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    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    1.
    发明公开
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒的大环内酯类抑制剂

    公开(公告)号：EP1919899A1

    公开(公告)日：2008-05-14

    申请号：EP06778070.0

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd. ,  MEDIVIR AB

    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; 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 formula (II) 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是N，CH，其中X带有一个双键，它是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; R3是氢，C1-6烷基，C1-6烷氧基C1-6烷基或C3-7环烷基; n是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）的双环系统，其中所述环系统可以任选地被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，芳基或用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，芳基或用Het取代的C 1-6烷基; 芳基是苯基或萘基，它们中的每一个可以任选被1-3个取代基取代; Het是含有1至4个各自独立地选自N，O或S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1-3个取代基药物组合物取代，所述药物组合物含有化合物（I） 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用组合。

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    2.
    发明公开
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒的大环内酯类抑制剂

    公开(公告)号：EP1912981A2

    公开(公告)日：2008-04-23

    申请号：EP06764268.6

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd. ,  MEDIVIR AB

    发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  HU, Lili ,  SIMMEN, Kenneth, Alan ,  LINDQUIST, Karin Charlotta ,  LINDSTRÖM, Mats Stefan ,  BELFRAGE, Anna Karin Gertrud Linnea ,  WÄHLING, Horst Jürgen ,  NILSSON, Karl Magnus ,  SAMUELSSON, Bengt Bertil ,  ROSENQUIST, Åsa Annica Kristina ,  SAHLBERG, Sven Crister ,  WALLBERG, Hans, Kristian ,  KAHNBERG, Pia, Cecilia ,  CLASSON, Björn, Olof

    IPC分类号： C07D417/04

    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; ---- 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 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-C3alkyleneheterocyclyl, 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是OR1，NHS（= O）PR2; 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是3,4,5或6; ----定义一个可选的双键; L是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C1-C6烷基; 任选被一个或两个或三个各自独立地选自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亚烷基碳环基和C 0 -C 3亚烷基杂环基; R5是氢，C1-C6烷基，C1-C6烷氧基C1-C6烷基或C3-C7环烷基; R 6为氢，C 1 -C 6烷基，C 1 -C 6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诸如HCV的黄病毒感染。

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    4.
    发明授权
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒大环抑制剂

    公开(公告)号：EP1919899B1

    公开(公告)日：2011-01-19

    申请号：EP06778070.0

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals ,  MEDIVIR AB

    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; 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 formula (II) 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.

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    7.
    发明公开
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒的大环内酯类抑制剂

    公开(公告)号：EP1919898A1

    公开(公告)日：2008-05-14

    申请号：EP06778069.2

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd. ,  MEDIVIR AB

    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; 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，其中每条虚线（由------表示）表示任选的双键; X是N，CH，其中X带有一个双键，它是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; R3是氢，C1-6烷基，C1-6烷氧基C1-6烷基或C3-7环烷基; n是3,4,5或6; R4和R5彼此独立地为氢，卤素，羟基，硝基，氰基，羧基，C1-6烷基，C1-6烷氧基，C1-6烷氧基C1-6烷基，C1-6烷基羰基，C1-6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，芳基或用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，芳基或用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个各自独立地选自N，O或S的杂原子且任选被1-3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）的药物组合物和用于制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可用组合。