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公开(公告)号：US20100041728A1
公开(公告)日：2010-02-18
申请号：US12526085
申请日：2008-02-08
申请人： Dmitry Antonov , Susana Ayesa Alvarez , Anna Karin Gertrud Linnea Belfrage , Carl Erik Daniel Jönsson , David Craig Mc Gowan , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bengt Bertil Samuelsson
发明人： Dmitry Antonov , Susana Ayesa Alvarez , Anna Karin Gertrud Linnea Belfrage , Carl Erik Daniel Jönsson , David Craig Mc Gowan , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bengt Bertil Samuelsson
IPC分类号： A61K31/407 , C07D245/04 , A61K31/33 , A61P31/12
CPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
摘要： Compounds of the formula 1: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译： 式1的化合物：包括其立体异构体或N-氧化物，药学上可接受的加成盐或其药学上可接受的加成溶剂合物; 用作HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。
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公开(公告)号：US08383584B2
公开(公告)日：2013-02-26
申请号：US12526085
申请日：2008-02-08
申请人： Dmitry Antonov , Susana Ayesa Alvarez , Anna Karin Gertrud Linnea Belfrage , Carl Erik Daniel Jönsson , David Craig McGowan , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bengt Bertil Samuelsson
发明人： Dmitry Antonov , Susana Ayesa Alvarez , Anna Karin Gertrud Linnea Belfrage , Carl Erik Daniel Jönsson , David Craig McGowan , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bengt Bertil Samuelsson
CPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
摘要： Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译： 式I化合物：包括其立体异构体或N-氧化物，药学上可接受的加成盐或其药学上可接受的加成溶剂合物; 用作HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。
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公开(公告)号：US07659245B2
公开(公告)日：2010-02-09
申请号：US11995900
申请日：2006-07-28
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Karin Charlotta Lindquist , Mats Stefan Lindström , Anna Karin Gertrud Linnea Belfrage , Horst Jürgen Wähling , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Sven Crister Sahlberg , Hans Kristian Wallberg , Pia Cecilia Kahnberg , Björn Olof Classon
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Karin Charlotta Lindquist , Mats Stefan Lindström , Anna Karin Gertrud Linnea Belfrage , Horst Jürgen Wähling , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Sven Crister Sahlberg , Hans Kristian Wallberg , Pia Cecilia Kahnberg , Björn Olof Classon
IPC分类号： A61K38/00
CPC分类号： C07D487/10 , C07D245/04
摘要： Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(═O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.
摘要翻译： 式I的化合物及其N-氧化物，盐和立体异构体，其中A是OR 1，NHS（-O）p R 2; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3亚烷基环羰基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3亚烷基环羰基，C 0 -C 3亚烷基杂环基; p独立地为1或2; n为3,4,5或6; “img id =”CUSTOM-CHARACTER-00001“he =”2.46mm“wi =”5.25mm“file =”US07659245-20100209-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>表示可选的双键; L为N或CRz; Rz是H或与星号碳形成双键; Rq为H或当L为CRz时，Rq也可为C1-C6烷基; Rr是喹唑啉基，任选地被一个两个或三个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，卤素，卤代C 1 -C 6烷基，氨基，单或二烷基氨基，单或二烷基氨基羰基，C 1 -C 6烷基 - 羰基氨基 ，C 0 -C 3亚烷基环基和C 0 -C 3亚烷基杂环基; R 5是氢，C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C 7环烷基; R 6是氢，C 1 -C 6烷基，C 1 -C 6烷氧基，C 0 -C 3亚烷基环基，C 0 -C 3亚烷基 - 杂环基，羟基，溴，氯或氟可用于治疗或预防黄病毒感染如HCV。
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公开(公告)号：US20100113440A1
公开(公告)日：2010-05-06
申请号：US12526553
申请日：2008-02-08
申请人： Anna Karin Gertrud Linnea Belfrage , Björn Olof Classon , Karin Charlotta Lindquist , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bertil Bengt Samuelsson , Horst Jürgen Wähling
发明人： Anna Karin Gertrud Linnea Belfrage , Björn Olof Classon , Karin Charlotta Lindquist , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bertil Bengt Samuelsson , Horst Jürgen Wähling
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/395 , C07D245/04 , C07D413/14 , C07D403/12
CPC分类号： C07K5/06165 , A61K38/00 , C07D403/12 , Y02A50/385 , Y02A50/387
摘要： Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译： 包括其立体异构体或N-氧化物的式（I）化合物，其药学上可接受的加成盐或其药学上可接受的加成溶剂合物; 用作HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。
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公开(公告)号：US08937080B2
公开(公告)日：2015-01-20
申请号：US12526553
申请日：2008-02-08
申请人： Pierre Jean-Marie Bernard Raboisson , Anna Karin Gertrud Linnea Belfrage , Björn Olof Classon , Karin Charlotta Lindquist , Karl Magnus Nilsson , Åsa Annica Kristina Rosenquist , Bertil Bengt Samuelsson , Horst Jürgen Wähling
发明人： Pierre Jean-Marie Bernard Raboisson , Anna Karin Gertrud Linnea Belfrage , Björn Olof Classon , Karin Charlotta Lindquist , Karl Magnus Nilsson , Åsa Annica Kristina Rosenquist , Bertil Bengt Samuelsson , Horst Jürgen Wähling
IPC分类号： A61K31/506 , C07D245/02 , C07K5/078 , C07D403/12 , A61K38/00
CPC分类号： C07K5/06165 , A61K38/00 , C07D403/12 , Y02A50/385 , Y02A50/387
摘要： Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译： 式I化合物：包括其立体异构体或N-氧化物，药学上可接受的加成盐或其药学上可接受的加成溶剂合物; 用作HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。
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公开(公告)号：US20090281140A1
公开(公告)日：2009-11-12
申请号：US11632102
申请日：2006-07-28
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelson , Åsa Annica Kristina Rosenquist , Vladimir Ivanov , Michael Pelcman , Anna Karin Gertrud Linnea Belfrage , Per-Ola Mikael Johansson , Sandrine Marie Helene Vendeville
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelson , Åsa Annica Kristina Rosenquist , Vladimir Ivanov , Michael Pelcman , Anna Karin Gertrud Linnea Belfrage , Per-Ola Mikael Johansson , Sandrine Marie Helene Vendeville
IPC分类号： A61K31/4709 , C07D245/00 , A61P31/12
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译： 式（I）的HCV复制抑制剂和N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR7，-NH-SO2R8; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 3-7环烷基; R4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R6是C1-6烷氧基或二甲基氨基; R7是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R8是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。 含有化合物（I）的药物组合物和制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。
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公开(公告)号：US20090118312A1
公开(公告)日：2009-05-07
申请号：US11995900
申请日：2006-07-28
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Karin Charlotta Lindquist , Mats Stefan Lindstrom , Anna Karin Gertrud Linnea Belfrage , Horst Jurgen Wahling , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Sven Crister Sahlberg , Hans Kristian Wallberg , Pia Cecilia Kahnberg , Bjorn Olof Classon
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Karin Charlotta Lindquist , Mats Stefan Lindstrom , Anna Karin Gertrud Linnea Belfrage , Horst Jurgen Wahling , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Sven Crister Sahlberg , Hans Kristian Wallberg , Pia Cecilia Kahnberg , Bjorn Olof Classon
IPC分类号： A61K31/517 , C07D403/12 , A61P31/12
CPC分类号： C07D487/10 , C07D245/04
摘要： Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(═O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; — denotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV
摘要翻译： 式I的化合物及其N-氧化物，盐和立体异构体，其中A是OR 1，NHS（-O）p R 2; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3亚烷基环羰基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3亚烷基环羰基，C 0 -C 3亚烷基杂环基; p独立地为1或2; n为3,4,5或6; -
表示任选的双键; L为N或CRz; Rz是H或与星号碳形成双键; Rq为H或当L为CRz时，Rq也可为C1-C6烷基; Rr是喹唑啉基，任选地被一个两个或三个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，卤素，卤代C 1 -C 6烷基，氨基，单或二烷基氨基，单或二烷基氨基羰基，C 1 -C 6烷基 - 羰基氨基 ，C 0 -C 3亚烷基环基和C 0 -C 3亚烷基杂环基; R 5是氢，C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C 7环烷基; R 6是氢，C 1 -C 6烷基，C 1 -C 6烷氧基，C 0 -C 3亚烷基环羰基，C 0 -C 3亚烷基 - 杂环基，羟基，溴，氯或氟可用于治疗或预防黄病毒感染如HCV
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公开(公告)号：US20110295012A1
公开(公告)日：2011-12-01
申请号：US13197226
申请日：2011-08-03
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Abdellah Tahri , Dominque Louis Nestor Ghislai Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Vladimir Ivanov , Michael Pelcman , Anna Karin Gertrud Linnea Belfrage , Per-Ola Mikael Johansson , Sandrine Marie Helene Vendeville
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Abdellah Tahri , Dominque Louis Nestor Ghislai Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Vladimir Ivanov , Michael Pelcman , Anna Karin Gertrud Linnea Belfrage , Per-Ola Mikael Johansson , Sandrine Marie Helene Vendeville
IPC分类号： C07D417/04 , C07C225/22 , C07D277/56
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7 or —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译： 式（I）的HCV复制抑制剂和N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR7或-NH-SO2R8; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基或C 3-7环烷基; R4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R6是C1-6烷氧基或二甲基氨基; R7是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R8是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。 含有化合物（I）的药物组合物和制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。
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公开(公告)号：US20120171157A1
公开(公告)日：2012-07-05
申请号：US13412997
申请日：2012-03-06
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Karl Magnus Nilsson , Bengt Bertril Samuelsson , Asa Annica Kristina Rosenquist , Vladimir Ivanov , Michael Pelcman , Anna Karin Gertrud Linnea Belfrage , Per-Ola Mikael Johansson , Sandrine Marie Helene Vendeville
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Karl Magnus Nilsson , Bengt Bertril Samuelsson , Asa Annica Kristina Rosenquist , Vladimir Ivanov , Michael Pelcman , Anna Karin Gertrud Linnea Belfrage , Per-Ola Mikael Johansson , Sandrine Marie Helene Vendeville
IPC分类号： A61K31/4709 , A61K31/7056 , C07D487/04 , A61K38/21 , C07D417/14 , A61P31/14
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译： 式（I）的HCV复制抑制剂和N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR7，-NH-SO2R8; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 3-7环烷基; R4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R6是C1-6烷氧基或二甲基氨基; R7是氢; 芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R8是芳基; Het; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。 含有化合物（I）的药物组合物和制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。
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