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11. 发明申请

WO2011039221A3 PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDES 审中-公开
标题翻译：核苷磷酰胺衍生物
公开(公告)号：WO2011039221A3
公开(公告)日：2011-06-16
申请号：PCT/EP2010064413
申请日：2010-09-29
申请人： CENTOCOR ORTHO BIOTECH PRODUCTS L P , MEDIVIR AB , JONCKERS TIM HUGO MARIA , RABOISSON PIERRE JEAN-MARIE BERNARD , VANDYCK KOEN , PELCMAN MICHAEL , SUND BENGT CHRISTIAN , WAEHLING HORST JUERGEN , PASSOS PINHO PEDRO MANUEL , WINQVIST ANNA , NILSSON KARL MAGNUS
发明人： JONCKERS TIM HUGO MARIA , RABOISSON PIERRE JEAN-MARIE BERNARD , VANDYCK KOEN , PELCMAN MICHAEL , SUND BENGT CHRISTIAN , WAEHLING HORST JUERGEN , PASSOS PINHO PEDRO MANUEL , WINQVIST ANNA , NILSSON KARL MAGNUS
IPC分类号： C07H19/10 , A61K31/7072 , A61P31/14
CPC分类号： C07H19/10
摘要： Compounds of formula I : including any possible stereoisomers thereof, wherein: R1 is hydrogen, -C(=O)R6 or -C(=O)CHR7-NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, Ci-C6alkyl, benzyl; R4 is hydrogen, Ci-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7Cyclo- alkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.
摘要翻译：式I化合物：包括其任何可能的立体异构体，其中：R 1是氢，-C（= O）R 6或-C（= O）CHR 7 -NH 2; R2是氢; 或C1-C6烷基或苯基，它们任一个任选被1,2或3个各自独立地选自卤素，C1-C6烷基，C2-C6链烯基和C1-C6烷氧基，羟基或氨基的取代基取代，或者R2为萘基; 或者R 2是吲哚基，R 3是氢，C 1 -C 6烷基，苄基; R 4是氢，C 1 -C 6烷基，苄基; 或者R 3和R 4与它们所连接的碳原子一起形成C 3 -C 7环烷基; R 5为C 1 -C 10烷基，C 3 -C 7环烷基，苄基或苯基，它们中的任一个任选被1,2或3个各自独立地选自羟基，C 1 -C 6烷氧基，氨基，单和二C 1 -C 6烷基氨基的取代基取代; R6是C1-C6烷基; R7是C1-C6烷基; R8是氢或卤素; 或其药学上可接受的盐或溶剂合物可用于预防或治疗HCV感染。

12. 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。}

13. 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。}

14. 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。}}

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