JP2003530401A5 - - Google Patents

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Publication number: JP2003530401A5
Authority: JP; Japan
Prior art keywords: alkyl; conhch; aryl; compound; conr
Prior art date: 2001-04-03
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.): Granted

Application number

JP2001575586A

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English (en)

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JP2003530401A (ja

JP4748911B2 (ja

Filing date

2001-04-03

Publication date

2008-02-28

2001-04-03 Application filed filed Critical

2001-04-03 Priority claimed from PCT/US2001/010869 external-priority patent/WO2001077113A2/en

2003-10-14 Publication of JP2003530401A publication Critical patent/JP2003530401A/ja

2008-02-28 Publication of JP2003530401A5 publication Critical patent/JP2003530401A5/ja

2011-08-17 Application granted granted Critical

2011-08-17 Publication of JP4748911B2 publication Critical patent/JP4748911B2/ja

2021-04-03 Anticipated expiration legal-status Critical

Status Expired - Fee Related legal-status Critical Current

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150000001875 compounds Chemical class 0.000 description 23
125000000217 alkyl group Chemical group 0.000 description 12
239000008194 pharmaceutical composition Substances 0.000 description 9
-1 aryl-heteroaryl Chemical group 0.000 description 8
125000000753 cycloalkyl group Chemical group 0.000 description 6
0 CCCC(C(C(NCC(NC(C(CC(C)C)=O)c1ccccc1)=O)=O)=O)NC(C(CCC1)N1C([C@@](CC=CC(Cc1cccc(OCCC*)c1)=*=C)C(CC1)CCC1C(O)=O)=O)=O Chemical compound CCCC(C(C(NCC(NC(C(CC(C)C)=O)c1ccccc1)=O)=O)=O)NC(C(CCC1)N1C([C@@](CC=CC(Cc1cccc(OCCC*)c1)=*=C)C(CC1)CCC1C(O)=O)=O)=O 0.000 description 5
102000033147 ERVK-25 Human genes 0.000 description 5
241000711549 Hepacivirus C Species 0.000 description 5
108091005771 Peptidases Proteins 0.000 description 5
239000004365 Protease Substances 0.000 description 5
125000002877 alkyl aryl group Chemical group 0.000 description 5
125000003118 aryl group Chemical group 0.000 description 5
125000004404 heteroalkyl group Chemical group 0.000 description 5
125000001072 heteroaryl group Chemical group 0.000 description 5
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 5
201000010099 disease Diseases 0.000 description 4
XSQUKJJJFZCRTK-UHFFFAOYSA-N urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 4
125000003710 aryl alkyl group Chemical group 0.000 description 3
239000003937 drug carrier Substances 0.000 description 3
125000000592 heterocycloalkyl group Chemical group 0.000 description 3
239000000203 mixture Substances 0.000 description 3
125000004433 nitrogen atoms Chemical group N* 0.000 description 3
125000004437 phosphorous atoms Chemical group 0.000 description 3
125000004434 sulfur atoms Chemical group 0.000 description 3
125000000008 (C1-C10) alkyl group Chemical group 0.000 description 2
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 2
102000014150 Interferons Human genes 0.000 description 2
108010050904 Interferons Proteins 0.000 description 2
150000001299 aldehydes Chemical class 0.000 description 2
125000003342 alkenyl group Chemical group 0.000 description 2
125000003545 alkoxy group Chemical group 0.000 description 2
150000001346 alkyl aryl ethers Chemical class 0.000 description 2
150000005215 alkyl ethers Chemical class 0.000 description 2
125000005213 alkyl heteroaryl group Chemical group 0.000 description 2
125000004414 alkyl thio group Chemical group 0.000 description 2
239000003443 antiviral agent Substances 0.000 description 2
125000005110 aryl thio group Chemical group 0.000 description 2
125000004104 aryloxy group Chemical group 0.000 description 2
235000013877 carbamide Nutrition 0.000 description 2
125000004432 carbon atoms Chemical group C* 0.000 description 2
125000000113 cyclohexyl group Chemical class [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 2
125000001511 cyclopentyl group Chemical class [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
150000002148 esters Chemical class 0.000 description 2
XPXMKIXDFWLRAA-UHFFFAOYSA-N hydrazinide Chemical compound [NH-]N XPXMKIXDFWLRAA-UHFFFAOYSA-N 0.000 description 2
229940079322 interferon Drugs 0.000 description 2
150000002576 ketones Chemical class 0.000 description 2
125000004430 oxygen atoms Chemical group O* 0.000 description 2
125000004076 pyridyl group Chemical class 0.000 description 2
150000003839 salts Chemical class 0.000 description 2
239000011780 sodium chloride Substances 0.000 description 2
239000012453 solvate Substances 0.000 description 2
125000001544 thienyl group Chemical class 0.000 description 2
125000006725 C1-C10 alkenyl group Chemical group 0.000 description 1
125000006374 C2-C10 alkenyl group Chemical group 0.000 description 1
GGEHEYIXIKBQLC-XTFHHSQUSA-N CCC#C[C@@H](C(C(NCC(N[C@@H](C1Cc2ccccc2C1)C(N(C)C)=O)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O Chemical compound CCC#C[C@@H](C(C(NCC(N[C@@H](C1Cc2ccccc2C1)C(N(C)C)=O)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O GGEHEYIXIKBQLC-XTFHHSQUSA-N 0.000 description 1
CNDIAFGIFQFOBC-JUBWKJJFSA-N CCCC(C(C(NCC(NC(C(OC(C)(C)C)=O)c1ccccc1)=O)=O)=O)NC(C(C[C@H](C1)OCCCCOc2cc(CC(N[C@H]3C)=O)ccc2)N1C3=O)=O Chemical compound CCCC(C(C(NCC(NC(C(OC(C)(C)C)=O)c1ccccc1)=O)=O)=O)NC(C(C[C@H](C1)OCCCCOc2cc(CC(N[C@H]3C)=O)ccc2)N1C3=O)=O CNDIAFGIFQFOBC-JUBWKJJFSA-N 0.000 description 1
JQYOUERZBDLNBO-RPSWEREUSA-N CCCC(C(C(NCC(N[C@H](C(O)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCCOc2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O Chemical compound CCCC(C(C(NCC(N[C@H](C(O)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCCOc2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O JQYOUERZBDLNBO-RPSWEREUSA-N 0.000 description 1
RUQJIWAEEPLRQC-OXHSURQKSA-N CCCC(CC(NCC(N[C@@H](C1Cc2ccccc2C1)C(N(C)C)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O Chemical compound CCCC(CC(NCC(N[C@@H](C1Cc2ccccc2C1)C(N(C)C)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O RUQJIWAEEPLRQC-OXHSURQKSA-N 0.000 description 1
QKVAUVHKZPMIEL-XJUSNKPOSA-N CCCCCCCC(C(C(NCC(NCc1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OC(C)(C)CCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O Chemical compound CCCCCCCC(C(C(NCC(NCc1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OC(C)(C)CCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O QKVAUVHKZPMIEL-XJUSNKPOSA-N 0.000 description 1
GVKXBPKXZQLESA-XIARVLQKSA-N CCCC[C@@H](C(C(NCC(NC(C(N(C)C)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCOc2cccc(CC(N[C@H]3C(C)(C)C)=O)c2)N1C3=O)=O Chemical compound CCCC[C@@H](C(C(NCC(NC(C(N(C)C)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCOc2cccc(CC(N[C@H]3C(C)(C)C)=O)c2)N1C3=O)=O GVKXBPKXZQLESA-XIARVLQKSA-N 0.000 description 1
229940042795 Hydrazides for tuberculosis treatment Drugs 0.000 description 1
102000006992 Interferon-alpha Human genes 0.000 description 1
108010047761 Interferon-alpha Proteins 0.000 description 1
IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical group N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 description 1
229960000329 Ribavirin Drugs 0.000 description 1
229940090121 Sulfonylureas for blood glucose lowering Drugs 0.000 description 1
239000004480 active ingredient Substances 0.000 description 1
125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
125000003282 alkyl amino group Chemical group 0.000 description 1
125000004947 alkyl aryl amino group Chemical group 0.000 description 1
125000004448 alkyl carbonyl group Chemical group 0.000 description 1
125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
125000004422 alkyl sulphonamide group Chemical group 0.000 description 1
125000000304 alkynyl group Chemical group 0.000 description 1
125000001769 aryl amino group Chemical group 0.000 description 1
125000005129 aryl carbonyl group Chemical group 0.000 description 1
125000004350 aryl cycloalkyl group Chemical group 0.000 description 1
150000008378 aryl ethers Chemical class 0.000 description 1
125000005161 aryl oxy carbonyl group Chemical group 0.000 description 1
125000004391 aryl sulfonyl group Chemical group 0.000 description 1
125000004421 aryl sulphonamide group Chemical group 0.000 description 1
UZMZVDOOVXLRID-UHFFFAOYSA-N azanylidyne-(nitrosulfonylamino)methane Chemical class [O-][N+](=O)S(=O)(=O)NC#N UZMZVDOOVXLRID-UHFFFAOYSA-N 0.000 description 1
229910052794 bromium Inorganic materials 0.000 description 1
KXDHJXZQYSOELW-UHFFFAOYSA-M carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
150000004657 carbamic acid derivatives Chemical class 0.000 description 1
239000004202 carbamide Substances 0.000 description 1
150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
150000001735 carboxylic acids Chemical class 0.000 description 1
229910052801 chlorine Inorganic materials 0.000 description 1
125000004965 chloroalkyl group Chemical group 0.000 description 1
125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 description 1
125000001559 cyclopropyl group Chemical class [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
230000001747 exhibiting Effects 0.000 description 1
229910052731 fluorine Inorganic materials 0.000 description 1
229910052736 halogen Inorganic materials 0.000 description 1
150000002367 halogens Chemical class 0.000 description 1
125000004446 heteroarylalkyl group Chemical group 0.000 description 1
125000005223 heteroarylcarbonyl group Chemical group 0.000 description 1
125000005349 heteroarylcycloalkyl group Chemical group 0.000 description 1
125000005143 heteroarylsulfonyl group Chemical group 0.000 description 1
125000000623 heterocyclic group Chemical group 0.000 description 1
229910052739 hydrogen Inorganic materials 0.000 description 1
125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 1
230000002401 inhibitory effect Effects 0.000 description 1
150000002678 macrocyclic compounds Chemical class 0.000 description 1
238000004519 manufacturing process Methods 0.000 description 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
IBGCXOFOCKCBNQ-UHFFFAOYSA-N nitro cyanate Chemical compound [O-][N+](=O)OC#N IBGCXOFOCKCBNQ-UHFFFAOYSA-N 0.000 description 1
229910052757 nitrogen Inorganic materials 0.000 description 1
229910052760 oxygen Inorganic materials 0.000 description 1
125000005936 piperidyl group Chemical class 0.000 description 1
150000003457 sulfones Chemical class 0.000 description 1
150000003462 sulfoxides Chemical class 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1

Description

【特許請求の範囲】
【請求項１】式Ｉ
【化１】

式Ｉ
［式中、部分；
【化２】

は、以下を表し：
【化３】

ＸおよびＹは、独立して、アルキル、アルキル−アリール、ヘテロアルキル、ヘテロアリール、アリール−ヘテロアリール、シクロアルキル、アルキルエーテル、アルキル−アリールエーテル、アリールエーテル、アルキルアミノ、アリールアミノ、アルキル−アリールアミノ、アルキルスルフィド、アルキル−アリールスルフィド、アリールスルフィド、アルキルアミド、アルキル−アリールアミド、アリールアミド、アルキルスルホンアミド、アルキル−アリールスルホンアミド、アリールスルホンアミド、アルキルスルホニル、アリールスルホニル、ヘテロアルキルスルホニル、ヘテロアリールスルホニル、アルキルカルボニル、アリールカルボニル、ヘテロアルキルカルボニル、ヘテロアリールカルボニル、アルコキシカルボニル、アリールオキシカルボニル、ヘテロアリールオキシカルボニル部分またはそれらの組合わせから選択され、ただしＸおよびＹは、さらに芳香族、アルキル、アルキル−アリール、ヘテロアルキルおよびシクロアルキルからなる群より選択される部分により置換され得るものとし、
Ｒ^１＝ＣＯＲ^５、ここでＲ^５＝Ｈ、ＯＨ、ＯＲ^８、ＮＲ^９Ｒ^１０、ＣＦ_３、Ｃ_２Ｆ_５、Ｃ_３Ｆ_７、ＣＦ_２Ｒ^６、Ｒ^６、ＣＯＲ^７、ここでＲ^７＝Ｈ、ＯＨ、ＯＲ^８、ＣＨＲ^９Ｒ¹⁰またはＮＲ^９Ｒ¹⁰、ここでＲ^６、Ｒ^８、Ｒ^９およびＲ¹⁰は、独立して、Ｈ、アルキル、アリール、ヘテロアルキル、ヘテロアリール、シクロアルキル、シクロアルキル、アリールアルキル、ヘテロアリールアルキル、ＣＨ(Ｒ^1')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＲ¹²Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＲ^1２Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')Ｒ'、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＨＣＨ(Ｒ^３')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＨＣＨ(Ｒ^３')ＣＯＮＲ¹²Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＨＣＨ(Ｒ^３')ＣＯＮＨＣＨ(Ｒ^４')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＨＣＨ(Ｒ^３')ＣＯＮＨＣＨ(Ｒ^４')ＣＯＮＲ¹²Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＨＣＨ(Ｒ^３')ＣＯＮＨＣＨ(Ｒ^４')ＣＯＮＨＣＨ(Ｒ^５')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＨＣＨ(Ｒ^３')ＣＯＮＨＣＨ(Ｒ^４')ＣＯＮＨＣＨ(Ｒ^５')ＣＯＮＲ¹²Ｒ¹³からなる群より選択され、ここで、Ｒ^１'、Ｒ^２'、Ｒ^３'、Ｒ^４'、Ｒ^５'、Ｒ¹¹、Ｒ¹²、Ｒ¹³およびＲ'は、独立して、Ｈ、アルキル、アリール、ヘテロアルキル、ヘテロアリール、シクロアルキル、アルキル−アリール、アルキル−ヘテロアリール、アリール−アルキルおよびヘテロアリールアルキルからなる群より選択されるものとし、
Ｚは、Ｏ、ＮまたはＣＨから選択され、
Ｗは存在してもよくまたは存在しなくてもよく、そしてＷが存在する場合、ＷはＣ＝Ｏであり、
Ｒ ^４はＨ、Ｃ１−Ｃ１０アルキル、Ｃ１−Ｃ１０アルケニルまたはＣ３−Ｃ８シクロアルキルであり；そして
Ｒ ^２およびＲ ^３は、独立して、Ｈ、Ｃ１−Ｃ１０アルキル、Ｃ２−Ｃ１０アルケニル、Ｃ３−Ｃ８シクロアルキル、Ｃ３−Ｃ８ヘテロシクロアルキル、アルコキシ、アリールオキシ、アルキルチオ、アリールチオ、アミノ、アミド、エステル、カルボン酸、カルバメート、尿素、ケトン、アルデヒド、シアノ、ニトロ、酸素、窒素、硫黄またはリン原子（ただし、酸素、窒素、硫黄またはリン原子は０〜６の数である)、(シクロアルキル)アルキルおよび（ヘテロシクロアルキル）アルキル（ただし、シクロアルキルは３〜８個の炭素原子、および０〜６個の酸素、窒素、硫黄またはリン原子を含み、アルキルは１〜６個の炭素原子を有する）、アリール、ヘテロアリール、アルキル−アリール、およびアルキル−ヘテロアリールからなる群より選択され、
ただし、上記アルキル、ヘテロアルキル、アルケニル、ヘテロアルケニル、アリール、ヘテロアリール、シクロアルキルおよびヘテロシクロアルキル部分は置換され得、この「置換され」の語は、アルキル、アルケニル、アルキニル、アリール、アラルキル、シクロアルキル、複素環、ハロゲン、ヒドロキシ、チオ、アルコキシ、アリールオキシ、アルキルチオ、アリールチオ、アミノ、アミド、エステル、カルボン酸、カルバメート、尿素、ケトン、アルデヒド、シアノ、ニトロ、スルホンアミド、スルホキシド、スルホン、スルホニルウレア、ヒドラジドおよびヒドロキサメートからなる群より選択される１個またはそれ以上の部分による適切な置換をいうものとする］
で示される一般構造を有する大環状化合物であって、上記化合物の鏡像異性体、立体異性体、回転異性体および互変異性体、ならびに上記化合物の医薬上許容される塩または溶媒和物を含む、化合物。
【請求項２】Ｒ^１＝ＣＯＲ^５、およびＲ^５がＨ、ＯＨ、ＣＯＯＲ^８、ＣＯＮＲ^９Ｒ¹⁰である、請求項１記載の化合物。
【請求項３】Ｒ^１＝ＣＯＣＯＮＲ^９Ｒ¹⁰、およびＲ^９がＨ、Ｒ¹⁰がＨ、ＣＨ(Ｒ^１')ＣＯＯＲ¹¹、ＣＨ(Ｒ^１')ＣＯＮＲ¹²Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＲ¹²Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')(Ｒ')である、請求項２記載の化合物。
【請求項４】Ｒ¹⁰＝ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＯＲ¹¹、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')ＣＯＮＲ¹²Ｒ¹³、ＣＨ(Ｒ^1')ＣＯＮＨＣＨ(Ｒ^2')(Ｒ')であり、Ｒ^1'がＨまたはアルキルであり、Ｒ^２'が、フェニル、置換フェニル、ヘテロ原子置換フェニル、チオフェニル、シクロヘキシル、シクロペンチル、シクロプロピル、ピペリジル、ピリジルおよび２−インダニルである、請求項３記載の化合物。
【請求項５】Ｒ^1'がＨである、請求項４記載の化合物。
【請求項６】Ｒ^２'＝フェニル、チオフェニル、シクロヘキシル、２−インダニル、シクロペンチル、ピリジル、フェニル(４−ＨＮＳＯ_２ＮＨ_２)、Ｒ¹¹がＨまたはｔｅｒｔ−ブチルであり、Ｒ¹²およびＲ¹³がメチルであり、Ｒ'がヒドロキシメチルまたはｔｅｒｔ−ブトキシメチルである、請求項５記載の化合物。
【請求項７】Ｒ^２が以下の部分：
【化４】

からなる群より選択される、請求項１記載の化合物。
【請求項８】Ｒ^１＝ＣＯＲ^５、およびＲ^５が、Ｈ、ＯＨ、ＣＯＯＲ^８、ＣＯＮＲ^９Ｒ^１０である、請求項７記載の化合物。
【請求項９】Ｒ^３が、
【化５】

（式中、Ｒ³⁰＝Ｈ、ＣＨ_３または他のアルキル基、
Ｒ³¹＝ＯＨ、Ｏ−アルキル、ＮＨ_２、Ｎ−アルキル、および
Ｒ³²およびＲ³³は、同一または異なり得、独立してＨ、Ｆ、Ｃｌ、ＢｒおよびＣＨ_３から選択される）
からなる群より選択される、請求項１記載の化合物。
【請求項１０】Ｚ＝ＮおよびＲ^４＝Ｈである、請求項９記載の化合物。
【請求項１１】ＸおよびＹが、独立して、アルキル、アルキル−アリール、ヘテロアルキル、ヘテロアリール、アルキルエーテルまたはアルキルアリールエーテルである、請求項１０記載の化合物。
【請求項１２】Ｘ−Ｙ部分が、以下の構造：
【化６】

からなる群より選択される、請求項１０記載の化合物。
【請求項１３】有効成分として請求項１記載の化合物を含む、医薬組成物。
【請求項１４】さらに医薬上許容される担体を含む、請求項１３記載の医薬組成物。
【請求項１５】Ｃ型肝炎ウイルス（「ＨＣＶ」）プロテアーゼに関連した疾患の処置方法であって、請求項１記載の化合物の治療有効量を含む医薬組成物を、処置を必要とする非ヒト患者に投与する工程を包含する方法。
【請求項１６】Ｃ型肝炎ウイルス（「ＨＣＶ」）ＮＳ３プロテアーゼに関連した疾患を処置するために使用される、請求項１３または１４記載の医薬組成物。
【請求項１７】Ｃ型肝炎ウイルス（「ＨＣＶ」）プロテアーゼに関連した疾患を処置するための医薬組成物の製造方法であって、請求項１記載の化合物および医薬上許容される担体を緊密に接触させる工程を包含する方法。
【請求項１８】Ｃ型肝炎ウイルス（「ＨＣＶ」）プロテアーゼ阻害活性を示す化合物であって、上記化合物の鏡像異性体、立体異性体および互変異性体、ならびに上記化合物の医薬上許容される塩または溶媒和物を包含し、下記に列挙した構造：
【化７】

【化８】

【化９】

【化１０】

を有する化合物から選択される化合物。
【請求項１９】Ｃ型肝炎ウイルス（「ＨＣＶ」）プロテアーゼに関連した疾患を処置するための医薬組成物であって、請求項１８に記載の１種またはそれ以上の化合物の治療有効量および医薬上許容される担体を含む組成物。
【請求項２０】さらに抗ウイルス剤を含む、請求項１９記載の医薬組成物。
【請求項２１】さらにインターフェロンを含む、請求項１９または請求項２０記載の医薬組成物。
【請求項２２】抗ウイルス剤がリバビリンであり、インターフェロンがα−インターフェロンである、請求項２１記載の医薬組成物。

JP2001575586A 2000-04-05 2001-04-03 Ｎ−環状ｐ２部分を含むｃ型肝炎ウイルスの大環状ｎｓ３‐セリンプロテアーゼ阻害剤 Expired - Fee Related JP4748911B2 (ja)

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2001
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- 2001-04-03 KR KR1020027013276A patent/KR20030036152A/ko not_active Application Discontinuation
- 2001-04-03 IL IL15193401A patent/IL151934A0/xx unknown
- 2001-04-03 JP JP2001575586A patent/JP4748911B2/ja not_active Expired - Fee Related
- 2001-04-03 HU HU0400456A patent/HUP0400456A3/hu unknown
- 2001-04-03 DE DE60137207T patent/DE60137207D1/de not_active Expired - Lifetime
- 2001-04-03 AR ARP010101579A patent/AR029903A1/es unknown
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- 2001-04-03 AT AT01926601T patent/ATE419270T1/de not_active IP Right Cessation
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- 2001-04-03 CN CN01810568A patent/CN1441806A/zh active Pending
- 2001-04-03 MX MXPA02009920A patent/MXPA02009920A/es active IP Right Grant
- 2001-04-03 CZ CZ20023321A patent/CZ20023321A3/cs unknown
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- 2001-04-03 BR BR0109861-6A patent/BR0109861A/pt not_active IP Right Cessation
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2002
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2003
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