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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
Applicant: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
Inventor: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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
Applicant: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
Inventor: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
IPC: 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 classification number: 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
Abstract: 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.
Abstract translation: 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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23.
公开(公告)号:US20060089300A1
公开(公告)日:2006-04-27
申请号:US11298443
申请日:2005-12-10
Applicant: Montse Llinas-Brunet , Murray Bailey
Inventor: Montse Llinas-Brunet , Murray Bailey
IPC: A61K38/12 , C07K5/12 , A61K31/496
CPC classification number: C07K5/0802 , A61K38/00
Abstract: 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.
Abstract translation: 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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24.
公开(公告)号:US20050192212A1
公开(公告)日:2005-09-01
申请号:US11039698
申请日:2005-01-19
Applicant: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
Inventor: Montse Llinas-Brunet , Murray Bailey , Punit Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
CPC classification number: C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
Abstract: 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.
Abstract translation: 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:US06642204B2
公开(公告)日:2003-11-04
申请号:US10353589
申请日:2003-01-29
Applicant: Montse Llinas-Brunet , Vida J. Gorys
Inventor: Montse Llinas-Brunet , Vida J. Gorys
IPC: A61K3806
CPC classification number: C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
Abstract: 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.
Abstract translation: 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
Applicant: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
Inventor: Pierre L. Beaulieu , Pasquale Forgione , Alexandre Gagnon , Cedrickx Godbout , Marc-Andre Joly , Montse Llinas-Brunet , Julie Naud , Martin Poirier , Jean Rancourt
IPC: 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 classification number: 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
Abstract: 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
Applicant: 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
Inventor: 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: A61K31/04 , C07D215/38
CPC classification number: A61K31/4709 , A61K38/06 , A61K38/212 , C07K5/0808 , C07K5/0827 , Y02A50/463 , A61K2300/00
Abstract: 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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28.
公开(公告)号:US07749961B2
公开(公告)日:2010-07-06
申请号:US11039698
申请日:2005-01-19
Applicant: Montse Llinas-Brunet , Murray Bailey , Punit K. Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
Inventor: Montse Llinas-Brunet , Murray Bailey , Punit K. Bhardwaj , Francois Bilodeau , Pasquale Forgione , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Jean Rancourt
IPC: A61K38/12
CPC classification number: C07K5/0808 , A61K38/00 , C07K5/0812 , C07K5/0827
Abstract: 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.
Abstract translation: 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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29.
公开(公告)号:US20050075279A1
公开(公告)日:2005-04-07
申请号:US10686755
申请日:2003-10-16
Applicant: Montse Llinas-Brunet , Murray Bailey
Inventor: Montse Llinas-Brunet , Murray Bailey
CPC classification number: C07K5/0802 , A61K38/00
Abstract: 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.
Abstract translation: 式(I)化合物:其中R 1为(C 1-8)烷基,(C 3-7)环烷基,{(C 1-6)烷基 - (C 3-7)环烷基}或Het, 卤素,氰基,硝基,O-(C 1-6)烷基,酰氨基,氨基或苯基,或R 1是任选被卤素取代1至3次的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; 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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30.
公开(公告)号:US06608027B1
公开(公告)日:2003-08-19
申请号:US09760946
申请日:2001-01-16
Applicant: Youla S. Tsantrizos , Dale R. Cameron , Anne-Marie Faucher , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet
Inventor: Youla S. Tsantrizos , Dale R. Cameron , Anne-Marie Faucher , Elise Ghiro , Nathalie Goudreau , Teddy Halmos , Montse Llinas-Brunet
IPC: A61K3805
CPC classification number: C07K5/06139 , A61K38/00 , C07K5/0802
Abstract: The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. wherein W, R21, R22, R3, R4, D and A are as defined herein, or a pharmaceutically acceptable salts or ester thereof.
Abstract translation: 本发明包括在体外和在针对丙型肝炎病毒的NS3蛋白酶的细胞测定中的式I的大环化合物。其中W,R 21,R 22,R 3,R 4,D和A如本文所定义,或药学上可接受的 盐或酯。
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