JP2000512990A - 過増殖性疾患を処置するためのフェニルアミノ置換三環式誘導体 - Google Patents
過増殖性疾患を処置するためのフェニルアミノ置換三環式誘導体Info
- Publication number
- JP2000512990A JP2000512990A JP10502594A JP50259498A JP2000512990A JP 2000512990 A JP2000512990 A JP 2000512990A JP 10502594 A JP10502594 A JP 10502594A JP 50259498 A JP50259498 A JP 50259498A JP 2000512990 A JP2000512990 A JP 2000512990A
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- Prior art keywords
- cancer
- compound
- formula
- alkyl
- mammal
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 式: [式中、nは、0〜2であり; R1は、水素;または、ハロ、C1−C4アルコキシ、−NR6R7および−SO2 R5からなる群より独立に選択される1個〜3個の置換基によって任意に置換さ れたC1−C6アルキルであり; 各R2は、ハロ、ヒドロキシ、C1−C6アルキル、−NR6R7およびC1−C4 アルコキシからなる群より独立に選択され、前記R2基の前記アルキル基および アルキル部分は、ハロ、C1−C4アルコキシ、−NR6R7および−SO2R5から なる群より独立に選択される1個〜3個の置換基によって任意に置換され; R3は、アジド;または、−(エチニル)−R8{ここで、R8は、水素;また は、ヒドロキシ、−OR6または−NR6R7によって任意に置換されたC1−C6 アルキルである。}あり; R4は、H;C1−C4アルキル、(C1−C4アルコキシ)C1−C4アルキル、 C1−C4アルカノイル、C1−C4アルコキシまたは−S(O)x(C1−C4アル キル){ここで、xは、0〜2である。}であり、前記R4基の前記アルキル基 およびアルキル部分は、1個〜3個のハロゲン類によって任意に置換されており ; 各R5は、1個〜3個のハロゲン類によって任意に置換されたC1−C4アルキ ルであり; R6およびR7は、独立に、水素およびR5から選択され; Zは、O、SおよびNから選択される0個〜3個のヘテロ原子を含む5〜8員 環縮合環である。] で表される化合物またはその薬学的に許容可能な塩。 2. R3が−(エチニル)−R8である、請求項1に記載の化合物。 3. Zが式: から選択される、請求項2に記載の化合物。 4. R4がHまたはC1−C4アルキルであり、R1がHであり、nが0である、 請求項3に記載の化合物。 5. R8がHである、請求項4に記載の化合物。 6. 式: [式中、R1、R2、R3、R6およびnは、請求項1に記載した通りである。] で表される請求項1の化合物またはその薬学的に許容可能な塩。 7. nが0であり、R1がHであり、R3が−(エチニル)−R8であり、R6が Hまたはメチルである、請求項6に記載の化合物。 8. R8がHである、請求項7に記載の化合物。 9. 前記化合物が、 4−(3−エチニルアニリノ)−イミダゾ[4,5−g]キナゾリン; (3−エチニル−フェニル)−(3−メチル−3H−イミダゾ[4,5−g]キ ナゾリン−8−イル)−アミン; (3−エチニル−フェニル)−(1−メチル−1H−イミダゾ[4,5−g]キ ナゾリン−8−イル)−アミン; ベンゾ[g]キナゾリン−4−イル−(3−エチニル−フェニル)−アミン; [1,3]ジオキソロ[4,5−g]キナゾリン−8−イル−(3−エチニル− フェニル)−アミン;および、 前述の化合物の薬学的に許容可能な塩類からなる群より選択される請求項1に記 載の化合物。 10. 哺乳動物の過増殖性疾患を処置するための薬学的組成物であって、治療 学的に有効量の請求項1の化合物と、薬学的に許容可能な担体とを含む薬学的組 成物。 11. 前記過増殖性疾患が癌である、請求項10に記載の薬学的組成物。 12. 前記癌が、脳癌、肺癌、偏平上皮細胞癌、膀胱癌、胃癌、膵臓癌、胸部 癌、頭部癌、頸部癌、食道癌、婦人科癌、前立腺癌、結腸直腸癌または甲状腺癌 である、請求項11に記載の薬学的組成物。 13. 前記過増殖疾患が癌ではない、請求項10に記載の組成物。 14. 前記疾患が乾癬または皮膚もしくは前立腺の良性の増殖である、請求項 13に記載の薬学的組成物。 15. 哺乳動物の膵臓炎または腎臓病の処置のための薬学的組成物であって、 治療学的に有効量の請求項1の化合物と、薬学的に許容可能な担体とを含む薬学 的組成物。 16. 哺乳動物の未分化胚芽細胞の着床のための薬学的組成物であって、治療 学的に有効量の請求項1の化合物と、薬学的に許容可能な担体とを含む薬学的組 成物。 17. 哺乳動物の過増殖性疾患を処置する方法であって、前記哺乳動物に、治 療学的に有効量の請求項1の化合物を投与することを含む方法。 18. 前記過増殖性疾患が癌である、請求項17に記載の方法。 19. 前記癌が、脳癌、肺癌、偏平上皮細胞癌、膀胱癌、胃癌、膵臓癌、胸部 癌、頭部癌、頸部癌、食道癌、前立腺癌、結腸直腸癌、婦人科癌または甲状腺癌 である、請求項18に記載の方法。 20. 前記過増殖性疾患が、癌でない、請求項17に記載の方法。 21. 前記疾患が乾癬または皮膚もしくは前立腺の良性の増殖である、請求項 20に記載の方法。 22. 哺乳動物の膵臓炎または腎臓病を処置する方法であって、前記哺乳動物 に、治療学的に有効量の請求項1の化合物を投与することを含む方法。 23. 哺乳動物の未分化胚芽細胞の着床を予防する方法であって、前記哺乳動 物に、治療学的に有効量の請求項1の式1の化合物を投与することを含む方法。
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US2049196P | 1996-06-24 | 1996-06-24 | |
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PCT/IB1997/000675 WO1997049688A1 (en) | 1996-06-24 | 1997-06-11 | Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases |
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Cited By (5)
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JP2007523177A (ja) * | 2004-02-19 | 2007-08-16 | レクサーン コーポレーション | キナゾリン誘導体およびキナゾリン誘導体の治療への使用 |
JP4934432B2 (ja) * | 2004-02-19 | 2012-05-16 | レクサン ファーマシューティカルズ インコーポレイテッド | キナゾリン誘導体およびキナゾリン誘導体の治療への使用 |
US8404698B2 (en) | 2004-02-19 | 2013-03-26 | Rexahn Pharmaceuticals, Inc. | Quinazoline derivatives and therapeutic use thereof |
JP2017537154A (ja) * | 2015-01-13 | 2017-12-14 | 北京賽特明強医薬科技有限公司 | キナゾリン複素環式化合物、その製造方法及び癌を治療する上皮成長因子受容体阻害剤としての応用 |
JP2020536855A (ja) * | 2017-09-26 | 2020-12-17 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | がんを治療するための組成物及び方法 |
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ES2249800T3 (es) | 2006-04-01 |
HRP970346A2 (en) | 1998-06-30 |
DE69734513D1 (de) | 2005-12-08 |
EP0907642A1 (en) | 1999-04-14 |
CA2258548C (en) | 2005-07-26 |
ATE308527T1 (de) | 2005-11-15 |
ZA975543B (en) | 1999-01-25 |
AR007440A1 (es) | 1999-10-27 |
DE69734513T2 (de) | 2006-07-27 |
PA8432701A1 (es) | 2003-02-14 |
WO1997049688A1 (en) | 1997-12-31 |
BR9709959A (pt) | 2000-05-09 |
CA2258548A1 (en) | 1997-12-31 |
EP0907642B1 (en) | 2005-11-02 |
AP9701019A0 (en) | 1997-07-31 |
US6335344B1 (en) | 2002-01-01 |
MA24439A1 (fr) | 1998-10-01 |
ID19511A (id) | 1998-07-16 |
GT199700079A (es) | 1998-12-15 |
HN1997000083A (es) | 1998-02-26 |
TNSN97106A1 (fr) | 2005-03-15 |
AU2912997A (en) | 1998-01-14 |
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