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。

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

公开(公告)号：US20090281141A1

公开(公告)日：2009-11-12

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 ,  Åsa 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 ,  Åsa Annica Kristina Rosenquist ,  Hans Kristian Wallberg

IPC分类号： A61K31/4709 ,  C07D245/00 ,  A61P31/12

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 X is N, CH and where X bears a double bond it is C; R1 is —OR1, —NH—SO2R6; 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 isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhaloC1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or diC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by - - - - - ) represents an optional double bond; R5 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R6 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each 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, 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复制抑制剂及其N-氧化物，盐和立体异构体，其中X为N，CH，X为双键时为C; R1为-OR1，-NH-SO2R6; 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; R 4是任选被一个，两个或三个独立地选自C 1-6烷基，C 1-6烷氧基，羟基，卤素，多卤代C 1-6烷基，多卤代C 1-6烷氧基，氨基，单或二C 1-6烷基氨基，单或二-C 1-6烷基， C 1-6烷基氨基羰基，C 1-6烷基羰基 - 氨基，芳基和Het; n为3,4,5或6; 每个虚线（由 - - - - 表示）表示可选的双键; R5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; R6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; 每个芳基是任选被一个，两个或三个取代基取代的苯基; 并且每个Het是含有1至4个各自独立地选自氮，氧和硫的杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，并且任选地被一个，两个或三个取代基取代; 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。

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。

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。

公开(公告)号：US09023808B2

公开(公告)日：2015-05-05

申请号：US11995869

申请日：2008-01-16

申请人： Kenneth Alan Simmen ,  Herman Agustinus De Kock ,  Carl Erik Daniel Jonsson ,  Karl Magnus Milsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Susana Ayesa Alverez ,  Bjorn Olaf Classon ,  Hans Kristian Wallberg

发明人： Kenneth Alan Simmen ,  Herman Agustinus De Kock ,  Carl Erik Daniel Jonsson ,  Karl Magnus Milsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Susana Ayesa Alverez ,  Bjorn Olaf Classon ,  Hans Kristian Wallberg

IPC分类号： A61K38/12 ,  C07D245/00 ,  C07K5/12 ,  C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D487/04

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 the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.

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，其中虚线，X，R 1，R 2，R 3，R 4，R 5，R 6和R 7具有定义的含义; 其制备方法 包含式（I）化合物的组合物，包括与利托那韦的生物可利用组合; 及其药物用途。

公开(公告)号：US08592429B2

公开(公告)日：2013-11-26

申请号：US13515187

申请日：2010-12-10

申请人： Genadiy Kalayanov ,  Bart Rudolf Romanie Kesteleyn ,  Kevin Parkes ,  Bengt Bertil Samuelsson ,  Wim Bert Griet Schepens ,  Johannes Wilhelmus J. Thuring ,  Hans Kristian Wallberg ,  Jörg Kurt Wegner

发明人： Genadiy Kalayanov ,  Bart Rudolf Romanie Kesteleyn ,  Kevin Parkes ,  Bengt Bertil Samuelsson ,  Wim Bert Griet Schepens ,  Johannes Wilhelmus J. Thuring ,  Hans Kristian Wallberg ,  Jörg Kurt Wegner

IPC分类号： A61K31/18 ,  A61K31/17 ,  A61K31/325 ,  A61K31/38 ,  A61K31/42 ,  A61K31/44 ,  A61K31/495

CPC分类号： C07D213/64 ,  C07D213/74 ,  C07D277/30 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D493/04

摘要： HIV inhibitors of formula (I) wherein R1 is halo, C1-4 alkoxy, trifluoromethoxy; R2 is a group of formula (A); R3 is a group of formula (B); R4 is a group of formula (C); n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4 allyl, halo; R7 and R8 are C1-4 allyl or C1-4 alkoxy-C1-4 alkyl; R9 is C1-4 allyl, cyclopropyl, trifluoromethyl, C1-4 alkoxy, or dimethylamino; R10 is hydrogen, C1-4 alkyl, cyclopropyl, trifluoromethyl, C1-4 alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.

摘要翻译： 式（I）的HIV抑制剂，其中R 1是卤素，C 1-4烷氧基，三氟甲氧基; R2是式（A）的基团; R3是式（B）的基团; R4是式（C）的基团; n为0或1; A是CH或N; R5和R6是氢，C1-4烷基，卤素; R 7和R 8是C 1-4烯丙基或C 1-4烷氧基-C 1-4烷基; R 9为C 1-4烯丙基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; R 10是氢，C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; 其药学上可接受的加成盐和溶剂合物; 含有这些化合物作为活性成分的药物组合物和制备所述化合物的方法。

公开(公告)号：US20120295920A1

公开(公告)日：2012-11-22

申请号：US13515187

申请日：2010-12-10

申请人： Genadiy Kalayanov ,  Bart Rudolf Romanie Kesteleyn ,  Kevin Parkes ,  Bengt Bertil Samuelsson ,  Wim Bert Griet Schepens ,  Johannes Wilhelmus J. Thuring ,  Hans Kristian Wallberg ,  Jörg Kurt Wegner

发明人： Genadiy Kalayanov ,  Bart Rudolf Romanie Kesteleyn ,  Kevin Parkes ,  Bengt Bertil Samuelsson ,  Wim Bert Griet Schepens ,  Johannes Wilhelmus J. Thuring ,  Hans Kristian Wallberg ,  Jörg Kurt Wegner

IPC分类号： A61K31/4433 ,  C07D213/64 ,  A61K31/4418 ,  C07D409/12 ,  A61K31/4436 ,  C07D417/12 ,  A61K31/427 ,  C07D405/14 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  C07D493/04 ,  A61K31/443 ,  A61P31/18 ,  C07D405/12

CPC分类号： C07D213/64 ,  C07D213/74 ,  C07D277/30 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D493/04

摘要： HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.

摘要翻译： 下式的HIV抑制剂其中R1是卤素，C1-4烷氧基，三氟甲氧基; n为0或1; A是CH或N; R5和R6是氢，C1-4烷基，卤素; R 7和R 8是C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 9为C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; R 10是氢，C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; 其药学上可接受的加成盐和溶剂合物; 含有这些化合物作为活性成分的药物组合物和制备所述化合物的方法。