92 (m, 7I〇, 32 Example 26 Λ 1·«Η9Η;

第327頁 1 3-fe基- 4，6 -二氛d比叹丑「Qj 三丁則-乙酿之製備开[3, 4'小比唾―1，5_二缓酸5_第氣破酸乙自旨（8 n n .Page 327 1 3-fe base - 4,6 - two atmosphere d than sigh "Qj three Ding - the preparation of the brewing [3, 4 'small than saliva -1,5_ two slow acid 5_ gas Broken acid B from the purpose (8 nn.

[3，L m = 二氯-1Η 十各开 nTFArq? ^ .。羧馱第二丁酯（20克，89毫莫耳）及 2 升’ 528毫莫耳）於thf( 5 00毫升）之混合物。反應於同溫維持2小時然後讓反應達到室溫及攪拌隔夜。結果所得混合物真空蒸發至乾。殘餘物以乙酸乙酯及水萃取。有機相經分離，以硫酸鈉脫水及蒸發至乾。混合物藉 1327569[3, L m = dichloro-1 Η ten open nTFArq? ^ . A mixture of butyl carboxamide (20 grams, 89 millimoles) and 2 liters '528 millimoles) in thf (500 ml). The reaction was maintained at the same temperature for 2 hours and then allowed to reach room temperature and stirred overnight. The resulting mixture was evaporated to dryness in vacuo. The residue was extracted with ethyl acetate and water. The organic phase was separated, dried over sodium sulfate and evaporated to dryness. Mixture 1327569

五、發明說明（325) 急速層析術純化（洗提劑：乙酸乙醋/環己烧4 / 6至7 / 3 )彳it彳® 19克（72%產率）標題化合物呈白色固體。 & $ 實施例2 7 3-(2 -萘-2-基-丙醯胺基）-4,6 -二氫吡咯并[3, 4__c] n比唾 -1，5 -二羧酸5 -第三丁酯卜乙酯之製備於2-萘-2-基-丙酸（1. 48克，7. 4毫莫耳）於DCM(4〇毫升）及DMF催化劑之溶液内逐滴加入（c〇Cl )2(0. 83毫升，9 65 毫莫耳）於DCM ( 1 〇毫升）。混合物於室溫搜拌3 〇分鐘。反靡混合物經真空濃縮，以曱苯重新調製兩次及濃縮。所得^ 4·基氯於THF(40毫升）之溶液於〇-5。(：緩慢添加至3_胺基 -4,6-二氫吡咯并[3,4-(：]吡唑-1，5-二綾酸5_第三丁酯1_ 乙酯（2.0克’6.75毫莫耳）及〇1£六（5.8毫升，33.3毫莫耳）於THF (40毫升）之混合物。讓反應達到室溫及攪拌隔夜。混合物經過濾，溶液真空蒸發至乾。結果所得殘餘物溶解於DCM，所得溶液以鹽水洗滌，以硫酸鈉脫水，過濾及蒸發至乾。粗產物藉急逮層析術純化（洗提劑：乙酸乙酯/環己烷3/7然後4/6)獲得3. 〇克（93%產率）標題化合物呈白色固體。 11實施例2 8 3-(2-萘-2-基-丙醯胺基）_5 6_二氫_4H_吡咯并[3 4_c] 吡唑-1 -羧酸乙酯之製備 2.5克（5.2毫莫耳）3-(2-萘-2 -基-丙醢胺基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-1，5_二羧酸5_第三丁酯卜乙酯於15亳升DCM使用16毫升（1:1) TFA/DCM處理。反應混合物攪拌3〇V. Inventive Note (325) Purification by flash chromatography (eluent: ethyl acetate/cyclohexane 4/6 to 7 / 3 ) 彳it®® 19 g (72% yield) of title compound as white solid. & $ Example 2 7 3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydropyrrolo[3,4__c] n than saliva-1,5-dicarboxylic acid 5 - The preparation of the third butyl ester ethyl ester was added dropwise to a solution of 2-naphthalen-2-yl-propionic acid (1. 48 g, 7.4 mmol) in DCM (4 mL) and DMF catalyst ( c〇Cl ) 2 (0. 83 ml, 9 65 mmol) in DCM (1 mL). The mixture was mixed at room temperature for 3 minutes. The ruthenium mixture was concentrated in vacuo and re-digested twice with benzene and concentrated. A solution of the obtained chlorobenzene in THF (40 mL) was obtained from EtOAc. (: Slowly added to 3_amino-4,6-dihydropyrrolo[3,4-(:]pyrazole-1,5-dioxalate 5_t-butyl ester 1_ethyl ester (2.0 g '6.75 </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> </ RTI> <RTIgt; Dissolved in DCM, the~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~ Obtained 3. gram (93% yield) of the title compound as a white solid. 11 Example 2 8 3-(2-naphthalen-2-yl-propanylamino)-5 6-dihydro-4H-pyrrolo[3 4_c] Preparation of pyrazole-1-carboxylate ethyl ester 2.5 g (5.2 mmol) 3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydropyrrolo[3, 4 -c]pyrazole-1,5-dicarboxylic acid 5_t-butyl ester ethyl ester was treated in 15 ml of DCM using 16 ml (1:1) TFA/DCM.

C:\2D-CODE\91.01\90ll9473_ptdC:\2D-CODE\91.01\90ll9473_ptd

第328頁 1327569 五、發明說明（326) '--- 分鐘及蒸發至乾。結果所得殘餘物溶解於DCM ’溶液以鹽水洗務然後以碳酸氫鈉水溶液處理。所得沉澱經過濾，以水及DCM洗滌然後真空脫水獲得2· 〇克（定量產率）標題化合物。。貫施例2 9 Ν-{5-〇底咬-1-基）二基曱醢基二氫"比嘻并[3,4-c] 0比σ坐-3-基}-3-(2-萘-2-基）-丙醢胺基之製備氣曱酸4 -硝基笨酯（〇· 213克，1. 〇6毫莫耳）於無水THF (10毫升）之溶液逐滴添加至3-(2-萘-2-基-丙醯胺基） -5,6 -二氫- 4H-°比咯并[3,4-c]咄唑-1-羧酸乙酯（0.4克， 1.〇6毫莫耳）及1)1£人（0.184毫升，1.〇6毫莫耳）於無水<11^ C 1 〇毫升）之溶液。結果所得懸浮液於室溫攪拌約4小時。蒸發去除溶劑後，反應混合物溶解於DCM，以水洗滌，以硫酸鈉脫水及蒸發獲得黃色固體（〇 · 5 5克，定量）^固體溶解於乙腈（15毫升），使用4_DMAP(130毫克，1. 〇6毫莫耳）及哌啶（2. 75毫莫耳，〇. 27毫升）處理。反應混合物回流於 24小時’蒸發，溶解於DCM，以1N氫氧化鈉、鹽水、〇. 1N 鹽酸、鹽水洗滌，以硫酸鈉脫水’過濾及蒸發。使用 DCM/MeOH 95 : 5作為洗提劑於矽膠進行層析術純化後獲得標題化合物（0. 115克，26%產率）。 1H-NMR (DMS0-d6) d ppm:7.8-7.5(m)；4.4(m);4.0(m); 3.1(m);1.5(m)。以類似方式始於適當胺可製備下列衍生物： N，N-二甲基-Ν’ - {3-(2 -萘-2 -基-丙醯胺基）-4,6 -二氫吼Page 328 1327569 V. INSTRUCTIONS (326) '--- Minutes and evaporation to dryness. As a result, the obtained residue was dissolved in DCM' solution, washed with brine and then treated with aqueous sodium hydrogen carbonate. The resulting precipitate was filtered, washed with water and DCM and then evaporated in vacuo to give the title compound. . Example 2 9 Ν-{5-〇底 bit-1-yl)diylindenyldihydro"比嘻[3,4-c] 0 than σ sit-3-yl}-3-( Preparation of 2-naphthalen-2-yl)-propanylamine group 4-nitrosoester of citric acid (〇·213 g, 1. 〇6 mmol) added dropwise in anhydrous THF (10 ml) To 3-(2-naphthalen-2-yl-propionylamino)-5,6-dihydro-4H-°-pyrolo[3,4-c]indazole-1-carboxylic acid ethyl ester (0.4 g 1, 〇 6 mM) and 1) 1 £ person (0.184 ml, 1. 〇 6 mmol) in anhydrous <11^C 1 〇 ml). As a result, the resulting suspension was stirred at room temperature for about 4 hours. After evaporating to remove the solvent, the mixture was crystalljjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjjj 〇 6 mM) and piperidine (2.75 mmol, 〇. 27 ml). The reaction mixture was evaporated to dryness EtOAc (EtOAc)EtOAc. The title compound (0.115 g, 26% yield). 1H-NMR (DMS0-d6) d ppm: 7.8-7.5 (m); 4.4 (m); 4.0 (m); 3.1 (m); 1.5 (m). The following derivatives can be prepared starting from the appropriate amine in a similar manner: N,N-dimethyl-oxime-{3-(2-naphthalen-2-yl-propionamido)-4,6-dihydroindole

C: \2D-CDDE\91 -01 \90119473 .ptd 第329頁 1327569 五、發明說明（327) 咯并[3, 4-c]毗唑-5-基}脲 1H-NMR (DMS0-d6) d ppm:7.8-7.5(m)；4.4(m);4.0(m) ;2.8(s);1·5(d)。 1^，1^-二曱基-1^-{3-(2-苯基-吡唑-4-基）乙酿胺基-4,5, 6, 7 -四氫吡啶[3, 4-c]吡唑-5 -基}脲；1H-NMR (DMS0-d6) dppm: 2. 60-2.75(m,6H),3.30(t,2H),3.82(sJ2H),4.10(s, 2H)，7.40-7.55(m, 4H ) ,7.85-7.95( m，2H)。調配例實施例1 :乾膠囊劑 t 5 0 0 0個膠囊各含〇. 2 5克先前各實施例所述式（I )化合物之一作為活性成份，膠囊劑製備如後： -組成活性成份1 25 0克 *滑石1 8 0克 -小麥澱粉120克 -硬脂酸鎂8 0克 -乳糖2 0克製備方法：所述粉狀物質加壓通過篩目寬度〇 6毫来之筛。每份0.33克混合物借助於膠囊填袈填&於^。 ^施例2:軟膠囊劑旲展7、膠嚴 M00個軟明膠膠囊劑各含0.05克先前各實施例所述式 (I)化合物之一作為活性成份，膠囊劑製 -組成活性成份250克後. -月桂二醇2升製備方法：粉狀活性成份懸浮於月桂二醇C: \2D-CDDE\91 -01 \90119473 .ptd Page 329 1327569 V. INSTRUCTIONS (327) Cyclo[3,4-c]pyrazole-5-yl}urea 1H-NMR (DMS0-d6) d ppm: 7.8-7.5 (m); 4.4 (m); 4.0 (m); 2.8 (s); 1.5 (d). 1^,1^-dimercapto-1^-{3-(2-phenyl-pyrazol-4-yl)ethanoyl-4,5,6,7-tetrahydropyridine [3, 4- c]pyrazole-5-yl}urea; 1H-NMR (DMS0-d6) dppm: 2. 60-2.75 (m, 6H), 3.30 (t, 2H), 3.82 (sJ2H), 4.10 (s, 2H) , 7.40-7.55 (m, 4H), 7.85-7.95 (m, 2H). Formulation Example 1 : Dry capsules t 5 0 0 capsules each containing 〇. 2 5 g of one of the compounds of the formula (I) described in the previous examples as active ingredients, capsule preparation as follows: - composition of active ingredients 1 25 0 g * talc 1 80 g - wheat starch 120 g - magnesium stearate 80 g - lactose 20 g Preparation method: The powdery substance is pressurized through a mesh having a mesh width of 6 m. Each 0.33 gram of the mixture was filled with & ^Example 2: Soft capsules 旲、, 胶 M M 00 soft gelatin capsules each containing 0.05 grams of one of the compounds of formula (I) described in the previous examples as active ingredients, capsules - composed of active ingredients 250 grams After. -Lauryl diol 2 liter preparation method: powdery active ingredient suspended in lauryl diol

1327569 五、發明說明（328) -- (LauroglykoU)(月桂酸丙二醇酷，蓋特福思（GaUef〇ss) 公司，國聖普理斯特）及於濕粉化器研磨至粒徑約丨至3 克。每份各0. 41 9克混合物利用膠囊填裝劑填裝入軟明膠膠囊劑。實施例3 :軟膠囊劑 5000個軟明膠膠囊劑各含〇. 〇5克先前各實施例所述式 (I)化合物之一作為活性成份，膠囊劑製備如後： -組成活性成份250克 -PEG 400 1 升 -呑恩8 0 1升製備方法：粉狀活性成份懸浮於PEG 4 0 0 (分子量3 8 〇至約 420之聚乙二醇，西革瑪、福卡（Fluka)、亞利敘 . (Aldrich)美國公司及吞恩8〇(聚氧桂酸雖，亞特拉斯(AtUs)化學公司，美國，：西糖:-月福卡、亞利敘供給)於濕粉化器研磨至粒徑約：：、 J份各0. 43克混合物利用膠囊填裝劑填裝入軟明膠膠未囊1327569 V. INSTRUCTIONS (328) -- (LauroglykoU) (Glycol laurate, GaUef〇ss, St. Louis) and grinding in a wet powderizer to a particle size of about 丨3 grams. Each portion of 0.441 g of the mixture was filled with a soft gelatin capsule using a capsule filling agent. Example 3: Soft capsules 5000 soft gelatin capsules each containing 〇. 5 g of one of the compounds of the formula (I) described in the previous examples as the active ingredient, and the capsules were prepared as follows: - 250 g of the active ingredient - PEG 400 1 liter-呑恩8 0 1 liter Preparation: Powdered active ingredient suspended in PEG 40 (Polyethylene glycol with a molecular weight of 3 8 〇 to about 420, Sigma, Fluka, Yali Syria. (Aldrich) American company and Thun 8 〇 (Polyoxylic acid, Atlas Chemical Company, USA,: West Sugar: - Moon Fuka, Yarisu supply) in wet powderizer Grinding to a particle size of about::, J parts each 0. 43 grams of the mixture filled with soft gelatin gel without capsules

13275691327569

C:\2D-O0DE\91-01\90119473.ptd 第332頁C:\2D-O0DE\91-01\90119473.ptd第332页

Claims

一種式（I)雙環唯。坐化合物： HNA formula (I) double ring only. Sitting compound: HN

(CHzJm (CH2)n Ο) Ob 其中 R及心為相同或相異且分別為氫原子或視需要經取代基團選自R’ 、-COR’ 、-CQOR’ 、-CONHR，、-CONR，R"、 -S02R’ 、-S02NHR’或-S02NR’ R";其中R，及R"為相同或相異且分別係選自氫或視需要經進一步取代之直鏈或分支C广C6 烷基、芳基、C3-P6環焼基及芳基Q -c6烧基或R’及R"共同形成C4_ C6伸烧基鍵； Ra、Rb、Rc及Rd為相同或相異且分別係選自氫、視需要進一步經取代之直鏈或分支鏈心-C6烷基、芳基、芳基Cl -〇6 炫基或-CHaOR’基，其中R’定義如前，.或Ra及以及/或Rc及 Rd與其鍵結之碳原子共同形成一個視需要經取代之& 環烷基；其中該芳基為芳香族碳環系芳基或雜環系芳基，且該芳香族碳環系芳基包括苯基.、碎基·、聯苯萆基、苟基、U。-二氯惠基…基苯基、四：基Ί 異㈣琳基笨基’及該雜‘環系芳基包括、㈣基'味唾基、“并…心本ΐ、噻唑基、異噻唑基、°比咯基、呋喘基、其本并四氫呋味基、1唑基、異3唑基…比唑基、礼雜⑬基、噻吩基、苯并噻吩基、異叫哚啉基、苯并(CHzJm (CH2)n Ο) Ob where R and the core are the same or different and are each a hydrogen atom or, if desired, a substituent group selected from the group consisting of R', -COR', -CQOR', -CONHR, , -CONR, R", -S02R', -S02NHR' or -S02NR' R"; where R, and R" are the same or different and are respectively selected from hydrogen or, if desired, further substituted linear or branched C-C6 alkyl , aryl, C3-P6 cyclodecyl and aryl Q-c6 alkyl or R' and R" together form a C4_C6 extended alkyl bond; Ra, Rb, Rc and Rd are the same or different and are respectively selected from Hydrogen, optionally substituted linear or branched chain -C6 alkyl, aryl, aryl Cl -〇6 leumino or -CHaOR' group, wherein R' is as defined above, or Ra and/or Rc and Rd together with the carbon atom to which they are bonded form an optionally substituted & cycloalkyl group; wherein the aryl group is an aromatic carbocyclic aryl group or a heterocyclic aryl group, and the aromatic carbocyclic aryl group The group includes a phenyl group, a fragment, a biphenyl fluorenyl group, a fluorenyl group, and a U group. - Dichloromethyl phenyl phenyl, tetra yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl yl Base, ° pyryl, furazolyl, its tetrahydrofurfuryl, 1-oxazolyl, iso-oxazolyl...bazolyl, aryl 13-, thienyl, benzothienyl, iso-porphyrin Base, benzo

90119473(替換）-3.ptc 第333頁 1327569 案號901U3 曰修- MAR 1 2 2010 替換頁六、申請專利範圍咪唑基、四唑基、吡咯啶基四唑基、喳啉基、異喳琳基、 2，6 -二苯基咄啶基、喳1啉基、咄畊基、苯基喳啉基、苯基咬°贄基、1，2, 3 -三嗤基、1-苯基-1,2,3 -三唾基；以及 R、&、R’及R”、Ra、Rb、Rc及Rd於任何一個自由位置可進一步視需要藉一或多個選自下列之基團取代：鹵原子，硝基’氧基（ = 0)，羧基，氰基，烷基，全氟化烷基，烯基’炔基’環烷基，芳基，雜環基，胺基及其衍生物，包括烧基胺基、二烧基胺基、芳基胺基、二芳基胺基、脲基、烧基脈基及方基服基，綠基胺基及其衍生物，包括曱胺基、烷基羰基胺基、烯基羰基胺基、芳基羰基胺基、烧氧幾基胺基、磺醢胺基、烧基續醯胺基及芳基績酿胺基’羥基及其衍生物，包括烷氧基、芳氧基、烷基羰基氧基、芳基羰基氧基、環烯基氧基及亞烷基胺基氧基；羰基及其衍生物，包括烷基羰基、芳基羰基、烷氧羰基、芳氧獄基、％•烧氧幾基、胺基叛基、炫基胺基幾基、二烧基胺基幾基；硫化衍生物’包括烷硫基、芳硫基、烷基磺醯基、芳基磺醯基、烷基亞磺醯基、芳基亞磺醯基、芳基磺90119473 (replacement)-3.ptc Page 333 1327569 Case No. 901U3 曰修 - MAR 1 2 2010 Replacement Page VI, Patent Application Range Imidazolyl, tetrazolyl, pyrrolidinyltetrazolyl, porphyrinyl, isoindole , 2,6-diphenylacridinyl, 喳1 phenyl, hydrazine, phenyl porphyrin, phenyl phthalate, 1,2,3-trimethyl, 1-phenyl- 1,2,3-tris-sodium; and R,&, R' and R", Ra, Rb, Rc and Rd may be further substituted at any free position by one or more groups selected from the group consisting of : halogen atom, nitro 'oxy (= 0), carboxyl, cyano, alkyl, perfluorinated alkyl, alkenyl 'alkynyl' cycloalkyl, aryl, heterocyclic, amine and its derivatives And include an alkylamino group, a dialkylamino group, an arylamine group, a diarylamine group, a urea group, a decyl group and a aryl group, a green amine group and derivatives thereof, including a guanamine Base, alkylcarbonylamino group, alkenylcarbonylamino group, arylcarbonylamino group, alkoxyamino group, sulfonylamino group, alkyl group and aryl group, hydroxyl group and its derivative Matter, including alkoxy groups, Oxyl, alkylcarbonyloxy, arylcarbonyloxy, cycloalkenyloxy and alkyleneaminooxy; carbonyl and its derivatives, including alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxy Prison base, %•Oxygen-based, amine-based thiol, leucine-based, dialkylamino group; sulfurized derivatives 'including alkylthio, arylthio, alkylsulfonyl, aromatic Sulfosyl, alkylsulfinyl, arylsulfinyl, arylsulfonate

醯基氧基、胺基磺醯基、烷基胺基磺醯基及二烷基胺基磺 i基； m及η各自分別表示〇或1至2之整數，但規定： (a) m + n係小於或等於2(m + n$2); (b) 當m為0，η為1，Ra、Rb、Rc和Rd皆為氫原子時，則R 不為曱基或選擇性經取代之苯基；及其醫藥可接受性鹽。a mercaptooxy group, an aminosulfonyl group, an alkylaminosulfonyl group, and a dialkylaminosulfonyl group; m and η each represent an anthracene or an integer of 1 to 2, respectively, but stipulate: (a) m + n is less than or equal to 2 (m + n$2); (b) when m is 0, η is 1, and Ra, Rb, Rc and Rd are all hydrogen atoms, then R is not a thiol group or a selective substitution Phenyl; and pharmaceutically acceptable salts thereof.

第334頁 :· 90119473(替換）-3.ptc 1327569Page 334: · 90119473 (replace) - 3.ptc 1327569

C NHR /Λ利範圍第1項之化合物，其中R為_C〇R，或 J 、傭、_C〇NHR，，"”、谭白·; Λ或·S〇2NR，R"，其〇，及R"為才目同或相異且係選自虱或視㈤要經取代之直鏈或分支鏈C > n r -rffi U*. «- 1V^6 現暴、方巷、 C^C6壞烧基及芳基Ci _c6烧基或R’及R"共同形成C「C6伸烧基氫或直鏈或分支鏈q-Cs烷成C3~C6環烷基；C NHR / Compound of the first paragraph of the profit range, where R is _C〇R, or J, commission, _C〇NHR,, "", Tan Bai·; Λ or · S〇2NR, R" , and R" is the same or different and is selected from 虱 or 视 (5) to be replaced by a straight or branched chain C > nr -rffi U*. «- 1V^6 暴暴,方巷, C^ C6 bad alkyl and aryl Ci _c6 alkyl or R' and R " together form C "C6 extended alkyl hydrogen or linear or branched q-Cs alkane to C3 ~ C6 cycloalkyl;

Ra及Rb為相同或相異且係選自基’或與其鍵結之碳原子共同形 Rc及Rd皆為氫原子； m為0或1 ; η為0或1。 3. 如申請專利範圍第】項之化合物，其， -CONHR，及^為^、_C0R，、_C0NHR，一c〇nr，r"、_s〇2R，、 -S02NHR’或-S〇2NR’r"，其中R’及R"為相同或相異且』選自 ^或視需要經取代之直鏈或分支鏈Ci〜C6烷基、芳基、C3_C6 環烷基及芳基Q-C6烷基或R，及R"共同形成一個伸烷基鏈；Ra為氫；Rb為-CH2〇R，基，其中R，基定義如前；Rc及 Rd皆為氫原子；m為〇或1 ;11為0。Ra and Rb are the same or different and are selected from a base or a carbon atom bonded thereto. Rc and Rd are each a hydrogen atom; m is 0 or 1; and η is 0 or 1. 3. For the compound of the scope of the patent application, -CONHR, and ^ is ^, _C0R, _C0NHR, a c〇nr, r", _s〇2R, -S02NHR' or -S〇2NR'r&quot ;, wherein R' and R" are the same or different and are selected from ^ or optionally substituted straight or branched chain Ci~C6 alkyl, aryl, C3_C6 cycloalkyl and aryl Q-C6 alkyl Or R, and R" together form an alkyl chain; Ra is hydrogen; Rb is -CH2〇R, a group, wherein R, a group is as defined above; Rc and Rd are each a hydrogen atom; m is 〇 or 1; Is 0.

4. 如申清專剩範圍第1項之化合物，其中r為或 -CONHR’ 及R〗為尺，、-COR， -S02NHR’ 或-S〇2NR’ R"，其、-CONHR’、-c〇NR，R"、-S02R，、中R ’及R"為相同或相異且係選自氫或視需要經取代之直鏈或分支鏈c广Ce烷基、芳基、C3_c6 環烧基及芳基G -C：6烷基或R’及Rn共同形成一個C4_C6伸烷基鏈；Ra、Rb、Rc及Rd皆為氫原子；m&n皆為〇。4. If the compound of item 1 of the reserved scope is declared, where r is or -CONHR' and R is the ruler, -COR, -S02NHR' or -S〇2NR' R", its -CONHR', - c〇NR, R", -S02R, , R' and R" are the same or different and are selected from hydrogen or, if desired, substituted straight or branched c-Ce alkyl, aryl, C3_c6 ring-fired And aryl G-C: 6 alkyl or R' and Rn together form a C4_C6 alkyl chain; Ra, Rb, Rc and Rd are all hydrogen atoms; m&n are both oxime.

,90119473(替換）-2.ptc 第 335 頁 1327569 --tl_901l9473^-I--年 1 月.S-__ 六、申請專利範圍 5. 如申請專利範園第1項之化合物，其中R為_c〇R，或 -CONHR’ 及'為只，、一C〇K,、—C0NHR，、-CONR，R'，、-S〇2R，其中R’及R"為相同戒相異且係選自氫或視需要經取代之直鏈或分支鏈匕-^烷基、芳基、C3-C6環烷基及芳基Q-Ce烷基或 1 R ’及R ”共同形成一個Ο - G伸炫基鏈； ,Ra及Rb為相同或相異且係選自氫或直鏈或分支q -C3烷基或Ra及Rb與其鍵結的碳原子共同形成一個C3-C6環烷基； Rc及Rd皆為氫原子； m為1 ; #ι 為 0。 6. 如申請專利範園第1項之化合物’其中R為_C0R’或 -CONHR’ 及&為尺，、-C〇R，、-CONHR’ 、-C〇NR，R"或-S02R，，其中R’及R"為相同或相異且係選自氫或視需要經取代之直鏈或分支鏈(：广(：6燒基、芳基、C3_(：6環烷基及芳基口-(：6烷基或R，及Γ共同形成〆個C4_Ce伸烷基鏈； Ra及Rb為相同或相異且係選自氫或直鏈或分支q-C3烷基或Ra及Rb與其鍵结的碳原子共同形成一個C3-C6環燒基； Rc及Rd皆為氫原子；為 0 ; η為1 〇 7. 如申請專利範園第1項之化合物，其中R為-COR’或 -CONHR’ 及 1^為只，、一C〇R，、-C〇NHR，、-c〇NR，R”、-S02R，、-S02NHR，或-s〇2NR，R"，其中R’及尺"為相同或相異且係選、自氫或視需要經取代之直鏈或分支鏈匕-C6烷基、芳基、, 90119473 (replacement) - 2.ptc, p. 335, 1327569 - tl_901l9473^-I--January. S-__ VI. Patent application scope 5. If applying for patents, the compound of the first item, where R is _ c〇R, or -CONHR' and 'for only, one C〇K, -C0NHR, -CONR, R',, -S〇2R, where R' and R" are the same or different From a hydrogen or an optionally substituted straight or branched chain ^-alkyl, aryl, C3-C6 cycloalkyl and aryl Q-Ce alkyl or 1 R 'and R" together form a Ο - G extension a base chain; Ra and Rb are the same or different and are selected from hydrogen or a linear or branched q-C3 alkyl group or Ra and Rb together with a carbon atom to which they are bonded to form a C3-C6 cycloalkyl group; Rc and Rd is a hydrogen atom; m is 1; #ι is 0. 6. If you apply for a compound in the first paragraph of the patent garden, where R is _C0R' or -CONHR' and & is ruler, -C〇R, , -CONHR', -C〇NR, R" or -S02R, where R' and R" are the same or different and are selected from hydrogen or optionally substituted straight or branched chains (: broad (: 6 An alkyl group, an aryl group, a C3_(:6 cycloalkyl group and an aryl port-(:6 alkyl or R, and a total of Forming a C4_Ce alkylene chain; Ra and Rb are the same or different and are selected from hydrogen or a linear or branched q-C3 alkyl group or Ra and Rb together with a carbon atom bonded thereto to form a C3-C6 ring-burning Rc and Rd are all hydrogen atoms; 0; η is 1 〇7. For example, the compound of Patent No. 1, wherein R is -COR' or -CONHR' and 1^ is only, one C〇 R,, -C〇NHR,, -c〇NR, R", -S02R, -S02NHR, or -s〇2NR, R", where R' and ruler " are the same or different and are selected Hydrogen or a linear or branched chain 匕-C6 alkyl, aryl,

90119473(^^)-2.ptc 帛 336 頁 1327569 -El__90U9473_年月日修正__ 六、申請專利範圍 Ca-C6環烧基及芳基Ci-C6烷基或R’及R”共同形成一個C4_C6伸炫基鍵； m及η皆為0 ; Ra及Rb各自分別為氫或(^ -c4院基或Ra及Rb與其鍵結的碳原子共同形成一個環烷基環；以及Rc及“皆為氫。 8.如申凊專利範圍第1項之化合物，其中r為_c〇r，或 -CONHR 及^為只’、—c〇R,、-CONHR，、~c〇NR，R"、_S02R，、 -S〇2NHR’或-S〇2NR’R”，其中R，及R"為相同或相異且係選自氫或視需要經取代之直鏈或分支鏈Ci院基、芳基、C3_C6 環烧基及芳基q-C：6烷基或R，及R"共同形成〆個匕-匕伸烷基鏈； m及η皆為0 ; Ra、Rb、Rc及Rd皆為氫。 9.如申請專利範圍第1項之化合物，其係選自： 1. N-{5 -本基乙醯基-4，6 -二氫n比嚷并[3 4-c] 51比°坐-3- 基}笨基乙醯胺； ’ 2. N-{5-乙醯基-4, 6 -二氫吡咯并[3, U吡唑_3_基}笨基乙醯胺； ’ 3. N-苄基- Ν’ - {3 -苯基乙醯胺基-4, 6_二氫吡咯并 [3,4-(：]51比°坐-5-基}脲； 4· Ν-{5-甲本石頁醯基-4,6 -二氫0比嚷并[3 4 - c]e比嗤- 3- 基}苯基乙醯胺； ’ 5. Ν-乙基- Ν’ - {3 -苯基乙醯胺基-4, 6_二氫吡咯并 [3,4-(：]°比°坐-5-基}服；90119473(^^)-2.ptc 帛336 Page 1327569 -El__90U9473_年月日日 Revision__ VI. Patent application range Ca-C6 cycloalkyl and aryl Ci-C6 alkyl or R' and R" together form a C4_C6 extends the base bond; m and η are both 0; Ra and Rb are each hydrogen or (^-c4) or Ra and Rb together with the carbon atom to which they are bonded form a cycloalkyl ring; and Rc and "all 8. Hydrogen. 8. A compound according to claim 1, wherein r is _c〇r, or -CONHR and ^ are only ', -c〇R, -CONHR, ~c〇NR, R" , _S02R, -S〇2NHR' or -S〇2NR'R", wherein R, and R" are the same or different and are selected from hydrogen or, if desired, substituted straight or branched chains a group, a C3_C6 cycloalkyl group and an aryl group qC: 6 alkyl or R, and R" together form a 匕-匕 alkyl chain; m and η are both 0; Ra, Rb, Rc and Rd are all hydrogen. 9. The compound of claim 1, wherein the compound is selected from the group consisting of: 1. N-{5 - benzyl thiol-4,6-dihydron than 嚷[3 4-c] -3-yl} phenyl acetamide; ' 2. N-{5-ethenyl-4,6-dihydropyrrolo[3, U-pyrazole_3_ } stupyl acetamide; ' 3. N-benzyl- Ν' - {3-phenylethyl hydrazino-4,6-dihydropyrrolo[3,4-(:]51 than ° sit-5 -yl}urea; 4·Ν-{5-甲本石醯醯-4,6-dihydro 0 is more than 嚷[3 4 - c]e than 嗤-3-yl}phenylacetamide; 5. Ν-ethyl-Ν'-{3-phenylethylamino-amino-4,6-dihydropyrrolo[3,4-(:]° ratio ° sitting 5-base};

90119473(替換）-2.ptc 第337頁、--- 1327569 _案號 90119473_年月日__ 六、申請專利範圍 6· N-{5-乙醯基-4，6 -二氫"比口各并[3,4-c] 0比嗤- 3- 基}-4-(苯基）苯基乙醯胺； 7. N-{5-乙醯基-4, 6 -二氫°比σ各并[3,4-c] °比。坐- 3- 基}_2_秦基乙酿胺； * 8. N-{5-乙酿基-4，6 -二氯B比σ各并[3，4-c] 0比σ坐-3-基}- 呋喃-2 -羧醯胺； 9. Ν-{5-乙醯基-4，6 -二氫吼17各并[3,4-c] π比唾- 3- 基}-5 -氯噻吩-2 -羧醯胺；十10. Ν-{5-乙醯基-4,6 -二氫D比鸣并[3,4-c]0比0坐- 3- - 6 -氯菸鹼醯胺； 11. N_{5_ 乙酿·基 _4，6_ 二氮吼11各并[3，4-c] 0 比0坐-3-基}-苯并σ夫鳴-2-觀酿胺； 12. Ν_{5_乙酸基-4，6 -二氯0比洛弁[3，4_c] °比〇坐-3-基}-4-苯氧苯曱醯胺； 13_ N-{5-乙醯基-4，6 -二氫 D比0各并[3,4-c] 0比0坐- 3-基}-4-第三丁基苯曱醯胺； 14. N-{5-乙驢基-4，6 -二氫"比0各并[3,4-c] 0比0坐-3-基}-胡椒基酿胺， 15. N-{5-乙醯基-4，6 -二氫0 比 σ各并[3,4-c] 0 比0坐- 3-Μ-[2-甲基-5-苯基-呋喃-3-羧醯胺]; 16. Ν-{5-乙醯基-4，6 -二氫0比°各并[3,4-c] 0比0坐-3-基}-(喳啉-6-羧醯胺）； 17. N-{5-乙醯基-4，6 -二氫11比洛并[3,4-c] 0比唾-3-•基卜[5-(4-氯苯基）呋喃-2-羧醯胺];90119473 (replacement)-2.ptc Page 337, --- 1327569 _ Case No. 90119473_年月日日__ VI. Patent application scope 6. N-{5-Ethyl-4,6-dihydro" The ratio of [3,4-c] 0 to 嗤-3-yl}-4-(phenyl)phenyl acetamide; 7. N-{5-ethenyl-4,6-dihydrogen The ratio of σ is [3,4-c] °. Sit-3-base}_2_Qinyl Ethylamine; * 8. N-{5-Ethyl-4,6-dichloroB ratio σ[3,4-c] 0 ratio σ sitting-3 -yl}-furan-2-carboxycarboxamide; 9. Ν-{5-ethinyl-4,6-dihydroindole 17 and [3,4-c] π than salino-3-yl}-5 -chlorothiophene-2 -carboxamide; ten 10. Ν-{5-ethinyl-4,6-dihydro D ratio [ and [3,4-c]0 to 0 sit- 3--6-chloro Nicotine decylamine; 11. N_{5_ 乙乙·基_4,6_ diazepine 11 and [3,4-c] 0 to 0 -3-yl}-benzo σ 鸣 -2- -2-酿_{5_Acetyl-4,6-dichloro- 0 弁弁 [3,4_c] ° than 〇-3-yl}-4-phenoxybenzamine; 13_ N-{ 5-Ethyl-4,6-dihydro D is 0 and each [3,4-c] 0 is 0-position - 3-yl}-4-t-butylbenzamide; 14. N-{ 5-Ethyl-4,6-dihydro" ratio 0 and [3,4-c] 0 to 0--3-yl}-piperonylamine, 15. N-{5-ethenyl -4,6-dihydrogen 0 is more than σ and [3,4-c] 0 is 0-position - 3-Μ-[2-methyl-5-phenyl-furan-3-carboxyguanamine]; Ν-{5-Ethyl-4,6-dihydrogen 0 ratio °[3,4-c] 0 to 0--3-yl}-(porphyrin-6-carboxyguanamine); N-{5-ethylindolyl-4,6-dihydro-11 is more than ruthenium [3,4-c] 0 than saliva-3-•kib [5-(4) -Chlorophenyl)furan-2-carboxyguanamine];

90119473(替換）-2.ptc 第338頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍 18. N_{5_甲烧績聽·基_4，6_二氮0比洛弁[3，4-c]吼〇坐_3_ 基}-4-第三丁基苯甲醯胺； 19. N-{5 -苯績醯基- 4,6 -二氫D比11 各并[3,4-c] °比°坐- 3-基}-4-第三丁基苯甲醯胺； 20. ^{5-苯甲醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-第三丁基苯甲醯胺； 21. Ν-{5-(1-萘）磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑 -3-基}-4-第三丁基苯曱醯胺； 22. Ν-{5-(1-萘甲醯基）-4,6 -二氫D比0各并[3,4-c] D比唑 -3-基}-4_第三丁基苯曱醯胺； 23. N_{5-苯乙酿基_4，6_二氫p比11 各并[3，4_c] 11比0坐_3_ 基}-4-第三丁基苯甲醯胺； 24. N-苯基_N’ - {3_(4-第三丁基-苯曱驗胺基）-4，6 -二氫°比°各并[3，4-c]吼°坐-5-基}脲； 25. Ν-異丙基-Ν’ - {3-(4-第三丁基-苯甲醯胺基）-4,6-二氫°比σ各并[3，4 - c ] °比。坐-5 -基}脲； 26.1{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-苯氧苯曱醯胺； 27.1^-{5-苯曱醯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-4-苯氧苯甲醯胺； 28. Ν-{5-(卜萘曱醯基）-4,6 -二氫吡咯并[3,4-c]吼唑 -3-基}-4-苯氧苯曱醯胺； 29. N_異丙基_N’_{3-(4-苯氧-苯曱酿胺基）-4，6_二氫。比σ各并[3，4 - c ] D比。坐-5 -基}脲；90119473 (replacement)-2.ptc Page 338 1327569 _ Case No. 90119473_Year of the month __ Six, the scope of application for patents 18. N_{5_甲烧听听·基_4,6_二氮0比洛弁[3,4-c] 吼〇3_ yl}-4-t-butylbenzamide; 19. N-{5-phenylindole- 4,6-dihydro-D ratio 11 each [ 3,4-c] ° ratio - 3-yl}-4-t-butylbenzamide; 20. ^{5-benzimidyl-4,6-dihydropyrrolo[3,4 -(:]pyrazol-3-yl}-4-t-butylbenzamide; 21. Ν-{5-(1-naphthalene)sulfonyl-4,6-dihydropyrrolo[3, 4-(:]oxazol-3-yl}-4-t-butylbenzamide; 22. Ν-{5-(1-naphthylmethyl)-4,6-dihydrogen D to 0 each And [3,4-c] D-pyrazol-3-yl}-4_t-butylbenzamide; 23. N_{5-phenylethylidene_4,6-dihydrop ratio 11 [3,4_c] 11 to 0 sitting _3_ ki}-4-t-butylbenzamide; 24. N-phenyl_N' - {3_(4-t-butyl-benzoquinoneamine -4,6-dihydrogen ratio °[3,4-c]吼° sit-5-yl}urea; 25. Ν-isopropyl-Ν' - {3-(4-third -benzylamino)-4,6-dihydrogen ratio σ and [3,4 - c ] ° ratio. sit-5-yl}urea; 26.1{5-methanesulfonyl-4,6 -two Pyrrolo[3,4-(:]pyrazol-3-yl}-4-phenoxybenzamine; 27.1^-{5-benzoinyl-4,6-dihydropyrrolo[3,4 -〇]pyrazol-3-yl}-4-phenoxybenzamide; 28. Ν-{5-(b-naphthyl)-4,6-dihydropyrrolo[3,4-c] Oxazol-3-yl}-4-phenoxybenzamine; 29. N_isopropyl_N'_{3-(4-phenoxy-benzoquinone)-4,6-dihydrogen Ratio σ to [3,4 - c ] D ratio. sit -5 -yl} urea;

90119473(替換）-2.ptc 第339頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 30. N_{5-乙酿基_4，6_二氮0比0各弁[3，4_c] σ比吐_3_ 基}-[2-(2 -寨基）丙酿胺]; 31. Ν-異丙基-Ν’ - {3 -胡椒基羧醯胺基）-4, 6 -二氫吡咯并[3,4-〇]°比°坐-5-基}脲； • 32. Ν-環己基-Ν’ - {3-(4-第三丁基-笨甲醯胺基）-4,6- 二氫吼11各并[3，4 - c ] °比α坐-5 -基}脲； 33. Ν-乙基-Ν’-{3-(4-第三丁基-苯甲醯胺基）-4,6 -二氫°比σ各并[3，4 - c ] °比α坐-5 -基}脲； 34. Ν-(2, 6 -二乙基苯基）-Ν’ - {3-(4 -第三丁基-苯甲醯修基）-4, 6 -二氫吼0各并[3, 4-c] 11比唾-5-基}脲； 35. Ν-環己基-Ν’-{3-(2-乙基-丁醯胺基）-4,6 -二氳吡口各并[3，4 - c ]吼坐-5 -基}脲； 36. N-(2，6_二乙基苯基）_N’ _{3-(胡椒基叛酿胺基）-4, 6 -二氫11比洛并[3,4-c]°比峻-5-基}脲； 37. N-2 -曱氧苯基-N’-{3-(2 -萘-2 -基-丙醯胺基）-4,6-二氫°比B各并[3，4 - c ]吼°坐-5 -基}脲； 38. N-(卜苯基）乙基-N’-{3-(2-萘-2 -基-丙醯胺基）-4, 6 -二氫吼11 各并[3,4-c] °比°坐-5-基}脲； 9 . N_{5_ 苯基酸胺基_4，6_ 二氯 π 比 13各弁[3，4_c] 坐 _3_ $-3-(2-萘-2-基）-丙醯胺； 40. N-(2,5 -二曱基苯基）-N’-{3-(4 -第三丁基-苯曱醯胺基）-4, 6 -二氫D比B各并[3, 4-c]吡唑-5-基}脲； 41. N-(2,5 -二曱基苯基）-N’-{3-(2-乙基-丁醯胺，基）-4,6-二氫吡咯并[3,4-c]吡唑-5-基}脲；90119473 (replacement)-2.ptc Page 339 1327569 _ Case number 90119473_Yearly revision _ Six, the scope of application for patents 30. N_{5-Ethylene base_4,6_Dinitrogen 0 to 0 弁[3 , 4_c] σ ratio spit _3_ base}-[2-(2-zyl) propylamine]; 31. Ν-isopropyl-Ν' - {3 -piperonylcarboxamide)-4, 6 - dihydropyrrolo[3,4-〇]° ratio °-5-yl}urea; • 32. Ν-cyclohexyl-Ν' - {3-(4-t-butyl-stupylamino) -4,6-dihydroindole 11 each [3,4 - c ] ° ratio α sitting -5 -yl}urea; 33. Ν-ethyl-Ν'-{3-(4-t-butyl -benzamide amino)-4,6-dihydrogen ratio σ[3,4 - c ] ° ratio α sit-5-yl}urea; 34. Ν-(2,6-diethylbenzene Base)-Ν' - {3-(4-tributyl-benzhydryl)-4,6-dihydroindole 0 and [3,4-c] 11 than sal-5-yl}urea 35. Ν-cyclohexyl-Ν'-{3-(2-ethyl-butyrylamino)-4,6-dipyridinium each [3,4 - c ] 吼-5-yl} Urea; 36. N-(2,6-diethylphenyl)_N' _{3-(Pepperyl adenine)-4,6-dihydro 11 piroxi[3,4-c]°峻君-5-yl}urea; 37. N-2 -nonyloxyphenyl-N'-{3-(2-naphthalen-2-yl-propionylamino)-4,6-di ° ratio B and [3,4 - c ]吼° sit-5-yl}urea; 38. N-(buphenyl)ethyl-N'-{3-(2-naphthalene-2-yl-propyl Amidino)-4,6-dihydroindole 11 each [3,4-c] ° ratio -5-yl}urea; 9 . N_{5_ phenyl acid amine _4,6_ dichloro π More than 13 弁[3,4_c] sit _3_ $-3-(2-naphthalen-2-yl)-propanamide; 40. N-(2,5-dimercaptophenyl)-N'-{ 3-(4-T-butyl-benzoguanamine)-4,6-dihydrogen D is more than B and [3,4-c]pyrazol-5-yl}urea; 41. N-(2 ,5-dimercaptophenyl)-N'-{3-(2-ethyl-butylammonium,yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-yl Urea

90119473(替換）-2.ptc 第340頁 1327569 ：_案號 90119473_年月日__ 六、申請專利範圍 42. N-(4-氟爷基）-N’-{3-(2-乙基-丁醯胺基）-4,6-二氫0比洛并[3，4 - c ]吼α坐-5 -基}脲； 43.1{5-芊基磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑-3-基} -4-第三丁基苯甲醯胺； 44. Ν-2 -氯苯基-Ν’-{3-(2 -萘-2 -基-丙醯胺基）-4,6 -二氫°比洛并[3,4-(：]11比。坐-5-基}脲； 45. ^{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-2-(2_萘基）-丙醯胺； 46. Ν-{5-(3-甲基-丁醯基）-4,6 -二氫吡咯并[3,4-c] 唑-3-基}-4-苯氧苯甲醯胺； 47.1^1-{5-(2-苯基-噻唑-4-基）乙醯基-4,6-二氫吡咯并 [3,4-c]吡唑-3-基}-4 -苯氧苯曱醯胺； 48. N-{5-(2 -噻吩基-乙醯基）-4,6 -二氫咄咯并[3,4-c] 0比唑-3-基}-4-第三丁基苯甲醯胺； 49. N-{5-(3 -吡啶基-乙醯基）-4,6 -二氫咄咯并[3, 4-c] 吡唑-3 -基}-4-第三丁基苯甲醯胺； 50. ^{5-爷基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-苯氧苯甲醯胺； 51. N-{5-(2-曱基丙基）羰基-4,6-二氩吡咯并[3,4-〇] 吡唑-3 -基}-4-第三丁基苯甲醯胺； 52. N-{5_(2 -苯基比。坐_4_基）乙酿基_4，6_二氮1*比洛并 [3,4-〇:]咄唑-3-基}-4-第三丁基苯曱醯胺； 53. Ν-{5-(2 -噻吩基-乙醯基）-4,6 -二氫咄咯并[3,4-c] 吡唑-3-基}-4-苯氧苯甲醯胺；90119473 (replacement)-2.ptc Page 340 1327569: _ case number 90119473_年月日日__ VI. Patent application scope 42. N-(4-fluoro-based)-N'-{3-(2-B -butyrylamino)-4,6-dihydro 0-pyrolo[3,4-c]吼α-sodium-5-yl}urea; 43.1{5-mercaptosulfonyl-4,6-di Hydropyrrolo[3,4-(:]oxazol-3-yl}-4-t-butylbenzylideneamine; 44. Ν-2-chlorophenyl-Ν'-{3-(2-naphthalene) -2 -yl-propionylamino)-4,6-dihydropyrazine [3,4-(:]11 ratio. sit-5-yl}urea; 45. ^{5-aminocarbonyl- 4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-2-(2-naphthyl)-propanamine; 46. Ν-{5-(3-methyl- Butyl) 4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-phenoxybenzamide; 47.1^1-{5-(2-phenyl-thiazole-4 -yl)ethinyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 48. N-{5-(2-thiophene -ethylamino)-4,6-dihydroindolo[3,4-c] 0-pyrazol-3-yl}-4-t-butylbenzamide; 49. N-{5- (3-pyridyl-ethenyl)-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 50. ^{ 5-arylsulfonyl-4,6-dihydropyrrole And [3,4-(:]pyrazol-3-yl}-4-phenoxybenzamide; 51. N-{5-(2-mercaptopropyl)carbonyl-4,6-difluoropyrrole And [3,4-〇]pyrazol-3-yl}-4-t-butylbenzamide; 52. N-{5_(2-phenyl ratio. sitting_4_yl) ethyl ketone _ 4,6-diaza 1*piro[3,4-indene]oxazol-3-yl}-4-t-butylbenzamide; 53. Ν-{5-(2-thiophenyl) -ethinyl)-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide;

卯 119473(替換）-2.ptc 第341頁 1327569 _案號90119473_年月日__ 六、申請專利範圍 54.1{5-(苯并[1，3]二氧伍圜-5-基）乙醯基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}-3-甲基丁醯胺； 55. Ν-{5-(1-萘）續酿基-4,6-二氫咄略并[3,4-〇]吼唾 -3 -基卜環丙基羧醯胺； 56. N-{5-(2-甲氧苯基）-4,6 -二氫咄洛并[3,4-c] 11比峻 -3 -基}_3_(2 -秦_2_基）-丙酸胺； 57. Ν-{5-(2-π夫喃曱蕴基）-4,6-二氫0比洛并[3,4-c] 0比〇坐-3 -基}-3-(2_萘-2-基）-丙醯胺； 58. Ν-{5-[5-(1-嗎琳基甲基）咬喃_2-幾基]-4,6 -二氫 φ咯并[3,4_c]吡唑-3_基}_4 -第三丁基苯甲醯胺； 59. Ν-{5-{4-[2-(1-°比咯啶基）乙氧]苯基}乙醯基-4,6-二氫吡咯并[3, 4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 60. N-{5-(1-Η-苯并三β坐-5-幾基）-4，6 -二氫°比17各并[3， 4-c]吡唑-3-基}-4-第三丁基苯甲醯胺； 61· Ν-{5-(吡咯-3 -羰基）乙醯基-4, 6-二氫吡咯并 [3,4-(：]吡唑-3-基}-4-第三丁基苯甲醯胺； 62. Ν-{5-{4-[2 -氧基-2-(卜吼咯啶基）乙氧]苯基}乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-苯氧苯曱醯 *63. N-{ 5-(4-甲基磺醯胺基-苯基）乙醯基-4, 6 -二氫咄咯并[3,4-c]吡唑-3-基}-4-苯氧苯甲醯胺； 64. Ν-{5-[2-(6 -氧基-1(6H) -嗒畊基}乙醯基-4, 6 -二氫 0比0各并[3，4-c] 0比σ坐-3-基}-4_苯氧苯甲酿胺； 65. ?^-{5_(3-胺基甲醯基甲氧-苯基）乙醯基-4,6-二氫卯119473 (replacement)-2.ptc Page 341 1327569 _ Case No. 90119473_年月日日__ VI. Patent application scope 54.1{5-(Benzo[1,3]dioxos-5-yl)B Mercapto-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-3-methylbutanamine; 55. Ν-{5-(1-naphthalene) continuation-- 4,6-dihydroindole and [3,4-indolyl]pyry-3-ylbucyclopropylcarboxamide; 56. N-{5-(2-methoxyphenyl)-4,6- Dihydroindolo[3,4-c] 11 is more than -3 -yl}_3_(2 - Qin_2_yl)-propionic acid amine; 57. Ν-{5-(2-π夫曱曱蕴-4,6-dihydro- 0-bi-[3,4-c] 0 is more than -3 -yl}-3-(2-naphthalen-2-yl)-propanamide; 58. {5-[5-(1-Merynylmethyl)-anthracene-2-amino]-4,6-dihydro-pyrrolo[3,4_c]pyrazole-3-yl}_4-third Benzobenzamide; 59. Ν-{5-{4-[2-(1-°-pyridyl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3, 4 -c]pyrazol-3-yl}-4-t-butylbenzamide; 60. N-{5-(1-indole-benzotris[beta]--5-yl)-4,6- Dihydrogen ratio of 17-[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 61·Ν-{5-(pyrrole-3-carbonyl)ethenyl -4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}- 4-t-butylbenzamide; 62. Ν-{5-{4-[2-oxy-2-(b-pyridyl)ethoxy]phenyl}ethenyl-4,6- Dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-phenoxybenzoquinone*63. N-{ 5-(4-methylsulfonylamino-phenyl)acetamidine 4-,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide; 64. Ν-{5-[2-(6-oxyl) -1(6H) - 嗒耕基}Ethyl-4,6-dihydrogen 0 to 0 each [3,4-c] 0 σ -3--3-yl}-4 phenoxybenzamide 65. ?^-{5_(3-Aminomethylmercaptomethoxy-phenyl)ethinyl-4,6-dihydrogen

I 90119473(替換）-2.ptc 第 342 頁 1327569 案號90119473 年月日修正六、申請專利範圍吡咯并[3,4-c]咄唑-3-基}-4-苯氧苯甲醯胺； 66. N-{5-(4-胺基甲醯基曱氧-苯基）乙醯基-4, 6 -二氫吡咯并[3,4-c]吡唑-3-基}-4-苯氧苯甲醯胺； 67. ^1-{5-[4-(1-咄咯啶基）苯基]乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4-苯氧苯甲醯胺； 68. N-{5 -胺基曱醯氧基乙醯基-4, 6 -二氫吡咯并 [3,4-c]吡唑-3-基}-4_苯氧苯甲醯胺； 69. N-{5-{4-[2-(4-甲基哌。井-2 -基）乙氧]苯基}乙醯基 -4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-4-苯氧苯甲醯胺； 70. Ν-{5-{4-[2-(1-吡咯啶基）乙氧]苯基}乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 71. N-{5-{4-[2 -氧基-2-U -吡咯啶基）乙氧]苯基}乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-第三丁基苯曱醯胺； 72. N-{5_(4_甲基石黃酸胺基-苯基）乙蕴基-4，6 -二氮°比咯并[3,4-c]吡唑-3-基}-4-第三丁基苯甲醯胺； 73. N-{5-(吡啶-3 -羰基）-4,6 -二氫吡咯并[3,4-c]吡唑 -3-基}-4-第三丁基苯曱醯胺； 74· N-{5-( D比咬-3-羰基）-4, 6 -二氫°比"各并[3, 4-c] °比嗤 -3-基}-4-第三丁基苯甲醯胺； 75. N-{5-( D比咬-4-羰基）-4, 6 -二氫°比°各并[3,4-c]吼〇坐 -3 -基丨_4_第三丁基苯甲酿胺； 76. N-{5-(2-甲基-〇比咬-3 -幾基）-4，6_二氫0比σ各并 [3,4-c]咄唑-3-基}-4-第三丁基苯曱醯胺；I 90119473 (replacement)-2.ptc Page 342 1327569 Case No. 90119473 Revised on the day of the month 6. Patent application range pyrrolo[3,4-c]oxazol-3-yl}-4-phenoxybenzamide 66. N-{5-(4-Aminomethylmercaptooxy-phenyl)ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4 -phenoxybenzamide; 67. ^1-{5-[4-(1-Pyryridinyl)phenyl]ethenyl-4,6-dihydropyrrolo[3,4-c]pyridyl Zylidene-3-yl}-4-phenoxybenzamide; 68. N-{5-aminomethoxyethoxyethyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3-yl}-4-phenoxybenzamide; 69. N-{5-{4-[2-(4-methylpiperidin-2-yl)ethoxy]phenyl}ethenyl -4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-4-phenoxybenzamide; 70. Ν-{5-{4-[2-(1-pyrrole) Acryl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 71. N-{ 5-{4-[2-ethoxy-2-U-pyrrolidinyl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3- } 第三第三第三第三 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 72 ,4-c]pyrazole-3- }-4-t-butylbenzamide; 73. N-{5-(pyridin-3-carbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl} -4-t-butylbenzamide; 74· N-{5-(D ratio bit-3-carbonyl)-4,6-dihydrogen ratio " each [3, 4-c] ° ratio Indole-3-yl}-4-t-butylbenzylideneamine; 75. N-{5-(D-Bit-4-carbonyl)-4,6-dihydrogen ratio °[3,4 -c] 吼〇 -3 - 丨 _4_ butyl butyl benzoate; 76. N-{5-(2-methyl- 〇咬 -3 -1) -4,6_ Dihydrogen 0 to σ each and [3,4-c]oxazol-3-yl}-4-t-butylbenzamide;

90119473(替換）-2.ptc 第343頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 77. N-{5-(2 -硫甲基-吡啶-3 -羰基）-4,6 -二氫吡咯并 [3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 78. N-{5-( °比畊-2 -幾基）-4, 6 -二氫η比洛并[3, 4-c]吼唾 -3-基}-4-第三丁基苯甲醯胺； 79. Ν-{5-(3-σ夫喃曱醯基）-4,6 -二氫0比洛并[3,4-c] 0比唑-3-基}-4-苯氧苯曱醯胺； 80. N-{5-(2 - D塞吩曱醯基）-4,6 -二氫0比洛并[3,4-c] D比唑-3-基}-4-苯氧苯曱醯胺； 81. N-{ 5-(7-甲氧-苯并呋喃-2 -羰基）-4, 6 -二氫吡咯并 [04-c]咄唑-3-基}-4-第三丁基苯甲醯胺； ^82. N-{5-(苯并π夫喃-2-叛基）-4，6 -二氫°比洛并[3，4_c] 吡唑-3 -基}-4-第三丁基苯甲醯胺； 83. N-{5-(2 -呋喃甲醯基）-4,6-二氫吡咯并[3,4-c]呲唑-3-基}-4-第三丁基苯曱醯胺； 84. N-{5-(3 -口夫喃甲醯基）-4,6 -二氫11比洛并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 85. Ν-{5-(2-σ夫喃曱醯基）-4, 6 -二氫π比0各并[3,4-c]吡唑-3-基}-4-苯氧苯甲醯胺； ^^8 6. N_{5_(3_0塞吩曱酿基）_4，6_ 二氮 n 比0各弁[3，4_c] π 比 β-3-基}-4-第三丁基苯甲醯胺； 87· Ν-{5-(喳 G啉-2 -羰基）-4, 6 -二氫吡咯并[3, 4-c] 口比唑-3-基}-4-苯氧苯曱醯胺； ' 88. N-{5-(2 -噻吩基）乙醯基-4, 6 -二氫吡咯并[3, 4-c] •吡唑-3 -基}-4-第三丁基苯甲醯胺；90119473 (replacement)-2.ptc Page 343 1327569 _ Case No. 90119473_Yearly revision _ 6. Patent application scope 77. N-{5-(2-thiomethyl-pyridine-3-carbonyl)-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 78. N-{5-(° ratio tillage-2-single base)- 4,6-Dihydro-n-bi-[3,4-c]pyran-3-yl}-4-t-butylbenzylideneamine; 79. Ν-{5-(3-σ夫曱Indenyl)-4,6-dihydro 0-pyrolo[3,4-c] 0-pyrazol-3-yl}-4-phenoxybenzamine; 80. N-{5-(2 - D塞曱醯 ) -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 -4 3 3 81 81 81 81 81 81 81 81 81 81 81 81 81 81 81 81 81 81 81 81 7-methoxy-benzofuran-2-carbonyl)-4,6-dihydropyrrolo[04-c]oxazol-3-yl}-4-t-butylbenzamide; ^82. N -{5-(Benzo-π-f-am-2-yl)-4,6-dihydro-pyrolo[3,4_c]pyrazol-3-yl}-4-t-butylbenzamide 83. N-{5-(2-Furylmercapto)-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-t-butylbenzamide 84. N-{5-(3-mouthfusylcarbenyl)-4,6-dihydro 11-pyrolo[3,4-c]pyrazol-3-yl}-4-t-butyl Phenylamine; 85. Ν- {5-(2-[rho]-pyranosyl)-4,6-dihydroπ~0-[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide; ^8 6. N_{5_(3_0Cetene brewing base)_4,6_Dinitrogen n ratio 0 弁[3,4_c] π ratio β-3-yl}-4-t-butylbenzamide; 87·Ν-{5-(喳G-ropolin-2-carbonyl)-4,6-dihydropyrrolo[3,4-c]-oroxazol-3-yl}-4-phenoxybenzamine; '88. N-{5-(2-Thienyl)ethenyl-4,6-dihydropyrrolo[3,4-c]•pyrazol-3-yl}-4-t-butylbenzyl Guanamine

90119473(替換）-2.ptc 第344頁 1327569 ,_案號90119473_年月曰修正_ 六、申請專利範圍 89. N-{5-(喳啉-6 -羰基）-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}_4_第二丁基苯曱酸胺， 90. Ν-{5-(3-σ夫喃曱醯基）-4,6 -二氫0比11 各并[3,4-c]吡唑-3-基}-4-苯氧苯曱醯胺； 91_ Ν-{5_( 井 _2_ 幾基）-4，6_ 二氣吼11 各并[3，4-c] B 比0坐 _3_基}_4_苯氧苯甲酿胺， 92.1'1-{5-[2-(6-氧基-1(61〇-嗒畊基}乙醯基-4,6-二氫吼咯并[3,4-c]吼唑-3-基}-4 -第三丁基苯曱醯胺； 93.1{5-(4-胺基曱醯基曱氧-苯基）乙醯基-4,6-二氫吼咯并[3,4-c]吡唑-3-基}-4 -第三丁基苯甲醯胺； 94. N-{5 -胺基甲醯基乙醯基-4,6-二氫吡咯并[3,4-(：] 吼唑-3-基}-4-第三丁基苯甲醯胺； 95. N-{5-{4-[2-(4-曱基哌啡-2 -基）乙氧]苯基}乙醯基 -4,6-二氫吡咯并[3,4-〇]°比唑-3-基}-4-第三丁基苯甲醯胺； 96. N-{5-(2-曱基磺醯胺基噻唑-4 -碳基）-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 97. N-{5-(苯并D夫喃-2-数基）-4，6 -二氫β比咯并[3，4-c] 吡唑-3-基}-4_苯氧苯甲醯胺； 98. N-{5-(吼咬-2-羰基）-4, 6 -二氫 11比 11 各并[3, 4-c] °比唑 -3-基}-4-苯氧苯甲醯胺； 99. N-{5-(2-甲基-吡啶-3 -羰基）-4,6 -二氫吡咯并 [3,4-c]吡唑-3-基}-4-苯氧苯甲醯胺； 100. Ν-{5-(°έ 琳-4-羰基）-4,6 -二氫吼11各并[3,4-c]吡90119473 (replacement)-2.ptc Page 344 1327569, _ case number 90119473_Yearly revision _ 6. Patent application scope 89. N-{5-(porphyrin-6-carbonyl)-4,6-dihydrogen Pyrrolo[3,4-(:]pyrazol-3-yl}_4_t-butylphthalic acid amine, 90. Ν-{5-(3-σf-amyl)-4,6- Dihydrogen 0 to 11 each [3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 91_ Ν-{5_(well_2_ yl)-4,6_dioxin 11 each [3,4-c] B sits _3_base}_4_phenoxybenzamide, 92.1'1-{5-[2-(6-oxy-1(61〇-嗒) Arachidyl}ethinyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-4-tert-butylbenzamide; 93.1{5-(4-amine Base oxime oxy-phenyl)ethyl hydrazino-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4 -t-butylbenzamide; 94 N-{5-aminocarbamimidyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-4-t-butylbenzamide; 95. N-{5-{4-[2-(4-Mercaptopipen-2-yl)ethoxy]phenyl}ethenyl-4,6-dihydropyrrolo[3,4-anthracene] °Bizozol-3-yl}-4-t-butylbenzamide; 96. N-{5-(2-mercaptosulfonylaminothiazole-4 -carbyl)-4,6-dihydrogen Pyrrole [3, 4 -c]pyrazol-3-yl}-4-t-butylbenzamide; 97. N-{5-(benzo-D-am-2-yl)-4,6-dihydro-β ratio [3,4-c]pyrazol-3-yl}-4-phenoxybenzamide; 98. N-{5-(bite-2-carbonyl)-4,6-dihydro-11 ratio 11 each [3, 4-c] ° oxazol-3-yl}-4-phenoxybenzamide; 99. N-{5-(2-methyl-pyridin-3-carbonyl)-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamide; 100. Ν-{5-(°έ琳-4-carbonyl)-4,6 -indoline 11 and [3,4-c]pyridyl

90119473(替換）-2.ptc 第345頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍唑-3-基}-4_苯氧苯曱醯胺； 101.1{5-[4-(卜吡咯啶-2-酮）苯曱醯基]-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4 -第三丁基苯甲醯胺； 102. N-{5_苯基乙基-4，6_二氫吼洛并[3，4-c] π比〇坐_3-基}-4-第三丁基苯甲醯胺； 103. Ν -正丁基-Ν’ - {3-(2 -蔡-2 -基-丙酿胺基）-4，6 -二氫°比洛并[3，4-c] °比°坐-5-基}脲； 104. N-異丙基-Ν’ - {3-(2 -萘-2-基-丙蕴胺基）-4，6 -二氫0比D各并[3，4 - c ]吼°坐-5 -基}脲； 0105. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇:]吡唑 _3_基}·_2 -秦基丙酿胺； 10 6. Ν-{5-乙氧羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基}_3-(2_蔡_2_基）_丙酿胺； 107. Ν-{5-(3-曱基丁醯基）-4, 6 -二氫吼咯并[3, 4-c]吡 c坐一3-基}-3-(2 -蔡_2_基）-丙酿胺； 108· N-{5 -胺基羰基甲基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_3-(2_蔡-2_基）-丙酿胺； ,109. N-{5-〇比咯-3 -基羰基）-4,6 -二氫咄咯并[3,4-c] &唾-3-基}-3-(2 -萘-2-基）-丙醯胺； —110. N-{5-乙氧羰基-4,6-二氫吡咯并[3,4-c]吡唑-3- 基卜4-第三丁基苯甲醯胺； 111. [{5-異戊基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-第三丁基苯曱醯胺； 112. N- 丁基-Ν’ - {3-(4-第三丁基-苯曱醯胺基）-4,6 -二90119473 (replacement)-2.ptc Page 345 1327569 _ Case number 90119473_Yearly date correction _ 6. Patent application range Zin-3-yl}-4_phenoxybenzamine; 101.1{5-[4- (Bipyrrolidin-2-one)phenylhydrazino]-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 102 N-{5_Phenylethyl-4,6-dihydroindolo[3,4-c] π is _3-yl}-4-t-butylbenzamide; 103. Ν-n-butyl-Ν' - {3-(2 -Cai-2-yl-propylamino)-4,6-dihydro-pyrylene[3,4-c] °°°-5 -yl}urea; 104. N-isopropyl-Ν'-{3-(2-naphthalen-2-yl-propionylamino)-4,6-dihydrogen 0 to D each [3,4 - c ]吼° sit-5-yl}urea; 0105. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-anthracene]pyrazole_3_yl}·_2 -Qinyl propylamine; 10 6. Ν-{5-ethoxycarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_3-(2_蔡_2_ )) 丙酿胺; 107. Ν-{5-(3-mercaptobutyl fluorenyl)-4,6-dihydroindolo[3,4-c]pyranidin-3-yl}-3-( 2 -Cai_2_yl)-propanol; 108·N-{5-aminocarbonylmethyl-4,6-dihydropyrrolo[3,4-indolylpyrazole_3_yl}_3- (2 _Cai-2_yl)-propanol; 109. N-{5-indolepy-3-ylcarbonyl)-4,6-dihydroindolo[3,4-c] & saliva- 3-yl}-3-(2-naphthalen-2-yl)-propanamide; -110. N-{5-ethoxycarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3- kib 4-tert-butylbenzamide; 111. [{5-Isoamyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}- 4-tert-butylbenzamide; 112. N-butyl-indole-{3-(4-t-butyl-benzoguanamine)-4,6-di

I 90119473(替換）-2.ptc 第346頁 1327569 修正案號 90119473 六、申請專利範圍氫吡11各并[3，4 - c ] D比唑-5 -基}脲； 113. N-{5-(吲哚-2 -基）羰基-4, 6 -二氫吡咯并[3,4-c] 吡唑-3-基}-4-第三丁基苯甲醯胺； 114. ^{5-(1-曱基-吲哚-3-基）乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4-第三丁基苯曱醯胺； 115.1\1-{5-[4-(1-咪唑基曱基）苯曱醯基]-4,6-二氫吡咯并[3,4-c]°比唑-3-基}-4-苯氧苯甲醯胺； 116..{5-[4-(1-咪唑基曱基）苯甲醯基]-4,6-二氫吡咯并[3,4-c]°比唑-3-基}-4-苯氧苯甲醯胺； 117. ^{5-[4-(1-吡咯啶-2-酮）苯曱醯基]-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-4 -苯氧苯甲醯胺；氫B比咯并[3,4-c]咄唑-3-基卜4-苯氧苯曱醯胺； 119. N-{5-(5-乙醯胺基-2 -呋喃甲醯基）-4,6 -二氫吡咯并[3,4-c]吼唑-3 -基}-3-(2_萘-2-基）-丙醯胺； 120.1{5-(4-曱基-哌畊-1-基）乙醯基-4,6-二氳咄咯并[3,4-c]吼唑-3-基}-3-(2 -萘-2 -基）-丙醯胺； 121.^{5-(哌啶-1_基）乙醯基-4,6-二氫吡咯并 [3,4-c]吡唑-3-基}-3-(2 -萘-2 -基）-丙醯胺； 122.1{5-(吡咯啶-1-基羰基）甲基-4,6-二氫咄咯并 [3,4-c]吡唑-3-基}-3-(2 -萘-2 -基）-丙醯胺； 123. N-{5-乙醯基-4,6-二氫0比σ各并[3,4-c]0比o坐-3- 基}-(4-D比咯啶-l-基）苯基乙醯胺； 124· N-{5-乙醯基-4, 6 -二氫 °比0各并[3, 4-c] 0 比嗤-3- 118. N-{5-(2 -嗎啉基曱基-5 -呋喃曱醯基）-4,6-I 90119473 (replacement)-2.ptc Page 346 1327569 Amendment No. 90119473 VI. Patent application range Hydropyrrol 11 and [3,4 - c ] D-biazole-5-yl}urea; 113. N-{5 -(吲哚-2-yl)carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylbenzamide; 114. ^{5 -(1-decyl-indol-3-yl)ethinyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-t-butylphenylhydrazine Amine; 115.1\1-{5-[4-(1-imidazolylhydrazyl)phenylhydrazino]-4,6-dihydropyrrolo[3,4-c]°bazol-3-yl}- 4-phenoxybenzamide; 116..{5-[4-(1-imidazolylhydrazyl)benzylidene]-4,6-dihydropyrrolo[3,4-c]°bazole -3-yl}-4-phenoxybenzamide; 117. ^{5-[4-(1-pyrrolidin-2-one)phenylhydrazinyl]-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-4-phenoxybenzamide; hydrogen B ratio of p-[3,4-c]oxazol-3-ylbu- 4-phenoxybenzamine; 119. N-{5-(5-Ethylamino-2-furanmethyl)-4,6-dihydropyrrolo[3,4-c]indazole-3-yl}-3-(2) _Naphthalen-2-yl)-propanamine; 120.1{5-(4-indolyl-piperidin-1-yl)ethenyl-4,6-dipyrrolo[3,4-c]indole Zyrazin-3-yl}-3-(2-naphthalen-2-yl) -propanamide; 121.^{5-(piperidin-1_yl)ethenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-(2 -naphthalen-2-yl)-propanamine; 122.1{5-(pyrrolidin-1-ylcarbonyl)methyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl }-3-(2-naphthalen-2-yl)-propanamine; 123. N-{5-ethenyl-4,6-dihydrogen 0 to σ and [3,4-c]0 to o -3--3-yl}-(4-D-pyridyl-l-yl)phenyl acetamide; 124· N-{5-ethenyl-4,6-dihydrogen ratio 0 and [3, 4-c] 0 is 嗤-3-118. N-{5-(2-morpholinylindolyl-5-furanyl)-4,6-

i 90119473(替換）-2.ptc 第347頁 1327569 修正案號 90119473 六、申請專利範圍基}-2-((4-吡咯啶-1-基）苯基）丙醯胺； 125. Ν-{5-乙驢基-4，6 -二氫吼17各并[3，4-c] D比0坐-3-基}-(4-(2-氧基比咯啶-1-基）苯基）乙醯胺； 126. ^{5-乙醯基-4，6-二氫吼11各并[3,4-(：]吼〇坐-3-基}-2-(4-(2-氧基-吼咯啶-1-基）苯基）丙醯胺； 12 7. Ν-2-曱氧苯基-Ν’ -{2-[4-(2 -氧基-。比咯啶-1-基）苯基]-丙醯胺基-4, 6 -二氫吡咯并[3, 4-c]吡唑-5 -基}脲； 128. N-2,4 -二氟苯基-N’-{2-[4-(2 -氧基-吡咯啶-1-基）苯基]-丙酿胺基-4，6 -二氫吼11 各并[3，4-c] 11比0坐_5_基} 129. N-(l -苯基）乙基-N’-{2-[4-(2 -氧基-吡咯啶-1-基）苯基]-丙酸胺基-4，6 -二氫π比p各并[3，4-c] °比。坐_5-基} 脲； 130. N-2-曱氧苯基-N’-{2-(4 -吡咯啶-1-基-苯基）-丙醯胺基-4, 6 -二氫吼略并[3,4-c] n比嗤-5-基}脲； 131. N-2,4-二氟苯基-Ν’ - {2-(4 -吡咯啶-1-基-苯基）-丙醯胺基-4, 6 -二氫吡咯并[3,4-c] π比唑-5-基}脲； 132. N-(l -苯基）乙基-Ν’ - {2-(4-0比各咬-1_基-苯基）-良醯胺基-4, 6-二氫吼咯并[3, 4-c]吡唑-5-基}脲； ®133. Ν-{5 -苯基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}-2-(4-咄咯啶-1-基-苯基）丙醯胺； 134. Ν-2-曱氧苯基- Ν’ _{[4-(2-氧基_ D比σ各0定-1-基）-苯基]-乙酿胺基- 4,6 -二氫°比0各并[3，4-c]e比嗤-5-基}脈； 13 5. N-2-氯苯基-Ν’ - { [4-(2-氧基-吡咯啶-1-基）-苯i 90119473 (replace)-2.ptc Page 347 1327569 Amendment No. 90119473 VI. Patent application base}-2-((4-pyrrolidin-1-yl)phenyl)propanamine; 125. Ν-{ 5-Ethyl-4,6-dihydroindole 17 each [3,4-c] D is 0--3-yl}-(4-(2-oxypyrrolidin-1-yl)benzene Ethylamine; 126. ^{5-Ethyl-4,6-dihydroindole 11 and [3,4-(:]吼〇-3-yl}-2-(4-(2) -oxy-indolyl-1-yl)phenyl)propanamine; 12 7. Ν-2-曱oxyphenyl-Ν' -{2-[4-(2-oxy-.pyrrolidine) -1-yl)phenyl]-propionylamino-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea; 128. N-2,4-difluorophenyl -N'-{2-[4-(2-oxy-pyrrolidin-1-yl)phenyl]-propenylamino-4,6-dihydroindole 11 each [3,4-c] 11 ～5_基} 129. N-(l-phenyl)ethyl-N'-{2-[4-(2-oxy-pyrrolidin-1-yl)phenyl]-propionic acid amine Base-4,6-dihydroπ ratio p and each [3,4-c] ° ratio. sit _5-yl} urea; 130. N-2-nonyloxyphenyl-N'-{2-(4 -pyrrolidin-1-yl-phenyl)-propionylamino-4,6-dihydroindole[3,4-c]n-pyridin-5-yl}urea; 131. N-2,4 -difluorophenyl-Ν' - {2-(4-pyrrole Pyridin-1-yl-phenyl)-propionylamino-4,6-dihydropyrrolo[3,4-c]pyridazole-5-yl}urea; 132. N-(l-phenyl) Ethyl-Ν' - {2-(4-0 than each bit-1-yl-phenyl)-benzamine-4,6-dihydroindolo[3,4-c]pyrazole-5 -yl}urea; ®133. Ν-{5-phenylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-2-(4-anthrolidine -1-yl-phenyl)propanamine; 134. Ν-2-曱oxyphenyl- Ν' _{[4-(2-oxy-D ratio σ each 0-decyl-1-yl)-phenyl ]-Ethylamino- 4,6-dihydrogen ratio 0 and [3,4-c]e is more than 嗤-5-yl} vein; 13 5. N-2-chlorophenyl-Ν' - { [4-(2-oxy-pyrrolidin-1-yl)-benzene

90119473(替換）-2.ptc 第348頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍基]-乙醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲； 136. N-(l -苯基）乙基-N’-{[4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲； 137. N -正丁基-N’-{[4-(2 -氧基-吡咯啶-1-基）-苯基]-乙醯胺基-4, 6 -二氫咄咯并[3, 4-c]吡唑-5 -基}脲； 138. N-{5 -苯基績臨基-4，6 -二氫°比洛并[3,4-c] D比0坐 -3 -基}-4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺； 139. N -正丁基-N’-{2-[4-(2 -氧基-吡咯啶-1-基）-苯基]-丙醯胺基-4, 6 -二氫°比咯并[3, 4-c]咄唑-5 -基}脲； 140.1^-{5-苯基磺醯基-4,6-二氬吡咯并[3,4-〇]咄唑 -3-基}-2-[4-(2 -氧基-吡咯啶-1-基）-苯基]-丙醯胺； 141. ^{5-胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-4-(2 -氣基-0比略°定-1_基）-苯基-乙酿胺； 142. N -正丁基-Ν’ - {2-(4 -吡咯啶-1-基-苯基）-丙醯胺基- 4,6 -二氫°比°各并[3,4-c]吼°坐-5-基}脲； 143. N-{5_胺基幾基_4，6_二氮吼0各并[3，4~c] °比°垒-3_ 基}-2-(4-吡咯啶-1-基）-苯基-丙醯胺； 144. N-2-甲氧苯基-『-{(4-咄咯啶-1-基-苯基）-乙醯胺基-4,6-二氫吼11各并[3,4-(：]11比°坐-5-基}脲； 145. N-2-氯苯基-Ν’ - {(4 -吡咯啶-1-基-苯基）-乙醯胺基- 4,6 -二氫°比°各并[3,4-c]吼嗤-5-基}脲； 146. N-(l -苯基）乙基-1^’-{(4-吡咯啶-1-基-苯基）-乙酉篮胺基_4，6_二氮π比11 各并[3，4_c] D比β坐_5_基}服； 147. Ν -正丁基-Ν’ - {(4 -吡咯啶-1-基-苯基）-乙醯胺基90119473 (replacement)-2.ptc Page 348 1327569 _ Case No. 90119473_Yearly __ Six, the scope of the patent application base]-acetamido-4,6-dihydroindole [3, 4-c Pyrazol-5-yl}urea; 136. N-(l-phenyl)ethyl-N'-{[4-(2-oxy-pyrrolidin-1-yl)-phenyl]-acetamidine Amino-4,6-dihydroindolo[3,4-c]pyrazol-5-yl}urea; 137. N-n-butyl-N'-{[4-(2-oxy-pyrrole) Acridine-1-yl)-phenyl]-acetamido-4,6-dihydroindolo[3,4-c]pyrazol-5-yl}urea; 138. N-{5-phenyl临临基-4,6-Dihydro-bipiro[3,4-c] D is 0-position -3 -yl}-4-(2-oxy-pyrrolidin-1-yl)-phenyl- Acetamine; 139. N-n-butyl-N'-{2-[4-(2-oxy-pyrrolidin-1-yl)-phenyl]-propanylamino-4,6-dihydrogen °Bedo[3,4-c]oxazol-5-yl}urea; 140.1^-{5-phenylsulfonyl-4,6-di-ar-pyrrolo[3,4-indole]carbazole- 3-yl}-2-[4-(2-oxy-pyrrolidin-1-yl)-phenyl]-propanamine; 141. ^{5-Aminocarbonyl-4,6-dihydroanthracene And [3,4-(:]pyrazol-3-yl}-4-(2-propenyl-0-succinyl-1)-phenyl-ethenylamine; 142. N-n-butyl -Ν' - {2-(4-pyrrolidin-1-yl-benzene ) 醯醯 4 4 4 4 4 4 3 3 3 3 3 3 3 3 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 143 6_diazepine 0 and [3,4~c] ° ratio -3 - base}-2-(4-pyrrolidin-1-yl)-phenyl-propanamide; 144. N-2- Methoxyphenyl-"-{(4-oxaridin-1-yl-phenyl)-acetamido-4,6-dihydroindole 11 each [3,4-(:]11 than ° sitting -5-yl}urea; 145. N-2-chlorophenyl-Ν'-{(4-pyrrolidin-1-yl-phenyl)-acetamido- 4,6-dihydrogen ratio And [3,4-c]indole-5-yl}urea; 146. N-(l-phenyl)ethyl-1^'-{(4-pyrrolidin-1-yl-phenyl)-acetamidine Basket amine group _4,6_diaza π ratio 11 and [3,4_c] D ratio β sitting _5_ base}; 147. Ν-n-butyl-Ν' - {(4-pyrrolidine-1 -yl-phenyl)-acetamido

! 90119473(替換）-2.ptc 第 349 頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 -4，6 -二氫D比p各并[3，4 - c ] °比D坐-5 -基}脲； 14 8. N-{ 5 -苯基磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3-基}-(4-吡咯啶-1-基-苯基）-乙醯胺； 149. N-乙基-Ν’-{[4-(2 -氧基-咄咯啶-1-基）-苯基]-乙 - 醯胺基- 4,6 -二氫D比D各并[3,4-c] D比β坐-5-基}脲； 150. Ν-異丙基-Ν’ -{ [4-(2-氧基-吼咯啶-1-基）-苯基]-乙酷胺基- 4，6 -二氫吼11各并[3,4-c] 0比。坐-5-基}脲； 151. N-{ 5-(2 -呋喃甲醯基）-4, 6 -二氫吡咯并[3, 4-c] 唑-3 -基}-4-(2 -氧基-吡咯啶-1-基）-苯基-乙醯胺；鲁15 2. N-{5-(2-曱氧苯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-(2 -氧基-咄咯啶-1-基）-苯基-乙醯胺； 15 3. N-{5 -胺基羰基曱基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-(2 -氧基比咯啶-1-基）-苯基-乙醯胺； 154. N-異丙基-Ν’ -{(4 -吡咯啶-1-基-苯基）-乙醯胺基 -4，6 -二氫吼11 各并[3，4-c] °比°坐-5-基}脲； 15 5. Ν-乙基-Ν’ -{(4 -吡咯啶-1-基-笨基）-乙醯胺基-4, 6 -二氫°比°各并[3，4 - c ] °比°坐-5 -基}脲； 156.^1-{5-胺基羰基曱基-4,6-二氫吡咯并[3,4-(：]咄唑 ^-基}-(4-咄咯啶-1-基-苯基）-乙醯胺； —157. Ν-{5-(3-曱基丁醯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-4-(2 -氧基-π比咯啶-1-基）-苯基-乙醯胺； 158. Ν -正丁基-Ν’ - {3-(2_萘-2-基）乙酿胺基-4，6 -二氫 0比D各并[3，4 - c ] °比°坐-5 -基}脲； 159. N -正丁基-Ν’ - {3-(3-甲基-苯基）乙醯胺基-4,6 -二90119473 (replacement)-2.ptc Page 349 1327569 _ Case No. 90119473_Yearly revision _ Six, the scope of patent application -4,6 - dihydrogen D ratio p and [3,4 - c ] ° ratio D Sodium-5-yl urea; 14 8. N-{ 5 -phenylsulfonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-(4-pyrrolidine -1-yl-phenyl)-acetamide; 149. N-ethyl-Ν'-{[4-(2-ethoxy-indolyl-1-yl)-phenyl]-ethyl-decylamine -4,6-dihydrogen D ratio D and [3,4-c] D ratio β sit-5-yl}urea; 150. Ν-isopropyl-Ν' -{ [4-(2-oxygen吼-Pyridine-1-yl)-phenyl]-ethylamino- 4,6-dihydroindole 11 each [3,4-c] 0 ratio. Sodium-5-yl}urea; 151. N-{ 5-(2-Furylmercapto)-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-(2 -oxy-pyrrolidin-1-yl)-phenyl-acetamide; Lu 15 2. N-{5-(2-indolylphenyl)-4,6-dihydropyrrolo[3, 4- c]pyrazol-3-yl}-4-(2-oxy-indolyl-1-yl)-phenyl-acetamide; 15 3. N-{5-aminocarbonylindenyl-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-(2-oxypyrrolidin-1-yl)-phenyl-acetamide; 154. N-isopropyl Base-Ν'-{(4-pyrrolidin-1-yl-phenyl)-acetamido-4,6-dihydroindole 11 each [3,4-c] ° ratio -5-based }urea; 15 5. Ν-ethyl-Ν'-{(4-pyrrolidin-1-yl-phenyl)-acetamido-4,6-dihydrogen °° each [3,4 - c ] ° ratio ° sit-5-yl} urea; 156.^1-{5-aminocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-(:]carbazole^-yl}- (4-oxaridin-1-yl-phenyl)-acetamide; -157. Ν-{5-(3-mercaptobutyl)-4,6-dihydropyrrolo[3,4-c] Pyrazol-3-yl}-4-(2-oxy-π-pyrrolidin-1-yl)-phenyl-acetamide; 158. Ν-n-butyl-Ν' - {3-(2_ Naphthalen-2-yl)ethinyl-4,6-dihydrogen 0 to D And [3,4 - c ] ° ratio ° sit-5-yl}urea; 159. N-n-butyl-Ν' - {3-(3-methyl-phenyl)acetamido-4,6 -two

! 90119473(替換）-2.ptc 第350頁 1327569 修正案號 90119473 六、申請專利範圍氫吼π各并[3, 4 - c ] D比。坐-5 -基}脲； 160. N-正丁基_N’ _{3-(3-氟-苯基）乙酿胺基_4, 6 -二氫 0比B各并[3，4 - c ] °比°坐-5 -基}脲； 161. N -正丁基-Ν’ - {3-(3_吡啶基）乙醯胺基-4, 6 -二氫 D比0各并[3，4 - c ] °比α坐-5 -基}脲； 162. Ν-正丁基-Ν’ - {3-(雙環[4. 2.0·]辛1，3, 5 -三烯-7-叛醯胺基）-4, 6 -二氫吼11 各并[3,4-c] π比唑-5-基}脲； 163. Ν-正丁基-Ν’ - {3 -苯氧乙醯胺基-4, 6 -二氫吡咯并 [3, 4-c] °比唑-5-基}脲； 164. Ν -正丁基-Ν’ - {3-(4-甲基-苯基）乙醯胺基-4, 6 -二氫吨σ各并[3，4 - c ] °比。坐-5 -基}脲； 165. Ν-正丁基-Ν’ - {3-(4-氟-苯基）乙醯胺基-4, 6 -二氫口比σ各并[3，4 - c ] D比β坐-5 -基}脲； 166. Ν-正丁基-Ν’ - {3-(3, 4-二氟-苯基）乙醯胺基-4, 6-二氫°比D各并[3, 4 - c ] ρ比α坐-5 _基}脲； 167. Ν-正丁基-Ν’ - {3-(4 -三氟甲氧-苯基）乙醯胺基-4, 6 -二氫°比ρ各并[3，4-c]°比。坐-5-基}脲； 168. N_正丁基_N’ _{3-(2_曱基-苯基）乙酿胺基_4，6_二氫°比B各并[3，4-c] °比β坐-5-基}脲； 16 9. Ν-正丁基-Ν’ -{3-(2 -溴-苯基）乙醯胺基-4, 6-二氫 0比0各并[3，4 - c ] D比唾-5 -基}脲； 170. N_正丁基_N’ - {3-(2，5_二苯基）乙蕴胺基_4，6-二氫啦11 各并[3，4-c] °比°坐-5-基}脲； 171. N-正丁基-Ν’ -{ 3-(4-(咣咯啶-1-基-羰基甲氧）-苯90119473 (replacement)-2.ptc Page 350 1327569 Amendment Case No. 90119473 VI. Patent application range Hydrogen 吼 π and [3, 4 - c ] D ratio. Sodium-5-yl urea; 160. N-n-butyl _N' _{3-(3-fluoro-phenyl)ethinyl-4,6-dihydrogen 0 to B each [3,4 - c ] ° ratio ° sitting -5 -yl} urea; 161. N-n-butyl-Ν' - {3-(3_pyridyl)acetamido-4,6-dihydrogen D is 0 [3,4 - c ] ° ratio α--5-yl}urea; 162. Ν-n-butyl-Ν' - {3-(bicyclo[4.2.0·] octane 1,3,5-triene- 7-rebel-amino)-4,6-dihydroindole 11 each [3,4-c] π-biazole-5-yl}urea; 163. Ν-n-butyl-Ν' - {3-benzene Oxyacetamido-4,6-dihydropyrrolo[3,4-c] °biazol-5-yl}urea; 164. Ν-n-butyl-Ν' - {3-(4-methyl -Phenyl)acetamido-4,6-dihydrotonium σ and [3,4 - c] ° ratio. Sodium-5-yl}urea; 165. Ν-n-butyl-Ν'-{3-(4-fluoro-phenyl)acetamido-4,6-dihydrogen port ratio σ[3,4 - c ] D is more than β--5-yl}urea; 166. Ν-n-butyl-Ν' - {3-(3, 4-difluoro-phenyl)acetamido-4,6-dihydro ° ratio D and [3, 4 - c ] ρ ratio α sitting -5 _ yl} urea; 167. Ν-n-butyl-Ν' - {3-(4-trifluoromethoxy-phenyl) acetamidine The ratio of amino-4,6-dihydrogen to ρ is [3,4-c]. Sodium-5-yl urea; 168. N_n-butyl _N' _{3-(2-mercapto-phenyl)ethinyl _4,6-dihydrogen ratio B and [3, 4-c] ° ratio β--5-yl} urea; 16 9. Ν-n-butyl-Ν' -{3-(2-bromo-phenyl)acetamido-4,6-dihydro 0比[3,4 - c ] D is more than spani-5-yl}urea; 170. N_n-butyl_N' - {3-(2,5-diphenyl)ethenyl _4 , 6-dihydrola 11 each [3,4-c] ° ratio -5-yl}urea; 171. N-n-butyl-Ν' -{ 3-(4-(pyrrolidin-1) -yl-carbonylmethoxy)-benzene

90119473(替換）-2.ptc 第351頁 1327569 ,_案號90119473_年月曰修正_ 六、申請專利範圍基）乙酿胺基-4，6_二氫各弁[3，4_c] °比0坐_5_基}脈； 172. N -正丁基-Ν’ - {3-（3-(胺基幾基甲氧）-苯基）乙驢胺基-4, 6 -二氫吼咯并[3, 4-c] °比唑-5-基}脲； 173. Ν -正丁基-Ν’ - {3-(咄啶-4-基-乙醯胺基）-4,6 -二 . 氫°比σ各并[3, 4 - c ] °比°坐-5 -基}脲； 174. Ν-正丁基-Ν’-{3-(4-(嗎啉-1-基）-苯基）乙醯胺基 -4，6 -二氫吼σ各并[3 , 4 - c ] °比°坐-5 -基}脲； 17 5. Ν-正丁基-Ν’ - {3-(2-氟-苯基）乙醯胺基-4, 6 -二氫口比0各并[3，4 - c ] Β比°坐-5 -基}脲；鲁176. Ν-正丁基-Ν’- {3-(3, 5 -二氟-苯基）乙醯胺基-4, 6-二氫°比11各并[3，4 - c ] °比。坐-5 -基}脲； 177. Ν-正丁基-Ν’-{3-(6 -氧基-6Η-嗒畊-1-基）乙醯胺基- 4,6 -二氫D比σ各并[3,4-c] β比吐-5-基}脲； 178. Ν-{5-曱基吡啶甲醯基-4, 6 -二氩吼咯并[3, 4-c]吡唑-3 -基}-4-( 2 -氧基-4唑啶-3 -基）-苯基-乙醯胺； 179. N-{ 5-(噻吩-2 -基）乙醯基-4, 6 -二氫吡咯并 [3, 4-c]吡唑-3 -基} - 4-(2 -氧基唑啶-3 -基）-苯基-乙醯胺； 1 8 0. N - { 5 - ( 2 -呋喃曱醯基）-4，6 -二氫吡咯并[3，4 - c ]吡 -基}-4-(2 -氧基-坐啶-3 -基）-苯基-乙醯胺； 181, N-{5-(2-乙氧乙醯基）-4, 6 -二氫咄咯并[3, 4-c]吡唾-3 -基}_4-(2 -氧基_ ^吐°定-3_基）-苯基乙酸胺； * 182. N-{5-(3-曱基-丁醯基）-4, 6 -二氫吡咯并[3, 4-c] ' 〇比。坐_3-基}_4-(2-氧基。坐咬-3-基）-苯基-乙酿胺；90119473 (replacement)-2.ptc Page 351 1327569, _ case number 90119473_Yearly revision _6, the scope of the patent application base) ethoxylated 4,6_ dihydrogen 弁 [3,4_c] ° ratio 0 _5_基} vein; 172. N-n-butyl-Ν' - {3-(3-(amino methoxy)-phenyl)acetamido-4,6-dihydroanthracene咯[3,4-c] °Biazol-5-yl}urea; 173. Ν-n-butyl-Ν' - {3-(acridin-4-yl-acetamido)-4,6 - II. Hydrogen ratio σ and [3, 4 - c ] ° ratio ° sit-5 -yl} urea; 174. Ν-n-butyl-Ν'-{3-(4-(morpholin-1- ))-phenyl)acetamido-4,6-dihydroindole σ[3,4 - c ] ° ratio ° sit-5-yl}urea; 17 5. Ν-n-butyl-Ν' - {3-(2-Fluoro-phenyl)acetamido-4,6-dihydrogen port ratio 0 and [3,4 - c ] Β ratio ° sit-5-yl} urea; Lu 176. Ν - n-Butyl-Ν'- {3-(3,5-difluoro-phenyl)acetamidoamine-4,6-dihydrogen ratio 11 and [3,4 - c] ° ratio. Sodium-5-yl}urea; 177. Ν-n-butyl-Ν'-{3-(6-oxy-6Η-嗒耕-1-yl)acetamido- 4,6-dihydro-D ratio σ 并 [3,4-c] β 比 -5-5-yl} urea; 178. Ν-{5-mercaptopyridine carbazino-4,6-diarhydron-[3, 4-c] Pyrazol-3-yl}-4-(2-oxy-4-oxaridin-3-yl)-phenyl-acetamide; 179. N-{ 5-(thiophen-2-yl)ethenyl- 4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-(2-oxoxazolidin-3-yl)-phenyl-acetamide; 1 8 0. N - { 5 - ( 2 -furanthyl)-4,6 -dihydropyrrolo[3,4 - c ]pyridyl}-4-(2-oxy-sodium-3-yl)-benzene Benzylamine; 181, N-{5-(2-ethoxyethyl)-4,6-dihydroindolo[3,4-c]pyrazin-3-yl}_4-(2 -oxy _ oxime -3 -yl)-phenylacetic acid amine; * 182. N-{5-(3-indolyl-butenyl)-4,6-dihydropyrrolo[3, 4-c ] ' Debbie. Sitting _3-yl}_4-(2-oxy. sit--3-yl)-phenyl-ethylamine;

90119473(替換）-2.ptc 第352頁 1327569 修正案號 90119473 六、申請專利範圍 183. N-{5 - 丁酿基-4，6_ 二氫 σ比 11 各并[3，4-c] °比°坐- 3-基}-4-(2-氧基-0¾唑啶-3-基）-苯基-乙醯胺； 184. N-異丙基-Ν’ -{3-[4-(2 -氧基-A唑啶-3 -基）-苯基 -乙醯胺基]-4,6 -二氫°比17各并[3,4-c]0比0坐-5-基}脲； 185. N-(正丁基）-N’-{3-[4-(2-氧基-。气唑啶-3 -基）-苯基-乙醯胺基]-4, 6 -二氫咄咯并[3, 4-c]"比唑-5 -基}脲； 186. N-{5-乙氧羰基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}-4-(2-氧基-。fl¾唑啶-3-基）-苯基-乙醯胺； 187. ^異丙基-『-{3-[2-(3-氧基-3,4,43,83-四氫 -2H-苯并[1，4]稀'3°¾ D井-6 -基）乙酿胺基]-4,6 -二氫吼11 各并 [3, 4-c]吡唑-5-基}脲； 18 8. N-異丙基-Ν’ -{ 3-(3 -溴-苯甲醯胺基）-4, 6 -二氫吡 0各并[3,4-c]D&^-5-*}脲； 189. N-{5 -苯續醯基-4,6 -二氫°比洛并[3,4-c] °比°坐-3-基}-3-溴苯甲醯胺； 190. N-{5-乙臨基-4, 6 -二氫 0比°各并[3, 4-c] °比唾-3-基}-[4-(1-吡咯啶-2-酮）苯甲醯胺]; 191. N-乙基-Ν’ - {3-(3 -溴-苯甲醯胺基）-4,6 -二氫吡咯并[3, 4-c]吡唑-5-基}脲； 192. N-{5-(8 -喳啉）磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑-3 -基卜對曱苯曱醯胺； 19 3. N-苯基-Ν’ -{3-(3 -溴-苯甲醯胺基）-4, 6 -二氫吡咯并[3, 4-c]吡唑-5-基}脲； 194. Ν-{5 -苯磺乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑90119473 (replacement)-2.ptc Page 352 1327569 Amendment No. 90119473 VI. Patent application scope 183. N-{5 - butyl-based 4,6_ dihydro-sigma ratio 11 each [3,4-c] °比. 3-yl}-4-(2-oxy-03⁄4oxazolidine-3-yl)-phenyl-acetamide; 184. N-isopropyl-Ν' -{3-[4- (2-Oxo-AZoxazin-3-yl)-phenyl-acetamido]-4,6-dihydrogen ratio 17 and [3,4-c]0 to 0--5-based Urea; 185. N-(n-butyl)-N'-{3-[4-(2-oxy-.oxazolidin-3-yl)-phenyl-acetamido]-4, 6 - Dihydroindolo[3,4-c]"Bizozol-5-yl}urea; 186. N-{5-Ethoxycarbonyl-4,6-dihydropyrrolo[3,4-c] Oxazol-3-yl}-4-(2-oxy-.fl3⁄4oxazolidine-3-yl)-phenyl-acetamide; 187. ^isopropyl-"-{3-[2-(3 -oxy-3,4,43,83-tetrahydro-2H-benzo[1,4]diluted '3°3⁄4 D well-6-yl)ethanoyl]-4,6-dihydroindole 11 Each [3,4-c]pyrazol-5-yl}urea; 18 8. N-isopropyl-Ν'-{3-(3-bromo-benzamide)-4, 6-di Hydropyrrolidino[3,4-c]D&^-5-*}urea; 189. N-{5-Benzene fluorenyl-4,6-dihydro-pyrolo[3,4-c ° ° °-3-yl}-3-bromobenzamide; 190. N-{5-临基-4,6-Dihydrogen 0°°[3, 4-c] ° than sial-3-yl}-[4-(1-pyrrolidin-2-one)benzamide]; 191 N-ethyl-Ν'-{3-(3-bromo-benzylamino)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea; 192. N-{5-(8-carboline)sulfonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl-p-benzoquinone; 19 3. N -phenyl-Ν'-{3-(3-bromo-benzylamino)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl}urea; 194. Ν- {5 - phenylsulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole

90119473(替換）-2.ptc 第353頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 -3 -基} - 3 -溴苯甲醯胺； 195. N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4_〇]咄唑 -3-基}-3-溴苯曱醯胺； 196. N-異丙基-Ν’-{3-[4-(1-吡咯啶-2 -酮）-苯基醯胺基]-4，6 -二氫σ比咯并[3, 4 - c ]吼°坐-5 -基}脲； 197.1{5-(8-喳啉）羰基-4,6-二氫咣咯并[3,4-〇]吡唑 -3 -基卜對甲苯甲醯胺； 198.1'1-{5-(1-萘）石黃酸基-4,6-二氫吡11各并[3,4-(：]'1比。坐 -3_基}_4_苯基苯曱S盛胺； •199. Ν-{5-(1-萘曱醯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}_4 -苯基苯曱酸胺； 200. Ν-{5-(1-萘曱醯基）-4,6 -二氫吡咯并[3,4-c]吡唑 -3-基}-4-苯氧苯曱醯胺； 2 01. N-苯基-Ν’ - {3-(4_苯基-苯甲醯胺基）-4, 6 -二氫吡 σ各并[3，4 - c ]吼°坐-5 -基}脲； 202.\-{5-苯基乙醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-4-苯基苯曱醯胺； 20 3. Ν-{5-(1-萘）磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑基}-對甲苯甲醯胺； •20 4. N-{5-(1-萘甲醯基）-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-對曱苯甲醯胺； 205. N-{5_ 乙酿基_4，6 -二氫吼17各并[3，4_c] 0比0坐_3~ 基}-3-苯氧苯曱醯胺； 206.1^-[5-(4_氯-2,5-二氟苯甲醯基）-4,6-二氫吡咯并90119473 (replacement)-2.ptc Page 353 1327569 _ Case number 90119473_Yearly revision _ VI. Patent application scope -3 - base} - 3 -Bromobenzamide; 195. N-{5-decane Sulfhydryl-4,6-dihydropyrrolo[3,4_indene]oxazol-3-yl}-3-bromophenylamine; 196. N-isopropyl-Ν'-{3-[ 4-(1-pyrrolidin-2-one)-phenylguanidino]-4,6-dihydroσ-pyrolo[3,4-c]吼°-5-yl}urea; 197.1{5 -(8-porphyrin)carbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl-p-tolylcarbamide; 198.1'1-{5-(1-naphthalene) Rhein-based-4,6-dihydropyrene 11 each [3,4-(:]'1 ratio. Sodium-3_yl}_4_phenylphenylhydrazine S-amine; •199. Ν-{5 -(1-naphthylfluorenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenylbenzoate; 200. Ν-{5-(1 -naphthyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenoxybenzamine; 2 01. N-phenyl-Ν' - {3-(4-Phenyl-benzhydrylamino)-4,6-dihydropyridinium each [3,4 - c ]吼° sit-5-yl}urea; 202.\-{5- Phenylethyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-4-phenylbenzamide; 20 3. Ν-{5-(1-naphthalene Sulphur 4-,6-dihydropyrrolo[3,4-c]pyrazolyl}-p-tolylcarbamide; •20 4. N-{5-(1-naphthylmethyl)-4,6- Dihydropyrrolo[3,4-c]pyrazole-3-yl}-p-benzoic acid amide; 205. N-{5_ ethoxylated _4,6-dihydroindole 17 each [3,4_c ] 0 to 0 sitting _3~ yl}-3-phenoxybenzamine; 206.1^-[5-(4-chloro-2,5-difluorobenzhydryl)-4,6-dihydropyrrole and

90119473(替換）-2.ptc 第354頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍 [3,4-c]吼唑-3-基]-2-(2 -萘基）乙醯胺； 207. N-{5-[第三丁基羧酸根]-4, 6 -二氫吡咯并[3, 4-c] 吡唑-3-基}-2-(2 -萘基）乙醯胺； 20 8. Ν-{5-[(1-曱基環丙基）羰基]-4, 6-二氫吼咯并[3, 4-c]吡唑-3-基}-2-(2 -萘基）乙醯胺； 209. N-[5-(環丁基羰基）-4,6 -二氫吡咯并[3,4-c]吡唑 _3_基]- 2- (2_秦基）乙酸胺； 210. N-[5-(2-氟苯甲醯基）-4,6 -二氫吼咯并[3,4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 211. N-[5-(吡啶-3 -基羰基）-4,6 -二氫吡咯并[3,4-c] 吡唑-3 -基]-2-(2 -萘基）乙醯胺； 212. 1^-{5-[(2,2,2,3，-四甲基環丙基）羰基]-4,6-二氫吡咯并[3,4-c]吼唑-3-基}-2-(2 -萘基）乙醯胺； 213. N-[5-(2, 4,5 -三氟苯甲醯基）-4,6 -二氫吡咯并[3, 4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 214. N-[5-(2-甲基戊-4 -烯醯基）-4,6 -二氫吡咯并 [3, 4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 215. N-[5-(環丙基乙醯基）-4,6 -二氫吡咯并[3,4-c] 唑-3 -基]-2-(2 -萘基）乙醯胺； 216. N-[5-(5-氟-2-曱基苯甲醯基）-4, 6 -二氫吡咯并 [3，4-c]吡唑-3 -基]-2-(2 -萘基）乙醯胺； 217. ^{5-[2-氟-5-(三氟曱基）苯甲醯基]-4,6-二氫咄咯并[3,4-c]咄唑-3-基}-2-(2_萘基）乙醯胺； 218.1{5-[(3-甲氧環己基）羰基]-4,6-二氫°比咯并[3,90119473 (replacement)-2.ptc Page 354 1327569 _ Case No. 90119473_年月日日__ VI. Patent application scope [3,4-c]oxazol-3-yl]-2-(2-naphthyl) Acetamine; 207. N-{5-[Tertiary butyl carboxylate]-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-(2-naphthyl) Ethylamine; 20 8. Ν-{5-[(1-indolylcyclopropyl)carbonyl]-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}- 2-(2-naphthyl)acetamide; 209. N-[5-(cyclobutylcarbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl]- 2 - (2_Qinyl)acetic acid amine; 210. N-[5-(2-fluorobenzhydryl)-4,6-dihydroindolo[3,4-c]pyrazole-3-yl] -2-(2-naphthyl)acetamide; 211. N-[5-(pyridin-3-ylcarbonyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl ]-2-(2-naphthyl)acetamide; 212. 1^-{5-[(2,2,2,3,-tetramethylcyclopropyl)carbonyl]-4,6-dihydropyrrole And [3,4-c]oxazol-3-yl}-2-(2-naphthyl)acetamide; 213. N-[5-(2, 4,5-trifluorobenzhydryl)- 4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl]-2-(2-naphthyl)acetamide; 214. N-[5-(2-methylpent-4 -methenyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-3 - -2-(2-naphthyl)acetamide; 215. N-[5-(cyclopropylethylhydrazino)-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl -2-(2-naphthyl)acetamide; 216. N-[5-(5-fluoro-2-mercaptobenzylidene)-4,6-dihydropyrrolo[3,4-c Pyrazol-3-yl]-2-(2-naphthyl)acetamide; 217. ^{5-[2-Fluoro-5-(trifluoromethyl)benzimidyl]-4,6- Dihydroindolo[3,4-c]oxazol-3-yl}-2-(2-naphthyl)acetamide; 218.1{5-[(3-methoxycyclohexyl)carbonyl]-4, 6-dihydrogen ratio is [3,

90119473(替換）-2.ptc 第355頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍 4-c]吡唑-3-基}-2-(2 -萘基）乙醯胺； 219. N-[5-(2,4 -二氯-5 -氟苯甲醯基）-4,6-二氳吡咯并 [3，4-c] π比0坐-3-基]-2-(2 -萘基）乙醯胺； 220. N-[5-(2 -氯-4,5-二氟苯曱醯基）-4,6-二氫吡咯并 [3，4-c]°比唑-3 -基]-2-(2 -萘基）乙醯胺； 221. ^{5-[4-(1}1-咪唑-：1-基）苯曱醯基]-4,6-二氫咣口各并[3,4-c] 0比0坐-3-基}-2-(2 -萘基）乙醯胺； 222. N-{5-[4-(胺基石黃臨基）丁酿基]-4，6 -二氮吼11 各弁 [3，4-c] π比β坐-3_基}-2-(2 -萘基）己酿胺；籲^23. N-{5-[(8 -氧基-5，6，7，8_ 四氫蔡-2-基）截基]- 4,6 -二氫咄咯并[3,4-c]吡唑-3-基}-2-(2 -萘基）乙醯胺； 224. N-(5_丙嗣酿基_4，6_二氣0比哈并[3，4_c] B比0坐_3-基）_2-(2_秦基）乙酿胺； 225. N-[5-(2, 2 -二曱基丙醯基）-4,6 -二氫吡咯并 [3, 4-c]呲唑-3 -基]-2-(2 -萘基）乙醯胺； 226. N-(5 - 丁_2_ 酿基-4，6_ 二氮 D比 11 各并[3，4_c] π比 11 坐_3_ 基）-2-(2_秦基）乙酷胺； 227. Ν-[5-(3 -碘-4-曱基苯甲醯基）-4,6 -二氫吡咯并 4_c]D比哇_3_基]_2~(2_秦基）乙酿胺； ®228. N-{5-[(苄基氧）乙醯基]-4, 6 -二氫吼咯并[3, 4-c] 吡唑-3-基}-2-(2 -萘基）乙醯胺； 229. N-{5-(2-氟-2 -苯基乙醯基）-4,6 -二氫吡咯并 [3,4-c]吡唑-3-基}-4-第三丁基苯甲醯胺； 230. N-{5-(2-氟-2 -苯基乙醯基）-4, 6 -二氫吡咯并90119473 (replacement)-2.ptc Page 355 1327569 _ Case No. 90119473_Yearly revision _ VI. Patent scope 4-c]pyrazol-3-yl}-2-(2-naphthyl)acetamide 219. N-[5-(2,4-dichloro-5-fluorobenzhydryl)-4,6-dipyrido[3,4-c] π ratio 0--3-yl]- 2-(2-naphthyl)acetamide; 220. N-[5-(2-chloro-4,5-difluorobenzoinyl)-4,6-dihydropyrrolo[3,4-c ]°Bizozol-3-yl]-2-(2-naphthyl)acetamidamine; 221. ^{5-[4-(1}1-imidazolium-:1-yl)benzoinyl]-4 , 6-dihydropurine each [3,4-c] 0 to 0--3-yl}-2-(2-naphthyl)acetamide; 222. N-{5-[4-(amine基石黄临基)丁丁基]-4,6-diazepine 11 弁[3,4-c] π ratio β sit-3_yl}-2-(2-naphthyl)hexylamine; N-{5-[(8-oxy-5,6,7,8-tetrahydroxan-2-yl))- 4,6-dihydroindolo[3,4-c]pyrazole -3-yl}-2-(2-naphthyl)acetamidamine; 224. N-(5_ propyl aryl _4,6_two gas 0 than ha and [3,4_c] B ratio 0 sitting _ 3-yl)_2-(2_methylidene)ethinamide; 225. N-[5-(2,2-dimercaptopropyl)-4,6-dihydropyrrolo[3, 4-c ]carbazole-3-yl]-2-(2-naphthyl)acetamide; 22 6. N-(5-butyl-2_-bristyl-4,6-dinitrogen D ratio 11 and [3,4_c] π ratio 11 sitting _3_yl)-2-(2_methylidyl) acetamide; 227 . Ν-[5-(3 -iodo-4-mercaptobenzylidene)-4,6-dihydropyrrolo-4_c]D than wow_3_yl]_2~(2_Qinyl) ® 228. N-{5-[(benzyloxy)ethenyl]-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-2-(2-naphthalene) Ethylamine; 229. N-{5-(2-fluoro-2-phenylethenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}- 4-tert-butylbenzamide; 230. N-{5-(2-fluoro-2-phenylethenyl)-4,6-dihydropyrrole

90119473(替換）-2.ptc 第356頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍 [3,4-c]咄唑-3-基}-4 -苯氧苯曱醯胺； 231. N-{5-(2 -噻吩基-乙醯基）-4,6 -二氫°比咯并 [3,4-c]吡唑-3-基}-4-(4-曱基哌畊基）苯甲醯胺； 232. N-{5-(3-曱基-丁醯基）-4,6_ 二氫"比咯并[3,4-c] 吡唑-3-基}-4-(4_甲基哌畊基）苯曱醯胺； 233. ^-{5-(2-口夫喃子驢基）_4，6_ 二氫0比0各弁[3，4-〇] 吡唑-3 -基} - 4 - (4 -曱基哌畊基）苯曱醯胺； 234.1^-{5-苯基乙醯基-4,6-二氫吡17各并[3,4-(：]°比。坐 -3-基}-4-(4-甲基哌畊基）苯甲醯胺； 235. N-{5 -苯磺醯基-4,6-二氫咄咯并[3,4-c]°比唑-3-基}-4-(4-曱基哌畊基）苯甲醯胺； 236. N-(2,6 -二乙基苯基）-N’-{3-[4-(4-甲基哌啡基）苯甲醯胺]-4，6 -二氫0比°各并[3,4-c] 0比。坐-5-基}脲； 237. N-乙基-N’-{3-[4-(4-曱基哌畊基）苯甲醯胺] -4,6 -二氫β比B各并[3，4-c]吼吐-5 -基}脲； 238. N-{5-(2-氟-2 -苯基乙醯基）-4,6 -二氫"比咯并 [3,4-c]0比唑-3-基}-[4-(1_吡咯啶-2 -酮）苯甲醯胺]; 239. N_{5-(2-敦_2_苯基乙酿基）-4，6_二氫0比17各并 [3,4-c]。比唑-3 -基}-4-(4-曱基哌。丼基）苯甲醯胺； 240. N-{5-(2 -噻吩基乙醯基）-4,6 -二氫咄咯并[3,4-c] 〇比唾-3 _基} _胡椒基酿胺； 241. N-{5-(3-曱基-丁醯基）-4,6 -二氫咄咯并[3, 4-c] 吡唑-3 -基}-胡椒基醯胺； 242. 夫喃甲醯基）-4,6 -二氫 11 比洛并[3,4-c]90119473 (replacement)-2.ptc Page 356 1327569 _ Case number 90119473_年月日日__ VI. Patent application scope [3,4-c]oxazol-3-yl}-4-phenoxybenzoquinone 231. N-{5-(2-Thienyl-ethenyl)-4,6-dihydro-pyrolo[3,4-c]pyrazol-3-yl}-4-(4-oxime Benzylamine benzoguanamine; 232. N-{5-(3-indolyl-butenyl)-4,6-dihydro"bido[3,4-c]pyrazol-3-yl} -4-(4_methylpipedyl)benzamide; 233. ^-{5-(2-mouthmanatene)_4,6_ dihydrogen 0 to 0 弁[3,4-〇 Pyrazol-3-yl}-4-(4-carbylpipedyl)benzamide; 234.1^-{5-phenylethenyl-4,6-dihydropyridyl 17[3, 4-(:]° ratio. Sodium-3-yl}-4-(4-methylpipedyl)benzamide; 235. N-{5-Benzenesulfonyl-4,6-dihydroanthracene [3,4-c]°bazol-3-yl}-4-(4-mercaptopiperidinyl)benzamide; 236. N-(2,6-diethylphenyl)- N'-{3-[4-(4-methylpiperidinyl) benzamide]-4,6-dihydrogen 0 ratio °[3,4-c] 0 ratio. Sit-5-based Urea; 237. N-ethyl-N'-{3-[4-(4-mercapto-peptidyl) benzamide] -4,6-dihydro-β ratio B and [3,4- c] 吼吐-5-基}urea; 238 . N-{5-(2-Fluoro-2-phenylethenyl)-4,6-dihydro"bido[3,4-c]0-pyrazol-3-yl}-[4- (1_pyrrolidin-2-one)benzamide> 239. N_{5-(2-Den-2-phenylethyl)-4,6-dihydrogen 0 to 17 each [3, 4-c].Bizozol-3 -yl}-4-(4-mercaptopiperazinyl)benzamide; 240. N-{5-(2-thiophenylethenyl)-4,6 -dihydroindolo[3,4-c]pyrene than salino-3_yl}-pipelined amine; 241. N-{5-(3-indolyl-butenyl)-4,6-dihydroanthracene [3,4-c]pyrazol-3-yl}-piperonyl decylamine; 242. fluarmyryl)-4,6-dihydro 11 piroxi[3,4-c]

90119473(替換）-2.ptc 第357頁 1327569 修正案號 90119473 六、申請專利範圍口比唑-3-基}-胡椒基醯胺； 243· Ν-{5 -苯基乙醯基）-4,6 -二氫π比σ各并[3,4-c] π比0坐 -3 _基}-胡椒基酷胺； 244. Ν-{5 -苯磺醯基）-4, 6 -二氫吼咯并[3, 4-c]吡唑-3- 基}_胡 245. 4 - c ] 0比 246. [3, 4-c φ24 7. 基}-乙 248. 基}-環 249. 基}-異 25 0. 基}-環 251. •25 2. 基}-甲 253. 基}_於 254. 椒基醢胺； N-{ 5-(2-三氟甲基）苯磺醯基-4, 6 -二氫吼咯并[3, 唑-3-基}-胡椒基醯胺； N-乙基-Ν’ -{3-胡椒基羧醯胺基-4, 6-二氫吡咯并 ]〇比σ坐-5 -基}脲； Ν-{5-乙酸基-4，6 -二氫D比0各并[3，4-c] 0比0坐-3_ 醯胺； N-{5-乙醯基-4，6 -二氫11比洛并[3，4-c] 0比唾-3-丙烷羧醯胺； N-{5-乙趨基-4，6 -二氫D比D各并[3, 4-c]吼0坐- 3-丁醯胺； N-{5-乙醯基-4, 6 -二氫π比B各并[3, 4-c] °比0坐- 3-戊烷羧醯胺； N-{5-乙酿基_4，6 -二氮0比0各弁[3，4-c] °比0坐_3_ 曱醯胺； N-{5-乙醯基-4, 6 -二氫0比D各并[3，4-c] °比0坐- 3-基吡啶甲醯胺； N-{5_乙酿基-4，6 -二氫13比σ各并[3，4-c] 0比°坐_3_ 鹼醯胺； Ν-{5_乙酸基_4, 6 -二氮吼11各并[3，4_c] π比0坐_3_90119473 (replacement)-2.ptc Page 357 1327569 Amendment No. 90119473 VI. Patent application range: oxazol-3-yl}-piperidinamide; 243·Ν-{5-phenylethenyl)-4 , 6-dihydro π ratio σ and [3,4-c] π ratio 0 sitting -3 _ yl}-piperonylamine; 244. Ν-{5 - phenylsulfonyl)-4, 6 - two Hydropyrrolo[3,4-c]pyrazol-3-yl}_hu245. 4 - c ] 0 to 246. [3, 4-c φ24 7. yl}-ethyl 248. yl}-ring 249 . base}-iso 25 0. ki}-ring 251. •25 2. yl}-- 253. yl} _ 254. sulphonylamine; N-{ 5-(2-trifluoromethyl)benzenesulfonate Mercapto-4,6-dihydroindolo[3,oxazol-3-yl}-piperidinylamine; N-ethyl-Ν'-{3-piperylcarboxamide-4,6-di Hydropyrrolo]pyrene ratio σ5-5-urea urea; Ν-{5-acetoxy-4,6-dihydro D ratio 0 and [3,4-c] 0 to 0 sit-3_decylamine; N-{5-ethinyl-4,6-dihydro 11-pyrolo[3,4-c] 0 is more than saliva-3-propanecarboxamide; N-{5-ethylthio-4,6- Dihydrogen D is more than D and [3, 4-c]吼0 sits - 3-butyramine; N-{5-ethinyl-4,6-dihydropi is more than B[3, 4-c ° ° sit 0 - 3-pentane carboxamide; N-{5-ethyl ketone _4,6 - diaza 0 to 0 弁 [3,4-c] ° ratio 0 sitting _3_ decylamine; N-{5-ethinyl-4,6-dihydrogen 0 to D each [3,4-c] ° ratio 0-3-pyridine pyridine carbenamide; N-{5_乙乙基-4,6-dihydro 13 ratio σ[3,4-c] 0 ratio ° sitting_3_ alkali decylamine; Ν-{5_acetic acid group _4, 6 - two Nitrogen 吼11 each [3,4_c] π is 0 _3_

90119473(替換）-2.ptc 第358頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍基} _異菸鹼醯胺； 255. N-{5-乙酿基-4, 6 -二氫0比0各并[3, 4-c] °比《坐-3-基}-3-甲基-2 -呋喃曱醯胺； 256_ N-{5“ 乙驢基_4，6_ 二氫 °比洛弁[3，4-c] 51 比 0坐-3_ 基} - σ塞吩-2 -缓隨胺； 257.1^-{5-乙醯基-4,6-二氫。比咯并[3,4-〇]吡唑-3-基} - π塞吩-3 -缓疏胺； 258. Ν-{5-乙臨基-4, 6 -二氫 0比°各并[3, 4-c] 0比0坐- 3-基}-鄰-甲苯甲醯胺； 259. Ν_{5-乙酸基_4，6 -二氮0比 σ各弁[3，4_c] 0 比0坐 _3_ 基}-間-甲苯甲醯胺； 260. Ν-{5 -乙醯基-4, 6 -二氫0比 0各并[3, 4-c] °比0坐-3-基}-對-甲苯甲醯胺； 261. Ν-{5-乙醯基-4, 6 -二氫吼11 各并[3, 4-c] 0 比唾- 3-基} _水楊酿胺， 262. Ν-{5-乙 Si 基-4, 6 -二氫吼11各并[3, 4-c] σ 比唾- 3-基}-2-氟苯甲醯胺； 263. Ν-{5-乙臨基-4,6 -二氫 0 比 σ各并[3,4-c] 0 比0坐- 3-基卜3-氟苯甲醯胺； 264. N_{5-乙隨基_4，6_ 二氫 π比0各弁[3，4_c] 0 比。坐-3_ 基}-4-氟苯曱醯胺； 265. N-{5-乙醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基卜噻吩-2-乙醯胺； 266. N-{5-乙醯基-4,6-二氫°比咯并[3,4-(：]吡唑-3-90119473 (replacement)-2.ptc Page 358 1327569 _ Case No. 90119473_Year of the month __ VI. Patent application base} _Isonicotinium amide; 255. N-{5-Ethyl-4, 6 - dihydrogen 0 to 0 each [3, 4-c] ° ratio "sodium-3-yl}-3-methyl-2-furanium amide; 256_ N-{5" acetamyl _4,6_ Dihydropyrazine [3,4-c] 51 is more than -3 - yl} - σ septene-2 - accompaniment to amine; 257.1^-{5-ethenyl-4,6-dihydro.咯[3,4-〇]pyrazol-3-yl}-π-cephen-3-propanamide; 258. Ν-{5-ethionyl-4,6-dihydrogen 0°°[ 3, 4-c] 0 to 0 sitting - 3-yl}-o-toluamylamine; 259. Ν_{5-acetic acid _4,6-diaza 0 ratio σ 弁 [3,4_c] 0 ratio 0 sit _3_ base}-m-toluamylamine; 260. Ν-{5-acetamido-4,6-dihydrogen 0 to 0 each [3, 4-c] ° ratio 0 sitting -3- }.-p-toluamylamine; 261. Ν-{5-acetamido-4,6-dihydroindole 11 each [3, 4-c] 0 than salino-3-yl} _ water yang Amine, 262. Ν-{5-ethyl-4-yl-4,6-dihydroindole 11 each [3, 4-c] σ than sal-3-yl}-2-fluorobenzamide; 263. Ν -{5-ethionyl-4,6-dihydrogen 0 is more than σ and [3,4-c] 0 is 0-position - 3-kib 3-fluorobenzamide; 264. N_{5-Bisinyl_4,6_Dihydroπ ratio 0 弁[3,4_c] 0 ratio. Sit-3_yl}-4-fluorophenylamine; 265. N-{5-B Mercapto-4,6-dihydropyrrolo[3,4-c]oxazol-3-ylthiophene-2-acetamide; 266. N-{5-ethenyl-4,6-dihydro ° 比比和[3,4-(:]pyrazole-3-

卯 119473(替換）-2.ptc 第359頁 1327569 案號 90119473 年月曰修正六、申請專利範圍基}-噻吩-3-乙醯胺； 267. N-{5-乙酿基-4，6 -二氫 ° 比 c各并[3,4-c] 0 比0坐-3-基}-苯基丙炔醯胺； 268. N-{5_ 乙隨基 _4，6_ 二氫 0 比洛并[3，4-c] 0 比0坐- 3-基}-3_氛基苯曱酿胺； 269. N-{5-乙酸基-4,6 -二氫各并[3，4-c] π 比0坐- 3-基}-4-氰基苯甲酿胺； 270. Ν-{5-乙酿基-4，6 -二氫 0比°各并[3,4-c] 0比峻-3-基}_反-桂皮酸胺； _271.^-{5-乙酷基-4，6-二氫0比11各并[3,4-〇;]11比°坐-3-基}-順-桂皮酿胺； 272. N-{5-乙醯基-4，6 -二氫 0比 D各并[3, 4-c] 0比 °坐-3-基} - 3 - ( 3 -吡啶基）丙烯醯胺； 273. N-{5-乙酿基-4,6 -二氫吼°各并[3,4-c]吼〇坐-3-基} - 3 - ( 4 -吡啶基）丙烯醯胺； 274. N-{5_ 乙酸基_4，6_ 二氮 B 比 17各并[3，4-c] 0 比0坐-3_ 基}_2-苯基丙酿胺， 275. N-{5-乙酿基-4,6 -二氫吼0各并[3,4-c] 0 比0坐- 3-g -鄰-甲苯基乙醯胺； 276. N-{5-乙酿基-4，6 -二氫。比口各并[3，4-c] π比0坐-3-基}-間-甲苯基乙醯胺； 277· Ν-{5-乙醯基-4,6 -二氫 °比°各并[3,4-c] 11 比。坐- 3-基}-對-甲苯基乙醯胺； 278. N-{5-乙醒基-4,6 -二氫。比0各并[3,4-c] 0 比唆- 3-卯119473 (replacement)-2.ptc Page 359 1327569 Case No. 90119473 Amendment 六6, the scope of the patent application}-thiophene-3-acetamide; 267. N-{5-ethyl aryl-4,6 - dihydrogen ratio c and each [3,4-c] 0 to 0 -3-yl}-phenylpropynylamine; 268. N-{5_ 乙其基_4,6_ dihydro 0 洛洛And [3,4-c] 0 is 0 to 0 - 3-yl} -3 - aryl benzoate; 269. N-{5-acetoxy-4,6-dihydro-[3,4- c] π is 0-position - 3-yl}-4-cyanobenzamide; 270. Ν-{5-ethyl-branched-4,6-dihydrogen 0 ratio °[3,4-c] 0 than jun-3-yl}_trans-cinnamic acid amine; _271.^-{5-ethyl keto-4,6-dihydro 0 to 11 each [3,4-〇;] 11 than ° sitting - 3-yl}-cis-cinnamin; 272. N-{5-ethinyl-4,6-dihydrogen 0 to D and [3, 4-c] 0 to °-3-yl} 3-(3-pyridyl)propenylamine; 273. N-{5-ethyl-branched-4,6-dihydroindole °[3,4-c]indole-3-yl} - 3 - ( 4 -pyridyl)propenylamine; 274. N-{5_acetic acid group 4,6_ dinitrogen B ratio 17 and [3,4-c] 0 to 0 sitting -3_yl}_2-phenylpropane Amine, 275. N-{5-Ethyl-4,6-dihydroindole 0 and [3,4-c] 0 to 0 - 3-g - o- Phenyl as acetamide; 276. N- {5- yl stuffed ethyl 4,6 - dihydro. Comparing with each mouth [3,4-c] π is 0 -3-yl}-m-tolyl acetamide; 277· Ν-{5-ethenyl-4,6-dihydrogen ° ° And [3,4-c] 11 ratio. Sodium 3-yl}-p-tolylacetamide; 278. N-{5-Ethyl-4,6-dihydrogen. More than 0 and [3,4-c] 0 is more than - 3-

第360頁 90119473(替換）-2.ptc 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍基}-鄰-茴香醯胺； 279. N-{5-乙酿基-4, 6 -二氫0比洛并[3, 4-c] 0 比0坐-3-基}-3-甲氧苯曱醯胺； 280. N-{5-乙酿基-4，6 -二氫 °比洛并[3，4-c] 0比0坐- 3-基卜對-茴香驢胺； 281. N-{5-乙酿基-4, 6 -二氫0比 ^各并[3, 4-c] 0 比。坐-3-基}-苯氧乙醯胺； 282. Ν-{5-乙醒基-4, 6 -二氫吼11 各并[3, 4-c] 0 比0坐-3-基}_2_氣苯基乙酿胺； 283.1{5-乙醯基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3-氟苯基乙醯胺； 284. Ν-{5-乙醯基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}_4-氟苯基乙酸胺； 285. Ν-{5-乙酸基-4, 6 -二氫0比 σ各并[3, 4-c] »比〇坐- 3-基}-3_(2_°塞吩基）丙稀酸胺； 286. Ν-{5_ 乙酿基-4，6 -二氫0比哈并[3，4-c] 0比0坐-.3_ 基卜3 - ( 3 -噻吩基）丙烯醯胺； 287. Ν-{5-乙醯基-4，6 -二氫 °比°各并[3，4-c] 0比唾-3 二基}-3-(2-噻吩基）丙醯胺； 288. Ν-{5-乙醯基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}-2-氯苯曱醯胺； 289.1^-{5-乙醯基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基} - 3 -氯苯曱醯胺； 290. Ν-{5-乙酸基-4，6 -二氫0比 ρ各并[3，4-c] 0比0坐- 3-Page 360 90119473 (replacement) - 2.ptc 1327569 _ case number 90119473_Yearly revision _ 6. Patent application base}-o-anisoleamine; 279. N-{5-ethyl aryl-4, 6 - dihydro 0-pyrolo[3,4-c] 0 is 0-O--3-yl}-3-methoxybenzamine; 280. N-{5-ethyl-branched-4,6-dihydrogen °Biluo[3,4-c] 0 to 0 sitting - 3-kib-p-anisamine; 281. N-{5-ethyl-branched-4,6-dihydro- 0-^^[3 , 4-c] 0 ratio. -3--3-yl}-phenoxyacetamide; 282. Ν-{5-ethylidene-4,6-dihydroindole 11 each [3, 4-c] 0 to 0 -3-yl} _2_ gas phenylethylamine; 283.1 {5-acetamido-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-fluorophenylacetamide; 284. Ν-{5-Ethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-fluorophenylacetic acid amine; 285. Ν-{5-acetoxy -4,6-dihydrogen 0 to σ and [3, 4-c] » 〇 - - 3-yl}-3_(2_°secenyl) acrylamide; 286. Ν-{5_ -4-4,6-dihydrogen 0 is more than hexamethylene [3,4-c] 0 to 0 sitting -.3_ kib 3 - (3 -thienyl) acrylamide; 287. Ν-{5-ethyl fluorenyl -4,6-dihydrogen ratio °[3,4-c] 0-salt-3-diyl}-3-(2-thienyl)propanamine; 288. Ν-{5-ethenyl -4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-2-chlorobenzamide; 289.1^-{5-ethinyl-4,6-dihydropyrrole And [3,4-〇]pyrazol-3-yl}-3-chlorobenzamide; 290. Ν-{5-acetoxy-4,6-dihydro- 0 ratio ρ[3,4- c] 0 to 0 sitting - 3-

! 90119473(替換）-2.ptc I 第361頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍基} -4-氯苯曱醯胺； 2 91. N-{5-乙醯基-4，6 -二氫 ° 比0各并[3，4-c] ° 比0坐-3-基} - ；!-哌啶丙醯胺； 292. N-{5-乙酿基-4，6 -二氫 D 比 σ各并[3, 4-c] 0 比0坐- 3-基}-2-乙醯基苯曱醯胺； 293. Ν-{5-乙醯基-4,6 -二氫 0比0各并[3,4-c] 0 比0坐-3-基} - 4 -乙醯基苯甲醯胺； 294. N-{5-乙龜基-4,6 -二氫吼口各并[3,4-c]吼0坐-3-基} - 1 -萘甲醯胺；籲2 95. N-{5-乙醯基-4,6 -二氫°比0各并[3,4-c] 0比。坐-3- 基} - 2 -萘曱醯胺； 296. N-{5-乙醯基-4，6 -二氫 0 比 17各并[3,4-c]吼0坐-3-基} - 3 -苯甲醯基丙醯胺； 297. N_{5_ 乙酸基-4，6_ 二氮 D 比洛弁[3，4 - c] 0 比0坐_3_ 基}-4-乙醯胺基苯曱醯胺； 298.1^-{5-乙醯基-4，6-二氫吼11各并[3,4-〇]°比峻-3-基}-2, 5-二甲氧苯曱醯胺； 299. N-{5-乙醯基-4，6 -二氫 D比0各并[3, 4-c] «比〇坐- 3- g- 2, 6 -二甲氧苯曱醯胺； 300· N_{5_ 乙酿基_4，6_二氫° 比洛并[3，4-c] π 比0坐 _3_ 基}-3, 4-二甲氧苯甲醯胺； 301. Ν-{5-乙酿基_4，6_ 二氮 π 比 ρ各弁[3，4_c] 0 比0坐 _3_ 基}- 3,5 -二曱氧苯曱醯胺； 302. N_{5-乙酿基_4，6_二氫B比洛并[3，4-c] 0比嗤_3_90119473 (replacement)-2.ptc I Page 361 1327569 _ Case No. 90119473_Year of the month __ VI. Patent application base} -4-Chlorobenzoquinone; 2 91. N-{5-Ethyl Base-4,6-dihydrogen ratio 0 and each [3,4-c] ° is 0 -3-yl} - ;!-piperidine propylamine; 292. N-{5-ethyl aryl- 4,6-dihydrogen D ratio σ and [3, 4-c] 0 to 0-spin-3-yl}-2-ethenylbenzamine; 293. Ν-{5-ethenyl-4 , 6-dihydrogen 0 to 0 each [3,4-c] 0 to 0--3-yl} - 4 -ethenylbenzamide; 294. N-{5-ethanetosyl-4, 6-dihydropurine each [3,4-c]吼0--3-yl}-1 -naphthylamine; 2 95. N-{5-ethenyl-4,6-dihydrogen ° is 0 and each is [3,4-c] 0 ratio. -3--3-yl} - 2 -naphthylamine; 296. N-{5-ethenyl-4,6-dihydrogen 0 to 17 and [3,4-c]吼0--3-yl } - 3 - benzhydryl propylamine; 297. N_{5_ acetate-4,6_diaza D, piroxime [3,4 - c] 0 ratio 0 _3_ yl}-4-acetamide Benzobenzamine; 298.1^-{5-ethenyl-4,6-dihydroindole 11 each [3,4-〇]° ratio jun-3-yl}-2, 5-dimethoxybenzene Indoleamine; 299. N-{5-ethenyl-4,6-dihydrogen D is 0 and each [3, 4-c] «比〇- 3- g- 2, 6-dimethoxybenzene Indoleamine; 300· N_{5_ ethyl ketone _4,6_ dihydrogen piroxi[3,4-c] π ratio 0 sitting _3_ ki}-3, 4-dimethoxybenzamide 301. Ν-{5-ethyl ketone _4,6_ dinitrogen π ratio ρ 弁 [3,4_c] 0 to 0 sitting _3_ ki}} 3,5-dioxabenzoylamine; 302. N_{5-ethyl-branched _4,6_dihydro-B is more than [3,4-c] 0 than 嗤_3_

90119473(替換）-2.ptc 第362頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍基卜3-(2-噻吩甲醯基）-丙醯胺； 303. N-{5 -乙醯基-4，6 -二氫 °比0各并[3, 4-c] n比。坐-3-基}-1-秦基乙酸胺； 304. N-{5-乙酿基-4, 6 -二氫0比 0各并[3, 4-c] °比。坐- 3-基}-4_苯基苯甲醯胺； 305. N-{5-苄基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-乙醯胺； 306· N-{5-窄基 _4，6_ 二氫 0比°各并[3，4-c] π比0坐-3_ 基}- 環丙烷羧醯胺； 307. Ν-{5-笮基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-異丁醯胺； 308. Ν-{5-苄基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}-環戊烷羧醯胺； 309. Ν_{5_ 辛基_4, 6 -二氫 °比0各弁[3，4_c] °比0坐_3_ 基}_ 苯甲醯胺； 310. N-{5 -辛基 _4，6_ 二氫 π比 σ各并[3，4-c] 0比峻-3-基}-曱基吡啶甲醯胺； 311. Ν-{5-芊基-4,6-二氫吡咯并[3,4-cレ比唑-3-基}-菸鹼醯胺； 312. Ν-{5 -罕基-4，6 -二氫 σ比 ρ各并[3，4-c] 0比0坐-3_ 基}-異菸鹼醯胺； 313. Ν-{5 -节基_4，6 -二氫。比。各并[3，4-c] D比0坐-3_ 基}-3_曱基-2-呋喃甲醯胺； 314. N-{5 -亨基-4，6 -二氫 °比°各并[3，4-c] D比吐-3-基}-90119473 (replacement)-2.ptc Page 362 1327569 _ Case No. 90119473_Yearly revision _ 6. Patent application scope Kib 3-(2-thiophenemethyl)-propanamide; 303. N-{5 -Ethylidene-4,6-dihydrogen ratio is 0 and [3, 4-c] n ratio. Sodium-3-yl}-1-methylacetic acid amine; 304. N-{5-ethyl-branched-4,6-dihydro- 0- 0 each [3, 4-c] ° ratio. Sodium 3-yl}-4-phenylbenzamide; 305. N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-B Indoleamine; 306· N-{5-narrow base_4,6_dihydrogen 0 ratio °[3,4-c] π ratio 0 sitting -3_yl}-cyclopropanecarboxamide; 307. Ν-{ 5-mercapto-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-isobutylamine; 308. Ν-{5-benzyl-4,6-dihydroanthracene咯[3,4-c]pyrazol-3-yl}-cyclopentanecarboxamide; 309. Ν_{5_octyl_4,6-dihydrogen ratio 0 弁[3,4_c] ° ratio 0 sit _3_ base}_ benzepidine; 310. N-{5-octyl_4,6_ dihydro π ratio σ[3,4-c] 0 ratio jun-3-yl}-fluorenyl Pyridylcarbendazim; 311. Ν-{5-mercapto-4,6-dihydropyrrolo[3,4-cindazol-3-yl}-nicotinium amide; 312. Ν-{5 -罕基-4,6-dihydro σ ratio ρ[3,4-c] 0 to 0 sit-3_ ki}-isonicotinium amide; 313. Ν-{5 - nodal _4,6 - Dihydrogen. ratio. Each [3,4-c] D is more than 0--3_yl}-3_mercapto-2-furancarbamide; 314. N-{5-Henke-4,6-dihydrogen °° And [3,4-c] D is more than -3-yl}-

90119473(替換）-2.ptc 第363頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍噻吩-2-羧醯胺； 315. N-{5-苄基-4,6-二氫咄咯并[3,4-c]吡唑-3-基}-噻吩-3-羧醯胺； 316. N-{5 -苄基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}-. 鄰-曱苯曱醯胺； 317. ^{5-芊基-4,6-二氫吡咯并[3,4-〇]咄唑-3-基}-間-曱苯曱醯胺； 318. N-{5 -辛基- 4,6 -二氫 0 比 11 各并[3，4-c] °比〇坐-3_ 基}-對-甲苯甲醯胺；鲁319. N-{5 -芊基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}- 苯基乙醯胺； 320. N-{5 -苄基-4,6-二氫咄咯并[3,4-c]°比唑-3-基}-水楊醯胺； 321. N-{5 -苄基-4, 6 -二氫〇比0各并[3,4-c] 0比。坐- 3-基}-2-氟苯曱醯胺； 32 2· N-{5-苄基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-3-氟苯曱醯胺； 323. N-{5-苄基-4, 6 -二氫 11比咯并[3,4-c] D比唑- 3- g-4-氟苯曱醯胺； •3 24.1^-{5-芊基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-噻吩-2-乙醯胺； 325. N - {5 -辛基 -4，6 -二氮 D比 D各并[3,4-c] °比〇坐-3-基}-‘噻吩-3-乙醯胺； 326. N-{5-苄基-4, 6 -二氫 °比0各并[3,4_c] 〇比〇坐-3-基}-90119473 (replacement)-2.ptc Page 363 1327569 _ Case number 90119473_Yearly date correction _ 6. Patent application range thiophene-2-carboxamide; 315. N-{5-benzyl-4,6-two Hydroquino[3,4-c]pyrazol-3-yl}-thiophene-3-carboxamide; 316. N-{5-benzyl-4,6-dihydropyrrolo[3,4- c] oxazol-3-yl}-. o-nonylbenzamide; 317. ^{5-mercapto-4,6-dihydropyrrolo[3,4-indole]oxazol-3-yl} -m-p-benzoylamine; 318. N-{5-octyl- 4,6-dihydrogen 0 to 11 each [3,4-c] ° than sputum -3_yl}-p-toluene醯amine; Lu 319. N-{5-mercapto-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-phenylacetamide; 320. N-{5 - Benzyl-4,6-dihydroindolo[3,4-c]°bazol-3-yl}-salicylimamine; 321. N-{5-benzyl-4,6-dihydroindole More than 0 and [3,4-c] 0 ratio. Sodium 3-yl}-2-fluorobenzoguanamine; 32 2· N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3 - fluorobenzamide; 323. N-{5-benzyl-4,6-dihydro 11-pyrolo[3,4-c] D-pyrazole-3- g-4-fluorobenzoguanamine; • 3 24.1^-{5-mercapto-4,6-dihydropyrrolo[3,4-indolyl]pyrazol-3-yl}-thiophene-2-acetamide; 325. N - {5 - Octyl-4,6-diaza D ratio D and [3,4-c] ° ratio -3--3-yl}-'thiophene-3-acetamide; 326. N-{5-benzyl- 4, 6 - dihydrogen ° ratio 0 and [3,4_c] 〇〇 -3- -3- base}-

90119473(替換）-2_ptc 第364頁 1327569 _案號 90119473_年月日_jfi_ 六、申請專利範圍苯基丙炔醯胺； 327. N-{5-芊基-4,6-二氫咣咯并[3,4-c]吡唑-3-基}_3_氯基苯曱酸胺； 328. N-{5-爷基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-4-氰基苯甲醯胺； 329. N-{5 -苄基-4,6-二氫吡咯并[3,4-c]吼唑-3-基}-反-桂皮醯胺； 330· N-{5-芊基-4,6 -二氫吼咯并[3, 4-c]吡唑-3 -基}-順-桂皮酿胺； 331.1{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3-(3 -吡啶基）丙烯醯胺； 332. ^{5-苄基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基} - 3 - (4 - °比啶基）丙烯醯胺； 333. N-{5 -芊基-4,6 -二氫咄咯并[3,4-c]吡唑-3-基}_2_苯基丙酿胺； 334. N-{5_ 亨基-4，6_ 二氫0比 p各并[3，4-c] 0比0坐 _3_ 基}-鄰-曱苯基乙醯胺； 335.1^-{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-間-曱苯基乙醯胺； 336. N-{5 -辛基-4，6 -二氫°比°各并[3，4-c] D 比唾-3_ 基}-對-曱苯基乙醯胺； 337. N-{5-¥ 基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-鄰-茴香醯胺； 338. N-{5 -芊基-4,6 -二氫咄咯并[3, 4-c]吡唑-3-90119473 (replacement)-2_ptc Page 364 1327569 _ Case number 90119473_Year of the month _jfi_ VI. Patent application range Phenylpropynylamine; 327. N-{5-Mercapto-4,6-dihydroanthracene And [3,4-c]pyrazol-3-yl}_3_chlorobenzoylamine; 328. N-{5-yote-4,6-dihydropyrrolo[3,4-c]pyridinium Zyridin-3-yl}-4-cyanobenzamide; 329. N-{5-benzyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-inverse - cinnamylamine; 330· N-{5-mercapto-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}-cis-cinnamamine; 331.1{5-benzyl 4-,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-(3-pyridyl)propenylamine; 332. ^{5-benzyl-4,6 - dihydroindolo[3,4-(:]pyrazol-3-yl}-3-(4-pyridyl)propenylamine; 333. N-{5-mercapto-4,6- Dihydroindolo[3,4-c]pyrazol-3-yl}_2-phenylpropanol; 334. N-{5_ Henry-4,6_ dihydrogen 0 to p each [3,4 -c] 0 to 0 sitting _3_ ki}-o-indole phenyl acetamide; 335.1^-{5-benzyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3 -yl}-m-phenyl phenyl acetamide; 336. N-{5 -octyl-4,6-dihydrogen ratio °[3,4-c] D than sal-3_yl}-pair -曱phenyl Indoleamine; 337. N-{5-¥yl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-o-anisylamine; 338. N-{5-芊4-,6-dihydroindolo[3,4-c]pyrazole-3-

! 90119473(替換）-2.ptc 第365頁 1327569 案號 90119473 年月曰修正六、申請專利範圍基}-3-曱氧苯曱醯胺； 339. N-{5-窄基 _4，6_ 二氫 °比 17各并[3，4_c] π比〇坐 _3_ 基}-對-茴香醯胺； 34 0. Ν-{5-苄基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3 -基}-苯氧乙醯胺； 341.1^-{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-2-氟苯基乙醯胺； 342.. Ν-{5-辛基 _4，6_ 二氫 0 比 Β各并[3，4-c] 比0坐- 3_ 基}-3-氟苯基乙醯胺；籲843. N-{5 - 辛基 _4，6_ 二氫各并[3，4-c]吼。坐-3_ 基} - 4-氟苯基乙醯胺； 344. N-{5_ 辛基 _4，6 -二氫 π比 p各并[3，4-c] °比°坐-3_ 基}-3-(2_ π塞吩基）丙細酸胺， 345. Ν-{5-笮基- 4,6 -二氫 D 比 σ各并[3,4-c]吼〇坐- 3-基}-3-(3-噻吩基）丙烯醯胺； 346. N-{5_ 爷基 _4，6_ 二氮 D 比 B各并[3，4-c] 0 比0坐 _3_ 基}-3_(2_ π塞吩基）丙酿胺， 347. Ν-{5_ 辛基 _4，6_ 二氫 σ 比洛并[3，4-c] 0 比 σ坐-3_ g-2-氯苯曱醯胺； —34 8. N-{5-苄基-4, 6 -二氫咄咯并[3, 4-c]咄唑-3-基}_3_氯苯曱蕴胺， 349.1{5-苄基-4,6-二氫吡咯并[3,4-〇:]咄唑-3-基}-4-氯苯甲醯胺； 350. N-{5-苄基- 4,6 -二氫各并[3,4-c] 〇比°坐-3-90119473 (replacement)-2.ptc Page 365 1327569 Case No. 90119473 Amendment 六6, the scope of application for patents}-3-oxophenhydramine; 339. N-{5-narrow base_4,6_ Dihydrogen ratio 17 and [3,4_c] π is more than 〇3_ ki}-p-anisamine; 34 0. Ν-{5-benzyl-4,6-dihydropyrrolo[3, 4 -c]pyrazol-3-yl}-phenoxyacetamide; 341.1^-{5-benzyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}- 2-fluorophenylacetamidine; 342.. Ν-{5-octyl_4,6-dihydrogen 0 is more than [3,4-c] than 0-position - 3_yl}-3-fluorophenyl Acetamine; 843. N-{5 - octyl_4,6-dihydro-[3,4-c]indole. -3-yl} 4-fluorophenylacetamide; 344. N- {5_ octyl _4,6-dihydro π ratio p and [3,4-c] ° ratio ° sitting -3 yl}-3-(2_ π phenanthryl) propyl amide, 345. Ν- {5-fluorenyl- 4,6-dihydrogen D ratio σ[3,4-c] --3-yl}-3-(3-thienyl)propenylamine; 346. N-{ 5_ 贵基_4,6_ dinitrogen D is more than B and [3,4-c] 0 is 0 to 0 _3_ ki}}__(2_ π phenanthyl) propylamine, 347. Ν-{5_ octyl _4,6_ Dihydro σ Biluo[3,4-c] 0 than σ sitting-3 _ g-2-chlorophenylamine; -34 8. N-{5-benzyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl}_3_chlorobenzene Indoleamine, 349.1{5-benzyl-4,6-dihydropyrrolo[3,4-indene]oxazol-3-yl}-4-chlorobenzamide; 350. N-{5- Benzyl-4,6-dihydro each [3,4-c] 〇 ratio ° sitting -3-

第366頁 90119473(替換）-2.ptc 1327569 _案號90119473_年月日__ 六、申請專利範圍基} - 1 -哌啶丙醯胺； 351.1{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-2_乙酿基苯曱酿胺； 352.1{5-芊基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-乙醯基苯甲醯胺； 353.1^-{5-苄基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基} - ：!-萘曱醯胺； 354.1^-{5-苄基-4,6-二氫咄咯并[3,4-〇]吡唑-3-基} - 2 -萘甲醯胺； 355. N-{5 -苄基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-3-苯甲醯基丙醯胺； 356. N-{5-辛基-4,6-二氫吡咯并[3,4-c]吡唑_3-基}-4-乙醯胺基苯甲醯胺； 357. N-{5-苄基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-2,5-二甲氧苯甲醯胺； 358. N-{5-苄基-4,6-二氫°比咯并[3,4-c]吡唑-3-基}-2,6-二曱氧苯甲醯胺； 359.1{5-苄基-4,6-二氫吡咯并[3,4-〇]"比唑-3-基}-3, 4-二曱氧苯甲醯胺； 360. N-{5 -辛基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}-3,5-二曱氧苯曱醯胺； 361. N-{5-芊基-4，6 -二氫0比 0各并[3，4-c] 0比°坐-3-基}-3-( 2-噻吩甲醯基）-丙醯胺； 362. N-{5-苄基-4,6-二氫吡咯并[3,4-〇]吡唑-3-Page 366 90119473 (replacement)-2.ptc 1327569 _ case number 90119473_Year of the month __ VI. Patent application base} - 1 - piperidine propylamine; 351.1 {5-benzyl-4,6-two Hydropyrrolo[3,4-(:]pyrazol-3-yl}-2_ethylphenyl benzoate; 352.1{5-mercapto-4,6-dihydropyrrolo[3,4-( :]pyrazol-3-yl}-4-ethylmercaptobenzamide; 353.1^-{5-benzyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3- Base} - :!-naphthylamine; 354.1^-{5-benzyl-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-2 -naphthylcarboxamide 355. N-{5-Benzyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-phenylmercaptopropylamine; 356. N-{5 - octyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-4-acetamidobenzamide; 357. N-{5-benzyl-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2,5-dimethoxybenzamide; 358. N-{5-benzyl-4,6-dihydro Bisolo[3,4-c]pyrazol-3-yl}-2,6-dioxabenzoguanamine; 359.1{5-benzyl-4,6-dihydropyrrolo[3,4- 〇]"Bizozol-3-yl}-3,4-dioxabenzoguanamine; 360. N-{5-octyl-4,6-dihydropyrrolo[3,4-c]pyridyl Zyrid-3-yl}-3,5-dioxabenzoquinone; 3 61. N-{5-fluorenyl-4,6-dihydrogen 0 to 0 and [3,4-c] 0 to °-3-yl}-3-(2-thienylmethyl)-propyl Guanidine; 362. N-{5-benzyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3-

90119473(替換）-2.ptc 第367頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍基}_2 -蔡基乙酿胺； 363. N-{5 -亨基-4，6_ 二氫 °比°各并[3，4_c] ° 比0坐- 3-基}_1_秦基乙酿胺； 364. N-{5_ 竿基-4，6_ 二氫 D 比 0各并[3，4-c] 0 比0坐- 3-基}-4-苯基苯曱醯胺； 365. N-{5 -苯基乙基- 4,6 -二氫0比0各并[3，4-c] 0比0坐- 3-基}-乙醯胺； 366.1{5-苯基乙基-4,6-二氫吼咯并[3,4-(：]吡唑-3-基}-環丙烷羧醯胺； 0367.^{5-苯基乙基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基}-異丁醯胺； 36 8. N-{5 -苯基乙基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-環戊烷羧醯胺； 369.1{5-苯基乙基-4,6-二氫吡(1各并[3,4-(：]'1比唑-3-基}-苯曱醯胺； 370.1{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-甲基吡啶甲醯胺； 371.1{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-&}-菸鹼醯胺； _3 72.1{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基}-異菸鹼醯胺； 373. N-{5 -笨基乙基-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基}-3-甲基-2-呋喃曱醯胺； 374. N-{5 -苯基乙基-4, 6 -二氫吡咯并[3,4-c]咄唑-3-90119473 (replacement)-2.ptc Page 367 1327569 _ Case No. 90119473_Yearly revision _ 6. Patent application base}_2 - Cai Jiyi amine; 363. N-{5 - Henki-4,6_ dihydrogen °°°°[3,4_c] ° ratio 0 sitting - 3-base}_1_Qinyl ethylamine; 364. N-{5_ fluorenyl-4,6_ dihydrogen D is 0 each [3,4 -c] 0 to 0 sitting - 3-yl}-4-phenylbenzamide; 365. N-{5-phenylethyl-4,6-dihydrogen 0 to 0 each [3,4- c] 0 to 0 sitting - 3-yl}-acetamide; 366.1 {5-phenylethyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}- Cyclopropane carboxamide; 0367.^{5-Phenylethyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-isobutylamine; 36 8. N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-cyclopentanecarboxamide; 369.1{5-phenylethyl-4 ,6-dihydropyr (1 each [3,4-(:]'1-pyrazol-3-yl}-benzoguanamine; 370.1{5-phenylethyl-4,6-dihydropyrrole [3,4-〇]pyrazol-3-yl}-methylpyridinecarboxamide; 371.1{5-phenylethyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3 -&}-nicotinamide; _3 72.1{5-phenylethyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-iso Basic amide; 373. N-{5-stupylethyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-methyl-2-furanium amide 374. N-{5-Phenylethyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-

90119473(替換）-2.ptc 第368頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍基}-噻吩-2 -羧醯胺； 375.1{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]吼唑-3-基}-噻吩-3 -羧醯胺； 376. N-{5_苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3- 基}-鄰-甲苯曱醯胺； 377.1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-間-曱苯甲醯胺； 378. N-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]咄唑-3-基}-對-甲苯甲醯胺； 379. ?^-{5-苯基乙基-4,6-二氫吡咯并[3,4-〇:]吡唑-3-基}-笨基乙醯胺； 380. N-{5 -苯基乙基- 4,6 -二氫π比嘻并[3,4-c]吡唑- 3-基丨-水楊醯胺； 381.1{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]吡唑-3-基卜2-氟苯曱醯胺； 382.1{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基卜3-氟苯曱醯胺； 383. N-{5_苯基乙基_4，6_二氫D比σ各弁[3，4-c]吼α坐-3-基}-4-氟苯甲醯胺； 384_ Ν - {5_苯基乙基_4，6_二氫D比0各并[3，4-c] D比。坐-3_ 基}-噻吩-2-乙醯胺； 385.1{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑_3-基} - 11塞吩-3 _乙蕴胺， 386. N-{5_苯基乙基_4，6 -二氫°比0各并[3，4-c] π比0坐- 3_90119473 (replacement)-2.ptc Page 368 1327569 _ Case number 90119473_Yearly revision _ 6. Patent application base}-thiophene-2-carboxycarboxamide; 375.1{5-phenylethyl-4,6 -dihydropyrrolo[3,4-indole-3-oxazol-3-yl}-thiophene-3-carboxycarboxamide; 376. N-{5_phenylethyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-o-toluidine; 377.1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazole- 3-yl}-m-nonylbenzamide; 378. N-{5-phenylethyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-p- Toluamide; 379. ?^-{5-Phenylethyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazol-3-yl}-phenylacetamide; 380. N-{5-phenylethyl-4,6-dihydropi-pyrido[3,4-c]pyrazole-3-ylindole- salicylamine; 381.1{5-phenylethyl-4 ,6-dihydropyrrolo[3,4-indene]pyrazol-3-yl b 2-fluorobenzoguanamine; 382.1{5-phenylethyl-4,6-dihydropyrrolo[3,4 -(:]pyrazol-3-ylbu-3-fluorophenylguanamine; 383. N-{5_phenylethyl_4,6-dihydrogen D ratio σ 弁 [3,4-c]吼坐--3-yl}-4-fluorobenzamide; 384_ Ν - {5_phenylethyl_4,6-dihydro D ratio 0 and [3,4-c] D ratio. 3_yl}-thiophene-2-acetamide; 385.1{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}-11 phenophene-3 _B-amine, 386. N-{5_phenylethyl_4,6-dihydrogen ratio 0 and [3,4-c] π ratio 0 sitting - 3_

90119473(替換）-2.ptc 第369頁 1327569 案號 90119473 年修正六、申請專利範圍基}-苯基丙炔醯胺； 38 7. N-{5-苯基乙基-4, 6-基}_3-氰基苯曱酿胺； 388. N-{5-苯基乙基-4, 6-基}_4-氰基苯曱隨胺； 389. N_{5_ 苯基乙基-4，6-基}-反-桂皮醯胺；氫吡洛并[3，4 - c ] β比唾-3 - 氫°比ρ各并[3，4 - c ] °比吐-3 - 氫 0比 11各并[3，4 - 39 0. {5 -苯基乙基-4, 6 -二氫吼°各并[3, 4-c] 0比0坐- 3- 基}-順-桂皮酿胺；籲391. N-{5-苯基乙基-4,6-S}_3_(3_ntba定基）丙稀酿胺； 392. N-{5_ 苯基乙基_4，6_ 基}-3-(4_ °比啶基）丙烯醯胺；氫吼ρ各并[3，4 - c ] °比°坐-3 - 393. Ν-{5 -苯基乙基_4,6-二氫咄咯并[3,4-(：]吡唑-3- 基}_2 -苯基丙酿胺； 394. Ν-{5-苯基乙基-4, 6-基}-鄰-甲苯基乙醯胺； 395. Ν-{5_ 苯基乙基_4，6-間-曱苯基乙醯胺； 6. Ν-{5-苯基乙基-4,6- 基}-對-甲苯基乙醯胺； 397. Ν-{5_ 苯基乙基-4，6_ 基}-鄰-茴香醯胺； 398. Ν - {5 -苯基乙基-4，6_ 氫0比σ各并[3，4 - c ]吼°坐-3 - 二氫°比洛并[3，4 - c ]"比°坐-3 - 氫0比Β各并[3，4 - c ]吼°坐-3 - 氫0比D各并[3，4 - c ]吼η坐-3 -90119473 (replacement)-2.ptc Page 369 1327569 Case No. 90119473 Amendment VI, Patent Application Base}-Phenylpropynylamine; 38 7. N-{5-Phenylethyl-4,6-yl }_3-cyanobenzoquinone; 388. N-{5-phenylethyl-4,6-yl}_4-cyanobenzoquinone with amine; 389. N_{5_phenylethyl-4,6 -基}-反- cinnamamide; hydropyrazolo[3,4 - c ] β than saliva-3 - hydrogen ° ρ and [3,4 - c ] ° ratio torto-3 - hydrogen 0 to 11 Each [3,4 - 39 0. {5-phenylethyl-4,6-dihydroindole °[3, 4-c] 0 to 0 sitting - 3-yl}-cis-cinnamamine 391. N-{5-Phenylethyl-4,6-S}_3_(3_ntba-decyl) acrylamide; 392. N-{5_phenylethyl-4,6-yl}-3-( _-{5-phenylethyl-4,6-dihydroindole [3,4-(:]pyrazol-3-yl}_2-phenylpropanol; 394. Ν-{5-phenylethyl-4,6-yl}-o-tolylacetamide; 395. Ν-{5_Phenylethyl_4,6-m-indolephenylacetamide; 6. Ν-{5-phenylethyl-4,6-yl}-p-tolylacetamide ; 397. Ν-{5_ phenylethyl-4,6-yl}-o-anion Amine; 398. Ν - {5-phenylethyl-4,6_ hydrogen 0 to σ each [3,4 - c ]吼°-3 - dihydro-pyro[3,4 - c ]&quot ; than ° ° -3 - Hydrogen 0 than Β each [3,4 - c ] 吼 ° sitting -3 - Hydrogen 0 than D each and [3,4 - c ]吼η sitting -3

90119473(替換）-2.ptc 第370頁 ip7569 *_案號90119473_年月日修正_ 六、申請專到範圍基}-3-甲氧苯甲醯胺； 399. N-{5 -苯基乙基_4，6 -二氫0比洛并[3，4-c] 0比0坐- 3-基}-對-茴香酸胺； 400. N-{5 -苯基乙基-4, 6 -二氫D比p各并[3, 4-c] π比唑- 3-基}-苯氧乙醯胺； 401. Ν-{5 -苯基乙基-4，6 -二氫吼17各并[3,4-c] 0比。坐- 3-基}_2_氣苯基乙酿胺， 402. Ν-{5 -苯基乙基-4,6-二氫吼咯并[3,4-c]吡唑-3-基}_3_氣苯基乙酿胺； 403. Ν-{5 -苯基乙基-4,6 -二氫吼咯并[3, 4-c]吡唑-3-基}-4_氣苯基乙酿胺； 404. Ν-{5 -苯基乙基-4, 6 -二氫吡σ各并[3,4-c] 0比°坐-3-基} - 3 - (2 _嚷吩基）丙稀酿·胺， 405. ^{5-苯基乙基-4,6-二氫咄咯并[3,4-〇:]吡唑-3-基} _ 3 _ ( 3 _ π塞吩基）丙稀臨胺， 406. Ν-{5 -苯基乙基-4,6-二氫σ比咯并[3,4-c]吡唑-3-基}-3-(2 -噻吩基）丙醯胺； 407. N-{5 -苯基乙基-4,6 -二氫°比咯并[3,4-c]吡唑-3-基}-2 -氯苯甲醯胺； 408. N-{5 -苯基乙基-4, 6 -二氫0比ρ各并[3,4-c] 0比0坐- 3-基}-3-氯苯曱醯胺； 409. N-{5_苯基乙基_4，6_二氮n比洛并[3，4-c] °比°圭-3_ 基}-4-氯苯曱醯胺； 410. N-{5 -苯基乙基_4，6_二氮°比洛弁[3，4_c] 0比嗤_3_90119473 (replacement)-2.ptc Page 370 ip7569 *_Case No. 90119473_Yearly revision _ Six, application to the scope of the base}-3-methoxybenzamide; 399. N-{5-phenyl Ethyl- 4,6-dihydro- 0-pyrolo[3,4-c] 0-O-sodium-3-yl}-p-anisamine; 400. N-{5-phenylethyl-4, 6-dihydrogen D ratio p and [3, 4-c] π-biazole-3-yl}-phenoxyacetamide; 401. Ν-{5-phenylethyl-4,6-dihydroanthracene 17 each [3,4-c] 0 ratio. Sodium 3-yl}_2_ gas phenylethylamine, 402. Ν-{5-phenylethyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl} _3_ gas phenyl ethylamine; 403. Ν-{5-phenylethyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-4_henylphenyl Ethylamine; 404. Ν-{5-phenylethyl-4,6-dihydropyridinium each [3,4-c] 0 ratio °-3-yl} - 3 - (2 _ porphin Acetylamine, 405. ^{5-Phenylethyl-4,6-dihydroindolo[3,4-anthracene]pyrazol-3-yl} _ 3 _ ( 3 _ π Terpenyl) propylamine, 406. Ν-{5-phenylethyl-4,6-dihydroσ-pyrolo[3,4-c]pyrazol-3-yl}-3-(2 -thienyl)propanamide; 407. N-{5-phenylethyl-4,6-dihydropyrolo[3,4-c]pyrazol-3-yl}-2-chlorobenzyl Indoleamine; 408. N-{5-phenylethyl-4,6-dihydrogen 0 to ρ=[3,4-c] 0 to 0-sodium-3-yl}-3-chlorophenylamine 409. N-{5_Phenylethyl_4,6-diaza nbi Loep[3,4-c] ° ratio 圭 -3 - base -4- chlorophenyl hydrazide; 410. N -{5 -Phenylethyl_4,6_Dinitrogen than 洛弁[3,4_c] 0 嗤_3_

90119473(替換）-2.ptc 第371頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍基} - 1 -哌啶丙醯胺； 411. N_{5 -苯基乙基-4,6-二氫咣咯并[3,4-c]吡唑-3-基}-2-乙醯基苯甲醯胺； 412. N-{5_苯基乙基_4，6_二氫α比σ各并[3，4-c] π比0坐- 3- ，基}-4-乙醯基苯曱醯胺； 413. \-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基} - 1 -萘甲醯胺； 414.1^-{5-苯基乙基-4，6-二氫°比°各并[3,4-0：]〇比11坐-3-基}-2 -萘曱醯胺；籲415.1^-{5-笨基乙基-4,6-二氫0比'1各并[3,4-(：]0比°坐-3-基}-3-苯甲醯基丙醯胺； 416. Ν-{5 -苯基乙基-4,6-二氫吡咯并[3,4-c]吡唑-3- 基}-4-乙醯胺基苯甲醯胺； 417.1{5-苯基乙基-4,6-二氫吡咯并[3,4-〇]毗唑-3-基}-2, 5-二甲氧苯曱醯胺； 418. ~-{5-苯基乙基-4,6-二氫吡咯并[3,4-<:]°比'1坐-3-基}-2, 6-二甲氧苯曱醯胺； 419. Ν-{5_苯基乙基_4，6_二氮0比17各并[3，4-c] 0比〇坐-3_ &}-3, 4-二甲氧苯甲醯胺；胃4 20. Ν-{5 -苯基乙基-4, 6 -二氳吡咯并[3, 4-c]吡唑-3-基}-3, 5-二曱氧苯曱醯胺； 421.1^-{5-苯基乙基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-3-(2 -噻吩甲醯基）-丙醯胺； 422. Ν-{5_苯基乙基-4，6 -二氫0比0各并[3,4-c] 0比嗤- 3-90119473 (replacement)-2.ptc Page 371 1327569 _ Case No. 90119473_Yearly revision _ 6. Patent application base} - 1 - piperidine propylamine; 411. N_{5-phenylethyl-4 ,6-dihydroindolo[3,4-c]pyrazol-3-yl}-2-ethenylbenzamide; 412. N-{5_phenylethyl_4,6_2 Hydrogen α ratio σ and [3,4-c] π ratio 0 sit- 3-, ki}-4-ethylmercaptobenzamine; 413. \-{5-phenylethyl-4,6- Dihydropyrrolo[3,4-(:]pyrazol-3-yl}-1 -naphthylcarboxamide; 414.1^-{5-phenylethyl-4,6-dihydrogen °° 3,4-0:] 〇 is more than 11 -3-yl}-2-naphthylamine; 41415.1^-{5-stupylethyl-4,6-dihydro 0 is more than '1 each [3 , 4-(:]0 is more than -3-yl}-3-benzhydrylpropionamide; 416. Ν-{5-phenylethyl-4,6-dihydropyrrolo[3,4 -c]pyrazol-3-yl}-4-acetamidobenzamide; 417.1{5-phenylethyl-4,6-dihydropyrrolo[3,4-indole]-pyrazole-3 -yl}-2, 5-dimethoxybenzamine; 418. ~-{5-phenylethyl-4,6-dihydropyrrolo[3,4-<:]° sits at '1 -3-yl}-2,6-dimethoxybenzamine; 419. Ν-{5_phenylethyl_4,6-diaza 0 to 17 and [3,4-c] 0 ratio Sit -3_ &}-3, 4-Dimethoxybenzamide; stomach 4 20. Ν-{5-phenylethyl-4,6-dipyridolo[3,4-c]pyrazol-3-yl}-3, 5 - dioxobenzoguanamine; 421.1^-{5-phenylethyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-(2-thiophene Mercapto)-propanamide; 422. Ν-{5_phenylethyl-4,6-dihydrogen 0 to 0 each [3,4-c] 0 to 嗤- 3-

90119473(替換）-2.ptc 第372頁 1327569 _案號90119473_年月日__ 六、申請專利範圍基}-2 -蔡基乙酿胺； 423. N_{5_苯基乙基_4，6_二氮π比洛并[3，4_c] 0比〇坐-3_ 基} -1 -萘基乙醯胺； 424. N-{5 -苯基乙基_4，6_二氮°比17各并[3，4-c] 0比0坐- 3-基} -4-苯基苯曱醯胺； 425.1^-{5-甲烷磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑 -3 -基卜乙醯胺； 4 26. N-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3 -基}-環丙烧缓硫胺； _3_基}_異丁酿胺， 428_ N-{5-甲烷磺醯基-4, 6 -二氫口比咯并[3, 4-c]吡唑 _3_基}_環戊烧缓酿胺； 429. N-{5-曱烧石黃醯基- 4,6 -二氫°比0各并[3,4-c]吡唑 _3_基}_苯甲酿胺， 430. ^1-{5-曱炫石黃酸基-4,6-二氫〇比〇各并[3,4-〇]〇比唑 -3 -基}-甲基吡啶曱醯胺； 431· N-{5-甲烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-菸鹼醯胺； 432. N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3_基}_異於驗酿胺， 433· N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇]"比唑 -3-基}-3-曱基-2 -呋喃曱醯胺； 434. N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑90119473 (replacement)-2.ptc Page 372 1327569 _ Case No. 90119473_Yearly __ Six, the scope of the patent application base}-2 - Cai Jiyi amine; 423. N_{5_phenylethyl _4,6 _Dinitrogen π, biluo[3,4_c] 0 is more than -3 -naphthylacetamide; 424. N-{5-phenylethyl_4,6-diazepine ratio 17 Each [3,4-c] 0 to 0-(3-yl}-4-phenylbenzamide; 425.1^-{5-methanesulfonyl-4,6-dihydroindole[3 , 4-(:]pyrazol-3-ylideneamine; 4 26. N-{5-decanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole_3 -基}-cyclopropanthene sulfhydrylamine; _3_yl}_isobutylenamine, 428_ N-{5-methanesulfonyl-4,6-dihydro-perylpyr-[3,4-c]pyridyl Azole _3_yl}_cyclopentane slow-acting amine; 429. N-{5-曱石石黄醯基- 4,6-dihydrogen ratio 0 and [3,4-c]pyrazole _3_ group }_Benzene amine, 430. ^1-{5-曱Herbsyl-4,6-dihydroindole 〇[3,4-〇]indazole-3-yl}- Pyridylamine; 431· N-{5-methanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-nicotinium amide; 432. N- {5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3_yl} Amine, 433· N-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indene]"biazol-3-yl}-3-indolyl-2-furan Amine; 434. N-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole

90119473(替換）-2.ptc 第373頁 1327569 修正案號 90119473 六、申請專利範圍 -3 _基} _ °塞吩-2 _叛酸胺； 435. Ν-{5-曱烷磺醯基-4, 6--3-基}-售吩-3_叛酿胺； 436. Ν-{5-曱烷磺醯基-4, 6--3 -基卜鄰-曱苯曱醯胺； 437. Ν-{5-曱烷磺醯基-4, 6--3 -基卜間-曱苯甲醯胺；氫°比σ各并[3，4 - c ] D比0坐氫°比D各并[3, 4 - c ] °比〇坐氫"比B各并[3，4 - c ] °比吐氫°比σ各并[3，4 - c ] °比。坐 438. Ν-{5-曱烷磺醯基-4, 6--3 -基}-對-曱苯曱醯胺； φ4 39. Ν-{5-曱烧石黃醯基- 4,6 -二氫0比咯并[3,4-c] π比。坐 -3-基}-苯基乙酸胺， 440.^1-{5-曱院磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基}-水楊酿胺， 441_ Ν-{5-曱烧石黃醯基- 4,6 -二氫D比咯并[3,4-c] 0比0坐 -3-基}-2-氟苯甲醯胺； 442.1{5-甲烧石黃醯基-4,6-二氫吡咯并[3,4-(：]0比唑 -3-基}-3-氟苯甲醯胺； 443.1{5-曱烧石黃醯基-4,6-二氫吡咯并[3,4-(：]吡唑 ▲-基 •444 }-4-氟苯曱醯胺； .N-{5-甲烷磺醯基-4, 6- -3 _基} _ °塞吩_ 2 _乙酿胺； 445. ^1-{5-甲烧石黃醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-噻吩-3-乙醯胺； 446. N-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑90119473 (replacement)-2.ptc Page 373 1327569 Amendment No. 90119473 VI. Scope of Application -3 _ _} _ °Certamine-2 _ acid-reductive amine; 435. Ν-{5-decanesulfonyl- 4, 6--3-yl}- phenoxy-3-rebel amine; 436. Ν-{5-nonanesulfonyl-4,6--3-biso-nonylbenzamide; 437 Ν-{5-decanesulfonyl-4,6--3-yl-bu-benzamide; hydrogen ° ratio σ[3,4 - c ] D ratio 0 sitting hydrogen ratio D Each of the [3, 4 - c ] ° ratios of hydrogen is proportional to the ratio of B to [3,4 - c ] ° and the ratio of transpiration to σ and [3,4 - c ] °. 438. Ν-{5-decanesulfonyl-4,6--3-yl}-p-nonylbenzamide; φ4 39. Ν-{5-曱石石黄醯基 - 4,6 -二Hydrogen has a ratio of 0 to [3,4-c] π. Sodium-3-yl}-phenylacetic acid amine, 440.^1-{5-曱院 sulfomethoxy-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}- Salicylamine, 441_ Ν-{5-曱烧石黄醯基- 4,6-Dihydro D is more than [3,4-c] 0 to 0--3-yl}-2-fluorobenzamide 442.1{5-甲烧石黄醯基-4,6-Dihydropyrrolo[3,4-(:]0-pyrazol-3-yl}-3-fluorobenzamide; 443.1{5-曱烧石Xanthyl-4,6-dihydropyrrolo[3,4-(:]pyrazole ▲-yl•444}-4-fluorobenzamide; .N-{5-methanesulfonyl-4,6- -3 _ _ _ _ ° cetin _ 2 _ ethoxylated amine; 445. ^ 1-{5- 甲石石黄醯基-4,6-dihydropyrrolo[3,4-〇]pyrazol-3-yl }-thiophene-3-acetamide; 446. N-{5-nonanesulfonyl-4,6-dihydropyrrolo[3,4-(:]carbazole

90119473(替換）-2.ptc 第374頁 1327569 _案號 90119473_年月日_i±i._ 六、申請專利範圍 -3_基}-苯基丙快酿胺； 447. N-{5-甲烷磺醯基-4,6-二氫°比咯并[3,4-(：]吡唑 _3_基}-3_氰基苯曱臨胺； 448. ^1-{5-曱烧磺酿基-4,6-二氫〇比0各并[3,4-(：]0比唑 _3-基}-4_氛基苯曱酿胺； 449. N-{5-甲烧石黃驢基-4, 6 -二氫π比σ各并[3,4-c] 0比0坐 _3-基}_反-桂皮酿胺； 45 0. N-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基} _順-桂皮臨胺； 451. N-{ 5-甲烷磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑 _3_基}_3_(3_ 0比咬基）丙稀酿胺， 4 5 2. N-{5-甲烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_3-(4_11比咬基）丙稀趨胺； 453. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3_基}·_2_苯基丙酿胺； 454. Ν-{5-甲烷磺醯基_4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_鄰-甲苯基乙臨胺； 455. Ν-{5-甲烧石黃醯基- 4,6 -二氫吡0各并[3,4-c]吡唑 -3 _基} _間-曱苯基乙臨胺， 45 6. N-{5-甲烷磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-對-甲苯基乙醯胺； 457. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-〇:]吡唑 _3-基}_鄰-菌香酿胺， 458. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑90119473 (replacement)-2.ptc Page 374 1327569 _ Case number 90119473_年月日日_i±i._ VI. Patent application scope -3_ base}-phenyl propyl fast-acting amine; 447. N-{5 - methanesulfonyl-4,6-dihydropyrano[3,4-(:]pyrazole-3-yl}-3-cyanobenzoquinone; 448. ^1-{5-曱Sulfuric acid-based 4,6-dihydroindole ratio 0 and [3,4-(:]0-pyrazole-3-yl}-4-ylphenyl benzoate; 449. N-{5-A Scutellariae-4,6-dihydroπ ratio σ and [3,4-c] 0 to 0 sit _3-yl}_trans-cinnabaratine; 45 0. N-{5-decane Sulfhydryl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-cis-cinnaminin; 451. N-{ 5-methanesulfonyl-4, 6-di Hydroquino[3,4-c]pyrazole_3_yl}_3_(3_0 ratio bite) acrylamide, 4 5 2. N-{5-methanesulfonyl-4, 6-di Hydropyrrolo[3,4-c]pyrazole-3-yl}_3-(4_11 to butyl) acetamide; 453. N-{5-methanesulfonyl-4,6-dihydropyrrole [3,4-〇]pyrazole-3_yl}·_2_phenylpropanol; 454. Ν-{5-methanesulfonyl _4,6-dihydropyrrolo[3, 4-c] Pyrazol-3_yl}-o-tolylethylamine; 455. Ν-{5-methanthine xanthyl- 4,6-dihydropyridinium[3,4-c]pyridinium Azole-3 _yl} _ m-p-phenylethylamine, 45 6. N-{5-methanesulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3- }.-p-tolylacetamide; 457. N-{5-methanesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3-yl}-ortho-bacteria Fragrant amine, 458. N-{5-methanesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole

90119473(替換）-2.ptc 第375頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍 -3-基}_3-甲氧苯曱醯胺； 459. N-{5-甲烷磺醯基-4,6-二氫咣咯并[3,4-〇]吡唑 -3-基}-對-茴香醯胺； 460. ^'1-{5-曱炫石黃隨基-4,6-二氫〇比(1各并[3,4-(：]°比〇坐 • -3 -基}-苯氧乙醯胺； 461. ?^-{5-曱炫磺醯基-4,6-二氫吡咯并[3,4-(：]0比唾 -3 -基}-2-氟苯基乙醯胺； 462. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}_3_氣苯基乙疏胺， 04 63. N-{5-曱院石黃醯基-4, 6 -二氫咄咯并[3, 4-c] 11比唾 -3-基}-4_氟苯基乙醯胺； 464. N-{5-曱烷磺醯基-4, 6 -二氫0比咯并[3, 4-c]吡唑 -3-基}-3-(2 -噻吩基）丙烯醯胺； 465.1{5-甲烧石黃醯基-4,6-二氫咄咯并[3,4-(：]0比°坐 -3_基}-3_(3_<1塞吩基）丙稀酿胺； 466.1{5-曱烷磺醯基-4,6-二氫。比咯并[3,4-〇]吡唑 -3_基}_3-(2_π塞吩基）丙隨胺， 467. Ν-{5-甲烧磺醯基-4, 6 -二氫吡咯并[3,4-c]吡唑 -j-基}-2-氣苯曱醯胺； ®46 8. N-{5-甲烷磺醯基-4, 6 -二氫"比咯并[3, 4-c]吡唑 -3_基}·_3 -氣笨曱酿胺， 46 9. Ν-{5-曱烷磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-4-氣苯甲醯胺； 470.1^-{5-曱院石黃醯基-4,6-二氫吡咯并[3,4-<:]〇比°坐90119473 (replacement)-2.ptc Page 375 1327569 _ Case number 90119473_Yearly revision _ VI. Patent application scope -3-yl}_3-methoxybenzamide; 459. N-{5-methane sulfonate Mercapto-4,6-dihydroindolo[3,4-indolylpyrazol-3-yl}-p-anisylamine; 460. ^'1-{5-曱Hyunhuang Huangshen-4,6 - dihydroanthracene ratio (1 each [3,4-(:] ° than squat • -3 -yl}-phenoxyacetamide; 461. ?^-{5-曱 saponin-4, 6-dihydropyrrolo[3,4-(:]0 is more than sal-3-yl}-2-fluorophenylacetamide; 462. N-{5-methanesulfonyl-4,6-dihydro Pyrrolo[3,4-(:]pyrazol-3-yl}_3_qiphenylethylamine, 04 63. N-{5-曱院石黄醯基-4,6-dihydroindole[3 , 4-c] 11 than sial-3-yl}-4-fluorophenylacetamide; 464. N-{5-nonanesulfonyl-4,6-dihydro- 0-pyrano[3, 4 -c]pyrazol-3-yl}-3-(2-thienyl)propenylamine; 465.1{5-carbide xanthine-4,6-dihydroindole[3,4-(:]0 Ratio -3 - yl} -3 - (3_ < 1 phenanthryl) acrylamide; 466.1 {5-decanesulfonyl-4,6-dihydro. pyrrolo[3,4-〇] Pyrazole-3_yl}_3-(2_πsecenyl)propanylamine, 467. Ν-{5-methylsulfonyl-4,6-dihydrogen Pyrrolo[3,4-c]pyrazole-j-yl}-2-phenanthridine; ®46 8. N-{5-methanesulfonyl-4,6-dihydro" [3, 4-c]pyrazole-3_yl}·_3 - gas astringent amine, 46 9. Ν-{5-nonanesulfonyl-4,6-dihydroindole[3, 4 -c]pyrazol-3-yl}-4-oxabenzamide; 470.1^-{5-曱院石黄醯基-4,6-dihydropyrrolo[3,4-<:]〇 ratio° sit

90119473(替換）-2.ptc 第376頁 ip7569 1_案號 90119473_年月日__ 六、申請專利範圍 -3 -基} - 1 -哌啶丙醯胺； 471. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3~*基}·_2_乙酿基苯曱酿胺； 472. Ν-{5-曱烷磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑 -3-基}-4-乙醯基苯曱醯胺； 473. Ν-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-卜萘甲醯胺； 474. Ν-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3-基}_2_秦甲酿胺； 475. Ν-{5-曱烷磺醯基-4,6-二氫"比咯并[3,4-〇]吡唑 -3-基}-3 -苯甲醯基丙醯胺； 47 6_ Ν- { 5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-乙醯胺基苯甲醯胺； 477. Ν-{5-甲烧石黃醯基-4,6-二氫吼11各并[3,4-(：]'1比唑 -3-基}-2, 5-二甲氧苯曱醯胺； 478. Ν-{5-甲院石黃醯基- 4,6 -二氫σ比π各并[3,4-c] π比唑 -3-基}-2,6_二甲氧苯甲醯胺； 479· Ν-{5-甲烧石黃醯基-4, 6 -二氫0比口各并[3,4-c] 0比唾 -3-基}-3, 4-二甲氧苯甲醯胺； 480. N-{5-甲烧石黃隨基-4, 6 -二氫口比口各并[3,4-c] 0比0坐 _3_基}_3，5_二甲氧苯曱酿胺； 481. N-{5-曱烧石黃驢基-4, 6 -二氫〇比0各并[3,4-c] 0比0坐 -3-基}-3-(2 -噻吩甲醯基）-丙醯胺； 48 2. N-{5-甲烷磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑90119473 (replacement)-2.ptc Page 376 ip7569 1_Case No. 90119473_Yearly __ Six, the scope of application for patent -3 - base} - 1 - piperidine propylamine; 471. N-{5-methane Sulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3~*yl}·_2_ethyl phenyl benzoate; 472. Ν-{5-decanesulfonate 4-,6-dihydropyrrolo[3,4-indole-3-oxazol-3-yl}-4-ethenylbenzamide; 473. Ν-{5-methanesulfonyl-4,6 - dihydropyrrolo[3,4-(:]pyrazol-3-yl}-b-naphthylamine; 474. Ν-{5-methanesulfonyl-4,6-dihydropyrrolo[3, 4-(:]pyrazole-3-yl}_2_Hungercaptoamine; 475. Ν-{5-decanesulfonyl-4,6-dihydro"bi-[3,4-〇] Pyrazol-3-yl}-3-benzhydrylpropionamide; 47 6_ Ν- { 5-decanesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 -yl}-4-acetamidobenzamide; 477. Ν-{5-carbide xanthine-4,6-dihydroindole 11 and [3,4-(:]'1 azole- 3-yl}-2, 5-dimethoxybenzamine; 478. Ν-{5-甲院石黄醯基- 4,6-Dihydroσ ratio π[3,4-c] π-pyrazole -3-yl}-2,6-dimethoxybenzamide; 479·Ν-{5-methyst-xanthine-4,6-dihydro- 0 [3,4-c] 0 is more than spani-3-yl}-3,4-dimethoxybenzamide; 480. N-{5-metholst yellow with base-4,6-dihydrogen port And [3,4-c] 0 to 0 sitting _3_base}_3,5-dimethoxybenzoquinone; 481. N-{5-曱烧石黄驴基-4,6-dihydroanthracene 0-0[3,4-c] 0 to 0--3-yl}-3-(2-thiophenemethyl)-propanamine; 48 2. N-{5-methanesulfonyl-4 ,6-dihydropyrrolo[3,4-(:]pyrazole

90119473(替換）-2.ptc 第377頁 1327569 I 案號90119473 年月日修正六、申請專利範圍 _3_基}-2_秦基乙酿胺； 483. N-{5-曱烷磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}-1_奈基乙酸胺； 484. N-{5-曱烷磺醯基-4,6-二氫咄咯并[3,4-〇]吡唑 _3 -基}_4_苯基苯曱酸胺； 485. [{5-乙基胺基獄基-4,6-二氫吡1»各并[3,4-〇]0比'1坐 -3-基}-乙醯胺； 486. N-{5-乙基胺基羰基-4,6-二氳吡咯并[3,4-〇]咄唑 _3 -基}_環丙烧叛酸胺；秦487.^{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吼唑 -3 -基}-異丁醯胺； 488. N-{5-乙基胺基羰基-4, 6 -二氩吡咯并[3, 4-c]吼唑 - 3 -基}環戊院叛酿胺； 489. ^{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]°比唑 _3-基}_苯曱酿胺； 490.1{5-乙基胺基羰基-4,6-二氲咣咯并[3,4-〇]吡唑 -3-基}-甲基咄啶曱醯胺； 491. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]"比唑基}-菸鹼醯胺； 492. N-{5-乙基胺基幾基_4，6--3-基}-異菸鹼醯胺； 493. N_{5_乙基胺基幾基_4，6--3-基}-3-曱基-2 -呋喃甲醯胺； 494. N-{5-乙基胺基幾基-4,6- 氫°比ρ各并[3，4 - c ] π比°坐氫D比ρ各并[3，4 - c ] °比〇坐氫0比σ各并[3，4 - c ] °比〇坐90119473 (replacement)-2.ptc Page 377 1327569 I Case No. 90119473 Revised on the sixth day of the month, the scope of the patent application _3_ base}-2_Qinyl ethylamine; 483. N-{5-decanesulfonate Base-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-1_methyl acetate; 484. N-{5-decanesulfonyl-4,6-di Hydroquino[3,4-indolylpyrazole-3-yl}_4_phenylbenzoic acid amine; 485. [{5-ethylamine-based prison-4,6-dihydropyridinone» And [3,4-〇]0 is more than '1 sitting-3-yl}-acetamide; 486. N-{5-ethylaminocarbonyl-4,6-dipyrido[3,4-quinone ] carbazole _3 -yl} _ propyl propyl oxalate; Qin 487.^{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]carbazole-3 488.-Isobutylamine; 488. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}cyclopentene apocytamine; 489. ^{5-Ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]°biazole-3-yl}-benzoquinone; 490.1{5-ethylamino Carbonyl-4,6-dipyrrolo[3,4-indolylpyrazol-3-yl}-methylacridiniumamine; 491. N-{5-ethylaminocarbonyl-4,6 -dihydropyrrolo[3,4-(:]"Bizozolyl}-nicotinium amide; 492. N-{5-ethylamine Alkyl _4,6--3-yl}-isonicotinamine amide; 493. N_{5-ethylaminomethyl- 4,6--3-yl}-3-mercapto-2-furan Methionine; 494. N-{5-ethylamino group - 4,6- hydrogen ratio ρ and [3,4 - c ] π ratio ° sitting hydrogen D ratio ρ and [3,4 - c ] ° than 〇 sitting hydrogen 0 σ σ and [3,4 - c ] ° than sitting

90119473(替換）-2.ptc 第378頁 1327569 案號90119473 年月日修正六、申請專利範圍 -3 -基}-D塞吩_2_叛酿胺； 495. N-{5-乙基胺基幾基-4,6 -二氫D比11 各并[3,4-c] D比0坐 -3-基} - 11塞吩_3_魏酷胺； 496. N-{5 -乙基胺基羰基-4, 6 -二氫吡咯并[3,4-c]咄唑 _3-基}_間-甲苯曱酿胺； 497. N-{5 -乙基胺基羰基-4,6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-對-甲苯曱醯胺； 498. N-{5-乙基胺基羰基-4,6 -二氫吼11 各并[3,4-c] 11比唑 _3_基}_水楊酿胺， 499. N-{5-乙基胺基羰基-4,6 -二氫吡咯并[3, 4-c]吼唑 _3_基}-2_貌苯甲驢胺； 50 0. N-{5 -乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_3_氣苯曱驢胺； 501. N-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吼唑 _3 -基}·_4_氟苯甲酿胺； 502. ^1-{5-乙基胺基幾基-4,6-二氫〇比11各并[3,4-(：]11比〇坐 -3 -基} - π塞吩_ 2 -乙酿胺； 5 0 3. Ν-{5 -乙基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3 -基} _ α塞吩_ 3 _乙酿胺； 5 0 4. Ν-{5 -乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_苯基丙块酿胺， 505. Ν-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}-3_鼠基苯甲酸胺， 506. Ν-{5 -乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑90119473 (replacement)-2.ptc Page 378 1327569 Case No. 90119473 Revised on the day of the month, the scope of application for patents -3 -based}-D-sentene_2_ apoein; 495. N-{5-ethylamine The keto group-4,6-dihydro D ratio is 11 and [3,4-c] D is 0 -3-yl} - 11 phenanthrene _3_Wei carbamide; 496. N-{5 - B Amino-based carbonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}-m-toluene amide; 497. N-{5-ethylaminocarbonyl-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-p-toluidine; 498. N-{5-ethylaminocarbonyl-4,6-dihydroindole 11 And [3,4-c] 11-pyrazole_3_yl}_saponin, 499. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c] Carbazole_3_yl}-2_benzamide; 50 0. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole_3_ }._3_ gas benzoguanamine; 501. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}·_4_fluorobenzene甲. 502. ^1-{5-Ethylamino-yl-4,6-dihydroindole ratio 11 and [3,4-(:]11 than 〇-3-yl}- π _ 2 -Ethylamine; 5 0 3. Ν-{5-ethylaminocarbonyl-4,6-dihydroindolo[3,4-c]pyridyl -3 -yl} _ α塞苯_ 3 _ 乙乙胺; 5 0 4. Ν-{5 -ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole_3 _ _ _ phenyl propyl block amine, 505. Ν-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-〇]pyrazole _3_yl}-3_rat Benzoic acid amine, 506. Ν-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole

第379頁 90119473(替換）-2.ptc 1327569 _案號 90119473_年月日__ 六、申請專利範圍 -3-基}_4-氰基苯曱酿胺； 507. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基卜反-桂皮醯胺； 508. N-{5-乙基胺基羰基-4, 6 -二氫吡11 各并[3, 4-c]"比°坐 • -3-基}-順-桂皮醯胺； 509. N-{5-乙基胺基羰基-4, 6 -二氫吡σ各并[3, 4-c] 0比0坐 ^-基}·^-^-1^17定基）丙稀酿胺； 510. Ν-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}_3_(4_11比11定基）丙稀酸胺；鲁51 1. Ν-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_2 -苯基丙酿胺； 512. Ν-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基卜鄰-甲苯基乙醯胺；已^-^丨旦-乙基胺基羰基-斗^-二氫吡洛并!^，‘-…1^0^ -3_基}_間-甲苯基乙驢胺； 514. Ν-{5-乙基胺基羰基-4, 6 -二氫吡σ各并[3, 4-c] D比峻 -3 -基}-對-甲苯基乙醯胺； 515. N-{5-乙基胺基羰基-4,6-二氫吡咯并[3,4-〇:]吡唑基}_鄰-菌香驢胺；胃516. N-{5-乙基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基}-3_甲氧苯甲酿胺； 517. N-{5-乙基胺基羰基-4,6 -二氫咣咯并[3,4-c]吡唑 _3-基}_對-菌香酷胺； 518. N-{5-乙基胺基羰基-4, 6 -二氫吡咯并[3,4-c]吡唑Page 379 90119473 (replacement)-2.ptc 1327569 _ case number 90119473_年月日日__ VI. Patent application scope -3- base}_ 4-cyanobenzoquinone; 507. N-{5-ethyl Aminocarbonyl-4,6-dihydropyrrolo[3,4-indene]pyrazol-3-yl b- cinnamate; 508. N-{5-ethylaminocarbonyl-4,6-di Hydropyridyl 11 each [3, 4-c] " ° • -3-yl}-cis-cinnamate; 509. N-{5-ethylaminocarbonyl-4,6-dihydropyridyl σ each [3, 4-c] 0 to 0 sit ^-based}·^-^-1^17 base acrylamide; 510. Ν-{5-ethylaminocarbonyl-4,6- Dihydropyrrolo[3,4-(:]pyrazole-3-yl}_3_(4_11 to 11-based) acrylamide; Lu 51 1. Ν-{5-ethylaminocarbonyl-4,6- Dihydropyrrolo[3,4-c]pyrazole-3-yl}_2-phenylpropanol; 512. Ν-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3, 4-c]pyrazol-3-ylbu-o-tolylacetamide; ^-^丨旦-ethylaminocarbonyl-bucket^-dihydropyrrolo!^,'-...1^0^ -3_基}_m-tolylacetamide; 514. Ν-{5-ethylaminocarbonyl-4,6-dihydropyridinium each [3, 4-c] D is more than -3 }-p-tolyl acetamide; 515. N-{5-ethylamino 4-,6-dihydropyrrolo[3,4-indolyl]pyrazolyl}-o-bacteria; stomach 516. N-{5-ethylaminocarbonyl-4,6-dihydro Pyrrolo[3,4-c]pyrazol-3-yl}-3-methoxybenzoic acid; 517. N-{5-ethylaminocarbonyl-4,6-dihydroindole[3 , 4-c]pyrazole-3-yl}-p-bacteria; 518. N-{5-ethylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第380頁 1327569 案號 90119473 A_ a 修正六、申請專利範圍 _3_基}苯氧乙酿胺； 51 9. N-{5-乙基胺基羰基-4, 6 _3-基}_2-氟苯基乙臨胺； 520. N-{5_乙基胺基幾基_4，6’ _3_基}·-3-氣苯基乙酸·胺；氫0比洛并[3，4 - c ] °比唑二氫D比洛并[3，. 4 - c ] D比0坐 521. N-{5-乙基胺基羰基-4,6 -二氩吡咯并[3,4-c]咄唑 -3_基}_4-氟苯基乙酿·胺； 522. N_{5_乙基胺基獄基_4,6_ _3 -基}·_3_(2_ °塞吩基）丙稀' S藍胺， 52 3. Ν-{5-乙基胺基羰基-4, 6- -3-基}_3-(3-°塞吩基）丙稀酷胺； 524. Ν-{5-乙基胺基羰基-4,6--3-基}-3-(2-噻吩基）丙醯胺； 52 5. Ν-{ 5-乙基胺基羰基-4, 6- -3_基}_2_氣苯fS莲胺，二氳β比11各并[3，4 - c ] D比0坐氩吼°各并[3，4 - c ] D比0坐二氳°比11各并[3，4 - c ] °比〇坐二氫°比σ各并[3，4 - c ] π比0圭 52 6. Ν-{5 -乙基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}_3 -氯苯甲驢胺； 527. Ν-{5 -乙基胺基羰基-4, 6--3-基}-4-氣苯曱醯胺； 528. Ν_{5-乙基胺基羰基-4,6--3 -基} -1 -哌啶丙醯胺； 529. Ν-{5-乙基胺基叛基-4,6--3 -基卜2-乙醯基苯曱醯胺； 530. Ν-{5-乙基胺基裁基-4，6_ 二氫°比Β各并[3，4 - c ]吡唑氳0比D各并[3，4 - c ] 比0坐二氫吼洛并[3，4 - c ] D比0坐90119473 (replacement)-2.ptc Page 380 1327569 Case No. 90119473 A_ a Amendment VI, Patent Range _3_Base}Phenoxyethylamine; 51 9. N-{5-Ethylaminocarbonyl-4, 6 _3-yl}_2-fluorophenylethylamine; 520. N-{5-ethylaminomethyl _4,6' _3_yl}·-3-phenylphenylacetic acid amine; hydrogen 0 ratio洛和[3,4 - c ] ° azole dihydrogen D is more than [3,. 4 - c ] D is 0 521. N-{5-ethylaminocarbonyl-4,6-di-argonpyrrole And [3,4-c]carbazole-3_yl}_4-fluorophenylethylamine; 522. N_{5_ethylamine-based prison base_4,6_ _3 -yl}·_3_(2_ ° Terpenyl) propylene 'S leucine, 52 3. Ν-{5-ethylaminocarbonyl-4,6--3-yl}_3-(3-°secenyl) propylamine; 524 Ν-{5-ethylaminocarbonyl-4,6--3-yl}-3-(2-thienyl)propanamine; 52 5. Ν-{ 5-ethylaminocarbonyl-4, 6- -3_基}_2_ gas benzene fS-lanamine, two 氲β ratio 11 and [3,4 - c ] D ratio 0 argon 吼 ° each [3,4 - c ] D than 0 sitting two氲° ratio 11 and [3,4 - c ] ° than 〇二 dihydrogen ratio σ and [3,4 - c ] π ratio 0 gui 52 6. Ν-{5 -ethylaminocarbonyl-4 , 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}_3-chloro Methionine; 527. Ν-{5-ethylaminocarbonyl-4,6--3-yl}-4-phenhydrin; 528. Ν_{5-ethylaminocarbonyl-4,6 -3 -yl} -1 -piperidinepropionamine; 529. Ν-{5-ethylamino thiol-4,6--3-ylbu 2-ethylmercaptobenzamide; 530. Ν-{5-ethylamino group cleavage-4,6_ dihydrogen Β 并 [3,4 - c ]pyrazol oxime 0 is more than D and [3,4 - c ] is less than 0 quinone Luohe [3,4 - c ] D sits 0

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90119473(替換）-2.ptc 第382頁 1327569 案號 90119473 修正六、申請專利範圍 -3-基}_4-苯基苯甲酿胺； 543. Ν-{5 -苯基胺基幾基- 4,6 -二氫°比11 各并[3,4-c] D比0坐 -3 -基}-乙醯胺； 544· N-{5 -苯基胺基幾基-4,6-二氫吼17各并[3, 4-c]吡嗤 -3_基}_環丙院缓酷胺； 5 4 5. N-{5 -苯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吡唑 -基}-異丁醯胺；546. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑基- 4,6 -二氫"比11各并[3,4-c]吼〇坐 54 8. N-{5 -苯基胺基羰基-4, 6 -二氮吼咯并[3, 4-c]吡唑 -3 -基卜環戊烷羧醯胺； 547. N-{5-苯基胺基獄 _3_基}_苯甲酿胺； -3 -基}-曱基吡啶甲醯胺； 549. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-菸鹼醯胺； 5 5 0. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基卜異菸鹼醯胺； 551. N-{5 -苯基胺基幾基-4，6_ -3-基}_3_曱基_2_p夫喃曱酸胺； 55 2. N-{ 5 -苯基胺基羰基-4,6- 氫°比B各并[3，4 - c ] π比0坐氫0比β各并[3，4 - c ]吼0坐 -3-基}-噻吩-2-羧醯胺；5 5 3. Ν-{ 5 -苯基胺基羰基-4, 6- -3 -基}_α塞吩缓S蓝胺；554. Ν-{5 -苯基胺基幾基-4,6- 氫°比σ各并[3，4 - c ]吡唾氫0比σ各并[3，4 - c ]吼0坐90119473 (replacement)-2.ptc Page 382 1327569 Case No. 90119473 Amendment VI, Patent Application -3-Base}_4-Phenylbenzamide; 543. Ν-{5-Phenylamino-yl--4 , 6-dihydrogen ratio 11 each [3,4-c] D is 0-position -3 -yl}-acetamide; 544· N-{5-phenylamino group-4,6-di Hydroquinone 17 and [3, 4-c]pyridin-3-yl}-cyclopropene slow amine; 5 4 5. N-{5-phenylaminocarbonyl-4,6-dihydroindole And [3, 4-c]pyrazole-yl}-isobutylamine; 546. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazolyl - 4,6-dihydro" ratio 11 and [3,4-c] 5454 8. N-{5-phenylaminocarbonyl-4,6-diazaindole[3, 4 -c]pyrazol-3-ylbupentanecarboxamide; 547. N-{5-phenylamine prison _3_yl}_benzamide; -3 -yl}-mercaptopyridine Indoleamine; 549. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-nicotinium amide; 5 5 0. N- {5-Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl-isohistidine amide; 551. N-{5-phenylamino group -4,6_ -3-yl}_3_mercapto-2_p-furanuric acid amine; 55 2. N-{ 5 -phenylamino group Carbonyl-4,6-hydrogen ratio B and [3,4 - c ] π ratio 0 to hydrogen 0 to β and [3,4 - c ]吼0--3-yl}-thiophene-2-carboxylate Indoleamine; 5 5 3. Ν-{ 5 -Phenylaminocarbonyl-4,6-1,3-yl}_α-septene-sodium sulphate; 554. Ν-{5-phenylamino group-4 , 6- hydrogen ° ratio σ and [3,4 - c ] pyrithione 0 to σ each and [3,4 - c ]吼0 sit

90119473(替換）-2.ptc 第383頁 1327569 _案號 90119473_年月日_i±S._ 六、申請專利範圍 -3 -基}-鄰-甲苯曱醯胺； 555. N-{5 -笨基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基}-間-甲苯甲醯胺； 556.1'1-{5-苯基胺基羰基-4,6-二氫吡'1各并[3,4-〇]11比〇坐 .-3-基}-對-甲苯甲醯胺； 557.1{5-苯基胺基獄基-4,6-二氫吡(1各并[3,4-〇]°比〇坐 -3 -基}-苯基乙醯胺； 558. N-{5 -苯基胺基羰基-4,6-二氫咄咯并[3,4-〇]吡唑 -3 -基}-水楊醯胺； •5 5 9. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}_2_氟苯甲酸胺； 5 6 0. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3-氟苯甲醯胺； 561. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]咄唑 _3_基}_4_氣苯甲酷胺； 56 2. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 _基} _ °塞吩_ 2 _乙臨胺； 563. N-{5 -苯基胺基羰基-4,6-二氫咄咯并[3,4-(：]咄唑基}-噻吩-3-乙醯胺；胃5 64. N-{5 -苯基胺基羰基-4,6-二氫吼咯并[3,4-叫°比唑 -3-基卜苯基丙炔醯胺； 56 5. N-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3-氰基苯曱醯胺； 566. N-{5 -苯基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑90119473 (replacement)-2.ptc Page 383 1327569 _ Case number 90119473_Year of the month _i±S._ VI. Patent application scope -3 - base}-o-toluidine; 555. N-{5 - stupylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-m-toluamylamine; 556.1'1-{5-phenylaminocarbonyl- 4,6-dihydropyridinium 1 1 and [3,4-〇]11 is more than 〇 -3-.-3-yl}-p-toluamylamine; 557.1{5-phenylamine-based prison base-4,6 - dihydropyrid (1 each [3,4-〇] ° than 〇-3 -yl}-phenylacetamide; 558. N-{5-phenylaminocarbonyl-4,6-dihydro咄[3,4-〇]pyrazole-3-yl}-salicylimine; •5 5 9. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3, 4-c]pyrazol-3-yl}_2-fluorobenzoic acid amine; 5 6 0. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3-yl}-3-fluorobenzamide; 561. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]carbazole_3_yl}_4 _ gas benzomethamine; 56 2. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 _yl} _ ° thiophene _ 2 _ Ethylamine; 563. N-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-(:]carbazole N-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-pyrazole-3-ylbenzene Propylamine amide; 56 5. N-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-cyanobenzoquinone Amine; 566. N-{5-phenylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazole

90119473(替換）-2.ptc 第384頁 Ip27569 修正案號 90119473 六、申請專利範圍 _3_基}_4-氰基苯甲酿胺；氫0比°各并[3，4 - c ] π比嗤 567. Ν-{5 -苯基胺基羰基-4,6--3-基}-反-桂皮醯胺； 568. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基}-順-桂皮醯胺； 569. [^-{5-苯基胺基羰基-4,6-二氫吡17各并[3,4-(：]°比〇坐 -3_基}-3_(3_°比α定基）丙稀酿胺； 570. Ν-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_3-(4_ °比咬基）丙稀S藍胺； 571. ^{5-苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]咄唑 _3_基}-2_苯基丙臨胺， 57 2. Ν-{5 -苯基胺基羰基-4, 6 -二氳吡咯并[3, 4-c]咄唑 -3 -基}-鄰-甲笨基乙醯胺； 573· Ν-{5 -苯基胺基羰基-4,6-二氳"比咯并[3,4-〇]咄唑 - 3 -基} _間-甲苯基乙酿胺； 574. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-對-甲苯基乙醯胺； 575. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}_鄰-a香酿胺；基-4，6 -二氫吼ρ各并[3，4-c] D比0坐基- 4,6 -二氫D比洛并[3,4-c] D比0坐基-4，6 -二氫"比17各并[3, 4-c] B比嗤 57 6. N-{5-苯基胺基羰 -3-基}-3_甲氧苯甲醯胺； 57 7. N-{5-苯基胺基羰 3-基}-對-茴香醯胺； 578. N-{5-苯基胺基羰90119473 (replacement)-2.ptc Page 384 Ip27569 Amendment No. 90119473 VI. Patent scope _3_base}_4-cyanobenzamide; hydrogen 0°° and [3,4 - c ] π ratio嗤567. Ν-{5-Phenylaminocarbonyl-4,6--3-yl}-trans-cintoinamide; 568. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrole And [3,4-(:]pyrazol-3-yl}-cis-cinnamicin; 569. [^-{5-phenylaminocarbonyl-4,6-dihydropyridin 17 each [3, 4-(:]° is more than -3_base}-3_(3_° ratio α-based) acrylamide; 570. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazole _3_yl}_3-(4_ ° than bite) propylene S leucine; 571. ^{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-(:]carbazole-3-yl}-2-phenylpropanamine, 57 2. Ν-{5-phenylaminocarbonyl-4,6-dipyrido[3,4-c ] carbazole-3-yl}-o-methylphenyl acetamide; 573·Ν-{5-phenylaminocarbonyl-4,6-dioxime "bi-[3,4-〇]咄Oxazol-3-yl}-m-tolylylamine; 574. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl} - p-tolyl acetamide; 575. Ν-{5-phenylaminocarbonyl -4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-o-a-flavor amine; base-4,6-dihydroindole ρ[3,4-c] D is 0 to sit on the base - 4,6 - dihydrogen D is more than [3,4-c] D is 0 to sit on the base of 4,6-dihydro " than 17 and [3, 4-c] B ratio嗤57 6. N-{5-Phenylaminocarbonyl-3-yl}-3-methoxybenzamide; 57 7. N-{5-phenylaminocarbonyl-3-yl}-p-anion Indoleamine; 578. N-{5-phenylaminocarbonyl

90119473(替換）-2,ptc 第385頁 1327569 案號 90119473 A_η 修正六、申請專利範圍 -3 -基}-苯氧乙醯胺； 57 9. Ν-{ 5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}-2_氟苯基乙酿胺； 580. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3-基}_3-氟苯基乙酸胺；氫0比17各并[3，4 - c ]吼〇坐 581.1^-{5'~苯基胺基幾基-4，6--3 -基}·_4_氣苯基乙驢胺，氫°比ρ各并[3，4 - c ] β比0坐 582. Ν-{5 -苯基胺基幾基-4，6_ 二氫吡β各并[3，4 - c ] °比嗤 -3-基}-3-(2 -噻吩基）丙烯醯胺； φ5 8 3. Ν-{5 -苯基胺基羰基-4, 6- -3-基}_3-(3-°塞吩基）丙稀酿胺， 584. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}_3-(2_°塞吩基）丙驢胺； 58 5. Ν-{5-苯基胺基羰基-4, 6-二氫咄咯并[3, 4-c]咄唑 -3_基}-2_氯苯曱酿·胺； 58 6. Ν-{5 -苯基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]咄唑 -3_基}_3_氯苯甲酿胺； 58 7. Ν-{ 5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑基}-4-氯苯曱醯胺；氫0比洛并[3，4 - c ] D比0坐 58 8. Ν-{ 5-苯基胺基羰基-4, 6 -3 -基} - ：1 -哌啶丙醯胺； 589. N-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-(：]咄唑 -3-基}-2-乙醯基苯甲醯胺； 5 9 0. N-{5 -苯基胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑90119473 (replacement)-2, ptc p. 385 1327569 Case No. 90119473 A_η Amendment VI, Patent Application No. 3-based}-phenoxyacetamide; 57 9. Ν-{5-phenylaminocarbonyl-4, 6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-fluorophenylethylamine; 580. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrole And [3,4-〇]pyrazole-3-yl}_3-fluorophenylacetic acid amine; hydrogen 0 to 17 each [3,4 - c ] 吼〇 sitting 581.1^-{5'~phenylamino group Alkyl-4,6--3-yl}.___ phenyl phenyl acetamide, hydrogen ratio ρ and [3,4 - c ] β ratio 0 sitting 582. Ν-{5-phenylamino group Alkyl-4,6-dihydropyrrole β each [3,4 - c ] ° than indole-3-yl}-3-(2-thienyl)propenylamine; φ5 8 3. Ν-{5 - benzene胺-{5-phenylaminocarbonyl-4,6-dihydropyrrole [3,4-(:]pyrazol-3-yl}_3-(2_°secenyl)propanamine; 58 5. Ν-{5-phenylaminocarbonyl-4,6-dihydrofluorene And [3,4-c]carbazole-3-yl}-2-chlorobenzoquinone-amine; 58 6. Ν-{5-phenylaminocarbonyl-4,6-dihydroindole[3 , 4-c]carbazole-3_yl}_3_chlorobenzamide; 58 7. Ν-{ 5 -Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazolyl}-4-chlorobenzamide; Hydrogen 0 to Loxo[3,4 - c D is 0 to 58. 8. Ν-{ 5-Phenylaminocarbonyl-4,6-3-ol}-:1-piperidinepropanamine; 589. N-{5-phenylaminocarbonyl- 4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-2-ethenylbenzamide; 5 9 0. N-{5-phenylaminocarbonyl-4 , 6-dihydroindolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第386頁 1327569 案號 90119473 A_η 修正六、申請專利範圍 _3_基}·_4_乙酿基苯曱酸胺； 591. Ν-{5 -苯基胺基羰基-4,6- _3-基}_1-秦曱酿胺；氫0比洛并[3，4 - c ] D比0坐 59 2. Ν-{5-苯基胺基羰基-4, 6- -3-基}-2-萘曱醯胺； 593. Ν-{5 -苯基胺基羰基-4,6--3-基}-3 -苯曱醯基丙醯胺；氫0比η各并[3，4 - c ] D比。坐 594. Ν-{5 -苯基胺基羰基-4,6--3-基}-4_乙酿胺基苯甲酿胺，二氫°比σ各并[3，4 - c ] D比0坐 595. Ν-{5 -苯基胺基羰基-4,6--3-基}-2, 5-二甲氧苯甲醯胺； 596. Ν-{5 -苯基胺基羰基-4,6--3-基}-2, 6-二甲氧苯甲醯胺； 59 7. Ν-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3, 4-二甲氧苯甲醯胺； 5 9 8. Ν-{ 5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3,5 -二甲氧苯甲醯胺； 599. Ν-{5 -苯基胺基羰基-4, 6 -二 -3-基}-3-(2 -噻吩曱醯基）-丙醯胺氫0比σ各并[3，4 - c ] β比0坐 600. Ν-{5 -苯基胺基羰基-4, 6-二 -3-基}_2_秦基乙酿胺， 601. Ν-{5 -苯基胺基羰基-4, 6 -二氫吡咯并[3,4-c]吡唑 _3_基}_1_秦基乙酸胺， 60 2. N-{ 5 -苯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑90119473 (replace)-2.ptc Page 386 1327569 Case No. 90119473 A_η Amendment 6. Patent scope _3_基}·_4_Ethyl benzoyl amide; 591. Ν-{5-phenylaminocarbonyl -4,6- _3-yl}_1-Qin-brown amine; hydrogen 0 piroxi[3,4 - c ] D is 0 to sit 59 2. Ν-{5-phenylaminocarbonyl-4, 6- -3-yl}-2-naphthylamine; 593. Ν-{5-phenylaminocarbonyl-4,6--3-yl}-3-phenylmercaptopropylamine; hydrogen 0 to η Each [3,4 - c ] D ratio. Sitting 594. Ν-{5-phenylaminocarbonyl-4,6--3-yl}-4_ethylaminobenzamide, dihydrogen ratio σ and [3,4 - c ] D 595. Ν-{5-phenylaminocarbonyl-4,6--3-yl}-2, 5-dimethoxybenzamide; 596. Ν-{5-phenylaminocarbonyl -4,6--3-yl}-2,6-dimethoxybenzamide; 59 7. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3, 4- c]pyrazol-3-yl}-3,4-dimethoxybenzamide; 5 9 8. Ν-{ 5 -phenylaminocarbonyl-4,6-dihydropyrrolo[3, 4- c]pyrazol-3-yl}-3,5-dimethoxybenzamide; 599. Ν-{5-phenylaminocarbonyl-4,6-di-3-yl}-3-(2 - thiophene decyl)-propionamine hydrogen 0 to σ each [3,4 - c ] β is 0 to sit at 600. Ν-{5-phenylaminocarbonyl-4,6-di-3-yl} _2_Qinyl ethylamine, 601. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_1-methylglycolic acid amine, 60 2. N-{ 5 -Phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

! 90119473(替換）-2.ptc 第387頁 1327569 修正案號 90119473 六、申請專利範圍 -3-基} -4-苯基苯甲醯胺； 603_ Ν-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-(；]°比唑 -3 -基}-乙醯胺； 604. Ν-{5-苄基胺基羰基-4,6-二氫咣咯并[3,4-〇]吼唑 -3 -基卜環丙烷羧醯胺； 60 5. Ν-{5-苄基胺基羰基-4, 6 -二氫咣咯并[3, 4-c]吡唑 -3 -基}-異丁醯胺； 606. Ν-{5-罕基胺基羰基-4,6 -二氫咄咯并[3, 4-c]咄唑 -3-基卜環戊烷羧醯胺； •60 7. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_苯曱酿胺； 60 8. Ν-{ 5-芊基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-甲基吡啶甲醯胺； 609. Ν-{5-苄基胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑 -3_基}-於驗酷胺； 61 0. Ν-{ 5 -苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吼唑 - 3 -基} _異於驗酿胺， 61 1. Ν-{5-苄基胺 -3-基}-3_曱基-2-呋胃612. Ν-{5-苄基胺 -3 -基}_ °塞吩_2_叛酉藍 613. Ν_{5-辛基胺 -3 -基} _ α塞吩_ 3 -觀酿 614. Ν-{5-苄基胺基羰基-4，6 -二氫吡洛并[3，4 - c ] 11比0坐喃曱醯胺；基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑胺；基羰基-4，6 -二氫咄11各并[3，4 - c ] °比°坐胺；基羰基-4, 6 -二氫咄Β各并[3,4-c] D比。坐90119473 (replacement)-2.ptc Page 387 1327569 Amendment No. 90119473 VI. Scope of Application -3-Base} -4-Phenylbenzamide; 603_ Ν-{5-Benzylaminocarbonyl-4 ,6-dihydroindolo[3,4-(;]°bizozol-3-yl}-acetamide; 604. Ν-{5-benzylaminocarbonyl-4,6-dihydroanthracene And [3,4-〇]oxazol-3-ylcyclopropanecarboxamide; 60 5. Ν-{5-benzylaminocarbonyl-4,6-dihydroindole[3, 4-c Pyrazol-3-yl}-isobutylamine; 606. Ν-{5-Hanylaminocarbonyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl Cyclopentane carboxamide; 60 7. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-benzoic acid; 60 8. Ν-{ 5-decylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-methylpyridinecarboxamide; 609. Ν-{5 -benzylaminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}- for the test amine; 61 0. Ν-{ 5 -benzylaminocarbonyl -4,6-dihydropyrrolo[3,4-c]carbazole-3-yl} _ different from the amine, 61 1. Ν-{5-benzylamine-3-yl}-3_曱Benzene-furose 612. Ν-{5-benzylamine-3-yl}_ °Sentence_2_ rebel Indigo 613. Ν_{5-octylamine-3-yl} _ α塞苯_ 3 - 470. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrazolo[3, 4 - c ] 11 to 0 oxime; carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazolamine; carbonylcarbonyl-4,6-dihydroindole 11 each [3 , 4 - c ] ° ratio ° amine; carbonyl-4,6-dihydroindole each [3,4-c] D ratio.

90119473(替換）-2.ptc 第388頁 1327569 案號 90119473 _η 修正六、申請專利範圍 -3 -基}-鄰-甲苯曱醯胺； 615. Ν-{ 5-苄基胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吡唑 _3-基}_間-曱苯曱臨胺；基-4, 基-4, 62 0. Ν-{5-苄基胺基羰基-4, 616. Ν-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -基}-對-甲苯曱醯胺； 617. Ν-{5-芊基胺基羰基-4， - 3 -基} _水楊酿·胺； 618. Ν-{5-苄基胺基数 _3 -基}_2_氟苯曱酿胺； 619. Ν-{5-苄基胺基羰 _3-基}_3-亂苯曱酷胺； 6 -二氫°比ρ各并[3，4 - c ] Β比唾 6 -二氫吼ρ各并[3，4 - c ] β比0坐 6 -二氫η比洛并[3，4 - c ] α比。坐 6 -二氫吼各并[3，4 - c ] D比嗤 _3-基}_4_氟苯甲酿胺； 621. N-{5 -苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基卜噻吩-2-乙醯胺； 622. N-{ 5 -苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-噻吩-3-乙醯胺； 6 -二氫吼p各并[3，4 - c ] n比嗤 6 -二氫p比11各并[3，4 - c ] D比0坐 6 -二氫吼p各并[3，4 - c ] D比0坐 6 2 3. N-{5-苄基胺基羰基-4， _3_基}_苯基丙快酿胺； 624. N-{5_辛基胺基獄基- 4， -3-基}_3-氰基苯曱酿胺； 625. N-{5_辛基胺基獄基-4， -3-基}-4-氰基苯甲醯胺； 626. N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 388 1327569 Case No. 90119473 _η Amendment VI, the scope of patent application -3 -yl}-o-toluidine; 615. Ν-{ 5-benzylaminocarbonyl-4, 6-dihydroindolo[3,4-c]pyrazole-3-yl}-m-nonylbenzoin; base-4, yl-4, 62 0. Ν-{5-benzylamino Carbonyl-4, 616. Ν-{ 5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-yl}-p-toluidine; 617. Ν-{ 5-mercaptoaminocarbonyl-4,-3-yl} _hydrophyllin amine; 618. Ν-{5-benzylamino group _3 -yl}_2_fluorobenzoquinone; 619. {5-Benzylaminocarbonyl-3-yl}_3-puroquinone; 6-dihydrogen ratio ρ[3,4 - c ] Β is more than sal 6-dihydro 吼ρ[3 , 4 - c ] β is more than 0 sitting 6 - dihydro η piroxime [3,4 - c ] α ratio. 6-Dihydroindole each [3,4 - c ] D is more than 嗤3-3-}}_4_fluorobenzamide; 621. N-{5-benzylaminocarbonyl-4,6-dihydrogen Pyrrolo[3,4-c]pyrazol-3-ylthiophene-2-acetamide; 622. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3, 4- c]pyrazol-3-yl}-thiophene-3-acetamide; 6-dihydroindole p each [3,4 - c ] n is more than 嗤6-dihydrop ratio 11 and [3,4 - c ] D is 0 to sit 6-dihydroindole p and [3,4 - c ] D is 0 to sit 6 2 3. N-{5-benzylaminocarbonyl-4, _3_yl}_phenylpropane Fast-brown amine; 624. N-{5_octylamine-based phenyl- 4,-3-yl}-3-cyanobenzoquinone; 625. N-{5-octylamine-based prison-4 -3-yl}-4-cyanobenzamide; 626. N-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第389頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 -3 -基卜反-桂皮醯胺； 627. N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-順-桂皮醯胺； 62 8· N-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 --3_基}-3_(3_0比α定基）丙稀臨胺， 62 9. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3 -基} - 3 _ ( 4 - π比σ定基）丙炸酸胺， 63 0. Ν-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}·-2_苯基丙酸胺， •631. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吼唑 -3-基} -鄰-曱苯基乙醯胺； 632. Ν-{5 -苄基胺基羰基-4,6-二氫咣咯并[3,4-(：]吡唑 -3-基}-間-甲苯基乙醯胺； 6 3 3. Ν-{ 5 -苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3-基}-對-甲苯基乙醯胺； 634.1\1-{5-苄基胺基羰基-4,6-二氫吡咯并[3,4-(：]°比唑 -3_基}_鄰-茵香酿胺； 63 5. Ν-{5-苄基胺基羰基-4, 6-二氫咄咯并[3, 4-c]咄唑基}_3_甲氧苯甲酿·胺；響63 6. Ν-{5-苄基胺基羰基-4, 6 -二氫咣咯并[3, 4-c]咄唑 _3_基}_對-菌香酿胺， 63 7. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_苯氧乙酿胺， 6 3 8. Ν-{5-苄基胺基羰基-4, 6-二氫吡咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 389 1327569 _ Case No. 90119473_Yearly revision _ 6. Patent application scope - 3 - kipbu-cinnamicin; 627. N-{5-benzylaminocarbonyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-cis-cinnamate; 62 8· N-{ 5-benzylaminocarbonyl-4,6-dihydrol Pyrrolo[3,4-c]pyrazole-3-yl}-3_(3_0 ratio α-based) propylamine, 62 9. Ν-{5-benzylaminocarbonyl-4,6-dihydro Pyrrolo[3,4-c]oxazol-3-yl} - 3 _ ( 4 - π ratio σ decyl) propanuric acid amine, 63 0. Ν-{ 5-benzylaminocarbonyl-4, 6 - Dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-phenylpropanoate, •631. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrole [3,4-c]oxazol-3-yl}-o-indolephenylacetamide; 632. Ν-{5-benzylaminocarbonyl-4,6-dihydroindole[3,4 -(:]pyrazol-3-yl}-m-tolylacetamide; 6 3 3. Ν-{ 5 -benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c] Oxazol-3-yl}-p-tolylacetamide; 634.1\1-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]°bazole-3 _基}_o-infranin; 63 5. Ν-{5-benzyl Alkylcarbonyl-4,6-dihydroindolo[3,4-c]oxazolyl}_3_methoxybenzoic acid; ring 63 6. Ν-{5-benzylaminocarbonyl-4, 6-dihydroindolo[3,4-c]carbazole_3_yl}_p-bacteria, 63 7. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrole And [3, 4-c]pyrazole_3_yl}-phenoxyethylamine, 6 3 8. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3, 4- c]pyrazole

! 90119473(替換）-2.ptc 第390頁 1327569 修正案號 90119473 六、申請專利範圍 _3-基}-2_說苯基乙酸胺；氳0 th D各并[3，4 - c ] D比0坐 639. N_{5-辛基胺基幾基_4，6-_3 -基}·_3_氟苯基乙酿胺； 640. Ν-{5-芊基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 _3-基}_4-氟1苯基乙酸胺； 641. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3-(2-噻吩基）丙烯醯胺； 64 2. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3-基}_3-(3_°塞吩基）丙稀酸胺； 64 3. Ν-{5-芊基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3-(2-噻吩基）丙醯胺；二氫°比σ各并[3，4 - c ] °比0坐 644. Ν-{5-辛基胺基幾基_4，6--3-基}-2-氯苯甲醯胺；二氫D比ρ各并[3，4 - c ]吼°坐 645. Ν-{5-苄基胺基羰基-4,6-_3-基}-3_氯苯曱趨胺， 646. Ν-{5 -苄基胺基羰基-4, 6_二氫吡咯并[3, 4-c]吡唑 - 3 -基}·_4 -氣苯曱酿胺， 647. Ν-{5-辛基胺基叛基-4,6 -二氫π比σ各并[3，4-c] π比0坐 -3 -基} -1 -哌啶丙醯胺； 648. Ν-{5-亨基胺基幾基-4，6_二氫D比11 各弁[3，4~c] 0比唾 -3-基}-2-乙醯基苯曱醯胺； 64 9. N-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吼唑 -3-基}-4-乙醯基苯曱醯胺； 650. N-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 390 1327569 Amendment No. 90119473 VI. Patent scope _3-base}-2_ said phenylacetic acid amine; 氲0 th D and [3,4 - c ] D 639. N_{5-octylaminomethyl_4,6-_3-yl}·_3_fluorophenylethylamine; 640. Ν-{5-decylaminocarbonyl-4,6 - dihydropyrrolo[3,4-indolylpyrazole-3-yl}_4-fluorophenylacetic acid amine; 641. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazol-3-yl}-3-(2-thienyl)propenylamine; 64 2. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazole-3-yl}_3-(3_°secenyl)acrylic acid amine; 64 3. Ν-{5-decylaminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-3-(2-thienyl)propanamide; dihydrogen ratio σ and [3,4 - c ] ° ratio 0 sitting 644. Ν-{5- Octylamino benzyl 4,6--3-yl}-2-chlorobenzamide; dihydrogen D ratio ρ and [3,4 - c ]吼° sitting 645. Ν-{5-benzyl Aminocarbonyl-4,6--3-yl}-3-chlorobenzoquinone, 646. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c] Pyrazole-3-yl}·_4-gas benzoquinone, 647. Ν-{5-octylamine Rebel-4,6-dihydroπ ratio σ[3,4-c] π ratio 0 sitting -3 -yl} -1 -piperidine propylamine; 648. Ν-{5-henrylamine Alkyl-4,6-dihydrogen D is 11 弁[3,4~c] 0 is more than spani-3-yl}-2-ethenylbenzamide; 64 9. N-{ 5-benzyl Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-ethenylbenzamide; 650. N-{5-benzylaminocarbonyl- 4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第391頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍 -3-基}_1-蔡甲驢胺； 651. N-{5-苄基胺基羰基-4, 6 -二氫吡σ各并[3, 4-c] π比0坐 -3 -基卜2 -萘甲醯胺； 652. ^{5-辛基胺基羰基-4,6-二氫吡*1各并[3,4-(：]11比〇坐 -3 -基}-3 -苯甲醯基丙醯胺； 653. Ν-{5-辛基胺基数基-4,6 -二氫η比π各并[3,4-c]吼〇坐 _3_基}·_4_乙酸胺基苯甲酿胺； 654. Ν-{5-苄基胺基幾基-4,6 -二氫°比°各并[3,4-c] 0比唾 _3_基}·_2，5 -二甲氧苯甲酸胺；鲁6 55. Ν-{5-苄基胺基幾基-4,6 -二氫DtbD各并[3,4-c]吼0坐 _3_基}_2，6_二甲氧苯甲酸胺； 656. N-{5-爷基胺基幾基-4，6_二氫0比13各并[3，4-c] 0比〇坐 -3-基}-3,4 -二曱氧苯甲醯胺； 657. N-{5-苄基胺基羰基-4, 6 -二氫吡11 各并[3, 4-c]吼〇坐 _3_基}_3，5_二甲氧苯甲酿胺； 658. N-{5-苄基胺基魏基-4，6 -二氫°比0各并[3，4-c] °比唾 -3-基}-3-(2_噻吩甲醯基）-丙醯胺； 659. N-{5-苄基胺基羰基-4, 6 -二氫吡σ各并[3, 4-c]吼〇坐 -3-基}_2 -蔡基乙酿胺； ®6 6 0. Ν-{5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑 -3 -基}-：!-萘基乙醯胺； 6 6 1. Ν-{ 5-苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4_苯基苯曱酿胺； 6 6 2. Ν-{ 5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]90119473 (replacement)-2.ptc Page 391 1327569 _ Case No. 90119473_Year of the month __ Six, the scope of application for patent -3- base}_1-caemeamide; 651. N-{5-benzylamine Carbonyl-4,6-dihydropyridinium each [3, 4-c] π is 0-position -3 -yl 2 -naphthylcarboxamide; 652. ^{5-octylaminocarbonyl-4,6 - dihydropyridyl*1[3,4-(:]11 is more than s--3-yl}-3-benzhydrylpropionamide; 653. Ν-{5-octylamino group-4 , 6-dihydro-n-ratio π[3,4-c] 吼〇3_yl}·_4_acetic acid benzylamine; 654. Ν-{5-benzylamino group- 4,6-dihydrogen ratio °[3,4-c] 0 is more than salicin-3-yl}·_2,5-dimethoxybenzoic acid amine; Lu 6 55. Ν-{5-benzylamine N-{5-ylaminolamine Alkyl-4,6-dihydrogen 0 to 13 and [3,4-c] 0 is more than s--3-yl}-3,4-dioxabenzoguanamine; 657. N-{5- Benzylaminocarbonyl-4,6-dihydropyrrole 11 each [3,4-c]indole_3_yl}_3,5-dimethoxybenzoic acid; 658. N-{5- Benzylamino-Wiki--4,6-dihydrogen ratio 0 and [3,4-c] ° than sial-3-yl}-3-(2- thiophenemethyl fluorenyl) - propylamine; 659. N-{5-benzylaminocarbonyl-4,6-dihydropyridinium[3,4-c]indole-3-yl}_2-cacoylamine; 6 6 0. Ν-{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}-:!-naphthylacetamide; 6 6 1 Ν-{ 5-Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-4-phenylphenyl amide; 6 6 2. Ν- { 5 -Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]

90119473(替換）-2.ptc 第392頁 1327569 案號90119473 年月日修正六、申請專利範圍吼唑-3 -基}-乙醯胺； 663. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3 -基}-環丙烷羧醯胺； 664. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3 -基}-異丁醯胺； 665.1^-{5-苯曱醯基胺基羰基-4,6-二氫°比咯并[3,4-〇] 吼唑-3 -基卜環戊烷羧醯胺； 666. N-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-〇] 咄唑-3 -基}-苯曱醯胺； 667. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] »比唑-3 -基}-甲基13比啶曱醯胺； 6 6 8. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫咄咯并[3, 4-c] °比α坐-3 -基}-於鹼酸胺； 669. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-〇] 吡唑-3-基卜異菸鹼醯胺； 670. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫吼咯并[3,4-(：] 吼。坐- 3-基}-3-曱基-2-0夫喃甲酿胺； 671. Ν-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 〇比。坐_ 3 -基} - °塞吩-2 -魏酿胺； 672. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫吼咯并[3,4-(：] σ比。坐-3 -基} - °塞吩_ 3 -叛Sg胺； 673. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吼咯并[3, 4-c] 吡唑-3 -基卜鄰-曱苯曱醯胺； 674. N-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] II ιϊΛ m 190119473 (replacement)-2.ptc Page 392 1327569 Case No. 90119473 Revised on the day of the month 6. Patent application range carbazole-3-yl}-acetamide; 663. N-{5-benzoguanidinocarbonyl -4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-cyclopropanecarboxamide; 664. N-{5-benzoylaminocarbonyl-4,6- Dihydropyrrolo[3,4-(:]pyrazol-3-yl}-isobutylamine; 665.1^-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydrogen ratio 3,4-〇] carbazole-3-ylbucyclopentane carboxamide; 666. N-{5-phenylhydrazinocarbonyl-4,6-dihydroindolo[3,4-quinone ] carbazole-3-yl}-benzoguanamine; 667. N-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrrolo[3,4-(:]»bazole-3 -yl}-methyl 13-pyridylamine; 6 6 8. N-{5-phenylhydrazinocarbonyl-4,6-dihydroindole[3,4-c] ° -3 -yl}-in the alkali acid amine; 669. Ν-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-ylpyr Nicotinamide; 670. Ν-{5-benzhydrylaminocarbonyl-4,6-dihydroindolo[3,4-(:] fluorene.sodium-3-yl}-3-indenyl -2-0 fumarine; 671. Ν-{5-benzoguanamine Carbonyl-4,6-dihydropyrrolo[3,4-c] ruthenium. Sodium-3-yl}- °Certene-2-Wei-enamine; 672. Ν-{5-Benzyl decylamino Carbonyl-4,6-dihydroindole[3,4-(:] σ ratio. Sodium-3-yl}- °Cetamine _ 3 - Rebel Sg amine; 673. N-{5-benzoquinone Aminocarbonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl-benza-nonylbenzamide; 674. N-{5-benzhydrylaminocarbonyl- 4,6-dihydropyrrolo[3,4-〇] II ιϊΛ m 1

90119473(替換）-2.ptc 第393頁 1327569 案號 90119473 曰修正六、申請專利範圍吡唑-3-基}-間-曱苯甲醯胺； 675. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3 -基}-對-曱苯曱醯胺； 67 6. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 吡唑-3-基}-苯基乙醯胺； 677. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] α比。坐_ 3 -基}-水楊酿胺； 678. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑_3-基}-2_氟苯甲醯胺； _67 9. Ν-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 吡唑-3-基}-3-氟苯曱醯胺； 68 0. Ν-{ 5 -苯甲醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] π比。坐-3 -基} - 4 -氟苯曱酿胺； 681. Ν-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] α比吐-3 -基} - α塞吩-2 -乙酿胺； 682. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫咄咯并[3,4-〇] 吡唑-3-基}-噻吩-3-乙醯胺； 6 8 3. Ν-{ 5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 1唑-3-基卜苯基丙炔醯胺； *6 84. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 咄唑-3-基}-3 -氰基苯甲醯胺； 685. Ν-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-(：] 吡唑-3-基}-4-氰基苯甲醯胺； 68 6. Ν-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]90119473 (replacement)-2.ptc Page 393 1327569 Case No. 90119473 曰 Amendment 6. Patent application range pyrazol-3-yl}-m-nonylbenzamide; 675. N-{5-benzoguanamine Carbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-p-nonylbenzamide; 67 6. N-{5-benzoguanidinocarbonyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-phenylacetamidamine; 677. N-{5-benzoylaminocarbonyl-4,6-di Hydropyrrolo[3,4-(:]α ratio. Sodium-3-yl}-hydropenic amine; 678. Ν-{5-phenylhydrinylaminocarbonyl-4,6-dihydropyrrolo[ 3,4-(:]pyrazole-3-yl}-2-fluorobenzamide; _67 9. Ν-{5-phenylhydrazinocarbonylcarbonyl-4,6-dihydropyrrolo[3, 4-c]pyrazol-3-yl}-3-fluorophenylamine; 68 0. Ν-{ 5 -benzimidylcarbonyl-4,6-dihydropyrrolo[3, 4-c π ratio. sitting -3 -yl} - 4 -fluorobenzoquinone; 681. Ν-{5 - benzhydrylaminocarbonyl-4,6-dihydropyrrolo[3,4-(:]比比吐-3 -基} - α-sentene-2-ethinamine; 682. Ν-{5-benzoguanidinocarbonyl-4,6-dihydroindolo[3,4-〇] Pyrazol-3-yl}-thiophene-3-acetamide; 6 8 3. Ν-{ 5-Benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-ylphenylpropynylamine; *6 84. Ν-{5-benzoquinone Mercaptoalkylcarbonyl-4,6-dihydropyrrolo[3,4-(:]oxazol-3-yl}-3-cyanobenzamide; 685. Ν-{5-benzoquinone Aminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-4-cyanobenzamide; 68 6. Ν-{5-benzoguanamine Alkylcarbonyl-4,6-dihydropyrrolo[3,4-c]

90119473(替換）-2.ptc 第394頁 1327569 案號 90119473 年月修正六、申請專利範圍 σ比唑-3 -基}-反-桂皮醯胺； 687. Ν-{5 -苯曱酿基胺基獄基-4，6_二氮0比σ各并[3，4-c] 口比唑-3 -基}-順-桂皮醯胺； 688. N-{5 -苯曱醯基胺基羰基-4, 6 -二氫吡咯并[3, 4-c] 吡唑-3-基}-3-(3 -咄啶基）丙烯醯胺； 689. N-{5_苯甲隨基胺基幾基-4，6_二氮〇比p各并[3, 4-c] 吡唑-3-基}-3-(4-°比啶基）丙烯醯胺； 6 9 0. N-{5_苯曱醯基胺基羰基-4, 6- 吡唑-3-基}-2_苯基丙醯胺；氫0比p各并[3，4 - c ] 691. N-{5 -苯甲縫·基胺基叛基_4，6-吡唑-3-基卜鄰-甲苯基乙醯胺； 692. N-{5 -苯曱醯基胺基羰基-4,6-二氫吼咯并[3,4-(：] 吼唑-3 -基卜間-甲苯基乙醯胺； 693. N-{5 -苯甲醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3-基}-對-甲苯基乙醯胺； 694. N-{5 -苯曱醯基胺基羰基-4,6-二氫吡咯并[3,4-〇] 吡唑-3 -基卜鄰-茴香醯胺； 695. N-{5 -苯甲醯基胺基羰基-4,6- 吡唑-3-基}-3-曱氧苯甲醯胺； 6 9 6. N-{ 5 -苯甲醯基胺基羰基-4, 6- 吡唑-3 -基}-對-茴香醯胺； 697. N-{5 -苯曱醯基胺基羰基-4,6-吡唑-3-基}_苯氧乙醯胺； 698. N-{5 -苯甲醯基胺基羰基-4,6- 氫吼B各并[3，4 - c ] 氫吼咯并[3，4 - c 氫0比咯并[3，4 - c ]90119473 (replacement)-2.ptc Page 394 1327569 Case No. 90119473 Revised June, the scope of application for patent σ-Bizozol-3 -yl}-trans-cinsinamide; 687. Ν-{5 - benzoquinone Kiba base-4,6_diaza 0 to σ each [3,4-c] oxazole-3-yl}-cis-cinnamin; 688. N-{5-benzoguanamine Carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-3-(3-anthridyl)propenylamine; 689. N-{5_benzamide The benzyl group-4,6-diazonium ratio p and [3,4-c]pyrazol-3-yl}-3-(4-pyridyl)propenylamine; 6 9 0. N- {5_Benzylaminocarbonyl-4,6-pyrazol-3-yl}-2-phenylpropanoxime; hydrogen 0 to p each [3,4 - c ] 691. N-{5 - Benzene syl-amino-amino- 4,6-pyrazol-3-yl-o-tolyl acetamide; 692. N-{5-benzoylaminocarbonyl-4,6-di Hydroquino[3,4-(:]carbazole-3-yl-b-tolylacetamide; 693. N-{5-benzhydrylaminocarbonyl-4,6-dihydropyrrole [3,4-〇]pyrazol-3-yl}-p-tolylacetamide; 694. N-{5-benzoylaminocarbonyl-4,6-dihydropyrrolo[3,4 -〇] pyrazole-3-carbo-anisamine; 6 95. N-{5-Benzyldecylaminocarbonyl-4,6-pyrazol-3-yl}-3-indolylbenzamide; 6 9 6. N-{ 5 -benzimidamide Alkylcarbonyl-4,6-pyrazol-3-yl}-p-anisoleamine; 697. N-{5-benzoylaminocarbonyl-4,6-pyrazol-3-yl}-phenoxy Acetamine; 698. N-{5-benzhydrylaminocarbonyl-4,6-hydroquinone B and [3,4 - c ] hydroquinone [3,4 - c hydrogen 0 [3,4 - c ]

90119473(替換）-2.ptc 第395頁 1327569 案號90119473 年月日修正90119473 (replace)-2.ptc Page 395 1327569 Case No. 90119473

90119473(替換）-2.ptc 第396頁 132756990119473 (replace)-2.ptc Page 396 1327569

90119473(替換）-2.ptc 第397頁 1327569 案號 90119473 年 Μ_a 修正六、申請專利範圍基}-乙醯胺； 723. N-{5-胺基幾基-4,6-二氫π比σ各并[3，4-c] °比°坐_3_ 基}-環丙烷羧醯胺； .氫°比°各并[3,4-c] °比吐-3- 72 5. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- }-環戊烷羧醯胺； 726. N-{5 -胺基戴基-4，6 -二氫D比n各并[3,4-c] D比α坐- 3- 724. N-{5 -胺基幾基-4，6 -. 基}-異丁醯胺；基}-苯曱醯胺； φ72 7. Ν-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3- 基}-甲基吡啶曱醯胺； 728.1^-{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-菸鹼醯胺； 72 9. Ν-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基}-異菸鹼醯胺； 73 0. Ν-{ 5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基}-3-甲基-2 -呋喃曱醯胺； 731. Ν-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-噻吩-2 -羧醯胺；擊7 3 2. Ν-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基} - °塞吩_ 3 -叛酿胺； 73 3. Ν-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基}-鄰-甲苯甲醯胺； 734. Ν-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-90119473 (replacement)-2.ptc Page 397 1327569 Case No. 90119473 Μ _a Amendment VII, the scope of the patent application}-acetamide; 723. N-{5-amino-based-4,6-dihydro-π ratio σ each [3,4-c] ° ratio _3_ ki}-cyclopropane carboxamide; hydrogen ratio ° and each [3,4-c] ° ratio -3-5 5. N- {5-Aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-}-cyclopentanecarboxamide; 726. N-{5-Amino Daichi-4, 6-dihydrogen D is more than n and [3,4-c] D is more than α-3-724. N-{5-amino-based-4,6-.yl}-isobutylamine; -phenylhydrazine; φ72 7. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-methylpyridiniumamine; 728.1^ -{5-Aminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-nicotinium amide; 72 9. Ν-{5-aminocarbonyl-4 , 6-dihydropyrrolo[3,4-c]oxazol-3-yl}-isonicotinamine amide; 73 0. Ν-{ 5 -aminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-3-methyl-2-furanamine; 731. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3, 4-c Pyrazol-3-thiophene-2-carboxycarboxamide; hit 7 3 2. Ν-{5-aminocarbonyl-4, 6 - two咄并 [3, 4-c]pyrazol-3-yl} - ° thiophene _ 3 - Apollin; 73 3. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl}-o-tolylcarbamide; 734. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3 -

1^90119473(替換）-2.ptc 第398頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍基}-間-曱苯曱醯胺； 735. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基}-對-甲苯曱醯胺； 73 6. N-{5 -胺基羰基-4, 6 -二氫吼咯并[3, 4-c]吡唑-3-基}-苯基乙醯胺； 737.1{5-胺基羰基-4,6-二氫。比咯并[3,4-〇]吡唑-3-基}-水楊臨胺； 738. N-{5 -胺基羰基-4,6-二氫吼咯并[3,4-c]咄唑-3-基}_2-氣苯曱酿胺； 739. N-{5 -胺基羰基-4,6-二氫吡咯并[3,4-c]吡唑-3-基}_3_氣苯曱酿胺， 74 0. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3-基}_4_氣苯曱酿胺； 741. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-噻吩-2-乙醯胺； 74 2. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基} - °塞吩-3-乙醯胺； 743.1{5-胺基羰基-4,6-二氫°比咯并[3,4-(：]吡唑-3-基}-苯基丙炔醯胺； 744. N-{5 -胺基羰基-4,6 -二氫π比咯并[3,4-c]吡唑-3- 基}-3-氰基苯曱醯胺； 745.1^-{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基}-4-氰基苯甲醯胺； 746. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-1^90119473 (replacement)-2.ptc Page 398 1327569 _ Case No. 90119473_Year of the month __ VI. Patent application base}-m-phenylarbenium; 735. N-{5-aminocarbonyl -4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-p-toluidine; 73 6. N-{5-aminocarbonyl-4,6-dihydroindole [3,4-c]pyrazol-3-yl}-phenylacetamide; 737.1 {5-aminocarbonyl-4,6-dihydro. Bis-[3,4-indolylpyrazol-3-yl}-salicylidene amine; 738. N-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c] Oxazol-3-yl}_2-gas benzoquinone; 739. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}_3_ Gas benzoquinone amine, 74 0. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}_4_ gas benzoquinone; 741. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-thiophene-2-acetamide; 74 2. N-{5-amino group Carbonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}- °cephen-3-acetamide; 743.1{5-aminocarbonyl-4,6-dihydrogen Bisolo[3,4-(:]pyrazol-3-yl}-phenylpropynylamine; 744. N-{5-aminocarbonyl-4,6-dihydropi-pyrene[3, 4-c]pyrazol-3-yl}-3-cyanobenzoquinone; 745.1^-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole- 3-yl}-4-cyanobenzamide; 746. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-

90119473(替換）-2.ptc 第399頁 1327569 案號 90119473 年月曰修正六、申請專利範圍基}-反-桂皮酸胺； 6 -二氫d比洛并[3, 4-c] °比°坐-3- 74 7. N-{5-胺基羰基- 基}-順-桂皮醯胺； 748. N-{5 -胺基獄基-4，6 -二氫β比'}各并[3，4-〇]°比°坐-3-基} - 3 - ( 3 - σ比啶基）丙烯醯胺； 749. Ν-{5 -胺基数基-4，6 -二氫°比°各并[3，4-c] π比°坐-3-基}-3-(4_11比。定基）丙稀酿胺； 750. Ν-{5 -胺基幾基-4，6 -二氫β比洛并[3，4-c] α比。坐- 3-基}-2 -苯基丙醯胺；鲁7 51. Ν-{5-胺基魏基-4，6-二氫吼σ各并[3, 4-c] °比°坐- 3-基}-鄰-曱苯基乙醯胺； 752. Ν-{5 -胺基幾基-4,6 -二氫D比ρ各并[3，4-c] η比。坐- 3- 基卜間-甲苯基乙醯胺；二氫吼σ各并[3，4 - c ] °比°坐-3 - 75 3. Ν-{5-胺基羰基-4, 6 基}-對-曱苯基乙醯胺； 754. Ν-{5-胺基羰基-4,6 -二氫吼17各并[3,4-c] °比唾- 3-基}-鄰-茴香醯胺； 755· N-{5 -胺基数基-4，6_二氫π比σ各并[3，4-c] °比°坐-3- 1卜3-曱氧苯曱醯胺； ®7 5 6. Ν-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]咄唑-3- 基}-對-茴香醯胺； 6 -二氫吼σ各并[3，4 - c ] °比°坐-3 - 75 7. Ν-{5-胺基羰基- 基卜笨氧乙醯胺； 758 -{5-胺基羰基-4, 6-二氫11比咯并[3, 4-c] 11比唑- 3-90119473 (replacement)-2.ptc Page 399 1327569 Case No. 90119473 Year of the month Amendment VI, the scope of the patent application base}-trans-cinnamic acid amine; 6-dihydrogen d is more than [3, 4-c] ° ° sit-3-74 7. N-{5-aminocarbonyl-yl}-cis-cinnamin; 748. N-{5-amine-prison-4,6-dihydro-β ratio [3,4-〇]°°°-3-yl} - 3 - (3 - σ-pyridyl) acrylamide; 749. Ν-{5-amino-based-4,6-dihydrogen ratio °[3,4-c] π ratio ° sit-3-yl}-3-(4_11 ratio. fixed base) acrylamide; 750. Ν-{5-amino group-4,6-two Hydrogen β is more than the ratio of [3,4-c] α. Sodium 3-yl}-2-phenylpropanamide; Lu 7 51. Ν-{5-Amino-Weiyl-4,6-dihydroindole σ[3, 4-c] °°°° 3- 3-yl}-o-indole phenylacetamide; 752. Ν-{5-amino-based-4,6-dihydro D ratio ρ and [3,4-c] η ratio. Sit- 3- benzyl-tolyl acetamide; dihydroanthracene σ [3,4 - c ] ° ratio ° -3 - 75 3. Ν-{5-aminocarbonyl-4, 6 }-p-indole phenylacetamide; 754. Ν-{5-aminocarbonyl-4,6-dihydroindole 17 each [3,4-c] ° than salid-3-yl}-ortho- Anisidine; 755· N-{5-amino-based group-4,6-dihydro-π ratio σ[3,4-c] ° ratio 坐-3- 1 曱3-曱 benzophenone ® 7 5 6. Ν-{5-aminocarbonyl-4,6-dihydroindolo[3,4-c]oxazol-3-yl}-p-anisylamine; 6-dihydroanthracene σ each [3,4 - c ] ° ratio ° -3 - 75 7. Ν-{5-aminocarbonyl- phenyl bromoxyacetamide; 758 -{5-aminocarbonyl-4, 6- Dihydrogen 11 is more than [3, 4-c] 11 azole - 3-

90119473(替換）-2.ptc 第400頁 1327569 j_案號90119473_年月曰修正_ 六、申請專利範圍基}_2_氣苯基乙酸胺； 759. N-{5 -胺基羰基-4,6-二氫吼咯并[3,4-c]吡唑-3-基}_3_氟苯基乙臨胺； 760. N-{5 -胺基幾基_4，6_二氮α比13各弁[3,4-c] π比唾-3-基丨_4_氟苯基乙酿胺； 761. Ν-{5-胺基羰基-4,6 -二氫吡咯并[3, 4-c]吡唑-3-基卜3 - ( 2 -噻吩基）丙烯醯胺； 762. ?^-{5_胺基羰基-4,6-二氫吼咯并[3,4-〇]吡唑-3-基} - 3 - ( 3 -噻吩基）丙烯醯胺； 7 6 3. Ν-{5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3- 基} - 3 - ( 2 -噻吩基）丙醯胺； 76 4· Ν-{ 5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基}_2 -氯苯曱酿胺； 765. Ν-{5-胺基羰基-4,6-二氫"比咯并[3,4-c]吡唑-3- 基}-3-氯苯曱醯胺； 766.1{5-胺基羰基-4,6-二氫咄咯并[3,4-(：]吡唑-3-基卜4-氯苯甲醯胺； 767.1^-{5-胺基羰基-4,6-二氫咄咯并[3,4-〇]咄唑-3-基} - 1 -哌啶丙醯胺； 768· Ν-{5 -胺基幾基_4，6 -二氫吼"各并[3，4-c] ρ比β坐-3-基} - 2 -乙醯基苯甲醯胺； 76 9. Ν-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3- 基} - 4 -乙醯基苯曱醯胺； 770. Ν-{5 -胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑-3-90119473 (replacement)-2.ptc Page 400 1327569 j_ Case No. 90119473_Yearly revision _ 6. Patent application base}_2_Phenylphenylacetic acid amine; 759. N-{5-Aminocarbonyl-4 , 6-dihydroindolo[3,4-c]pyrazol-3-yl}_3_fluorophenylethylamine; 760. N-{5-aminol-yl-4,6-diaza α Ratio 13 [3,4-c] π than spani-3-ylindole_4_fluorophenylethylamine; 761. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3 , 4-c]pyrazol-3-yl b 3-(2-thienyl)propenylamine; 762. ?^-{5_aminocarbonyl-4,6-dihydroindole[3,4- 〇]pyrazol-3-yl}-3-(3-thienyl)propenylamine; 7 6 3. Ν-{5-aminocarbonyl-4,6-dihydroindole[3, 4-c Pyrazol-3-yl}-3-(2-thienyl)propanamine; 76 4· Ν-{ 5 -aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3-yl}_2-chlorophenyl hydrazone; 765. Ν-{5-aminocarbonyl-4,6-dihydro"bido[3,4-c]pyrazol-3-yl}- 3-chlorobenzoin; 766.1{5-aminocarbonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-ylbu-4-chlorobenzamide; 767.1^ -{5-Aminocarbonyl-4,6-dihydroindolo[3,4-indolyl]oxazol-3-yl}-1 -piperidine醯 ; { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { Indoleamine; 76 9. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]oxazol-3-yl}-4-ethoxybenzhydrylamine; 770. Ν-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole-3-

90119473(替換）-2.ptc 第401頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍基卜1 -萘曱醯胺； 771. N-{ 5 -胺基羰基-4, 6 -二氫咄咯并[3, 4-c]吡唑-3-基}-2-萘曱醯胺； 772_ N-{5 -胺基幾基_4，6_二氫n比11 各并[3，4-c] π比β坐-3 -- 基}-3-苯曱醯基丙醯胺； 773. Ν-{5 -胺基截基-4,6 -二氫各并[3，4-c] °比°坐- 3-基} -4-乙醯胺基苯曱醯胺； 774. N-{ 5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3-基}-2,5_二甲氧苯曱醯胺； φ775. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基}-2,6 -二曱氧苯曱醯胺； 776. N-{5 -胺基幾基_4，6_二氫n比略并[3，4-c] D比°坐_3_ 基}-3,4 -二甲氧笨甲醯胺； 777· N-{5 -胺基幾基-4,6-二氫°比°各并[3，4-c] °比°坐_3_ 基}-3,5_二甲氧苯甲醯胺； . 778. N-{5 -胺基幾基-4，6 -二氫吼11 各并[3，4-c] °比°坐-3_ 基}-3-(2-噻吩曱醯基）-丙醯胺； 77 9_ N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 赢} -2-萘基乙醯胺； _7 8 0. N-{5 -胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑-3- 基丨_1「秦基乙酿胺， 781.1{5-胺基羰基-4,6-二氫吡咯并[3,4-(：]吡唑-3-基卜4-苯基苯曱醯胺； 7 8 2. N - { 5 -胺基績醯基-4，6 -二氫吡咯并[3, 4 - c ]吡唑90119473 (replacement)-2.ptc Page 401 1327569 _ Case No. 90119473_Yearly revision _ Six, the scope of application for patents 1 -Naphthylamine; 771. N-{ 5 -Aminocarbonyl-4, 6 - dihydroindolo[3,4-c]pyrazol-3-yl}-2-naphthylamine; 772_ N-{5-amino-based _4,6-dihydron-n ratio 11 [3,4-c] π ratio β--3-yl}-3-phenylmercaptopropylamine; 773. Ν-{5-amino-based cleaving-4,6-dihydro-[3] , 4-c] °°°-3-yl}-4-acetamidophenyl hydrazide; 774. N-{ 5 -aminocarbonyl-4,6-dihydropyrrolo[3, 4- c]pyrazol-3-yl}-2,5-dimethoxybenzoquinone; φ775. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyrazole -3-yl}-2,6-dioxabenzoylamine; 776. N-{5-aminol-based _4,6-dihydron n ratio slightly [3,4-c] D ratio Sit _3_ ki}-3,4-dimethoxybenzamide; 777· N-{5-amino benzyl-4,6-dihydrogen ratio °[3,4-c] ° ° sit _3_ base}-3,5-dimethoxybenzamide; . 778. N-{5-amino-based-4,6-dihydroindole 11 each [3,4-c] ° Ratio -3 - yl}-3-(2-thienyl)-propanamine; 77 9_ N-{5-aminocarbonyl-4,6-dihydrogen Pyrrolo[3,4-c]pyrazole-3-win}-2-naphthylacetamide; _7 8 0. N-{5-aminocarbonyl-4,6-dihydropyrrolo[3, 4 -c]pyrazole-3-ylindole_1 "Qinyl Ethylamine, 781.1{5-Aminocarbonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl b 4-phenylbenzamide; 7 8 2. N - { 5 -Amino-alkyl 4,6-dihydropyrrolo[3,4 - c ]pyrazole

90119473(替換）-2.ptc 第402頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 _3_基}_乙酿胺； 783. N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_環丙烧叛S藍胺； 78 4. N-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-異丁醯胺； 785.1^-{5-胺基續醯基-4,6-二氫吡洛并[3,4-(：]11比唑 _3-基}_環戊烧叛酿胺； 786. N-{5 -胺基續醯基- 4,6 -二氫°比°各并[3,4-c] D比唑 -3 -基}-苯甲醯胺； 78 7. N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-曱基吡啶曱醯胺； 788. N-{5 -胺基磺醯基-4,6-二氫咄咯并[3,4-〇:]吡唑 _ 3 -基} _於驗酷胺； 789.1{5-胺基績醯基-4,6-二氫吡<1各并[3,4-(：]11比。坐 _3_基}-異於驗臨胺； 790. N-{5 -胺基續醯基-4,6 -二氫D比11 各并[3,4-c] °比峻一3-基}—3-甲基一2 —11夫。南曱醯胺； 791. N-{5 -胺基績Si基- 4,6 -二氳吼11各并[3,4-c] °比〇坐 -3-基}-噻吩-2-羧醯胺； 79 2. N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_D塞吩_3_缓0藍胺； 793.1{5-胺基續醯基-4,6-二氫吼57各并[3,4-(：]°比峻 -3-基}-鄰-甲苯甲醯胺； 794. N-{5 -胺基績醯基-4, 6 -二氫吡11 各并[3,4-c] D比0坐90119473 (replacement)-2.ptc page 402 1327569 _ case number 90119473_year month 曰 amendment _ six, the scope of application for patent _3_ base} _ ethyl amine; 783. N-{5-aminosulfonyl- 4,6-dihydropyrrolo[3,4-indolylpyrazole-3-yl}}cyclopropanone S-sodium amide; 78 4. N-{5-aminosulfonyl-4,6-di Hydropyrrolo[3,4-c]pyrazole-3-yl}-isobutylamine; 785.1^-{5-aminodinyl-4,6-dihydropyrolo[3,4-( :]11-pyrazole-3-3-}}cyclopentanol; 786. N-{5-aminodinyl- 4,6-dihydrogen ratio °[3,4-c] D Bizozol-3 -yl}-benzamide; 78 7. N-{ 5 -aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}- Pyridylamine; 788. N-{5-aminosulfonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl} 789.1 {5-Amino-mercapto-4,6-dihydropyridin<1 each [3,4-(:]11 ratio. sitting_3_yl}- is different from the test amine; 790. N- {5-Amino-indenyl-4,6-dihydrogen D ratio 11 and [3,4-c] ° ratio jun-3-yl}-methyl- 2-11-nf. 791. N-{5-Amine-based Si- 4,6-diindole 11 and [3,4-c] ° 〇-3-yl}-thiophene-2- Indoleamine; 79 2. N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_D-cetin-3-3 793.1{5-Amino-indenyl-4,6-dihydroanthracene 57 each [3,4-(:]° than tern-3-yl}-o-toluamylamine; 794. N-{5 -Amine-based thiol-4,6-dihydropyrrole 11 each [3,4-c] D sits at 0

90119473(替換）-2.ptc 第403頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍 -3-基卜間-甲苯曱醯胺； 795. N-{5 -胺基績酸基-4, 6 -二氫D比咯并[3,4-c]吼°坐 -3-基}-對-甲苯曱醯胺； 7 9 6. N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 --3 -基}-苯基乙醯胺； 797.^{5-胺基績酸基-4,6-二氫吼11各并[3,4-(：]11比〇坐 -3_基}_水揚酿胺， 7 9 8. N - { 5 -胺基績醯基-4，6 -二氫吡咯并[3, 4 - c ] °比唑 -3-基卜2-氟苯甲醯胺； φ7 9 9 · N - { 5 -胺基續酸基-4，6 -二氫°比咯并[3，4 - c ] °比0坐 _3-基}-3-氟苯甲醯胺； 80 0. 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-氟苯曱醯胺； 8 0 1. N - { 5 -胺基績醯基-4，6 -二氫吡咯并[3，4 - c ] 11比0坐 -3 -基}-噻吩-2-乙醯胺； 8 0 2 · N _ { 5 -胺基續醯基-4，6 -二氫吼咯并[3, 4 - c ] π比0坐 -3 -基}-噻吩-3-乙醯胺； 8 0 3. Ν - { 5 -胺基續醯基-4，6 -二氫吡咯并[3，4 - c ] 11比唑基} _苯基丙快酿胺，鲁8 0 4. Ν - { 5 -胺基續醯基-4，6 -二氫吡咯并[3, 4 - c ] 比唑 -3-基}-3-氰基苯曱醯胺； 805.^{5-胺基續醯基-4,6-二氫吼咯并[3,4-(：]11比11坐 ‘ -3-基}-4-氰基苯曱醯胺； 8 0 6. Ν - { 5 -胺基磺醯基-4，6 -二氫吡咯并[3，4 - c ]吡唑90119473 (replacement)-2.ptc Page 403 1327569 _ Case No. 90119473_年月日日__ VI. Patent application scope -3- keb-toluidine; 795. N-{5-amino acid Base-4,6-dihydro D is more than [3,4-c] 坐坐-3-yl}-p-toluidine; 7 9 6. N-{ 5 -aminosulfonyl- 4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-phenylacetamidamine; 797.^{5-aminopic acid-4,6-dihydroindole 11 Each [3,4-(:]11 is more than 〇___}} _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ , 4 - c ] °, oxazol-3-yl b 2-fluorobenzamide; φ7 9 9 · N - { 5 -amino acid group-4,6-dihydrogen ratio [3,4 - c ] ° sits at 0 _3-yl}-3-fluorobenzamide; 80 0.5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole- 3-yl}-4-fluorobenzamine; 8 0 1. N - { 5 -aminodinyl-4,6-dihydropyrrolo[3,4 - c ] 11 to 0 -3 - }}-thiophene-2-acetamide; 8 0 2 · N _ { 5 -amino sulfonyl-4,6-dihydroindolo[3, 4 - c ] π ratio 0 sitting -3 -yl }-thiophene-3-acetamide; 8 0 3. Ν - { 5 -amino thiol-4,6-dihydropyridyl咯[3,4 - c ] 11 - oxazolyl} phenyl phenyl propylamine, Lu 8 0 4. Ν - { 5 -amino thiol-4,6-dihydropyrrolo[3, 4 - c ] Biazol-3-yl}-3-cyanobenzoquinone; 805.^{5-Amino-indenyl-4,6-dihydroindolo[3,4-(:]11 Sitting at 11 '-3-yl}-4-cyanobenzoquinone; 8 0 6. Ν - { 5 -aminosulfonyl-4,6-dihydropyrrolo[3,4 - c ]pyr Azole

90119473(替換）-2.ptc 第404頁 1327569 _案號90119473_年月日__ 六、申請專利範圍 -3 -基}-反-桂皮醯胺； 807. N-{5 -胺基績酸基-4，6 -二氫吨嘻并[3,4-c] 11比。坐 -3 -基}-順-桂皮醯胺； 808. N-{5 -胺基續醯基-4,6 -二氫啦17各并[3,4-c] σ比。坐 - 3-基}_3_(3_<7比°定基）丙稀酿胺； 809.1^-{5-胺基績醯基-4,6-二氫咄11各并[3,4-(：]11比。坐 -3_基}_3_(4_11比17定基）丙稀酿胺； 8 1 0 · Ν - { 5 -胺基續醯基-4，6 -二氫°比σ各并[3，4 - c ] D比。坐 _3-基}_2_苯基丙酿胺； 81 1. N-{ 5 -胺基磺醯基-4, 6 -二氫咄咯并[3, 4-c]咄唑 -3-基}-鄰-曱苯基乙醯胺； 81 2. N-{5 -胺基磺醯基-4, 6 -二氫哺咯并[3, 4-c]吡唑 - 3 -基}-間-曱苯基乙酷胺， 813. N-{5 -胺基磺醯基-4,6-二氫咄咯并[3,4-〇]吡唑 -3_基}_對-甲苯基乙酿胺； 81 4. N - { 5 -胺基續驢基-4，6 -二氫吼β各并[3，4 - c ] °比。坐 -3_基}_鄰-菌香醋胺； 815.1'1-{5-胺基石黃酸基-4,6-二氫吡°各并[3,4-(：]°比〇坐 -3-基}-3_曱氧苯甲醯胺； 816. Ν-{5 -胺基石黃酸基- 4,6 -二氫°比°各并[3,4-c] °比〇坐 -3-基}-對-茴香醯胺； 817. N-{5 -胺基磺醯基-4, 6 -二氫°比咯并[3, 4-c]吡唑 ~3-基}-苯氧乙醯胺； 818. N-{5 -胺基磺醯基-4,6-二氫吡咯并[3,4-(：]咄唑90119473 (replacement)-2.ptc Page 404 1327569 _ Case No. 90119473_Year of the month __ VI. Patent application scope -3 - base}-trans-cinnafloxacin; 807. N-{5-amino acid Base-4,6-dihydro ton oxime [3,4-c] 11 ratio. Sodium -3 -yl}-cis-cinnamicin; 808. N-{5-amino sulfonyl-4,6-dihydrola17 and [3,4-c] σ ratio. Sit-3-yl}_3_(3_<7 ratio to base) acrylamide; 809.1^-{5-amino benzyl-4,6-dihydroindole 11 each [3,4-(:] 11 ratio. Sitting -3_base}_3_(4_11 to 17-base) acrylamide; 8 1 0 · Ν - { 5 -amino group thiol-4,6-dihydrogen ratio σ[3, 4 - c ] D ratio. Sit _3-yl}_2_phenyl propylamine; 81 1. N-{ 5 -aminosulfonyl-4,6-dihydroindolo[3, 4-c ] oxazol-3-yl}-o-indole phenylacetamide; 81 2. N-{5-aminosulfonyl-4,6-dihydron-[3,4-c]pyrazole - 3 -yl}-m-phenylphenyl carbamide, 813. N-{5-aminosulfonyl-4,6-dihydroindolo[3,4-indolyl]pyrazole-3-yl }_p-tolylylamine; 81 4. N - { 5 -amino sulfonyl-4,6-dihydroindole β each [3,4 - c ] ° ratio. sit -3_ base} _ o--bacterial acetamide; 815.1'1-{5-amino fluorescein-4,6-dihydropyridyl each [3,4-(:] ° than 〇-3-yl}-3曱曱曱苯醯 ; ; 816 816 { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { - anisidine; 817. N-{5-aminosulfonyl-4,6-dihydropyrolo[3,4-c]pyrazole~3-yl}-phenoxyacetamide; 8 18. N-{5-Aminosulfonyl-4,6-dihydropyrrolo[3,4-(:]carbazole

90119473(替換）-2.ptc 第405頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 -3-基}_2_氣苯基乙酿胺； 819.1{5_胺基績酿基-4,6-二氫吼咯并[3,4-(：]'1比〇坐 -3-基}-3_氣苯基乙酿胺； 820.?^-{5-胺基續酸基-4,6-二氫11比咯并[3,4-(：]°比〇坐 • -3_基}-4_氣苯基乙酿胺； 8 2 1. N - { 5 -胺基績S藍基-4，6 -二氫D比咯并[3，4 - c ]吼。坐 -3_基}-3_(2_ °塞吩基）丙炸酿胺， 82 2. N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}-3_(3-°塞吩基）丙稀酿·胺；鲁82 3. N-{ 5 -胺基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-3-(2-噻吩基）丙醯胺； 824. N-{5 -胺基續醯基-4,6 -二氫D比咯并[3,4-c] β比0坐 -3-基}-2-氣苯曱醯胺； 825. ^}-{5-胺基續醯基-4,6-二氫吡咯并[3,4-(：]°比唑 -3-基}-3_氣苯甲酿胺； 826. Ν-{5 -胺基續醯基-4,6 -二氫D比咯并[3,4-c]吡嗤 _3-基}·_4_氣苯甲酿胺； 82 7. Ν-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑基} - ：1 -哌啶丙醯胺； •82 8. N-{5-胺基磺醯基-4, 6-二氫咄咯并[3, 4-c] °比唑 -3_基}_2_乙酿基苯甲酿胺； 8 2 9 · N _ { 5 -胺基績醯基-4，6 -二氫nb咯并[3，4 - c ] °比〇坐 -3-基}-4_乙醯基苯曱醯胺； 830. N-{5 -胺基續醯基-4, 6 -二氫吡咯并[3,4-c] 11比唑90119473 (replacement)-2.ptc page 405 1327569 _ case number 90119473_year month 曰 amendment _ six, the scope of application patent -3- base}_2_ gas phenyl ethylamine; 819.1 {5_amine base -4,6-dihydroindolo[3,4-(:]'1 is more than -3-yl}-3-phenylphenylethylamine; 820.?--{5-amino acid Base-4,6-dihydrogen 11 is more than [3,4-(:]° 〇 • • -3_基}-4_ phenyl phenylethylamine; 8 2 1. N - { 5 -amine Base performance S-blue-4,6-dihydro D ratio 咯[3,4 - c ]吼. Sitting -3_yl}-3_(2_ °sepeno)propanol, 82 2. N- { 5 -Aminosulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-3_(3-°secenyl)propanolamine; Lu 82 3 N-{ 5 -aminosulfonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-3-(2-thienyl)propanamine; 824. N-{5-aminodinyl-4,6-dihydro D is more than [3,4-c]β than 0--3-yl}-2-phenanthridine; 825. ^} -{5-Amino-indenyl-4,6-dihydropyrrolo[3,4-(:]°-pyrazol-3-yl}-3_peptazene; 826. Ν-{5 - Amino-based fluorenyl-4,6-dihydro-D-pyrolo[3,4-c]pyridin-3-yl}·_4_gasbenzamide; 82 7. Ν-{5-aminosulfonate Base -4,6-dihydropyrrolo[3,4-c]pyrazolyl}-:1-piperidinepropanamine; •82 8. N-{5-aminosulfonyl-4,6-di Hydropyrrolo[3,4-c] °pyrazole-3_yl}_2_ethyl-brenylbenzamide; 8 2 9 · N _ { 5 -aminol-alkyl-4,6-dihydrogen Nb 咯[3,4 - c ] ° than 〇-3-yl}-4_ ethenyl phenyl hydrazine; 830. N-{5-amino sulfonyl-4,6-dihydropyrrole And [3,4-c] 11 azole

90119473(替換）-2.ptc 第406頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 -3-基}-1_萘甲醯胺； 831. N-{5 -胺基續酿基-4, 6 -二氫。比11各并[3,4-c] D比0坐 -3-基}-2 -萘曱醯胺； 832. N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}·_3_苯曱臨基丙酷胺， 83 3. N-{5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-4-乙醯胺基苯甲醯胺； 83 4. N-{ 5 -胺基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_2，5 -二曱氧苯曱酿胺， 835. N-{5 -胺基磺醯基-4, 6 -二氫吡p各并[3,4-c] 11比唑 -3 -基}-2,6 -二曱氧苯曱醯胺； 836. ^{5-胺基續醯基-4,6-二氫咄>1各并[3,4-(：]°比唑 _3-基}-3，4 -二甲氧苯曱酿胺； 837.1{5-胺基續醯基-4,6-二氫吡洛并[3,4-(：]吡唑 -3-基}-3,5 -二甲氧苯甲醯胺； 838. ~-{5-胺基績醯基-4,6-二氫吡洛并[3,4-(：]°比唑 -3-基}-3-(2 -噻吩曱醯基）-丙醯胺； 839. N-{5 -胺基績醯基-4,6 -二氫咄0各并[3,4-c] °比唑 -3_基}_2_奈基乙酿胺； 8 4 0. N-{5 -胺基石黃酸基- 4,6 -二氫^比17各并[3,4-c]吼°坐 -3 -基}_1_奈基乙酿胺， 841. N-{5 -胺基績醯基-4,6 -二氫°比°各并[3,4-c] °比唑 _3-基}_4_苯基苯曱臨胺， 842. N-{5-甲苯磺醯基-4, 6 -二氫。比咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 406 1327569 _ Case No. 90119473_Yearly revision _ Six, application patent range -3- base}-1_naphthylguanamine; 831. N-{5-amine group continued Brewing base-4,6-dihydrogen. Ratio of 11 [3,4-c] D to 0--3-yl}-2-naphthylamine; 832. N-{ 5 -aminosulfonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazole_3_yl}·_3_benzoquinone propylamine, 83 3. N-{5-aminosulfonyl-4,6-dihydropyrrolo[3, 4 -c]pyrazol-3-yl}-4-acetamidobenzamide; 83 4. N-{5-aminosulfonyl-4,6-dihydropyrrolo[3,4-c Pyrazole _3_yl}_2,5-dioxabenzoquinone, 835. N-{5-aminosulfonyl-4,6-dihydropyridinyl[3,4-c] 11-pyrazol-3-yl}-2,6-dioxabenzoquinone; 836. ^{5-Amino-indenyl-4,6-dihydroanthracene>1[3,4- (:]°Biazole-3-yl}-3,4-dimethoxybenzoquinone; 837.1{5-Amino-indenyl-4,6-dihydropylo[3,4-(: Pyrazol-3-yl}-3,5-dimethoxybenzamide; 838. ~-{5-Amino-mercapto-4,6-dihydropyrazolo[3,4-(: ]°Bizozol-3-yl}-3-(2-thiophenanthryl)-propanamine; 839. N-{5-Amino-mercapto-4,6-dihydroindole 0 each [3 , 4-c] °Bizozol-3_yl}_2_Nylidenylamine; 8 4 0. N-{5-Amino-based phthalic acid- 4,6-dihydrogen-to-nine ratio [3, 4-c]吼°Sit-3 -yl}_1_Nylidene amine, 841. N-{ 5-Amino-based thiol-4,6-dihydrogen ratio °[3,4-c] ° azole-3-yl}_4_phenylbenzoquinone amine, 842. N-{5- Toluenesulfonyl-4,6-dihydro.pyrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第407頁 1327569 __案號90119473_年月曰修正_ 六、申請專利範圍 -3 -基}-乙臨胺； 843.1^-{5-曱苯磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑 _3-基}-環丙院叛酿胺； 844. N-{5-曱笨石黃酸基- 4,6 -二氫D比17各并[3,4-c] 0比。坐 • -3 -基}-異丁醯胺； 845.1{5-曱苯石黃隨基-4,6-二氫0比11各并[3,4-(：]11比唾 -3_基}-環戊烧叛酿胺； 846. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3_基}_苯甲酸胺； φ8 4 7, N-{5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-甲基吡啶曱醯胺； 84 8. Ν-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _ 3 _基} _於驗酿胺； 849. Ν-{5-曱苯磺醯基-4,6-二氫°比咯并[3,4-(：]吡唑 -3-基}-異菸鹼醯胺； 8 5 0. Ν-{ 5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}-3-曱基-2 -呋喃甲醯胺； 851.~-{5-曱苯石黃酸基-4,6-二氫0比咯并[3,4-(：]0比〇坐基} - π塞吩-2 -魏酿胺；胃85 2. Ν-{ 5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 _ 3 -基} - α塞吩-3 -叛酿胺； 853. Ν-{5-曱苯石黃醯基-4, 6 -二氫〇比0各并[3,4-c] 0比0坐 -3 -基}-鄰-甲苯曱醯胺； 8 5 4. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 407 1327569 __ Case No. 90119473_Yearly revision _ Six, patent application scope -3 - base}-ethylamine; 843.1^-{5-nonylbenzenesulfonyl- 4,6-dihydroindolo[3,4-(:]pyrazole-3-yl}-cyclopropane adenine; 844. N-{5-曱 stearyl- 4,6- Dihydrogen D ratio of 17 and [3,4-c] 0 ratio. Sodium • -3 -yl}-isobutylamine; 845.1{5-beanthine yellow with base-4,6-dihydro 0 to 11 each [3,4-(:]11 is more specific than saliva-3_yl}-cyclopentanol; 846. N-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4- 〇]pyrazole-3-yl}-benzoic acid amine; φ8 4 7, N-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl }-methylpyridiniumamine; 84 8. Ν-{ 5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole_3 _yl} _ 849. Ν-{5-nonylbenzenesulfonyl-4,6-dihydropyrolo[3,4-(:]pyrazol-3-yl}-isonicotinamine; 8 5 0. Ν-{ 5-nonylbenzenesulfonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-3-mercapto-2-furancarboxamide; 851.~ -{5-naphthyltrimyl-4,6-dihydro- 0-pyrrolo[3,4-(:]0 is more than 〇基} - π phene-2 - Wei Amine; stomach 85 2. Ν-{ 5-nonylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}-α-cetin-3-rebel 853. Ν-{5-bepholine xanthene-4,6-dihydroindole ratio 0 and [3,4-c] 0 to 0 sitting -3 -yl}-o-toluidine; 8 5 4. N-{ 5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第408頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍 -3-基}-間-曱苯曱醯胺； 855. N-{5-甲苯石黃酷基-4，6 -二氫〇比°各并[3,4-c] π比0坐 -3-基}-對-曱苯曱醯胺； 856. Ν-{5-甲苯石黃醯基-4，6 -二氫0比0各并[3，4-c] 0比0坐 _ 3 -基} _水楊酿胺； 857_ N-{5-曱苯石黃驢基-4，6 -二氫0比口各并[3,4-c] 0比。坐 _3_基}_2_氣苯甲酿胺； 858. N-{5-曱苯石黃驢基- 4,6 -二氫°比0各并[3,4-c]吼〇坐 _3_基}_3_氣苯甲酿胺， 859. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-4-氟笨曱醯胺； 860. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]咄唑 -3 -基} - °塞吩-2 -乙酿胺； 861. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-噻吩-3 -乙醯胺； 862. N-{5-曱苯磺醯基-4,6-二氫°比咯并[3,4-(：]吼唑 -3-基}_苯基丙快酿·胺； 863. N-{5-曱苯磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 _3_基}_3_鼠基苯曱1藍胺， 864. N-{5-甲苯磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑 -3_基}_4-氛基苯曱驢胺； 865. N-{5-甲苯磺醯基-4,6-二氫吼咯并[3,4-(：]吡唑 -3 -基}-反-桂皮隨胺； 866.1{5-曱苯石黃醯基-4,6-二氫〇比°各并[3,4-(：]0比〇坐90119473 (replacement)-2.ptc page 408 1327569 _ case number 90119473_year and day correction _ six, the scope of application for patent -3- base}-m-phenylhydrazine; 855. N-{5-toluene酷-{5-toluene 醯醯黄 { { -4 -4 -4 -4 -4 -4 { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { -4,6-dihydrogen 0 to 0 each [3,4-c] 0 to 0 sitting _ 3 -yl} _shuiyang amine; 857_ N-{5-beanthine fluorenyl-4,6 - Dihydrogen 0 is proportional to each [3,4-c] 0 ratio. Sit _3_基}_2_ gas benzoylamine; 858. N-{5-beanthine xanthine- 4,6-dihydrogen ratio 0 and [3,4-c] 吼〇 sitting_ 3_基}_3_气苯甲胺, 859. N-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-4- Fluorobenzamine; 860. N-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]carbazole-3-yl}- °Centene-2-ethyl Amine; 861. N-{ 5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-thiophene-3-acetamide; 862. N- {5-Indolylsulfonyl-4,6-dihydrogen-pyrano[3,4-(:]carbazol-3-yl}-phenylpropanol; amine 863. N-{5- Benzene sulfonyl-4,6-dihydroindolo[3,4-c]pyrazole-3-yl}_3_murine benzoquinone1 leucine, 864. N-{5-toluenesulfonyl -4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}- 4-aminobenzoquinone; 865. N-{5-toluenesulfonyl-4,6- Dihydroindolo[3,4-(:]pyrazol-3-yl}-trans-cassia with amine; 866.1{5-bepholine xanthine-4,6-dihydroindole ratio [3, 4-(:]0 is better than sitting

90119473(替換）-2.ptc 第409頁 1327569 _案號90119473 ‘ 年月日修正_ 六、申請專利範圍 -3 -基} _順'•桂皮酿胺； 867.1^-{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3 -基} - 3 - ( 3 - °比啶基）丙烯醯胺； 868. N-{5-甲苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 * -3 -基}_3_(4_ °比°定基）丙炸睡胺， 8 6 9. N-{ 5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-2_苯基丙醯胺； 87 0. N-{ 5-甲苯磺醯基-4, 6 -二氫咣咯并[3, 4-c]。比唑 -3 -基}-鄰-甲苯基乙醯胺； •871. N-{ 5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基}-間-曱苯基乙醯胺； 872.1{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基}_對-甲苯基乙醯胺； 8 7 3. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3 -基}-鄰-菌香酿胺， 874.1{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-3-曱氧苯曱醯胺； 875.^1-{5-甲苯磺醯基-4,6-二氫咄咯并[3,4-(：]咣唑基卜對-茴香醯胺；響8 7 6. N-{ 5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}_苯氧乙酿胺， 877. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}_2-乳苯基乙酿胺， 8 7 8. N-{ 5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc page 409 1327569 _ case number 90119473 'year and month correction _ six, the scope of application for patent -3 - base} _ shun '• cinnamon sulphate; 867.1^-{5-toluenesulfonyl -4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-(3-pyridyl)propenylamine; 868. N-{5-toluenesulfonyl -4,6-dihydropyrrolo[3,4-indene]pyrazole* -3 -yl}_3_(4_ ° ratio ° base) propanolamine, 8 6 9. N-{ 5-toluenesulfonyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-2-phenylpropanoxime; 87 0. N-{ 5-toluenesulfonyl-4,6-di Hydropyrrolo[3,4-c].Bizozol-3-yl}-o-tolylacetamide; •871. N-{ 5-Toluenesulfonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazol-3-yl}-m-indole phenylacetamide; 872.1{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-indolyl]pyrazole -3 -yl}-p-tolylacetamide; 8 7 3. N-{ 5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl }-o-bacteria, 874.1{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}-3-oxobenzoquinone Amine; 875.^1-{5-toluenesulfonyl-4,6-dihydroanthracene [3,4-(:]oxazolyl-p-anisole; ring 8 7 6. N-{ 5-toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole _3_基}_phenoxyethylamine, 877. N-{5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}_2- Lactophenylamine, 8 7 8. N-{ 5-toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第410頁 1327569 案號90119473 年月日修正六、申請專利範圍 -3_基丨-3_氣苯基乙酿·胺； 879.^{5-曱苯石黃酸基-4，6-二氫0比°各并[3,4-(：]0比〇坐 _3-基}~4_氣苯基乙酿胺； 880· N-{5-曱苯石黃酸基_4，6 -二氮°比°各并[3，4-c] D比0坐 -3-基}-3-(2_噻吩基）丙烯醯胺； 881. N-{5-曱苯石黃醯基-4，6_二氫0比0各并[3,4-c] 0比0坐 -3_基}-3_(3-°塞吩基）丙稀酸·胺； 882. ^{5-曱苯磺醯基-4,6-二氫咄咯并[3,4-(：]°比唑 -3-基}-3-(2_噻吩基）丙醯胺； 883. N-{5-曱苯石黃酿基-4, 6 -二氫吡0各并[3,4-c] 0比。坐 _3-基}-2_氣苯曱驢胺， 884. N - { 5-甲苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3_基}-3 -氯苯甲酿胺； 885. N-{5-曱苯磺醯基-4,6-二氫咄咯并[3,4-(：]吡唑 -3-基}-4-氣苯甲酿胺； 886. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基} - 1 -哌啶丙醯胺； 887. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3_基}~2_乙酸基苯曱臨胺； 888· N-{5-曱苯績醯基-4，6 -二氫0比0各并[3,4-c] 0比。坐 -3-基}-4-乙醯基苯甲醯胺； 88 9. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3 -基} - 1 -萘甲醯胺； 890. N-{5-曱苯磺醯基-4,6-二氫吼咯并[3,4-(：]吡唑90119473 (replacement)-2.ptc Page 410 1327569 Case No. 90119473 Revised on the sixth day of the month, the scope of the patent application -3_based -3_ gas phenyl ethyl amine; 879.^{5-beanthine yellow Acid group-4,6-dihydrogen 0 ratio °[3,4-(:]0 is more than 〇3-yl}~4_gas phenylethylamine; 880· N-{5-nonylbenzene The content of oleic acid group _4,6-diaza is °[3,4-c] D is 0 -3-yl}-3-(2_thienyl) acrylamide; 881. N-{ 5-indolyl xanthine-4,6-dihydrogen 0 to 0 each [3,4-c] 0 to 0 sitting -3_yl}-3_(3-°secenyl)acrylic acid amine; 882. ^{5-Indolylsulfonyl-4,6-dihydroindolo[3,4-(:]°pyrazol-3-yl}-3-(2-thienyl)propanamine; 883. N-{5-beanthine yellow-branched-4,6-dihydropyridinium each [3,4-c] 0 ratio. sitting _3-yl}-2_ phenbenzamine, 884 N - { 5-Toluenesulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}-3-chlorobenzamide; 885. N-{5-曱Phenylsulfonyl-4,6-dihydroindolo[3,4-(:]pyrazol-3-yl}-4-p-benzoic acid; 886. N-{ 5-nonylbenzenesulfonyl -4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl}-1 -piperidinepropanamine; 887. N-{5-nonylsulfonyl-4,6-di Pyrrolo[3,4-indolylpyrazole-3-yl}~2-acetoxybenzoylamine; 888·N-{5-indole fluorenyl-4,6-dihydrogen 0 to 0 each [3,4-c] 0 ratio. Sodium-3-yl}-4-ethylmercaptobenzamide; 88 9. N-{ 5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazol-3-yl}-1 -naphthylamine; 890. N-{5-nonylsulfonyl-4,6-dihydroindole[3,4-(: Pyrazole

90119473(替換）-2.ptc 第411頁 1327569 _案號90119473_年月日修正_ 六、申請專利範圍 -3_基}~2 -奈曱酸胺； 891.1^-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3_基}_3-苯曱酿基丙臨胺， 892. N-{5-曱苯磺醯基-4, 6 -二氫吡咯并[3,4-c]吡唑 _3_基}_4-乙酿胺基笨曱臨胺， 893. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_2，5_二曱氧笨曱驢胺； 894. N-{5-曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3_基}-2,6_二曱氧苯甲酿胺， φ8 9 5. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-3, 4-二甲氧苯曱醯胺； 896,1{5-甲苯石黃驢基-4,6-二氫吡咯并[3,4-(：]0比'1坐 -3-基卜3, 5-二甲氧苯甲醯胺； 897.1{5_曱苯磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-3-(2_噻吩甲醯基）-丙醯胺； 8 9 8. N-{5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3-基}_2_秦基乙酿胺； 8 9 9, N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑基}-1_秦基乙酿胺， ®9 00. N-{ 5-曱苯磺醯基-4, 6 -二氫吡咯并[3, 4-c]吼唑 -3_基}-4 -苯基苯曱醯胺； 9 01. N-{ 5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3_基}_乙驢胺； 9 0 2. N-{ 5 -苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 411 1327569 _ Case number 90119473_Yearly date correction _ VI. Patent application scope -3_ base}~2 -Nitrate; 891.1^-{5- benzene sulfonate 4-,6-dihydropyrrolo[3,4-(:]pyrazol-3-yl}_3-benzoquinone-propanylamine, 892. N-{5-nonylsulfonyl-4, 6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_4-ethylammonium alum, 893. N-{5-nonylbenzenesulfonyl-4,6-dihydro Pyrrolo[3,4-indolylpyrazole-3-yl}_2,5-dioxanoxacin; 894. N-{5-nonylsulfonyl-4,6-dihydropyrrolo[ 3,4-〇]pyrazole-3-yl}-2,6-dioxabenzoylamine, φ8 9 5. N-{ 5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[ 3, 4-c]pyrazol-3-yl}-3,4-dimethoxybenzoquinone; 896,1{5-tolylxanthyl-4,6-dihydropyrrolo[3,4 -(:]0 is more than '1 sitting-3-kib3, 5-dimethoxybenzamide; 897.1{5_nonylsulfonyl-4,6-dihydropyrrolo[3,4-anthracene Pyrazol-3-yl}-3-(2-thiophenemethyl)-propanamine; 8 9 8. N-{5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3, 4-c]pyrazole-3-yl}_2_methylglycolamine; 8 9 9, N-{ 5-nonylbenzenesulfonyl-4,6-dihydropyrrolo[3, 4-c Pyrazolyl}-1_methylglycolamine, ®9 00. N-{ 5-nonylsulfonyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl }-4-phenylbenzamide; 9 01. N-{ 5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole-3-yl}_acetamidine Amine; 9 0 2. N-{ 5 -benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第412頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 _3_基}_環丙烧叛酿胺； 9 0 3. N-{5_苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑 _3-基}_異丁酿胺； 904.1{5-芊基石黃酸基-4,6-二氫〇比各并[3,4-(：]〇比〇坐 _3_基}_壤戊烧缓酸胺， 905. N-{5-苄基磺醯基-4,6-二氫°比咯并[3,4-(：]吡唑 -3_基}_苯甲酿胺； 906. N-{5-苄基石黃臨基-4, 6 -二氫°比0各并[3,4-c] °比0坐 -3 -基}-曱基吡啶曱醯胺； 9 07. N-{5 -苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 _3-基}_於驗酿胺； 908. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基}-異菸鹼醯胺； 90 9. N-{ 5-苄基磺醯基-4, 6 -二氫吼咯并[3, 4-c]吡唑 -3-基}-3-甲基-2 -呋喃曱醯胺； 910. ^{5-苄基磺醯基-4,6-二氫吡'1各并[3,4-(：]11比〇坐 -3 -基丨-嗔吩-叛酿胺； 911. N-{5-苄基石黃酸基- 4,6 -二氫°比略并[3,4-c] 0比唾 -3 -基} - 11塞吩_ 3 -缓酿胺； 912. N-{5-苄基磺醯基-4,6-二氫吼咯并[3,4-(：]咄唑 -3 -基}-鄰-甲苯曱醯胺； 913. N-{5-芊基磺酿基-4,6 -二氫°比0各并[3,4-c] °比〇坐 -3 -基}-間-曱苯曱醯胺； 914. N-{5-r基磺醯基-4,6_二氫吡咯并[3,4-c]吡唑90119473 (replacement)-2.ptc Page 412 1327569 _ Case number 90119473_Yearly revision _ Six, the scope of application for patent _3_ base}_ Cyclopropyl burnt amine; 9 0 3. N-{5_Benzyl Sulfosyl-4,6-dihydropyrrolo[3,4-c]carbazole-3-yl}-isobutylenamine; 904.1{5-mercaptophosphoryl-4,6-dihydroanthracene Compared with each [3,4-(:]〇〇 _3_基}_ 戊烧缓缓缓, 905. N-{5-benzylsulfonyl-4,6-dihydrogen ratio And [3,4-(:]pyrazole-3-yl}_benzamide; 906. N-{5-benzyl feldsparin-4,6-dihydrogen ratio 0 and [3,4-c ° ° 0 -3 -yl}-mercaptopyridamine; 9 07. N-{5 -benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazole 3-yl}_---------------- 5- 5- 5- sulfonyl-4,6-dihydropyrrolo[3,4-indolepyrazol-3-yl}-isonicosine Amine; 90 9. N-{ 5-benzylsulfonyl-4,6-dihydroindolo[3,4-c]pyrazol-3-yl}-3-methyl-2-furan Amine; 910. ^{5-Benzylsulfonyl-4,6-dihydropyridin-1 each [3,4-(:]11 is more than stilbene-3-ylindole-porphin-rebel; 911. N-{5-benzyllithoic acid- 4,6-dihydrogen ratio slightly [3,4-c] 0 than sal -3 -yl} - 11 thiophene _ 3 - slow-acting amine; 912. N-{5-benzylsulfonyl-4,6-dihydroindolo[3,4-(:]carbazol-3-yl}-o-toluidine 913. N-{5-mercaptosulfonic acid-4,6-dihydrogen ratio 0 and [3,4-c] ° ratio -33-yl}-m-phenylphthalamide; 914. N-{5-r sulfamoyl-4,6-dihydropyrrolo[3,4-c]pyrazole

90119473(替換）-2.ptc 第413頁 1327569 ί__案號90119473_年月曰修正_ 六、申請專利範圍 -3 -基}-對-甲苯曱醯胺； 915.“-{5-苄基石黃醯基-4，6-二氫0比°各并[3,4-(：]'1比〇坐 -3_基}_苯基乙酿胺； 916.1'1-{5-苄基石黃蕴基-4，6-二氫0比11各并[3,4-〇]11比0坐 • - 3 _基} _水楊驢胺； 917. Ν-{5-辛基石黃酿基- 4,6 -二氫0比咯并[3,4-c] 0比0坐 -3-基}_2-氟苯甲酿胺； 918. N-{5 -苄基石黃醯基- 4,6 -二氫0比咯并[3,4-c] D比0坐 -3-基}-3-氟苯甲醯胺；鲁919.1^-{5-辛基石黃酸基-4,6-二氫0比咯并[3,4-<:]0比唑 -3 -基}·-4-氟苯曱酿胺， 920. Ν-{5-苄基磺醯基-4,6-二氫°比咯并[3,4-〇]吡唑 -3-基}-噻吩-2-乙醯胺； 921. Ν-{5-苄基磺醯基-4, 6 -二氫咄咯并[3, 4-c]咄唑 -3 -基}- °塞吩-3-乙醯胺； 92 2. Ν-{ 5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]咄唑 _3_基}_苯基丙快癒胺， 923.1^-{5-苄基石黃酸基-4,6-二氫0比咯并[3,4-〇]11比0坐 _基}_3_氛基苯曱酿胺， •9 2 4. Ν-{ 5-苄基磺醯基-4, 6 -二氫咄咯并[3, 4-c]吡唑 -3-基}_4-氰基苯曱酷胺， 9 2 5. Ν-{5-笮基磺醯基-4, 6 -二氫0比咯并[3, 4-c]吡唑 -3-基}_反_桂皮酿胺； 926.^{5-芊基磺醯基-4,6-二氫咄咯并[3,4-<:]吡唑90119473 (replacement)-2.ptc Page 413 1327569 ί__ Case No. 90119473_Yearly revision _ 6. Patent application scope -3 - base}-p-toluidine; 915. "-{5-benzyl stone Astragalus-4,6-dihydrogen 0 ratio °[3,4-(:]'1 is more than 〇--3_}}phenyl phenylamine; 916.1'1-{5-benzyl feldspar-4 , 6-dihydrogen 0 to 11 each [3,4-〇]11 to 0 sitting • - 3 _ group} _salylamine; 917. Ν-{5-octyl sylvestre base - 4,6 - Dihydrogen 0 is a ratio of [3,4-c] 0 to 0--3-yl}_2-fluorobenzamide; 918. N-{5-benzylglycosyl- 4,6-dihydro- 0-pyro And [3,4-c] D is 0--3-yl}-3-fluorobenzamide; Lu 99.1--{5-octyllithinyl-4,6-dihydro- 0-pyrrolo[ 3,4-<:]0-pyrazol-3-yl}-4-fluorobenzoin, 920. Ν-{5-benzylsulfonyl-4,6-dihydrogen ratio 3,4-〇]pyrazol-3-yl}-thiophene-2-acetamide; 921. Ν-{5-benzylsulfonyl-4,6-dihydroindole[3,4-c ]carbazole-3-yl}- °cephen-3-acetamide; 92 2. Ν-{ 5-benzylsulfonyl-4,6-dihydropyrrolo[3,4-c]carbazole _3_基}_Phenylpropanoid, 923.1^-{5-benzyllithoic acid-4,6-dihydro- 0-pyrano[3,4- ] 11 to 0 sitting _ base}_3_ aryl benzoquinone, • 9 2 4. Ν-{ 5-benzylsulfonyl-4,6-dihydroindolo[3,4-c]pyridinium Zyrid-3-yl}_4-cyanobenzoquinone, 9 2 5. Ν-{5-mercaptosulfonyl-4,6-dihydro- 0-pyrrolo[3,4-c]pyrazole- 3-based}_reverse-cinnamin; 926.^{5-mercaptosulfonyl-4,6-dihydroindolo[3,4-<:]pyrazole

卯 119473(替換）-2.ptc 第414頁 1327569 案號 90119473 年月曰修正六、申請專利範圍 -3 _基}-順-桂皮酿胺； 927. N-{5 -芊基石黃酸基- 4,6 -二氫°比11 各并[3,4-c] D比0坐 -3_基}-3_(3_ σ比咬基）丙稀酿·胺， 928. Ν-{5 -苄基石黃醯基-4, 6 -二氫咄°各并[3,4-c] D比0坐 _3_基}_3_(4_ D比咬基）丙稀酸·胺> 929. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}_2 -苯基丙蕴胺， 930. N-{5 -苄基石黃醯基- 4,6 -二氫D比p各并[3,4-c] °比°坐 -3 -基}-間-甲苯基乙醯胺； 931.1{5-苄基磺醯基-4,6-二氫吡11各并[3,4-(：]'1比。坐 -3-基}-對-曱苯基乙醯胺； 932. N-{5 -苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}_鄰-菌香酿胺； 933. N-{5-苄基石夤醯基- 4,6 -二氫°比°各并[3,4-c] D比唾 -3 -基}-3-甲氧苯曱醯胺； 934.1{5-苄基石黃醯基-4,6-二氫吡略并[3,4-(：]11比°坐 -3 -基}-對-菌香酷胺， 935.1{5-芊基石黃醯基-4,6-二氫吡11各并[3,4-(：]11比'1坐 _3-基}_苯氧乙酷胺； 936. N-{5-苄基磺醯基-4,6-二氫°比咯并[3,4-(：]吡唑 -3 -基}_2_氣苯基乙酿胺， 937.1{5-苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 _3_基}_3_氣苯基乙酿胺， 938. N-{5_苄基磺醯基-4,6-二氫°比咯并[3,4-〇]吡唑卯119473 (replacement)-2.ptc page 414 1327569 case number 90119473 year 曰六、、、、、、、、、、、、、、、、、、、、、、、、、、、、、、、、、、、 4,6-dihydrogen ratio 11 each [3,4-c] D is 0-by-3_yl}-3_(3_ σ ratio biting) propylene, amine, 928. Ν-{5-benzyl The basestone xanthine-4,6-dihydroindole °[3,4-c] D is 0 ≤3_base}_3_(4_D than bite base) acrylic acid amine 929. N-{5 -benzylsulfonyl-4,6-dihydropyrrolo[3,4-(:]pyrazole-3-yl}_2-phenylpropanylamine, 930. N-{5-benzyl fluorenyl- 4 ,6-dihydrogen D ratio p and [3,4-c] ° ratio -3 -yl}-m-tolylacetamide; 931.1{5-benzylsulfonyl-4,6-di Hydropyridyl 11 and [3,4-(:]'1 ratio. Sodium-3-yl}-p-indole phenylacetamide; 932. N-{5-benzylsulfonyl-4,6- Dihydropyrrolo[3,4-(:]pyrazole-3-yl}-o-bacteria; 933. N-{5-benzyl fluorenyl- 4,6-dihydrogen ratio And [3,4-c] D is more than spani-3-yl}-3-methoxybenzamide; 934.1{5-benzyl sulphate-4,6-dihydropyrho[3,4-(: ]11°° sitting -3 - base}-pair-bacteria fragrant amine, 935.1{5-芊基石黄醯-4,6-dihydropyryl 11 each [3,4-(:]11 to '1 sitting _3-yl}-phenoxyethylamine; 936. N-{5-benzylsulfonyl-4 ,6-dihydro-pyrano[3,4-(:]pyrazol-3-yl}_2-phenylphenylethylamine, 937.1{5-benzylsulfonyl-4,6-dihydropyrrole And [3,4-〇]pyrazole_3_yl}_3_gas phenylethylamine, 938. N-{5-benzylsulfonyl-4,6-dihydrogen ratio [3, 4-〇]pyrazole

90119473(替換）-2.ptc 第415頁 1327569 案號 90119473 A_A. 修正六、申請專利範圍 -3-基}-4-氟苯基乙醯胺； 939. N-{5-苄基磺醯基-4,6-二氫°比咯并[3,4-〇]°比唑 -3_基}-3-(2_°塞吩基）丙稀酿胺，氫0比咯并[3，4 - c ] n比峻 94 0. N-{5-苄基磺醯基-4, 6- -3 -基卜3-(3 -噻吩基）丙烯醯胺 941· N-{5 -笮基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基卜3-(2-噻吩基）丙醯胺； 942. N-{5 -苄基磺醯基-4,6-二氫吡咯并[3,4-〇]吡唑 -3-基}-2-氯苯甲醯胺；鲁943. N-{ 5-辛基磺醯基-4, 6-二氫吡咯并[3, 4-c]吡唑 -3-基卜3-氣苯曱醯胺； 944. N-{5-辛基石黃醯基- 4,6 -二氫π比咯并[3,4-c] °比〇坐 -3 -基} - 4 -氣苯甲醯胺； 945. N-{5-苄基磺醯基-4,6 -二氫°比咯并[3,4-c]0比唑 -3 -基} - ；1 -哌啶丙醯胺； 946. N-{5 -苄基石黃酿基-4，6 -二氫吼口各并[3, 4-c] °比〇坐 -3-基}-2-乙醯基苯甲醯胺； 947. N-{5-苄基石黃醯基- 4,6 -二氫σ比咯并[3,4-c]吡0坐基}_4_乙酿基苯曱酿胺，氫0比咯并[3，4 - c ] 0比。坐 948. N-{5_窄基石黃酿基_4，6 -二 -3-基}-1-萘甲醯胺； 94 9. N-{5-苄基磺醯基-4, 6 -二氫吡咯并[3, 4-c]吡唑 -3-基}-2 -萘甲醯胺； 950. N-{5 -苄基石黃醯基-4, 6 -二氫11比咯并[3, 4-c]吡唑90119473 (replacement)-2.ptc Page 415 1327569 Case No. 90119473 A_A. Amendment VI, Patent Application -3-Base}-4-fluorophenylacetamide; 939. N-{5-Benzylsulfonyl -4,6-dihydrogen ratio of [3,4-〇]°bazol-3_yl}-3-(2_°secenyl) acrylamide, hydrogen 0 ratio [3,4 - c ] n is more than 94. N-{5-benzylsulfonyl-4,6-1,3-butyl-3-(3-thienyl)propenylamine 941· N-{5-mercaptosulfonate Mercapto-4,6-dihydropyrrolo[3,4-(:]pyrazol-3-ylbu-3-(2-thienyl)propanamine; 942. N-{5-benzylsulfonyl -4,6-dihydropyrrolo[3,4-indolylpyrazol-3-yl}-2-chlorobenzamide; Lu 943. N-{ 5-octylsulfonyl-4, 6- Dihydropyrrolo[3,4-c]pyrazole-3-ylbu-3-benzophenone; 944. N-{5-octyl sulphate- 4,6-dihydropyrpyrrolo[3, 4-c] ° 〇 -3 -3 - yl} - 4 - benzophenone; 945. N-{5-benzylsulfonyl-4,6-dihydro-pyrano[3,4- c] 0-pyrazol-3-yl}-; 1-piperidine-propionamine; 946. N-{5-benzylphosphoryl-4,6-dihydropurine each [3, 4-c] ° 〇-3-yl}-2-ethylmercaptobenzamide; 947. N-{5-benzyl fluorenyl- 4 , 6-dihydro-sigma-pyrolo[3,4-c]pyridinyl}_4_ethyl-branched benzoylamine, hydrogen 0 to s-[3,4 - c] 0 ratio. Sitting 948. N -{5_Narrow bedrock yellow base_4,6-di-3-yl}-1-naphthylcarboxamide; 94 9. N-{5-benzylsulfonyl-4,6-dihydropyrrole [3, 4-c]pyrazol-3-yl}-2-naphthylcarbenamide; 950. N-{5-benzyl sulfonyl-4,6-dihydro-11-pyrano[3,4-c] Pyrazole

90119473(替換）-2.ptc 第416頁 1327569 案號 90119473 修正六、申請專利範圍 -3-基}-3-苯甲醯基丙醯胺； 951.1{5-芊基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_基}_4_乙驢胺基苯曱酿胺； 952. N-{5-苄基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 -3-基}-2,5 -二甲氧苯曱醯胺； 953. N-{5 -芊基磺醯基-4,6-二氫°比咯并[3,4-〇]°比唑 -3_基}-2,6_二甲氧苯曱醯胺； 954.1^-{5-苄基石黃醯基-4,6-二氫0比11各并[3,4-(：]11比〇坐 -3-基}-3,4 -二甲氧苯曱醯胺； 955. N-{5 -芊基磺醯基-4,6-二氫吡咯并[3,4-(：]吡唑 _3_ 基} - 3，5 甲氧苯曱醯胺； 95 6. N-{ 5 -苄基磺醯基-4, 6 -二氫》比咯并[3, -3-基}-3-(2 -噻吩曱醯基）-丙醯胺； 957. N-{5 -苄基磺醯基-4, 6 -二氫吡咯并[3, _3-基}-2_奈基乙醋胺， 958_1^-{5-苄基磺醯基-4,6-二氫°比咯并[3, 4-c ] 0比0坐 4 - c ] 11 比口坐 4 - c ]吼口坐 _3-基}-1_秦基乙酿胺； 959. N_{5 -芊基石黃酷基- 4,6 -二氫π比°各并[3,4-c] °比。坐 _3_基}_4_苯基苯曱酿胺； N-{5-乙臨基-4, 6 -二氫吼σ各并[3, 4-c] °比。坐-3-_(4_氣辛基）脈； 1^-{5-芊基-4,6-二氫°比咯并[3,4-〇]吡 96 0. 基}，Ν’ 961.1^-{5-芊基-4,6-二氫°比咯并|_3,4-〇」吡唑-3-基}，Ν’ -(4-氣芊基）脲； 962. Ν-{5 -苯基-4,6-二氫吡咯并[3,4-〇]吡唑-3-90119473 (replacement)-2.ptc Page 416 1327569 Case No. 90119473 Amendment VI, Patent Application -3-yl}-3-Benzylmercaptopropylamine; 951.1{5-decylsulfonyl-4,6 - dihydropyrrolo[3,4-(:]pyrazole-3-yl}_4_acetamidobenzoylamine; 952. N-{5-benzylsulfonyl-4,6-dihydro Pyrrolo[3,4-(:]pyrazol-3-yl}-2,5-dimethoxybenzamide; 953. N-{5-mercaptosulfonyl-4,6-dihydrogen咯并 [3,4-〇]°Bizozol-3_yl}-2,6-dimethoxybenzoquinone; 954.1^-{5-benzyl sulphate-4,6-dihydro 0:11 Each [3,4-(:]11 is more than -3-yl}-3,4-dimethoxybenzamine; 955. N-{5-mercaptosulfonyl-4,6-di Hydropyrrolo[3,4-(:]pyrazole-3-yl}-3,5-methoxybenzamine; 95 6. N-{5-benzylsulfonyl-4,6-dihydro" ratio [3,-3-yl}-3-(2-thiophenanthryl)-propanamine; 957. N-{5-benzylsulfonyl-4,6-dihydropyrrolo[3, _3-yl}-2_nylacetamide, 958_1^-{5-benzylsulfonyl-4,6-dihydrogen ratio [3, 4-c] 0 to 0 sitting 4 - c ] 11 than the mouth to sit 4 - c ] 吼口_3 base}-1_Qinyl ethylamine; 959. N_{5 - 芊基石黄酷基 - 4,6 - dihydro π ratio ° and [3,4-c] ° ratio. sit _3_ ki}_4_phenyl benzoquinone amine; N-{5-ethionyl-4,6-dihydroanthracene σ Each [3, 4-c] ° ratio. Sitting -3-_(4_gas octyl) vein; 1^-{5-mercapto-4,6-dihydrogen ratio [3,4- 〇]pyr 96 0. }}, Ν' 961.1^-{5-mercapto-4,6-dihydrogen ratio |_3,4-〇"pyrazol-3-yl},Ν' -(4 - gas sulfhydryl) urea; 962. Ν-{5-phenyl-4,6-dihydropyrrolo[3,4-indole]pyrazole-3-

901 19473(替換）-2.ptc 第417頁 1327569 ；_案號90Π9473_年月曰修正_ 六、申請專利範圍基},『_(4_氣竿基）脈； 963. N_{5 -胺基幾基-4, 6 -二氫°比咯并[3，4-c] °比°坐-3-基},1^’-（4-氯¥基）脈； 964. N-{5-乙基胺基獄基-4,6-二氫。比11 各并[3,4-c] °比唾 --3_S}，N’_(4_ 氯辛基）服； . 965· N-{5-曱烧石黃酿基- 4,6 -二氫°比0各并[3,4-c] 0比。坐 _3_基}，『_(4_氯罕基）脈； 966. N-{5-苄基績酿基-4,6 -二氫π比σ各并[3，4-c] 0比座 -3-基}，1^’_(4_氯^:基）脈，鲁9 67_1^-{5-曱苯磺醯基-4,6-二氫。比咯并[3,4-。]吡唑 -3-基}，Ν’ -(4-氯辛基）脲； 96 8. Ν_{5 -苄基胺基羰基-4, 6 -二氫吡咯并[3, 4-c]吡唑 - 3_基},1^’_(.4-氯辛基）服； 969. Ν-{5 -苯基胺基羰基-4,6-二氫吡咯并[3,4-〇]吡唑 -3 -基},『_(4_氯辛基）服； 970. N-(5-(l -萘羰基）-4,5,6,7-四氫吡啶[4,3-〇]吡唑 -3 -基）-3 -苯氧苯曱醯胺； 971. N-(5-(1-萘羰基）-4,5,6, 7 -四氫吡啶[4, 3-c]吡唑 _ -基）_4_第三丁基苯甲酿胺；胃9 7 2. N-(5-(2 -呋喃甲醯基）-4, 5, 6, 7-四氫吡啶[4, 3-c] 吼唑-3-基）-(4-苯基）苯基乙醯胺； 973. N-(5-(2 -呋喃曱醯基）-4, 5, 6, 7-四氫咄啶[4, 3-c] 吡唑-3 -基）-2-(2 -萘基）丙醯胺； 974. N-(5-(2 -呋喃曱醯基）-4,5,6,7-四氫咄啶[4,3-c]901 19473 (replacement)-2.ptc page 417 1327569; _ case number 90Π9473_年月曰曰 _6, the scope of the patent application scope}, __(4_气竿基)脉; 963. N_{5-amine The benzyl group-4,6-dihydrogen ratio is [3,4-c] ° ratio -3-yl}, 1^'-(4-chloro¥yl) vein; 964. N-{5 - Ethylamine-based Pegyl-4,6-dihydrogen. More than 11 [3,4-c] ° than saliva -3_S}, N'_(4_ chlorooctyl) served; . 965· N-{5-曱烧石黄粉基 - 4,6 - 二The hydrogen ratio is 0 and each is [3,4-c] 0 ratio. Sit _3_base}, __(4_ chlorogenic) vein; 966. N-{5-benzylic bristol-4,6-dihydro π ratio σ[3,4-c] 0 More than -3-yl}, 1^'_(4_chloro^:yl) vein, Lu 9 67_1^-{5-nonylbenzenesulfonyl-4,6-dihydro. More than [3,4-. Pyrazol-3-yl}, Ν'-(4-chlorooctyl)urea; 96 8. Ν_{5-benzylaminocarbonyl-4,6-dihydropyrrolo[3,4-c]pyridyl Oxazol-3_yl}, 1^'_(.4-chlorooctyl); 969. Ν-{5-phenylaminocarbonyl-4,6-dihydropyrrolo[3,4-indenyl]pyridinium Zylo-3 -yl}, "_(4-chlorooctyl); 970. N-(5-(l-naphthalenecarbonyl)-4,5,6,7-tetrahydropyridine [4,3-〇] Pyrazol-3-yl)-3-phenoxybenzamine; 971. N-(5-(1-Naphthalenecarbonyl)-4,5,6,7-tetrahydropyridine[4,3-c]pyridyl Azole _-yl)_4_t-butylbenzamide; stomach 9 7 2. N-(5-(2-furanylmethyl)-4, 5, 6, 7-tetrahydropyridine [4, 3 -c] oxazol-3-yl)-(4-phenyl)phenylacetamide; 973. N-(5-(2-furanyl)-4, 5, 6, 7-tetrahydroindole Acridine [4, 3-c]pyrazol-3-yl)-2-(2-naphthyl)propanamine; 974. N-(5-(2-furanyl)-4,5,6, 7-tetrahydroacridine [4,3-c]

90119473(替換）-2.ptc 第418頁 1327569 案號90119473 年月日修正六、申請專利範圍吼唑-3-基）-2-(3-氟-4-苯基-苯基）丙醯胺； 975. N-(5-(2-曱氧辛基）-4,5,6,7-四氫吡啶[4,3-c]吡 α坐-3 -基）-（2_秦）乙酿胺； 976. Ν-(5-(2-曱氧窄基）-4,5,6,7_ 四氫咄啶[4,3-c] 口比唑-3 -基）-[4-(1_吡咯啶-2 -酮）]苯基乙醯胺； 977. N-(5-(2_ 甲氧苯基）-4,5,6,7-四氫吼啶[4,3-c] 口比唑-3-基）-(4-苯基）苯基乙醯胺； 978. N-(5-(4-氟-苯曱醯基）-4,5,6,7-四氫吼啶 [4，3-c] 0比。坐_3_基）-4-氟苯甲酿胺； 979. N-(5-乙臨基-4，5，6，7-四氫-1H- D 比0定[4，3-c] 0 比0坐 -3 -基）_3-氧苯曱臨月安， 980. N-(5-乙醯基-4，5，6，7-四氫 π比咬[4，3-c]吼°坐-3-基）_(2_秦）乙酿胺， 981· Ν-(5-乙臨基-4，5，6，7-四氫0比0定[4，3-c] π比0坐- 3-基）乙醯胺； 982. Ν-(5-乙醯基-4，5, 6, 7-四氫 0比咬[4, 3-c] 0比唾-3-基）苯曱醯胺； 98 3. Ν-(5 -胺基羰基-4, 5, 6, 7 -四氫吡啶[4, 3-c]吡唑 _3_基）_苯基乙酷胺， 984. Ν-(5 -苯甲酸基-4,5，6，7-四氫11比咬[4,3-(：]吼11坐 _3_基）-(4_苯基）苯基乙驢胺， 985.1(5-苯甲醯基-4,5,6,7-四氫0比咬[4,3-。]°比〇坐 -3 -基）-3-氟苯曱醯胺； 986. Ν-(5 -苯甲醯基-4,5,6,7-四氫°比啶[4,3-〇]吡唑90119473 (replacement)-2.ptc Page 418 1327569 Case No. 90119473 Revised on the date of the sixth day, the scope of application for the patent carbazol-3-yl)-2-(3-fluoro-4-phenyl-phenyl)propanamide 975. N-(5-(2-Oxooctyl)-4,5,6,7-tetrahydropyridine [4,3-c]pyridin-3-yl)-(2_秦)B Acrylamine; 976. Ν-(5-(2-oxime-n-yl)-4,5,6,7-tetrahydroacridine [4,3-c] oxazole-3-yl)-[4-( 1_pyrrolidin-2-one)]phenyl acetamide; 977. N-(5-(2-methoxyphenyl)-4,5,6,7-tetrahydroacridine [4,3-c] Oroxazol-3-yl)-(4-phenyl)phenylacetamide; 978. N-(5-(4-fluoro-phenylhydrazino)-4,5,6,7-tetrahydroanthracene Acridine [4,3-c] 0 ratio. sit _3_yl)-4-fluorobenzamide; 979. N-(5-ethionyl-4,5,6,7-tetrahydro-1H- D is 0 to [4,3-c] 0 is 0 to 0 -3 -yl)_3-oxobenzoquinone, 980. N-(5-ethenyl-4,5,6,7-tetrahydroπ Than [4,3-c]吼° sit-3-yl)_(2_Qin) Ethylamine, 981·Ν-(5-Ethyl-4,5,6,7-tetrahydro 0 ratio 0定[4,3-c] π ratio 0 sit- 3-yl) acetamidine; 982. Ν-(5-ethinyl-4,5, 6, 7-tetrahydro 0 ratio bite [4, 3 -c] 0 than spani-3-yl)benzamide; 98 3. Ν-(5-Aminocarbonyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole-3-yl)-phenylethylamine, 984. Ν-(5-benzoic acid Base-4,5,6,7-tetrahydro 11 ratio bite [4,3-(:]吼11 sitting_3_yl)-(4-phenyl)phenylacetamide, 985.1 (5-benzamide) Mercapto-4,5,6,7-tetrahydro 0 ratio bite [4,3-.] ° than sputum -3 -yl)-3-fluorophenylamine; 986. Ν-(5-benzamide Mercapto-4,5,6,7-tetrahydropyridinium [4,3-indole]pyrazole

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90119473(替換）-2.ptc 第422頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 -3 -基]_(2_奈）乙酸胺， 1023.1[5-異丁酸基-4，5，6，7-四氫°比咬[4，3-<:]'3比〇坐 -3-基]-4-氟苯曱醯胺； 1024. N-[5 -苯基乙醯基-4，5，6，7-四氫D比咬[4，3-c] 口比 α坐_3_基]_3-氟苯甲酿胺； 1025. Ν-[5 -笨基乙醯基-4,5,6,7-四氫吡啶[4,3-〇]口比唑-3-基]-3-甲氧苯曱醯胺； 1026. Ν-[5 -苯基乙醯基-4, 5, 6, 7 -四氫吡啶[4, 3-c]吡 11 坐_3_基]-3 -苯氧苯曱酿胺； 1027. Ν-[5 -苯基乙醯基-4, 5, 6, 7 -四氫吼啶[4, 3-c] 比唑-3-基]-4-氟苯曱醯胺； 1028. Ν-[5 -苯基乙醯基-4,5,6,7-四氫吡啶[4,3-〇]吡唑-3-基]-4-苯氧苯曱醯胺； 1029. Ν-[5 -苯基乙醯基-4,5,6,7-四氫吡啶[4,3-(：]吡唑-3 -基]-4-第三丁基-苯曱醯胺； 1030. Ν-[5 -苯基乙醯基-4,5,6,7-四氫咄啶[4,3-〇]吡。坐_ 3 -基]環丙院缓酸胺， 1031. Ν-{5-(2-σ夫喃甲醯基）-4，5, 6，7-四氫0比咬 [4,3-c]吡唑-3-基}-4-第三丁基-苯曱醯胺； 1032. N-{5-(2 -萘磺醯基）-4,5,6,7-四氫吼啶[4,3-c] 吼唑-3-基}-3-溴苯曱醯胺； 1033. N-{5-(2 -噻吩基）乙醯基-4, 5, 6, 7-四氫吡啶 [4,3-c]吼唑-3-基}-3_曱氧苯曱醯胺； 1034. N-{5-(2-°塞吩基）乙酷基-4，5，6, 7 -四氫吼咬90119473 (replacement)-2.ptc Page 422 1327569 _ Case No. 90119473_Yearly revision _ VI. Patent scope -3 - base]_(2_na)acetic acid amine, 1023.1 [5-isobutyric acid- 4,5,6,7-tetrahydrogen ratio bite [4,3-<:]'3 is more than 〇-3-yl]-4-fluorobenzamide; 1024. N-[5-phenyl Ethyl-4,5,6,7-tetrahydro D is more than [4,3-c] than α, _3_yl]_3-fluorobenzamide; 1025. Ν-[5 - stupid Ethyl 4-,5,6,7-tetrahydropyridine [4,3-indole]-oroxazol-3-yl]-3-methoxybenzoquinone; 1026. Ν-[5-phenyl Mercapto-4,5,6,7-tetrahydropyridine[4,3-c]pyrylene 11 _3_yl]-3-phenoxybenzoquinone; 1027. Ν-[5-phenylethyl hydrazine 4-, 5, 6, 7-tetrahydroacridine [4, 3-c] oxazol-3-yl]-4-fluorophenylguanamine; 1028. Ν-[5-phenylethenyl- 4,5,6,7-tetrahydropyridine [4,3-indolyl]pyrazol-3-yl]-4-phenoxybenzamine; 1029. Ν-[5-phenylethenyl-4, 5,6,7-tetrahydropyridine [4,3-(:]pyrazol-3-yl]-4-t-butyl-benzoguanamine; 1030. Ν-[5-phenylethenyl- 4,5,6,7-tetrahydroacridine [4,3-〇]pyr. Sodium _ 3 -yl] Cyclopropanol, 1031. Ν-{5-(2-σ夫喃甲醯基)-4 5, 6,7-tetrahydro 0 to bite [4,3-c]pyrazol-3-yl}-4-t-butyl-benzoguanamine; 1032. N-{5-(2-naphthalenesulfonate Indenyl)-4,5,6,7-tetrahydroacridine [4,3-c]oxazol-3-yl}-3-bromophenylamine; 1033. N-{5-(2-thiophene Ethyl 4-yl, 4, 5, 6, 7-tetrahydropyridine [4,3-c]oxazol-3-yl}-3_nonoxybenzoquinone; 1034. N-{5-(2 -°Septyl) Ethyl-4,5,6,7-tetrahydrobite

90119473(替換）-2.ptc 第423頁 1327569 _案號90119473_年月曰修正_ 六、申請專利範圍 [4,3-c]吡唑_3-基}-3-苯氧苯甲醯胺； 1035.1{5-(2-噻吩基）乙醯基-4,5,6,7-四氫吡啶 [4,3-c]吡唑-3-基}-4_氟苯甲醯胺； 1036. N-{5-(2-°塞吩基）乙醯基-4, 5, 6, 7-四氫°比咬 -[4,3-c]吡唑-3-基}-4_苯氧苯甲醯胺； .1037. N-{5-(2-°塞吩基）乙醯基-4，5,6,7-四氫°比咬 [4,3-c]吡唑-3-基}-4-第三丁基-苯甲醯胺； 1038.1{5-(2-噻吩基）乙醯基-4,5,6,7-四氫吡啶 [4，3 - c ]吡唑-3 -基}乙醯胺；鲁1 0 39. N-{ 5-(2 -噻吩基）乙醯基-4, 5, 6, 7 -四氫吡啶 [4, 3-c]吡唑-3-基卜環丙烷羧醯胺； 1040. N-{5-(3 -三氟曱基苯）磺醯基-4, 5, 6, 7-四氫吡啶 [4, 3-c]吡唑-3 -基}-3 -溴苯曱醯胺； 1041. N-{ 5-(4-氣苯）磺醯基-4, 5, 6, 7-四氫。比啶 [4, 3-c]吡唑-3 -基}-3 -溴苯曱醯胺； 1042.1{5-(4-氟苯）磺醯基-4,5,6,7-四氫°比啶 [4, 3-c]吡唑-3 -基}-3_溴苯曱醯胺； 1043.1{5-(4-曱氧苯）磺醯基-4,5,6,7-四氫》比啶 3-c]吡唑-3 -基}-3_溴苯曱醯胺； 1044. N_{5_(4_第三丁基苯）石黃酿基-4, 5，6，7_四氮0比咬 [4，3 - c ] ^比。坐_ 3 _基} _ 3 _漠·苯曱酿胺； 1045. N-{5-(4-甲苯磺醯基）-4,5,6,7-四氫吡啶 [4, 3-c]吡唑-3 -基}-3 -溴苯甲醯胺； 1046. N-{5-(喳啉-8 -磺醯基）-4,5,6,7-四氫吡啶90119473 (replacement)-2.ptc Page 423 1327569 _ Case number 90119473_Yearly revision _ 6. Patent scope [4,3-c]pyrazole-3-yl}-3-phenoxybenzamide 1035.1{5-(2-Thienyl)ethenyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazol-3-yl}-4-fluorobenzamide; 1036 N-{5-(2-°Sepyl)ethinyl-4, 5, 6, 7-tetrahydro-bito-[4,3-c]pyrazol-3-yl}-4_benzene Oxybenzamide; .1037. N-{5-(2-°Septyl)ethenyl-4,5,6,7-tetrahydropyranite [4,3-c]pyrazole-3 -yl}-4-t-butyl-benzamide; 1038.1{5-(2-thienyl)ethenyl-4,5,6,7-tetrahydropyridine [4,3 - c ]pyrazole -3 -yl}acetamide; Lu 1 0 39. N-{ 5-(2-Thienyl)ethinyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole- 3-ylcyclopropane carboxamide; 1040. N-{5-(3-trifluorodecylbenzene)sulfonyl-4,5,6,7-tetrahydropyridine[4,3-c]pyrazole -3 -yl}-3-bromobenzoguanamine; 1041. N-{ 5-(4-Gapheno)sulfonyl-4,5,6,7-tetrahydro. Bis[4,3-c]pyrazol-3-yl}-3-bromobenzoguanamine; 1042.1{5-(4-fluorophenyl)sulfonyl-4,5,6,7-tetrahydrogen Bis[4,3-c]pyrazol-3-yl}-3-bromophenylamine; 1043.1{5-(4-indolylbenzene)sulfonyl-4,5,6,7-tetrahydro 》Bistidine 3-c]pyrazole-3-yl}-3_bromobenzoguanamine; 1044. N_{5_(4_Ternbutylbenzene) stellite-4, 5,6,7_ The ratio of tetrazolium 0 to bite [4,3 - c ] ^. Sit _ 3 _ _ _ 3 _ desert · benzoquinone amine; 1045. N-{5-(4-toluenesulfonyl)-4,5,6,7-tetrahydropyridine [4, 3-c] Pyrazol-3-yl}-3-bromobenzamide; 1046. N-{5-(porphyrin-8-sulfonyl)-4,5,6,7-tetrahydropyridine

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1327569 修正案號 90119473 六、申請專利範圍氫σ比σ各并[4，3-c]e比唾-5_基}脲； 1071. N-苄基-Ν’-{3-(2-(6-甲氧-2 -萘）丙醯胺基） -4, 5，6, 7-四氫11比p各并[4, 3-c] p比0坐-5-基}脲； 1072. N-爷基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7 -四氫口比 σ各并[4，3-(：]11比°坐-5-基}脲； 1073. Ν-苄基-Ν’ - {3-(3-甲氧-苯甲醯胺基）-4,5,6, 7-四氫π比11各并[4，3 - c ] °比α坐-5 -基}脲； 1074. Ν-苄基-Ν’-{3-(3-甲基-丁醯胺基）-4, 5, 6, 7 -四氫°比p各并[4, 3 - c ] °比°坐-5 -基}脲； 1075. N-爷基-Ν’ - {3-(4 -苯基）苯乙醯胺基-4, 5, 6, 7 -四氫°比σ各并[4，3 - c ] D比。坐-5 -基}脲； 1076. N- 丁基-N’-{3-(2-(2 -萘）丙醯胺基）-4,5,6,7 -四氫°比D各并[4，3 - c ] D比。坐-5 -基}脲； 1077. Ν-丁基-Ν’-{3-(2-(6-甲氧-2 -萘）丙醯胺基） -4,5,6,7-四氫°比11各并[4,3-(：]°比°坐-5-基}脲； 1078. Ν- 丁基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7 -四氫吼 0各并[4,3-c]D比唾-5-基}脲； 1079. N -丁基-Ν’ - {3-(3-甲氧-丁醯胺基）-4,5,6，7 -四氫吼D各并[4，3 - c ] °比°坐-5 -基}脲； 1080. N- 丁基-Ν’ - {3-[2-(4 -苯基-3-氟-苯基）丙醯胺基]-4，5，6，7 -四氫D比ρ各并[4, 3-c] °比°坐-5-基}脲； 1081. Ν -丁基-Ν’ - {3 -苯甲醯胺基-4, 5, 6, 7-四氫吡咯并 1082. Ν -丁基-Ν’ - {3 -苯乙醯胺基-4, 5,6,7-四氫吡咯并1327569 Amendment No. 90119473 6. The patent application scope hydrogen σ ratio σ and [4,3-c]e than sal-5_yl} urea; 1071. N-benzyl-Ν'-{3-(2-( 6-methoxy-2-naphthalene) propylamino) -4, 5,6, 7-tetrahydro 11 ratio p [4, 3-c] p to 0 sit-5-yl} urea; 1072. N-Yuji-Ν'-{3-(2-naphthalene)acetamido-4, 5, 6, 7-tetrahydrogen port ratio σ each [4,3-(:]11 than ° sitting-5 -yl}urea; 1073. Ν-benzyl-Ν' - {3-(3-methoxy-benzamide)-4,5,6,7-tetrahydropi ratio 11 and [4,3 - c ] ° ratio α--5-yl}urea; 1074. Ν-benzyl-Ν'-{3-(3-methyl-butyrylamino)-4, 5, 6, 7-tetrahydrogen Ratio p[4, 3 - c ] ° ratio ° sit-5-yl}urea; 1075. N-German-Ν' - {3-(4-phenyl)phenethylamine-4, 5 , 6, 7 - tetrahydrogen ratio σ and [4,3 - c ] D ratio. sit-5-yl}urea; 1076. N-butyl-N'-{3-(2-(2-naphthalene) Amidoxime)-4,5,6,7-tetrahydrogen ratio D and [4,3 - c ] D ratio. Sodium-5-yl}urea; 1077. Ν-butyl-Ν'- {3-(2-(6-methoxy-2-naphthalene)propanylamino) -4,5,6,7-tetrahydrogen ratio 11 and [4,3-(:]° ratio ° sitting- 5-based urea; 1078. Ν-butyl-Ν' - {3-(2 - Naphthylamino-5,5,6,7-tetrahydroindole 0 and [4,3-c]D than sal-5-yl}urea; 1079. N-butyl-Ν' - {3 -(3-methoxy-butylammonium)-4,5,6,7-tetrahydroindole D each [4,3 - c ] ° ratio ° sit-5-yl}urea; 1080. N-butyl Ν-Ν' - {3-[2-(4-phenyl-3-fluoro-phenyl)propanylamino]-4,5,6,7-tetrahydro D ratio ρ[4, 3- c] °°°-5-yl}urea; 1081. Ν-butyl-Ν' - {3 -benzamide-4, 5, 6, 7-tetrahydropyrrole 1082. Ν-butyl -Ν' - {3 - phenethylamino-4,5,6,7-tetrahydropyrrole

90119473(替換）-2.ptc 第427頁 1327569 案號 90119473 Λ_η 修正六、申請專利範圍 [4，3 - C ]吡唑-5 -基}脲； 1083. Ν-乙基-Ν’ - (3-(2-(2 -萘）丙醢胺基）-4, 5, 6, 7 -四氫0比B各并[4，3 - c ] °比α坐-5 -基}脲； 1084. Ν-乙基-Ν’-{3-(2-(6-曱氧-2 -萘）丙醯胺基） -4, 5, 6, 7-四氫吼11 各并[4, 3-c] D比0坐-5-基}脲； 1085. N-乙基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7 -四氫吡口各并[‘^-(^。比啥^-基丨脲； 1086. Ν-乙基-Ν’-{3-(3-甲氧-丁醯胺基）-4,5,6,7 -四氫0比D各并[4，3 - c ] D比a坐-5 -基}脲；鲁1 087. N-乙基-N’-{3-(4-氟苯甲醯胺基）-4,5,6,7-四氫 °比σ各并[4，3 - c ] °比α坐-5 -基}脲； 1088. Ν-乙基-Ν’ - {3-(4_苯基）苯乙醯胺基-4, 5, 6, 7-四氫0比11各并[4，3 - c ]吼°坐-5 -基}脲； 1089. Ν-乙基-Ν’ - {3-[2-(4 -苯基-3 -氟-苯基）丙醯胺基]-4，5，6, 7 -四氫吼11 各并[4，3-c] °比°坐-5 -基}脲； 1090. Ν-乙基-Ν’ _{3_苯甲醯胺基-4, 5, 6, 7-四氫咄咯并 [4，3 - c ]吡唑-5 -基}脲； 1091. Ν-乙基-Ν’ - {3 -苯乙醯胺基-4，5, 6, 7-四氫咄咯并 ·，3-c]11 比。坐-5-基}脲；胃1 092. Ν-異丙基-Ν’ - {3-U -曱基引哚-3 -基）乙醯胺基 -4, 5，6，7_四氯吼11各弁[4，3-c] °比°坐_5_基}脈； 1093. Ν-異丙基-Ν’ - (3-(2-(2 -萘）丙醯胺基）-4, 5,6,7-四氫°比D各并[4，3 - c ] °比°坐-5 -基}脲； 1094. N-異丙基-N’-{3-(2-(6-甲氧-2 -萘）丙醯胺基）90119473 (replacement)-2.ptc Page 427 1327569 Case No. 90119473 Λ_η Amendment 6. Patent application [4,3 - C ]pyrazol-5-yl}urea; 1083. Ν-ethyl-Ν' - (3 -(2-(2-naphthyl)propanylamino)-4, 5, 6, 7 -tetrahydro 0 to B each [4,3 - c ] ° ratio α sit-5-yl}urea; 1084. Ν-ethyl-Ν'-{3-(2-(6-oxime-2-naphthalene)propanylamino)-4,5,6,7-tetrahydroindole 11 each [4, 3-c D is 0 to 5 -5} urea; 1085. N-ethyl-Ν' - {3-(2-naphthyl)acetamido-4, 5, 6, 7-tetrahydropyrryl '^-(^. 啥^-carbazide; 1086. Ν-ethyl-Ν'-{3-(3-methoxy-butylamino)-4,5,6,7-tetrahydro 0 Ratio D [4,3 - c ] D is more than a sitting -5 -yl} urea; Lu 1 087. N-ethyl-N'-{3-(4-fluorobenzamide)-4, 5,6,7-tetrahydrogen ratio σ and [4,3 - c ] ° ratio α sit-5-yl}urea; 1088. Ν-ethyl-Ν' - {3-(4_phenyl) Phenylethylamino-4, 5, 6, 7-tetrahydro 0 to 11 each [4,3 - c ]吼° sit-5-yl}urea; 1089. Ν-ethyl-Ν' - {3 -[2-(4-Phenyl-3-fluoro-phenyl)propanylamino]-4,5,6,7-tetrahydroindole 11 each [4,3-c] °°°-5 -base urea; 109 0. Ν-ethyl-Ν' _{3_benzimidamide-4, 5, 6, 7-tetrahydroindolo[4,3 - c]pyrazol-5-yl}urea; 1091. Ν-ethyl-Ν' - {3-phenylethylamino-4,5,6,7-tetrahydroindole,3-c]11 ratio. sit-5-yl}urea; stomach 1 092 . Ν-isopropyl-Ν' - {3-U-mercapto-3-indolyl-3-yl)acetamido-4, 5,6,7-tetrachlorin 11 弁[4,3-c] ° ratio ° sitting _5_ base} vein; 1093. Ν-isopropyl-Ν' - (3-(2-(2-naphthalene) propylamino)-4, 5,6,7-tetrahydro Ratio D is [4,3 - c ] ° ratio ° sitting -5 -yl}urea; 1094. N-isopropyl-N'-{3-(2-(6-methoxy-2-naphthalene)-propyl Amidoxime

90119473(替換）-2.ptc 第428頁 1327569 修正案號 90119473 六、申請專利範圍 -4,5，6，7-四氫'1比11各并[4,3-(：]°比11坐-5-基}脲； 1095. N-異丙基-Ν’ - {3-(2 -苯基-1,3 -噻唑-4 -基）乙醯胺基-4,5，6，7-四氫°比11各并[4,3-(：]11比°坐-5-基}脲； 1096. Ν -異丙基-Ν’-{3-(3-氟苯甲醯胺基）-4,5,6,7-四氫°比α各并[4，3 - c ] °比β坐-5 -基}脲； 1097. Ν-異丙基-Ν’ _{3-(3-甲氧-苯甲醯胺基） -4,5，6，7—四氫0比口各并[4，3-c] 0比0坐一5-基}脈； 1098. Ν -異丙基-Ν’ - {3-(4-氟-苯甲醯胺基）-4,5,6,7-四氫°比α各并[4，3 - c ] °比。坐-5 -基}脲； 1099. Ν-異丙基-Ν’ - {3-(4 -苯基）苯乙醯胺基-4, 5, 6,7-四氫°比π各并[4，3 - c ] °比°坐-5 -基}脲； 1100. Ν-異丙基-Ν’ - {3-(4 -第三丁基-苯甲醯胺基） -4，5，6，7-四氫吼口各并[4，3-c]吼°坐-5-基}脲； 1101. Ν -異丙基-Ν’ _{3-[2-(4_苯基-3_敦_苯基）丙酿胺基]-4,5,6,7-四氫°比11各并[4,3-(：]0比唾-5-基}脲； 1102. Ν-異丙基-Ν’-{3-[4-(1-°比咯啶-2 -酮）]苯乙醯胺基-4，5, 6, 7-四氫σ比σ各并[4，3-c] °比。坐-5-基}脲； 1103. Ν-異丙基-Ν’ - {3-乙醯胺基-4, 5, 6, 7-四氫吡咯并 [4, 3-c]吡唑-5-基}脲； 1104. Ν-異丙基-Ν’ - {3 -苯甲醯胺基-4, 5,6,7-四氫吡咯并[4，3-c]B比唾-5-基}脲； 1105. N-異丙基-Ν’ - {3 -環丙烷羧醯胺基-4, 5, 6, 7-四氫 0比0各并[4，3 - c ] Β比α坐-5 -基}脲； 1106. Ν-異丙基-Ν’ - {3 -苯乙醯胺基-4, 5, 6, 7-四氫吡咯90119473 (replacement)-2.ptc Page 428 1327569 Amendment No. 90119473 VI. Patent scope -4,5,6,7-tetrahydro'1 to 11 and [4,3-(:]° ratio 11 -5-yl}urea; 1095. N-isopropyl-Ν'-{3-(2-phenyl-1,3-thiazol-4-yl)acetamido-4,5,6,7- Tetrahydrogen ratio 11 and [4,3-(:]11 ratio °-5-yl}urea; 1096. Ν-isopropyl-Ν'-{3-(3-fluorobenzamide) -4,5,6,7-tetrahydrogen ratio α and [4,3 - c ] ° ratio β sit-5-yl}urea; 1097. Ν-isopropyl-Ν' _{3-(3 -Methoxy-benzamide amino) -4,5,6,7-tetrahydro 0 is a ratio of [4,3-c] 0 to 0 sitting on a 5-base} pulse; 1098. Ν -isopropyl Ν-Ν' - {3-(4-fluoro-benzamide)-4,5,6,7-tetrahydrogen ratio α and [4,3 - c ] ° ratio. Sit-5-based Urea; 1099. Ν-isopropyl-Ν' - {3-(4-phenyl)phenethylamino-4, 5, 6,7-tetrahydrogen ratio π and [4,3 - c ° °°°-5-yl}urea; 1100. Ν-isopropyl-Ν' - {3-(4 -t-butyl-benzamide) -4,5,6,7-four Hydrogen oxime and [4,3-c]吼° sit-5-yl}urea; 1101. Ν-isopropyl-Ν' _{3-[2-(4_phenyl-3_敦_benzene Base Amino]-4,5,6,7-tetrahydrogen ratio 11 and [4,3-(:]0 than sal-5-yl}urea; 1102. Ν-isopropyl-Ν'-{3 -[4-(1-°Byrrolidin-2-one)]phenethylamino-4,5,6,7-tetrahydroσ ratio σ and [4,3-c] ° ratio. 5-yl}urea; 1103. Ν-isopropyl-Ν' - {3-acetamido-4, 5, 6, 7-tetrahydropyrrolo[4,3-c]pyrazole-5-yl Urea; 1104. Ν-isopropyl-Ν' - {3-phenylbenzylamino-4,5,6,7-tetrahydropyrrolo[4,3-c]B than sal-5-yl} Urea; 1105. N-isopropyl-Ν' - {3-cyclopropanecarboxyguanamine-4, 5, 6, 7-tetrahydro 0 to 0 each [4,3 - c ] Β than α sitting - 5-based urea; 1106. Ν-isopropyl-Ν' - {3-phenylethylamino-4, 5, 6, 7-tetrahydropyrrole

90119473(替換）-2.ptc 第429頁 1327569 修正案號 90119473 六、申請專利範圍并[4，3-〇]°比°坐-5-基}脲； 1107. Ν-苯基-Ν’ - {3-(2 -萘）乙醯胺基-4, 5, 6, 7 -四氫吡口各并[4，3-〇]°比°坐-5-基}脲； 1108. Ν-苯基-Ν’ - {3-(3 -氟苯曱醯胺基）-4, 5, 6, 7-四氫 0比洛并[4，3 - c ] Β比β坐-5 -基}脲； 1109. Ν-苯基-Ν’ - {3-(3-甲基-苯甲醯胺基）-4,5，6,7-四氫π比11各并[4，3 - c ] D比。坐-5 -基}脲； 1110. N-苯基-Ν’ - {3-(3 -苯氧-苯甲醯胺基）-4,5，6, 7-四氫°比11各并[4，3 - c ] °比α坐-5 -基}脲； 11 11. Ν -苯基-Ν’ - {3-(4 -苯氧-苯曱醯胺基）-4,5,6,7-四氫D比11各并[4，3 - c ] °比。坐-5 -基}脲； 1 1 12. N -苯基-Ν’ - {3-(4-第三丁基-苯曱醯胺基） -4，5,6，7-四氫0比咯并[4，3-(：]11比°坐-5-基}脲； 1113. Ν-笨基-Ν’ - {3-乙醯胺基-4, 5, 6, 7-四氫吡咯并 [4，3 - c ] °比 °坐-5 -基}脲； 1114. Ν-苯基-Ν’ - {3 -苯甲醯胺基-4, 5, 6, 7 -四氫吡咯并 [4，3 - c ] °比 σ坐-5 -基}脲； 1115. Ν-苯基-Ν’ - {3-環丙烷羧醯胺基-4, 5, 6, 7-四氫咄赢并[{。-(:^比唾^-基丨脲； 1116. Ν-苯基- Ν’ - {3 -苯乙酿胺基-4，5，6, 7-四氫吼洛并 [4，3 - c ] °比吐-5 -基}脲； 1117. Ν-丙基_Ν’ _{3-(4 -苯基）苯乙酿胺基_4，5, 6，7_四氫0比ρ各并[4，3 - c ] °比。坐-5 -基}脲； 1118. Ν- 丁基-Ν’ - {3-(2-萘）乙醯胺基-6, 6-二曱基90119473 (replacement)-2.ptc Page 429 1327569 Amendment No. 90119473 VI. Scope of application and [4,3-〇]° ratio ° sit--5-urea urea; 1107. Ν-phenyl-Ν' - {3-(2-naphthyl)acetamido-4,5,6,7-tetrahydropyrrole and [4,3-〇]°°°-5-yl}urea; 1108. Ν-Benzene Ν-Ν' - {3-(3-fluorophenylguanidino)-4, 5, 6, 7-tetrahydro 0 piroxi[4,3 - c ] Β than β -5-5-yl}urea 1109. Ν-Phenyl-Ν' - {3-(3-methyl-benzamide)-4,5,6,7-tetrahydroπ ratio 11 and [4,3 - c ] D ratio. Sodium-5-yl}urea; 1110. N-phenyl-indole-{3-(3-phenoxy-benzamide)-4,5,6,7-tetrahydrogen ratio 11 each [ 4,3 - c ] ° ratio α--5-yl}urea; 11 11. Ν-phenyl-Ν' - {3-(4-phenoxy-phenylguanidino)-4,5,6, The 7-tetrahydrogen D ratio is 11 [4,3 - c ] ° ratio. Sodium-5-yl}urea; 1 1 12. N-phenyl-indole-{3-(4-t-butyl-benzoguanamine)-4,5,6,7-tetrahydro- 0 ratio咯[4,3-(:]11°°坐-5-yl}urea; 1113. Ν-stupyl-Ν' - {3-acetamido-4, 5, 6, 7-tetrahydropyrrole And [4,3 - c ] ° ratio ° sit-5-yl}urea; 1114. Ν-phenyl-Ν' - {3 -benzamide-4,5,6,7-tetrahydropyrrole [4,3 - c ] ° ratio σ sits -5 -yl}urea; 1115. Ν-phenyl-Ν' - {3-cyclopropanecarboxyguanidino-4, 5, 6, 7-tetrahydrofurfuryl win And [{.-(:^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^ , 3 - c ] ° than spit-5-yl} urea; 1117. Ν-propyl _Ν' _{3-(4-phenyl)phenylethylamino-4 4,5, 6,7_tetrahydrogen 0 is greater than ρ and [4,3 - c ] ° ratio. Sodium-5-yl}urea; 1118. Ν-butyl-Ν' - {3-(2-naphthalene)acetamido-6, 6- Diterpenoid

90119473(替換）-2.ptc 第430頁 1327569 _案號 90119473_年月日__ 六、申請專利範圍 -4,6-二氮°比11各并[3，4_(3]'3比。坐_1_基}脈； 1119. N- 丁基-Ν’ - {3-(3 -溴）苯甲醯胺基-6, 6 -二甲基 -4,6-二氫°比11各并[3,4-(3]13比。坐-1-基}脲； 1120. Ν- 丁基-Ν’ - {3-(4-氟）苯甲醯胺基-6, 6 -二曱基 -4,6-二氫°比11各并[3,4-(：]°比。坐-1-基}脲； 1121. Ν- 丁基-Ν’ - {3-(4 -第三丁基）苯甲醯胺基-6, 6 -二曱基-4,6-二氫0比17各并[3,4-(：]°比〇圭-1-基}脲； 1122. Ν- 丁基-Ν’ - {3 -環丙烷羧醯胺基-6, 6 -二曱基 -4，6-二氮13比11各并[3，4_(1；]'3比°坐_1-基}脈； 1123. Ν- 丁基-Ν’ - {3 -苯乙醯胺基-6, 6 -二曱基-4, 6 -二氫°比π各并[3，4 - c ] π比β坐-5 -基}脲； 1124. Ν-乙基-Ν’ - {3-(2 -萘）乙醯胺基-6, 6 -二甲基 - 4，6 -二氫吼17各并[3，4 - c ] σ比唾-1 -基}脲； 1125. Ν-乙基-Ν’ - {3-(3 -溴）苯甲醯胺基-6,6 -二曱基 -4,6-二氫°比°各并[3,4-<3]°比。坐-1-基}脲； 1126. Ν-乙基-Ν’ - {3-(4-氟）苯甲醯胺基-6, 6 -二甲基 -4,6 -二氫α比π各并[3,4-(：]°比'1坐-1-基}脲； 1127. Ν-乙基-Ν’ - {3-(4-第三丁基）苯甲醯胺基-6, 6 -二甲基-4,6-二氫0比17各并[3,4-(：]0比。坐-1-基}脲； 1128. Ν-乙基-Ν’ - {3 -環丙烷羧醯胺基-6,6 -二甲基 -4,6-二氫'1比17各并[3,4-(3]'1比唾-1-基}脲； 1129. Ν-乙基-Ν’ _{3_苯乙酸胺基-6，6_二曱基_4，6_二氫°比11 各并[3，4-(：]吼。坐-5-基}脲； 1130. Ν-{5-(2 -噻吩基-乙醯基）-6, 6 -二曱基-4, 6 -二氫90119473 (replacement)-2.ptc Page 430 1327569 _ Case No. 90119473_Year of the month __ Six, the scope of application for patents -4,6-dia nitrogen ° ratio of 11 and [3,4_(3]'3 ratio. Sit _1_基} vein; 1119. N- butyl-Ν' - {3-(3-bromo)benzamide amino-6,6-dimethyl-4,6-dihydrogen ratio 11 And [3,4-(3]13 ratio. sit-1-yl}urea; 1120. Ν-butyl-Ν' - {3-(4-fluoro)benzimidamide-6,6-dioxin Base-4,6-dihydrogen ratio 11 and [3,4-(:]° ratio. sit-1-yl}urea; 1121. Ν-butyl-Ν' - {3-(4 - third Butyl)benzamide amino-6,6-dimercapto-4,6-dihydrogen 0 to 17 each [3,4-(:]° 〇 -1--1-yl}urea; 1122. Ν - Butyl-Ν'-{3-cyclopropanecarboxyguanamine-6,6-dimercapto-4,6-diaza 13 to 11 each [3,4_(1;]'3°° sitting_ 1-基}脉; 1123. Ν-butyl-Ν' - {3-phenylethylamino-6,6-dimercapto-4,6-dihydrogen ratio π[3,4 - c π ratio β sit-5-yl}urea; 1124. Ν-ethyl-Ν' - {3-(2-naphthyl)acetamido-6,6-dimethyl- 4,6-dihydroanthracene 17 each [3,4 - c ] σ is more than sal - 1 -yl} urea; 1125. Ν-ethyl-Ν' - {3-(3 -bromo)benzimidamide-6,6 - Mercapto-4,6-dihydrogen ratio °[3,4-<3]° ratio. sit-1-yl}urea; 1126. Ν-ethyl-Ν' - {3-(4- Fluoro)benzamide-6,6-dimethyl-4,6-dihydro-α is π[3,4-(:]° than '1 sitting-1-yl}urea; 1127. Ν -ethyl-Ν' - {3-(4-t-butyl)benzamide amino-6,6-dimethyl-4,6-dihydrogen 0 to 17 each [3,4-(: 0 ratio. sit-1-yl}urea; 1128. Ν-ethyl-Ν' - {3-cyclopropanecarboxyguanamine-6,6-dimethyl-4,6-dihydro'1 to 17 Each [3,4-(3]'1 than sal-1-yl}urea; 1129. Ν-ethyl-Ν' _{3-phenylacetic acid amine-6,6-didecyl_4,6 _Dihydrogen ratio 11 each [3,4-(:]吼. sit-5-yl}urea; 1130. Ν-{5-(2-thiophenyl-ethenyl)-6,6-di Base-4,6-dihydrogen

90119473(替換）-2.ptc 第431頁 1327569 ._案號90119473_年月曰修正_ 六、申請專利範圍吡啶[3,4_c]吡唑-1-基}-(3-溴）苯甲醯胺； 1131.1\1-{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶[3,4-c]吡唑-3-基}-(2 -萘）乙醯胺； 1132. N-{5-(2 -噻吩基-乙醯基）-6,6 -二甲基-4, 6 -二氫 ' 。比啶[3, 4-c]吼唑-3-基}-(4-氟）苯甲醯胺； 1133. ^{5-(2-噻吩基-乙醯基）-6,6-二曱基-4,6-二氫吡啶[3,4-c]吡唑-3-基}-(4-第三丁基）苯甲醯胺； 1134.1^-{5-(2-噻吩基-乙醯基）-6,6-二甲基-4,6-二氫 °比咬[3, 4 - c ] °比。坐-3 -基}環丙院綾酿胺；鲁1135.1{5-(2-噻吩基-乙醯基）-6,6-二甲基-4,6-二氫吡啶[3, 4-c]吡唑-3-基}苯乙醯胺； 1136. N-{5-(4- 苯甲酿基）-6，6-二甲基_4，6 -二氫吡啶[3, 4-c]吡唑-1-基}-(3-溴）苯甲醯胺； 1137.11-{5-(4-氟苯甲醯基）-6,6-二曱基-4,6-二氫吡啶[3,4-c]吡唑-1-基}-(4-氟）苯曱醯胺； 1138. N-{5-(4-氟苯甲驢基）-6，6 -二曱基-4，6_ 二氛吡啶[3,4-c]°比唑-3-基}-(2_萘）乙醯胺； 1139. N-{5-(4-氟笨甲醯基）-6,6 -二甲基-4,6 -二氫 Pli ^啶[3,4-c]°比唑-3-基}-(4_第三丁基）苯甲醯胺；胃1140.^{5-(4-氟苯甲醯基）-6,6-二甲基-4,6-二氫吡啶[3，4 - c ]吡唑-3 -基}環丙烷羧醯胺； 1141.[{5-(4-氟苯曱醯基）-6,6-二曱基-4,6-二氫 0比啶[3，4 - c ]吡唑-3 -基}苯乙醯胺； 1142.1{5-乙醯基-6,6-二曱基-4,6-二氫吼啶[3,4-(：]90119473 (replacement)-2.ptc Page 431 1327569 ._Case No. 90119473_Yearly revision _ VI. Patent pending pyridine [3,4_c]pyrazol-1-yl}-(3-bromo)benzamide Amine; 1131.1\1-{5-(2-thienyl-ethenyl)-6,6-diamidino-4,6-dihydropyridine [3,4-c]pyrazol-3-yl}- (2-naphthyl)acetamide; 1132. N-{5-(2-thiophenyl-ethenyl)-6,6-dimethyl-4,6-dihydro'. Bis[3,4-c]oxazol-3-yl}-(4-fluoro)benzamide; 1133. ^{5-(2-Thienyl-ethenyl)-6,6-diindole 4-,6-dihydropyridine [3,4-c]pyrazol-3-yl}-(4-t-butyl)benzamide; 1134.1^-{5-(2-thienyl-B Mercapto)-6,6-dimethyl-4,6-dihydrogen ratio bite [3, 4 - c] ° ratio. Sitting on -3 -yl} Cyclopropylamine stimulating amine; Lu 1135.1{5-(2-thienyl-ethenyl)-6,6-dimethyl-4,6-dihydropyridine [3, 4-c Pyrazol-3-yl}phenethylamine; 1136. N-{5-(4-Benzene)-6,6-dimethyl-4,6-dihydropyridine [3, 4-c Pyrazol-1-yl}-(3-bromo)benzamide; 1137.11-{5-(4-fluorobenzhydryl)-6,6-diamidino-4,6-dihydropyridine [ 3,4-c]pyrazol-1-yl}-(4-fluoro)benzoguanamine; 1138. N-{5-(4-fluorobenzhydryl)-6,6-dimercapto-4 , 6_ diacetyl pyridine [3,4-c]°boxazol-3-yl}-(2-naphthyl)acetamide; 1139. N-{5-(4-fluorobenzamide)-6,6 - dimethyl-4,6-dihydro Pli^pyridine [3,4-c]°bazol-3-yl}-(4_t-butyl)benzamide; stomach 1140.^{5- (4-fluorobenzhydryl)-6,6-dimethyl-4,6-dihydropyridine [3,4-c]pyrazol-3-yl}cyclopropanecarboxamide; 1141.[{5 -(4-fluorophenylindenyl)-6,6-dimercapto-4,6-dihydrooxinium [3,4 - c ]pyrazole-3-yl}phenethylamine; 1142.1{5 -Ethyl-6,6-dimercapto-4,6-dihydroacridine [3,4-(:]

901 19473(替換）-2.ptc 第432頁 1327569 案號 90119473 _η 修正六、申請專利範圍吡唑-3-基}-(2-萘）乙醯胺；氫D比咬[3，4 - c ] 氫π比咬[3，4 - c ] 氫0比咬[3，4 - c ] 1143. Ν-{5-乙醯基-6 ,6 -二甲基-4,6-吡唑-1 -基} - ( 3 -溴）苯甲醯胺； 1144. Ν-{5-乙醢基-6, 6 -二曱基-4, 6-吡唑-3 -基}-(4-氟）苯曱醯胺； 1145. Ν-{5-乙醯基-6,6 -二甲基-4,6- 。比唑-3-基}-(4_第三丁基）苯甲醯胺； 1146· Ν-{5-乙醯基-6,6-二曱基-4,6-二氫吡啶[3,4-〇] 吡唑-3 -基丨環丙烷羧醯胺； 1147. Ν-{5-乙醯基-6,6-二甲基_4,6-二氫吡啶[3,4-〇] 吡唑-3 -基}苯乙醯胺； 1148. Ν-{5 -苯乙醯基-6, 6 -二甲基-4, 6 -二氫咄啶 [3,4-c]°比唑-3 -基卜（2 -萘）乙醯胺； 1149. N-{5 -苯乙醯基-6, 6 -二甲基-4, 6 -二氫吡啶 [3,4-c]吡唑-1-基}-(3-溴）苯甲醯胺； 1150. N-{5 -苯乙醯基-6, 6 -二甲基-4, 6 -二氫吡啶 [3，4-c] 0比0坐-3-基}-(4-氟）苯曱酿胺； 1151. N-{5 -苯乙醯基-6, 6 -二甲基-4, 6 -二氫吼啶 [3,4-c]°比唑-3-基}-(4-第三丁基）苯甲醯胺； 1152. N-{5 -苯乙醯基-6, 6 -二曱基-4, 6 -二氫吡啶 [3, 4-c]吡唑-3-基}環丙烷羧醯胺； 1153. N-異丙基-Ν’ - {3-(4-第三丁基-苯曱醯胺基） -4，5，6，7-四氫°比°定[3,4-(：]°比〇坐-6-基}脲； 1154. Ν-{6-(2-°塞吩基）乙醯基-4, 5, 6，7-四氫吡啶901 19473 (replacement)-2.ptc Page 432 1327569 Case No. 90119473 _η Amendment 6. Patent application range pyrazol-3-yl}-(2-naphthalene)acetamide; hydrogen D ratio bite [3,4 - c Hydrogen π ratio bite [3,4 - c ] hydrogen 0 to bite [3,4 - c ] 1143. Ν-{5-ethenyl-6,6-dimethyl-4,6-pyrazole-1 -yl}-(3-bromo)benzamide; 1144. Ν-{5-ethenyl-6,6-dimercapto-4,6-pyrazole-3-yl}-(4-fluoro) Phenylamine; 1145. Ν-{5-Ethyl-6,6-dimethyl-4,6-. Bisazo-3-yl}-(4_t-butyl)benzamide; 1146·Ν-{5-acetamido-6,6-dimercapto-4,6-dihydropyridine [3, 4-〇]pyrazol-3-ylindole cyclopropanecarboxamide; 1147. Ν-{5-acetamido-6,6-dimethyl-4,6-dihydropyridine [3,4-〇] Pyrazole-3-yl}phenethylamine; 1148. Ν-{5-phenethyl fluorenyl-6,6-dimethyl-4,6-dihydroacridine [3,4-c]° azole -3 - kib (2-naphthyl) acetamidine; 1149. N-{5-phenethyl fluorenyl-6,6-dimethyl-4,6-dihydropyridine [3,4-c]pyrazole -1-yl}-(3-bromo)benzamide; 1150. N-{5-phenethylamino-6,6-dimethyl-4,6-dihydropyridine [3,4-c] 0 to 0 -3-yl}-(4-fluoro)benzoquinone; 1151. N-{5-phenethyl fluorenyl-6,6-dimethyl-4,6-dihydroacridine [3 , 4-c]°bazol-3-yl}-(4-t-butyl)benzamide; 1152. N-{5-phenethylamino-6,6-dimercapto-4, 6 -dihydropyridine [3,4-c]pyrazol-3-yl}cyclopropanecarboxamide; 1153. N-isopropyl-Ν' - {3-(4-t-butyl-benzoguanamine -4,5,6,7-tetrahydrogen ratio ° [3,4-(:] ° than 〇-6-yl} urea; 1154. Ν-{6-(2-° thiophene Ethyl 4-, 5, 6, 7-tetrahydropyridine

! 90119473(替換）-2.ptc 第433頁 1327569 _案號 90119473_年月日_魅_ 六、申請專利範圍 [3，4-c] °比。坐-3-基}-4-第三丁基-苯曱醯胺； 1155. N-{6-乙酷基-4，5，6，7-四氫0比唆[3，4_c] 0比。坐- 3- 基}_4_第三丁基-苯曱酿胺； 1156.1^-{6-曱烷磺醯基-4,5,6,7-四氫咄啶[3,4-(：] • 吡唑-3-基}-4-第三丁基-苯甲醯胺； , 1157. N-乙基-Ν’ -{3-(4-第三丁基-苯曱醯胺基） -4，5，6, 7 -四氫°比唆[3,4-c] °比。坐-6-基}脲； 1158.^{6-(3-曱基）丁醯基-4,5,6,7-四氫吡啶 [3,4-c]吡唑-3-基}-4-第三丁基-苯甲醯胺；癱1 1 5 9. N-{ 6-(2 -呋喃甲醯基）-4, 5, 6, 7-四氫吡啶 [3,4-c]吡哇_3-基}-4-第三丁基-苯甲醯胺； 1160. N~*{6 -苯乙醯基-4，5，6，7-四氫°比。定[3，4-c] π比唾 -3-基}-4-第三丁基-苯甲醯胺； 1161. Ν-{6 -苯基磺醯基-4,5,6,7-四氫咄啶[3,4-〇]吡唑-3 -基}-4-第三丁基-笨甲醯胺； 1162. Ν-{6-(喳啉-8 -磺醯基）-4,5,6,7_四氫吡啶 [3,4-c]吡唑-3-基}-4-第三丁基-苯甲醯胺； +:1163. N-丨5 -異戊基-4, 6 -二氫吡咯并[3, 4-c]咄唑-3--4-第三丁基-苯曱醯胺； 1164. N_{5 -苯乙基_4，6 -二氫吼11 各并[3，4-c] π 比 σ坐 _3_ 基}-4-第三丁基-苯曱醯胺； 1165. N-[ 5-(2 -噻吩-2 -基乙基）-4, 6 -二氫吡咯并 [3,4-c]吡唑-3-基]-4-第三丁基-苯甲醯胺； 1166. Ν,Ν -二甲基_N’-{3**(2 -萘-2 -基-丙酿胺基）-4，6-90119473 (replacement)-2.ptc Page 433 1327569 _ Case number 90119473_年月日日_魅_ Six, the scope of application for patent [3,4-c] ° ratio. Sodium-3-yl}-4-t-butyl-benzoguanamine; 1155. N-{6-ethyl keto-4,5,6,7-tetrahydro 0 唆[3,4_c] 0 ratio . -3-yl}_4_t-butyl-benzoquinone; 1156.1^-{6-decanesulfonyl-4,5,6,7-tetrahydroacridine [3,4-(:] • pyrazol-3-yl}-4-t-butyl-benzamide; 1157. N-ethyl-Ν'-{3-(4-t-butyl-benzoguanamine)- 4,5,6,7-tetrahydrogen ratio 唆[3,4-c] ° ratio. sit-6-yl}urea; 1158.^{6-(3-mercapto)butylidene-4,5,6 , 7-tetrahydropyridine [3,4-c]pyrazol-3-yl}-4-t-butyl-benzamide; 瘫1 1 5 9. N-{ 6-(2-furanformamidine 4-), 4, 5, 6, 7-tetrahydropyridine [3,4-c]pyva-3-yl}-4-t-butyl-benzamide; 1160. N~*{6-benzene醯-yl-4,5,6,7-tetrahydrogen ratio. [3,4-c] π than sparg-3-yl}-4-t-butyl-benzamide; 1161. {6-Phenylsulfonyl-4,5,6,7-tetrahydroacridine [3,4-indolyl]pyrazole-3-yl}-4-t-butyl-benzoamidamine; 1162. Ν-{6-(Porphyrin-8-sulfonyl)-4,5,6,7-tetrahydropyridine [3,4-c]pyrazol-3-yl}-4-t-butyl-benzene Methionamine; +: 1163. N-丨5-isopentyl-4,6-dihydropyrrolo[3,4-c]carbazole-3--4-t-butyl-benzoguanamine; 1164. N_{5 -Phenylethyl_4,6-dihydroindole 11 each [3,4-c] π ratio σ _3_ yl}-4-t-butyl-benzoguanamine; 1165. N-[ 5-(2-thiophen-2-ylethyl)-4,6-dihydropyrrolo[3,4- c]pyrazol-3-yl]-4-t-butyl-benzamide; 1166. Ν,Ν-dimethyl-N'-{3**(2-naphthalene-2-yl-propyl Amino)-4,6-

90119473(替換）-2.ptc 第434頁 1327569 案號90119473 年月日修正六、申請專利範圍二氫σ比11各并[3，4 - c ] °比。坐-5 -基]脲； 1167. Ν-{ 5-(哌啶-1-基）二基曱醯基-4, 6 -二氫吡咯并 [3,4-c]吡唑-3-基}-3-(2-萘-2-基）-丙醯胺基；以及 1168. N，N -二曱基-N’-{3-(2 -苯基-噻唑-4 -基）乙醯胺基-4，5，6,7-四氫°比咬[3，4-c]n比唾-5-基]脲。 1 0. —種用於治療由癌症和細胞增生病症組成之蛋白質激酶活性變更所引起及/或關聯疾病之醫藥組成物，包含申請專利範圍第1項定義之式（I)化合物或其醫藥可接受性鹽及醫藥可接受性載劑及/或稀釋劑。 11.如申請專利範圍第1項定義之式（I)化合物或其醫藥可接受性鹽，其係用作為藥物。 1 2. —種申請專利範圍第1項定義之式（I)化合物或其醫藥可接受性鹽之用途，其係用於製造治療患有由癌症和細胞增生病症組成之蛋白質激酶活性變更所引起及/或關聯疾病病人之藥物。 1 3 . —種式（I)化合物或其醫藥可接受性鹽之用途，其係用於製造藥物，該藥物係用於正在接受同時、分開或循序抗癌治療病人，治療由癌症和細胞增生病症組成之蛋白質激酶活性變更所引起及/或關聯的疾病。 1 4. 一種申請專利範圍第1項定義之式（I)化合物之製備方法，該方法包含： NC OH a)式（II)化合物 }={90119473 (replacement)-2.ptc Page 434 1327569 Case No. 90119473 Date of revision Sixth, the scope of application for patents Dihydro σ ratio 11 and [3,4 - c ] ° ratio. Sodium-5-yl]urea; 1167. Ν-{ 5-(piperidin-1-yl)diylindenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-3-yl }-3-(2-naphthalen-2-yl)-propaninamine; and 1168. N,N-dimercapto-N'-{3-(2-phenyl-thiazol-4-yl)acetamidine Amino-4,5,6,7-tetrahydrogen ratio bites [3,4-c]n than sal-5-yl]urea. A pharmaceutical composition for treating and/or associated a disease caused by a change in protein kinase activity consisting of cancer and a cell proliferative disorder, comprising a compound of formula (I) as defined in claim 1 or a pharmaceutical thereof Receptive salts and pharmaceutically acceptable carriers and/or diluents. 11. A compound of formula (I), or a pharmaceutically acceptable salt thereof, as defined in claim 1 of the patent application, for use as a medicament. 1 2. Use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, as defined in claim 1 for the manufacture of a medicament for the treatment of a protein kinase activity consisting of cancer and a cell proliferative disorder And/or drugs associated with disease patients. Use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a patient undergoing simultaneous, separate or sequential anticancer treatment for cancer and cell proliferation A disease caused and/or associated with a change in protein kinase activity of a disorder. 1 4. A method for preparing a compound of formula (I) as defined in claim 1 of the patent application, the method comprising: NC OH a) a compound of formula (II) }={

90119473(替換）-2.ptc 第435頁丄丄 _j 號 901194乃90119473 (replacement)-2.ptc Page 435 丄丄 _j No. 901194

六、申請專利範圍其中Ri定義如申請專 — Rb、Rc、Rd、^η定義1圍第1項’R丨非為氫以及Ra、與肼或拼鹽反應，請專利範圍第1項，及R1定義如申請專利範J付式⑴化合物，其中R為氫以 a’）如此所得式⑴Ϊ!;1項且非為氮；系樹脂反應 Q與式（1 1 1 )異氰酸酯聚笨乙烯 ResinSixth, the scope of application for patents, where the definition of Ri is as specified in the application - Rb, Rc, Rd, ^ η define the first item of the first item 'R丨 is not hydrogen and Ra, and 肼 or salt, please patent item 1, and R1 is defined as a compound of the formula J formula (1), wherein R is hydrogen with a') formula (1) Ϊ!; 1 item and not nitrogen; resin reaction Q and formula (1 1 1) isocyanate polystyrene Resin

(III) NCO 因而獲得式（IV)聚笨乙烯甲基脲(III) NCO thus obtaining formula (IV) polystyrene methyl urea

(IV) Resin(IV) Resin

其中 Ra、Rb、Rc、Rd、m&n > ，以及R〗定義如申請專利範義如申請專利範圍第1項一^)將如此所得式（IV)化人鉍±項且非為氫； 1 匕D物轉成式（V)化合物Wherein Ra, Rb, Rc, Rd, m&n >, and R are defined as the patent application, as claimed in the first paragraph of the patent application, wherein the formula (IV) is thus obtained and is not hydrogen; 1 匕D conversion to compound of formula (V)

90119473(替換）-2.Pt( 第436 頁一修正曰案號90】]Q473 六、申請專利範圍其中R如申請專利範圍第1項但 Rc:、“η定義如申請專利範圍第广項'及:及Ra、Rb、 c)於強驗條件下割罗彳m几人^ 及望之式⑴化合*，二需要：物=樹脂且獲得期 :式。)化合物及，或轉成其醫藥可二)：合物轉成任 a 15. 如申請專利範圍第14項之製凰。，式二化合物與㈣肼鹽之反應其J於步驟酸、乙酸或硫酸之酸存在下進行。惟化置之選自鹽 16. 如申凊專利範圍第1 4垣夕制^甚七1 式⑴或⑺化合物Λ第中二法’其係用於製備 _ΓΛη〇) ，再中選自非為氫的R，、-COR，、 2R 、_S〇2NHR’ 或-S〇2NR’ R"，其中R’ 及r"定義 ^申請專利範圍第1項4非為氫以及Ra、Rb、RC、Rd、t 義如申請專利範圍第1項，其中於步驟b)，式⑴化應掣備观具具有R 4於虱，與式（VI)化合物反 R-x (vi) 其中R定義如申請專利範圍第1項但氫除外，以及X為離去基° 、1 7.如申請專利範圍第1 4項之製備方法，其係用於製備式（1)或（V)化合物，其中R為-C0NHR，基，R，定義如中請專利範圍第1項但非為氣，R丨非為氫以及Ra、Rb、Rc、Rd、阳及定義如申請專利範圍第】項，其中於步驟㈧，具有R等於氫之式（I )化合物或式（丨v )化合物與式（v丨丨）化合物反應 R’NCO (VII) " 第437頁 90119473(替換）-2.ptc 1327569 年月修·^一六、申請專利範圍其中R’定義如申請專利範圍第1項但非為氫。 1 8.如申請專利範圍第丨4項之製備方法，其係用於製備式（I)或（V)化合物，其中r為_c〇NHR，Rll基，其中R，及R，，定義如前但非為氫，其中於步驟b)，式或”）化合物與 (V I I I)化合物反應、 Rn-x (viii) 其中R"定義如申請專利範圍第1項但非為氫，以及X為適者離去基。 1 9 .如申請專利範圍第1 4項之製備方法，其係用於製備馨⑴或（V)化合物，其中R為-CONR，R"基，其中R，及R"定 ^如前但非為氯，Ri非為氫以及Ra、Rb、Rc、Rd、^n定匕申= 利，範圍第1項’其中於步_，具有R等於氫如合物與氯甲酸4_硝基笨酷反應，以及隨後與式（I X)化合物反應 R’RmNH (IX) 其中R及R疋義如申往直刹$^阁梦1 s 广甲。月專利範圍第1項但非為氫。 γ Μ 利範圍第14項之製備方法，其係用於製備二非H’其中UR’CH2—基，其中R，定義如前 ♦&二、-“:步驟b)，具有R等於氫之式⑴或⑴化 ό物係於還原性條件下與式（χ)化合物反應 r，~ch〇 (X) 〜其中r定義如前但非為氫。90119473 (replacement)-2.Pt (p. 436, rev. 90案号 90]] Q473 VI. Patent application scope, where R is the first item of the patent application scope but Rc:, “η defines the scope of the patent application scope” And: and Ra, Rb, c) under the strong conditions of cutting a few people ^ and the formula (1) compound *, two need: material = resin and the acquisition period: formula.) Compound and, or into its medicine 2): The compound is converted into a. 15. The phoenix according to item 14 of the patent application scope. The reaction of the compound of the formula 2 with the (tetra) phosphonium salt is carried out in the presence of an acid of the step acid, acetic acid or sulfuric acid. It is selected from the salt 16. If the application of the patent is in the range of 1st, 4th, 1st, 1st, 1st, (1) or (7), the second method, which is used to prepare _ΓΛη〇, and then selected from non-hydrogen R,, -COR,, 2R, _S〇2NHR' or -S〇2NR' R", where R' and r" define ^ patent application scope item 1 is not hydrogen and Ra, Rb, RC, Rd, t is as claimed in the first item of the patent scope, wherein in step b), the formula (1) should be prepared to have R 4 in 虱, and the compound of formula (VI) is inverse Rx (vi) wherein R is as defined Please refer to the first item of the patent scope except for hydrogen, and X is a leaving group, and 7. 7. The preparation method of claim 14 is used to prepare a compound of the formula (1) or (V), wherein R For -C0NHR, base, R, as defined in the first paragraph of the patent scope but not gas, R丨 is not hydrogen and Ra, Rb, Rc, Rd, yang and as defined in the scope of the patent application, in the steps (8) A compound of the formula (I) or a compound of the formula (丨v) having R equal to hydrogen is reacted with a compound of the formula (v丨丨) R'NCO (VII) " Page 437 90119473 (replacement)-2.ptc 1327569修·^16, the scope of application for patents, where R' is defined as the first item of patent application but not hydrogen. 1 8. The preparation method of item 4 of the patent application is for the preparation of formula (I) or (V) a compound, wherein r is _c〇NHR, Rll, wherein R, and R, are as defined above but not hydrogen, wherein in step b), a compound of formula or ") is reacted with a compound of formula (VIII), Rn -x (viii) where R" is defined as claim 1 but not hydrogen, and X is the appropriate leaver. 1 9. The preparation method of claim 14 of the patent application, which is for preparing a compound of the genus (1) or (V), wherein R is a -CONR, R" group, wherein R, and R" For chlorine, Ri is not hydrogen and Ra, Rb, Rc, Rd, ^n 匕 = = =, range 1 'in which in step _, with R equal to hydrogen and chloroformic acid 4 nitro Reaction, and subsequent reaction with the compound of formula (IX) R'RmNH (IX) wherein R and R are as defined by the application of the direct brake $^阁梦1 s wide armor. The first patent range of the month is not hydrogen. γ Μ 范围范围第第第第第第第第第第第第制备制备制备制备制备制备 UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR UR The hydrazine of the formula (1) or (1) is reacted with a compound of the formula (χ) under reducing conditions, r,~ch〇(X)~ wherein r is as defined above but not hydrogen.