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公开(公告)号:US08354429B2
公开(公告)日:2013-01-15
申请号:US12742997
申请日:2008-09-11
Applicant: Youla S. Tsantrizos , Murray D. Bailey , Francois Bilodeau , Rebekah J. Carson , Rene Coulombe , Lee Fader , Teddy Halmos , Stephen Kawai , Serge Landry , Steven LaPlante , Sebastien Morin , Mathieu Parisien , Marc-Andre Poupart , Bruno Simoneau
Inventor: Youla S. Tsantrizos , Murray D. Bailey , Francois Bilodeau , Rebekah J. Carson , Rene Coulombe , Lee Fader , Teddy Halmos , Stephen Kawai , Serge Landry , Steven LaPlante , Sebastien Morin , Mathieu Parisien , Marc-Andre Poupart , Bruno Simoneau
IPC: C07D215/14 , C07D401/04 , A61K31/47 , A61K31/4709
CPC classification number: C07D215/14 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4741 , A61K31/538 , A61K31/5383 , C07D215/18 , C07D221/16 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D491/06 , C07D498/06
Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.
Abstract translation: 式I化合物(其中R 4,R 6和R 7在本文中定义)可用作HIV复制的抑制剂。
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公开(公告)号:US20110028464A1
公开(公告)日:2011-02-03
申请号:US12743138
申请日:2008-11-03
Applicant: Youla S. Tsantrizos , Murray D. Bailey , François Bilodeau , Rebekah J. Carson , Lee Fader , Teddy Halmos , Stephen Kawai , Serge R. Landry , Steven Laplante , Bruno Simoneau
Inventor: Youla S. Tsantrizos , Murray D. Bailey , François Bilodeau , Rebekah J. Carson , Lee Fader , Teddy Halmos , Stephen Kawai , Serge R. Landry , Steven Laplante , Bruno Simoneau
IPC: A61K31/538 , C07D413/14 , A61P31/18 , C07D405/10 , A61K31/4709 , C07D491/06 , A61K31/4741 , A61K31/506 , C07D405/14 , A61K31/496
CPC classification number: C07D413/14 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/48 , C07D401/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/12 , C07D417/14 , C07D491/04
Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.
Abstract translation: 式I化合物:其中c,R 2,R 3,R 4,R 5,R 6,R 7和R 8在本文中定义,可用作HIV复制的抑制剂。
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公开(公告)号:US08338441B2
公开(公告)日:2012-12-25
申请号:US12777406
申请日:2010-05-11
Applicant: Christiane Yoakim , Murray Bailey , Francois Bilodeau , Rebekah Carson , Lee Fader , Stephen Kawai , Sebastien Morin , Carl Thibeault , Bruno Simoneau , Simon Surprenant , Youla Tsantrizos , Steven Laplante
Inventor: Christiane Yoakim , Murray Bailey , Francois Bilodeau , Rebekah Carson , Lee Fader , Stephen Kawai , Sebastien Morin , Carl Thibeault , Bruno Simoneau , Simon Surprenant , Youla Tsantrizos , Steven Laplante
IPC: A01N43/40 , A61K31/435
CPC classification number: C07D213/81 , A61K31/4375 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4741 , A61K31/501 , A61K31/506 , A61K31/538 , A61K31/5383 , A61K45/06 , C07D213/55 , C07D401/12 , C07D405/10 , C07D405/14 , C07D411/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D491/06 , C07D498/06
Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
Abstract translation: 式I化合物:其中a,R 1,R 2,R 3,R 4,R 5和R 6在本文中定义,可用作HIV复制的抑制剂。
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公开(公告)号:US20100311735A1
公开(公告)日:2010-12-09
申请号:US12742997
申请日:2008-09-11
Applicant: Youla S. Tsantrizos , Murray D. Bailey , Francois Bilodeau , Rene Coulombe , Teddy Halmos , Stephen Kawai , Serge R. Landry , Steven LaPlante , Sebastien Morin , Marc-Andre Poupart , Bruno Simoneau , Lee Fader , Rebekah J. Carson , Mathieu Parisien
Inventor: Youla S. Tsantrizos , Murray D. Bailey , Francois Bilodeau , Rene Coulombe , Teddy Halmos , Stephen Kawai , Serge R. Landry , Steven LaPlante , Sebastien Morin , Marc-Andre Poupart , Bruno Simoneau , Lee Fader , Rebekah J. Carson , Mathieu Parisien
IPC: A61K31/5383 , C07D215/14 , A61K31/47 , C07D405/10 , A61K31/4709 , C07D401/10 , C07D491/16 , A61K31/4741 , C07D413/10 , A61K31/538 , C07D498/06 , A61P31/18
CPC classification number: C07D215/14 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4741 , A61K31/538 , A61K31/5383 , C07D215/18 , C07D221/16 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D491/06 , C07D498/06
Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.
Abstract translation: 式I化合物(其中R 4,R 6和R 7在本文中定义)可用作HIV复制的抑制剂。
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公开(公告)号:US20100292227A1
公开(公告)日:2010-11-18
申请号:US12777406
申请日:2010-05-11
Applicant: CHRISTIANE YOAKIM , MURRAY BAILEY , FRANCOIS BILODEAU , REBEKAH CARSON , LEE FADER , STEPHEN KAWAI , SEBASTIEN MORIN , CARL THIBEAULT , BRUNO SIMONEAU , SIMON SURPRENANT , YOULA TSANTRIZOS , STEVEN LAPLANTE
Inventor: CHRISTIANE YOAKIM , MURRAY BAILEY , FRANCOIS BILODEAU , REBEKAH CARSON , LEE FADER , STEPHEN KAWAI , SEBASTIEN MORIN , CARL THIBEAULT , BRUNO SIMONEAU , SIMON SURPRENANT , YOULA TSANTRIZOS , STEVEN LAPLANTE
IPC: A61K31/5383 , C07D405/02 , A61K31/4433 , C07D401/14 , A61K31/444 , C07D401/10 , A61K31/4439 , A61K31/506 , A61K31/501 , C07D413/12 , C07D417/02 , C07D413/02 , A61K31/538 , A61K31/4741 , C07D491/16 , C07D401/02 , A61K31/4709 , C07D417/12 , C07D498/16 , A61P31/18
CPC classification number: C07D213/81 , A61K31/4375 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4741 , A61K31/501 , A61K31/506 , A61K31/538 , A61K31/5383 , A61K45/06 , C07D213/55 , C07D401/12 , C07D405/10 , C07D405/14 , C07D411/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D491/06 , C07D498/06
Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
Abstract translation: 式I化合物:其中a,R 1,R 2,R 3,R 4,R 5和R 6在本文中定义,可用作HIV复制的抑制剂。
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6.Hepatitis C virus NS5B polymerase inhibitor binding pocket 有权
Title translation: 丙型肝炎病毒NS5B聚合酶抑制剂结合口袋公开(公告)号:US20050003348A1
公开(公告)日:2005-01-06
申请号:US10842046
申请日:2004-05-07
Applicant: Rene Coulombe , Pierre Beaulieu , Eric Jolicoeur , George Kukolj , Steven Laplante , Marc-Andre Poupart
Inventor: Rene Coulombe , Pierre Beaulieu , Eric Jolicoeur , George Kukolj , Steven Laplante , Marc-Andre Poupart
CPC classification number: C07K14/005 , C07K2299/00 , C12N9/127 , C12N2770/24222
Abstract: The HCV NS5B polymerase, when complexed with certain inhibitors, adopts a conformation in which the finger loop region defined by amino acid residues 18 to 35 is displaced to expose a binding pocket defined generally by amino acid residues 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 496, 500 and 503. This newly exposed binding pocket defines a novel target in the search of further chemical entities which are capable of binding to HCV NS5B and modulating, or preferably inhibiting, the polymerase activity of HCV NS5B.
Abstract translation: 当与某些抑制剂复合时,HCV NS5B聚合酶采用构象,其中由氨基酸残基18至35限定的指环区域被置换以暴露通常由氨基酸残基392,339,395,396,399定义的结合口袋 ,424,425,428,429,492,493,494,495,496,500和503.这个新近暴露的结合口袋定义了一种新的靶标,用于寻找其他能够结合HCV NS5B的化学实体, 或优选抑制HCV NS5B的聚合酶活性。
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7.Hepatitis C Virus NS5B polymerase inhibitor binding pocket 有权
Title translation: 丙型肝炎病毒NS5B聚合酶抑制剂结合口袋公开(公告)号:US07386398B2
公开(公告)日:2008-06-10
申请号:US10842046
申请日:2004-05-07
Applicant: René Coulombe , Pierre Beaulieu , Eric Jolicoeur , George Kukolj , Steven Laplante , Marc-André Poupart
Inventor: René Coulombe , Pierre Beaulieu , Eric Jolicoeur , George Kukolj , Steven Laplante , Marc-André Poupart
CPC classification number: C07K14/005 , C07K2299/00 , C12N9/127 , C12N2770/24222
Abstract: The HCV NS5B polymerase, when complexed with certain inhibitors, adopts a conformation in which the finger loop region defined by amino acid residues 18 to 35 is displaced to expose a binding pocket defined generally by amino acid residues 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 496, 500 and 503. This newly exposed binding pocket defines a novel target in the search of further chemical entities which are capable of binding to HCV NS5B and modulating, or preferably inhibiting, the polymerase activity of HCV NS5B.
Abstract translation: 当与某些抑制剂复合时,HCV NS5B聚合酶采用构象,其中由氨基酸残基18至35限定的指环区域被置换以暴露通常由氨基酸残基392,339,395,396,399定义的结合口袋 ,424,425,428,429,492,493,494,495,496,500和503.这个新近暴露的结合口袋定义了一种新的靶标,用于寻找其他能够结合HCV NS5B的化学实体, 或优选抑制HCV NS5B的聚合酶活性。
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