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1. 发明申请

US20120171157A1 Macrocyclic Inhibitors Of Hepatitis C Virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
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。

2. 发明授权

US08153800B2 Macrocyclic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
公开(公告)号：US08153800B2
公开(公告)日：2012-04-10
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 , Karl Magnus Nilsson , Bengt Bertril Samuelsson , Asa Annica Kristina Rosenquist
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Karl Magnus Nilsson , Bengt Bertril Samuelsson , Asa Annica Kristina Rosenquist
IPC分类号： C07D215/00 , C07D277/00 , C07C211/00
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。

3. 发明申请

US20090118312A1 Macrocylic Inhibitors of Hepatitis C Virus 有权
标题翻译：丙型肝炎病毒的大胆抑制剂
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

4. 发明授权

US08012939B2 Macrocyclic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
公开(公告)号：US08012939B2
公开(公告)日：2011-09-06
申请号：US11995714
申请日：2006-07-28
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Hans Kristian Wallberg
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Hans Kristian Wallberg
IPC分类号： A61K38/05 , C07D245/00
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14 , C07D487/04 , C07K5/06191
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each variable has specific definitions. Pharmaceutical compositions containing compounds (I) and process for preparing compounds (I) are also provided. Bioavailable combinations of the inhibitors of HCV of Formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV复制抑制剂及其N-氧化物，盐和立体异构体，其中每个变量具有特定定义。还提供了含有化合物（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。

5. 发明申请

US20090105302A1 Macrocylic Inhibitors of Hepatitis C Virus 有权
标题翻译：丙型肝炎病毒的大胆抑制剂
公开(公告)号：US20090105302A1
公开(公告)日：2009-04-23
申请号：US11995827
申请日：2006-07-28
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Oden , Susana Ayesa Alvarez , Bjorn Olof Classon
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Oden , Susana Ayesa Alvarez , Bjorn Olof Classon
IPC分类号： A61K31/427 , A61P31/14 , C07D401/12 , A61K31/4523 , A61K31/407 , C07D417/12 , A61K31/4155 , A61K31/395
CPC分类号： C07D401/12 , C07D225/04 , C07D245/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; 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; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 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 or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1-3 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复制抑制剂及其N-氧化物，盐或立体异构体，其中每个虚线（由 - - - - 表示）表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR6，-NH-SO2R7; 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; n为3,4,5或6; R 4和R 5彼此独立地是氢，卤素，羟基，硝基，氰基，羧基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6烷基羰基，C 1-6烷氧基羰基，氨基，叠氮基，巯基， C 1-6烷硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R6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; R7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; 芳基是苯基或萘基，各自任选被1-3个取代基取代; Het是含有1-4个杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，各自独立地选自N，O或S，并且任选被1-3个取代基取代; 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。

6. 发明申请

US20080200503A1 Macrocylic Inhibitors Of Hepatitis C Virus 有权
标题翻译：丙型肝炎病毒的巨噬细胞抑制剂
公开(公告)号：US20080200503A1
公开(公告)日：2008-08-21
申请号：US11995888
申请日：2006-07-27
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Mats Stefan Lindstrom , Pia Cecilia Kahnberg , Dmitry Antonov , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Mats Stefan Lindstrom , Pia Cecilia Kahnberg , Dmitry Antonov , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist
IPC分类号： A61K31/4709 , C07D401/14
CPC分类号： A61K31/4709 , C07K5/06165 , Y02A50/385 , Y02A50/387
摘要： Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV抑制剂。和其N-氧化物，盐和立体异构体，其中虚线表示原子C7和C8之间任选的双键; R 1为氢或C 1-6烷基; R 2是氢或C 1-6烷基; n为3,4,5或6; 提供含有化合物（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。

7. 发明申请

US20110295012A1 Macrocyclic Inhibitors Of Hepatitis C Virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
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。

8. 发明授权

US08754105B2 Macrocyclic inhibitors of hepatitis C virus 有权
公开(公告)号：US08754105B2
公开(公告)日：2014-06-17
申请号：US13109395
申请日：2011-05-17
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Rabiosson , Abdellah Tahri , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Rabiosson , Abdellah Tahri , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07D487/04 , C07D413/12
摘要： Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(═O)—, —O—C(═O)—NR4a— or —O—C(═O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(═O)OR5, —C(═O)R6, —C(═O)NR4aR4b, —C(═O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl; n is 3, 4, 5, or 6; p is 1 or 2; aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be 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 each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be 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.

9. 发明申请

US20090247512A1 MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译： HEPATITIS C病毒的大肠抑制剂
公开(公告)号：US20090247512A1
公开(公告)日：2009-10-01
申请号：US11995869
申请日：2008-01-16
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Susana Ayesa Alvarez , Bjorn Olof Classon , Hans Kristian Wallberg
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Carl Erik Daniel Jonsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Susana Ayesa Alvarez , Bjorn Olof Classon , Hans Kristian Wallberg
IPC分类号： A61K31/427 , C07D245/04 , A61K31/4709 , A61K31/538 , A61P31/04
CPC分类号： C07D403/12 , C07D401/12 , C07D413/12 , C07D487/04
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, 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 —OR6, —NH—SO2R7; 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; n is 3, 4, 5, or 6; R4 and R5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from wherein said ring system may optionally be substituted with 1-3 substituents; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 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 or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from N, O or S, and being optionally substituted with 1-3 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复制抑制剂及其N-氧化物，盐或立体异构体，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-OR6，-NH-SO2R7; 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; n为3,4,5或6; R4和R5与它们所连接的氮原子一起形成双环体系，其选自其中所述环系可以任选被1-3个取代基取代; R6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; R7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; 芳基是苯基或萘基，每个可以任选被1-3个取代基取代; Het是含有1至4个独立地选自N，O或S的杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，并且任选被1-3个取代基取代，含有化合物（I）的药物组合物和制备化合物（I）。还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

10. 发明申请

US20090062311A1 MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译： HEPATITIS C病毒的大肠抑制剂
公开(公告)号：US20090062311A1
公开(公告)日：2009-03-05
申请号：US11995835
申请日：2008-01-16
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Raboisson , Lili Hu , Dominique Louis Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Lourdes Salvador Oden
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Raboisson , Lili Hu , Dominique Louis Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Lourdes Salvador Oden
IPC分类号： A61K31/517 , C07D255/04 , C07D245/04 , A61P31/12 , A61K31/4709
CPC分类号： C07D487/04 , C07D245/04 , C07K5/06139
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which may be optionally substituted; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(═O)—NR5a— or —O—C(═O)—NR5a—C1-4alkanediyl-; 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, amino, mono- or diC1-6alkylamino; R4 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from O, S and N, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted; n is 3, 4, 5, or 6; p is 1 or 2; aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be optionally substituted with one, two or three substituents; and Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S, being optionally condensed with a benzene ring, and wherein Het may be optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：式（I）的HCV复制抑制剂及其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，为C; R 1a和R 1b是氢，C 3-7环烷基，芳基，Het，C 1-6烷氧基，任选被卤素，C 1-6烷氧基，氰基，多卤代C 1-6烷氧基，C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 或R 1a和R 1b与它们所连接的氮一起形成可任选被取代的4至6元杂环; L是直接键，-O - ， - O-C 1-4烷二基 - ， - O-CO - ， - O-C（-O）-NR 5a - 或-O-C（-O）-NR 5a -C 1-4烷二基 - 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，氨基，单或二C 1-6烷基氨基; R4是芳基或饱和的，部分不饱和的或完全不饱和的5或6元单环或9至12元双环杂环体系，其中所述环体系含有一个氮，以及任选地一至三个选自O，S和N的杂原子，并且其中剩余的环成员是碳原子; 其中所述环系可以任选地被取代; n为3,4,5或6; p为1或2; 芳基是苯基，萘基，茚满基或1,2,3,4-四氢萘基，其各自可以任选地被一个，两个或三个取代基取代; 并且Het是含有1至4个选自N，O和S的杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，任选地与苯环稠合，并且其中Het可以任选被一个，两个或三个取代基; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

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