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公开(公告)号:US08912182B2
公开(公告)日:2014-12-16
申请号:US13967922
申请日:2013-08-15
申请人: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
发明人: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
IPC分类号: C07D401/14 , C07D213/81 , C07D213/643 , C07D239/34 , A61K31/444 , C07D215/227 , C07D217/24 , C07D239/38 , C07D401/06 , C07D417/14 , C07D307/20 , C07D471/04 , C07D239/47 , C07D239/52 , C07D413/06 , C07D249/04 , C07D213/69 , A61K31/5377 , C07D211/38 , C07D417/06 , C07D333/32
CPC分类号: A61K31/444 , A61K31/5377 , C07D211/38 , C07D213/643 , C07D213/69 , C07D213/81 , C07D215/227 , C07D217/24 , C07D239/34 , C07D239/38 , C07D239/47 , C07D239/52 , C07D249/04 , C07D277/24 , C07D307/20 , C07D333/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04
摘要: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
摘要翻译: 式I化合物:其中X,R2,R3,R3a,R3b,R5和R6如本文所定义,可用作丙型肝炎病毒NS5B聚合酶的抑制剂。
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公开(公告)号:US08476257B2
公开(公告)日:2013-07-02
申请号:US12808220
申请日:2008-12-03
申请人: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
发明人: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
IPC分类号: A61K31/397 , A61K31/444 , A61K31/44 , A61K31/5377 , A61K31/4439 , A61K31/4545 , A61K31/497 , A61K31/4353 , A61K31/5355 , A61K31/506 , A61K31/551 , C07D401/12 , C07D401/04 , C07D213/643 , C07D413/04 , C07D417/04 , C07D471/04 , A61P31/14
CPC分类号: A61K31/444 , A61K31/5377 , C07D211/38 , C07D213/643 , C07D213/69 , C07D213/81 , C07D215/227 , C07D217/24 , C07D239/34 , C07D239/38 , C07D239/47 , C07D239/52 , C07D249/04 , C07D277/24 , C07D307/20 , C07D333/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04
摘要: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
摘要翻译: 式I化合物:其中X,R2,R3,R3a,R3b,R5和R6如本文所定义,可用作丙型肝炎病毒NS5B聚合酶的抑制剂。
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公开(公告)号:USRE40525E1
公开(公告)日:2008-09-30
申请号:US11241899
申请日:2005-09-30
申请人: Montse Llinas-Brunet , Murray D. Bailey , Dale R. Cameron , Anne-Marie Faucher , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Dominik M. Wernic
发明人: Montse Llinas-Brunet , Murray D. Bailey , Dale R. Cameron , Anne-Marie Faucher , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Marc-André Poupart , Jean Rancourt , Youla S. Tsantrizos , Dominik M. Wernic
IPC分类号: A61K38/00 , A61K31/47 , A61K31/40 , C07D215/16 , C07D405/00
CPC分类号: C12P13/02 , A61K38/21 , A61K45/06 , C07D207/16 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C12P41/005 , A61K2300/00
摘要: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10 aryl or C7-14 aralkyl optionally substituted, or R20 is Het or (lower alkyl)-Het, both optionally substituted, Het or (lower alkyl)-Het; carboxyl; carboxy(lower alkyl); C6 or C10 aryl, C7-14 aralkyl or Het, said aryl, aralkyl or Het being optionally substituted; and R1 is H; C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl, or C2-6 alkynyl, all optionally substituted with halogen; or a pharmaceutically acceptable salt or ester thereof.
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公开(公告)号:US20060089300A1
公开(公告)日:2006-04-27
申请号:US11298443
申请日:2005-12-10
IPC分类号: A61K38/12 , C07K5/12 , A61K31/496
CPC分类号: C07K5/0802 , A61K38/00
摘要: Compounds of formula (I): wherein R1 is (C1-8)alkyl, (C3-7)cycloalkyl, {(C1-6)alkyl-(C3-7)cycloalkyl} or Het, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O—(C1-6)alkyl, amido, amino or phenyl, or R1 is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O—(C1-6)alkyl, amido, amino or phenyl; or a pharmaceutically acceptable salt thereof, useful as an inhibitor of the HCV NS3 protease.
摘要翻译: 式(I)的化合物:其中R 1为(C 1-8 - )烷基,(C 3-7)环烷基,{( C 1-3烷基 - (C 3-7 N)环烷基}或Het,它们都可以任选被卤素,氰基,硝基,O - (C 1-6 - )烷基,酰胺基,氨基或苯基,或R 1是C 6或C 10 - 任选被卤素,氰基,硝基,(C 1-6 - )烷基,O-(C 1-6 - )烷基取代1至3次的芳基, ,酰胺基,氨基或苯基; 或其药学上可接受的盐,可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US20050192212A1
公开(公告)日:2005-09-01
申请号:US11039698
申请日:2005-01-19
申请人: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
发明人: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
CPC分类号: C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
摘要: Compounds of formula (I): wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease.
摘要翻译: 式(I)化合物:其中R 1,R 2,X,R 3,D和虚线b如上所定义 在这里 或其药学上可接受的盐或酯可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US06908901B2
公开(公告)日:2005-06-21
申请号:US10791318
申请日:2004-03-02
IPC分类号: A61K38/00 , C07C235/74 , C07K5/02 , A61K38/16
CPC分类号: C07C235/74 , A61K38/00 , C07C2601/08 , C07C2601/14 , C07K5/0205 , Y02A50/463
摘要: Compounds of formula (I): wherein B, Y, R3, R24, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
摘要翻译: 式(I)化合物:其中B,Y,R 3,R 24,R 2,R 1, >和R“C”在本文中定义。 该化合物可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US06642204B2
公开(公告)日:2003-11-04
申请号:US10353589
申请日:2003-01-29
IPC分类号: A61K3806
CPC分类号: C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
摘要: Disclosed herein are compounds of formula (1): wherein R1 is hydroxy or NHSO2R1A wherein R1A is (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O—(C1-6)alkyl, amido, amino or phenyl, or R1A is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O—(C1-6) alkyl, amido, amino or phenyl; R2 is (C4-6)cycloalkyl; R3 is t-butyl or (C5-6) cycloalkyl and R4 is (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease.
摘要翻译: 本文公开的是式(1)的化合物:其中R 1是羟基或NHSO 2 R 1A,其中R 1A是(C 1-8)烷基,(C 3-7)环烷基或{(C 1-6)烷基 - (C 3-7)环烷基},它们都可以任选被卤素,氰基,硝基,O-(C 1-6)烷基,酰胺基,氨基或苯基取代1至3倍,或者R 1A是C 6或C 10芳基 氰基,硝基,(C 1-6)烷基,O-(C 1-6)烷基,酰胺基,氨基或苯基任选被1-3个取代; R 2是(C 4-6)环烷基; R 3是叔丁基或(C 5-6)环烷基,R 4是(C 4-6)环烷基; 或其药学上可接受的盐。 该化合物可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号:US08541402B2
公开(公告)日:2013-09-24
申请号:US13463093
申请日:2012-05-03
申请人: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
发明人: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
IPC分类号: C07D211/38 , C07D213/643 , C07D213/69 , C07D213/81 , C07D215/227 , C07D217/24 , C07D239/38 , C07D239/47 , C07D239/52 , C07D249/04 , C07D277/24 , C07D307/20 , C07D333/32 , C07D401/06 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , A61K31/444
CPC分类号: A61K31/444 , A61K31/5377 , C07D211/38 , C07D213/643 , C07D213/69 , C07D213/81 , C07D215/227 , C07D217/24 , C07D239/34 , C07D239/38 , C07D239/47 , C07D239/52 , C07D249/04 , C07D277/24 , C07D307/20 , C07D333/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04
摘要: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
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公开(公告)号:US08067438B2
公开(公告)日:2011-11-29
申请号:US13078225
申请日:2011-04-01
申请人: Montse Llinas-Brunet , Murray Douglas Bailey , Punit R. Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida J. Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
发明人: Montse Llinas-Brunet , Murray Douglas Bailey , Punit R. Bhardwaj , Josee Bordeleau , Pasquale Forgione , Elise Ghiro , Vida J. Gorys , Nathalie Goudreau , Sylvie Goulet , Teddy Halmos , Jean Rancourt
IPC分类号: A61K31/04 , C07D215/38
CPC分类号: A61K31/4709 , A61K38/06 , A61K38/212 , C07K5/0808 , C07K5/0827 , Y02A50/463 , A61K2300/00
摘要: Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
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公开(公告)号:US07749961B2
公开(公告)日:2010-07-06
申请号:US11039698
申请日:2005-01-19
申请人: Montse Llinas-Brunet , Murray Bailey , Punit K. Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
发明人: Montse Llinas-Brunet , Murray Bailey , Punit K. Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
IPC分类号: A61K38/12
CPC分类号: C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
摘要: Compounds of formula (I): wherein R1, R2, X, R3, D, and the dotted line b are as defined herein; or a pharmaceutically acceptable salt or ester thereof, are useful as inhibitors of the HCV NS3 protease.
摘要翻译: 式(I)化合物:其中R1,R2,X,R3,D和虚线b如本文所定义; 或其药学上可接受的盐或酯可用作HCV NS3蛋白酶的抑制剂。
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