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1. 发明申请

WO2007014923A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014923A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064817
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , AYESA ALVAREZ, Susana , CLASSON, Björn Olof , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , WALLBERG, Hans Kristian
发明人： DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , AYESA ALVAREZ, Susana , CLASSON, Björn Olof , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , WALLBERG, Hans Kristian
IPC分类号： C07D401/12 , C07D403/12 , C07D413/12 , A61K31/538 , A61P31/14
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; R 1 is -OR 6 , -NH-SO 2 R 7 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, or C 3-7 cycloalkyl; n is 3, 4, 5, or 6; R 4 and R 5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from formula (II) wherein said ring system may optionally be substituted with 1-3 substituents; R 6 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 7 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, 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; R 1是-OR 6，-NH-SO 2 R 7， R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，或 ç_{3-7 环烷基; n为3,4,5或6; R 4和R 5与它们所连接的氮原子一起形成选自式（II）的双环体系，其中所述环系可任选地被 1-3个取代基; R 6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; R 7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。}

2. 发明申请

WO2007014922A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014922A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064816
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
IPC分类号： C07D401/12 , C07D403/12 , C07D245/04 , A61K31/4523 , A61P31/14
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; R 1 is -OR 6 , -NH-SO 2 R 7 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, or C 3-7 cycloalkyl; n is 3, 4, 5, or 6; R 4 and R 5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, C 1-6 alkoxy- carbonyl, amino, azido, mercapto, C 1-6 alkylthio, polyhaloC 1-6 alkyl, aryl or Het; W is aryl or Het; R 6 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 7 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, 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; R 1是-OR 6，-NH-SO 2 R 7， R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，或 ç_{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 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 烷基 - 羰基，氨基，叠氮基，巯基，C 1-6烷基硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R 6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; R 7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，部分不饱和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。}

3. 发明申请

WO2007014920A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014920A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064814
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , TAHRI, Abdellah , SIMMEN, Kenneth, Alan , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina , ANTONOV, Dmitry
发明人： DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , TAHRI, Abdellah , SIMMEN, Kenneth, Alan , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina , ANTONOV, Dmitry
IPC分类号： C07D487/04 , C07K5/078 , A61K38/05 , A61K31/33 , A61P31/14 , C07D413/12
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; R 1 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-C 1-4 alkanediyl-, -O-C(=O)-, -O-C(=O)-NR 4a - or -O-C(=O)-NR 4a C 1-4 alkanediyl-; R 2 is hydrogen, -OR 5 , -C(O)OR 5 , -C(=O)R 6 , -C(=O)NR 4a R 4b , -C(=O)NHR 4c ,-NR 4a R 4b , -NHR 4c , -NR 4a SO p NR 4a R 4b , -NR 4a SO p R 7 , or B(OR 5 ) 2 ; R 3 is hydrogen, and where X is C or CH, R 3 may also be C 1-6 alkyl; 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.
摘要翻译：式（I）的HCV复制抑制剂，其N-氧化物，盐和立体化学异构形式，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; R 1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，以及任选的一至三个另外的杂原子选自氧，硫和氮，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在任何碳或氮环原子上被一个，两个，三个或四个取代基取代; L是直接键，-O-。 -OC 1-4烷基 - ， - OC（= O） - ， - OC（= O）-NR 4a - 或-OC（= O） SUP>图4a C _{1-4 烷二; R 2是氢，-OR 5，-C（O）OR 5，-C（= O）R 6， -C（= O）NR 4a R 4b，-C（= O）NHR 4c， - NR 4a，4b，4b，4b，4b，4a，4a，4b，4b，或者B（OR）4，其中R 4，R 4，R 4， 5 ）_{2 ; R 3是氢，并且其中X是C或CH，R 3也可以是C 1-6烷基; 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; 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，任选地与苯环稠合，并且其中基团Het作为整体可以是任选的被一个，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。}}

4. 发明申请

WO2007014921A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014921A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064815
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , DORANGE, Ismet , VENDEVILLE, Sandrine Marie Helene , SURLERAUX, Dominique Louis Nestor Ghislain , TAHRI, Abdellah , SIMONNET, Yvan , VAN DE VREKEN, Wim , HU, Lili , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , WALLBERG, Hans Kristian
IPC分类号： C07D401/14 , C07K5/078 , A61K31/4725 , A61P31/14
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; R 1 is -OR 5 , -NH-SO 2 R 6 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, or C 3-7 cycloalkyl; R 4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C 1-6 alkyl, C 1-6 alkoxy, hydroxy, halo, polyhalo- C 1-6 alkyl, polyhaloC 1-6 alkoxy, amino, mono- or diC 1-6 alkylamino, mono- or DiC 1-6 alkylaminocarbonyl, C 1-6 alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by ) represents an optional double bond; R 5 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 6 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, 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; R 1是-OR 5，-NH-SO 2 R 6; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，或 ç_{3-7 环烷基; R 4是任选地被一个，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（代表）表示任选的双键; R 5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; R 6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。}

5. 发明申请

WO2011070131A1 5-AMINO- 4-HYDROXYPENTOYL AMIDES 审中-公开
标题翻译： 5-氨基-4-羟基苯甲酸
公开(公告)号：WO2011070131A1
公开(公告)日：2011-06-16
申请号：PCT/EP2010/069328
申请日：2010-12-10
申请人： TIBOTEC PHARMACEUTICALS , MEDIVIR AB , KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
发明人： KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
IPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04 , A61K31/506 , A61P31/18
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 R 1 is halo, C 1-4 alkoxy, trifluoromethoxy; R 2 is a group of formula (A); R 3 is a group of formula (B); R 4 is a group of formula (C); n is 0 or 1; A is CH or N; R 5 and R 6 are hydrogen, C 1-4 alkyl, halo; R 7 and R 8 are C 1-4 alkyl or C 1-4 alkoxyC 1-4 alkyl; R 9 is C 1-4 alkyl, cyclopropyl, trifluoromethyl, C 1-4 alkoxy, or dimethylamino; R 10 is hydrogen, C 1-4 alkyl, cyclopropyl, trifluoromethyl, C 1-4 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

6. 发明申请

WO2008096001A8 HCV INHIBITING MACROCYCLIC PHENYLCARBAMATES 审中-公开
公开(公告)号：WO2008096001A8
公开(公告)日：2008-08-14
申请号：PCT/EP2008/051556
申请日：2008-02-08
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , ANTONOV, Dmitry , AYESA ALVAREZ, Susana , BELFRAGE, Anna, Karin, Gertrud, Linnea , JÖNSSON, Carl, Erik, Daniel , MC GOWAN, David, Craig , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil
发明人： RABOISSON, Pierre Jean-Marie Bernard , ANTONOV, Dmitry , AYESA ALVAREZ, Susana , BELFRAGE, Anna, Karin, Gertrud, Linnea , JÖNSSON, Carl, Erik, Daniel , MC GOWAN, David, Craig , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil
IPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14 , A61K31/538 , A61P31/14
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;usefulas HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.

7. 发明申请

WO2008095999A1 PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS 审中-公开
标题翻译：哌嗪取代大环内酯类HCV抑制剂
公开(公告)号：WO2008095999A1
公开(公告)日：2008-08-14
申请号：PCT/EP2008/051553
申请日：2008-02-08
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , BELFRAGE, Anna, Karin, Gertrud, Linnea , CLASSON, Björn, Olof , LINDQUIST, Karin, Charlotta , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , WÄHLING, Horst, Jürgen
发明人： RABOISSON, Pierre Jean-Marie Bernard , BELFRAGE, Anna, Karin, Gertrud, Linnea , CLASSON, Björn, Olof , LINDQUIST, Karin, Charlotta , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , WÄHLING, Horst, Jürgen
IPC分类号： C07D403/12 , C07K5/06
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。

8. 发明申请

WO2007014927A3 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014927A3
公开(公告)日：2007-11-29
申请号：PCT/EP2006064822
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB , RABOISSON PIERRE JEAN-MARIE BE , DE KOCK HERMAN AUGUSTINUS , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROEM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LI , WAEHLING HORST JUERGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTIN , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJOERN OLOF
发明人： RABOISSON PIERRE JEAN-MARIE BE , DE KOCK HERMAN AUGUSTINUS , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROEM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LI , WAEHLING HORST JUERGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTIN , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJOERN OLOF
IPC分类号： C07D417/04 , A61K31/517 , A61P31/12 , C07D239/72
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 OR 1 , NHS(=O) P R 2 ; wherein; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkylene-heterocyclyl; R 2 is C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes 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 C 1 -C 6 alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxyl, halo, haloC 1 -C 6 alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C 1 -C 6 alkyl- carbonylamino, C 0 -C 3 alkylenecarbocyclyl and C 0 -C 3 alkyleneheterocyclyl; R 5 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxyC 1 -C 6 alkyl or C 3 -C 7 cycloalkyl; R 6 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.
摘要翻译：式（I）化合物及其N-氧化物，盐和立体异构体，其中A为OR 1，NHS（= O）2 R 2， / SUP>; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3 - 亚烷基碳环基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3 -C 3烷基，亚烷基碳环基，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; ----可选双键; L为N或CRz; Rz是H或与星号碳形成双键; Rq是H或当L是CRz时，Rq也可以是C 1 -C 6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亚烷基的取代基取代烷氧基，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 -C 6烷基羰基氨基，C 0 -C 3亚烷基碳环基和C 0 -C 亚烷基杂环基; R 5是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷基C 1 -C 6烷基或C 3 -C 7环烷基; C 1 -C 6烷基或C 3 -C 6环烷基; R 6是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6 - C 1 -C 3烷氧基，C 0 -C 3亚烷基碳环基，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。

9. 发明申请

WO2007014926A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译： HEPATITIS C病毒的大环境抑制剂
公开(公告)号：WO2007014926A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064820
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , HU, Lili , VENDEVILLE, Sandrine Marie Helene , TAHRI, Abdellah , SURLERAUX, Dominique Louis Nestor Ghislain , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , IVANOV, Vladimir , PELCMAN, Michael , BELFRAGE, Anna Karin Gertrud Linnea , JOHANSSON, Per-Ola Mikael
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , HU, Lili , VENDEVILLE, Sandrine Marie Helene , TAHRI, Abdellah , SURLERAUX, Dominique Louis Nestor Ghislain , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , IVANOV, Vladimir , PELCMAN, Michael , BELFRAGE, Anna Karin Gertrud Linnea , JOHANSSON, Per-Ola Mikael
IPC分类号： C07D487/04 , C07D245/04 , C07K5/078 , A61K38/05 , A61K31/33 , A61P31/14 , C07K5/06
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; R 1 is -OR 7 , -NH-SO 2 R 8 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, C 3-7 cycloalkyl; R 4 is aryl or Het; n is 3, 4, 5, or 6; R 5 is halo, C 1-6 alkyl, hydroxy, C 1-6 alkoxy, phenyl, or Het; R 6 is C 1-6 alkoxy, or dimethylamino; R 7 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 8 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, 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; R 1是-OR 7，-NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6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; R 4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; R 6是C 1-6烷氧基或二甲基氨基; R 7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; R 8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。}

10. 发明申请

WO2008096002A1 HCV INHIBITING MACROCYCLIC PHOSPHONATES AND AMIDOPHOSPHATES 审中-公开
标题翻译： HCV抑制大环磷酰胺和氨基磷酸酯
公开(公告)号：WO2008096002A1
公开(公告)日：2008-08-14
申请号：PCT/EP2008/051558
申请日：2008-02-08
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , ANTONOV, Dmitry , NILSSON, Karl, Magnus , RABOISSON, Pierre Jean-Marie Bernard , ROSENQUIST, Asa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , VENDEVILLE, Sandrine, Marie Hélène
发明人： ANTONOV, Dmitry , NILSSON, Karl, Magnus , RABOISSON, Pierre Jean-Marie Bernard , ROSENQUIST, Asa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , VENDEVILLE, Sandrine, Marie Hélène
IPC分类号： C07F9/6561 , A61K31/675 , A61P31/14
CPC分类号： C07F9/6561
摘要： Inhibitors of HCV replication of Formula (I) the /V-oxides, salts, and stcreochcmically isomeric forms thereof; pharmaceutical compositions containing compounds (1) and processes for preparin compounds (I). The side chain R 2 is an amidophosphate or a phosphonate group and X, R 1 , R 3 , E and n are as defined in the application.
摘要翻译：式（I）的HCV复制抑制剂的N-氧化物，盐和其它异构体形式; 含有化合物（1）的药物组合物和制备前体化合物（I）的方法。侧链R 2是酰氨基磷酸酯或膦酸酯基，X，R 1，R 3，E和n如应用。

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