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11 条记录 (耗时 0.024 秒)

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    1.
    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：EP1912996B1

    公开(公告)日：2012-06-20

    申请号：EP06764265.2

    申请日：2006-07-28

    申请人： Janssen R&D Ireland ,  Medivir Aktiebolag

    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; 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)-NR4aC1-4alkanediyl-; 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.

    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    9.
    发明公开
    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒大环抑制剂

    公开(公告)号：EP1912997A1

    公开(公告)日：2008-04-23

    申请号：EP06764267.8

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd. ,  Medivir Aktiebolag

    发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  HU, Lili ,  SURLERAUX, Dominique, Louis, Nestor, Ghislain ,  SIMMEN, Kenneth, Alan ,  SALVADOR ODÉN, Lourdes, Medivir AB ,  NILSSON, Karl, Magnus, Medivir AB ,  ROSENQUIST, Åsa Annica Kristina, Medivir AB ,  SAMUELSSON, Bengt Bertil, Medivir AB

    IPC分类号： C07D487/04 ,  C07D245/04 ,  C07K5/078 ,  A61K38/05 ,  A61K31/33 ,  A61P31/14 ,  C07K5/06

    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 Ν, 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, polyhaloC11-6alkoxy, 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)-ΝR5a - 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).

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    10.
    发明授权
    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：EP1912997B1

    公开(公告)日：2011-09-14

    申请号：EP06764267.8

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals ,  Medivir Aktiebolag

    发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  HU, Lili ,  SURLERAUX, Dominique, Louis, Nestor, Ghislain ,  SIMMEN, Kenneth, Alan ,  SALVADOR ODÉN, Lourdes, ,  NILSSON, Karl, Magnus, ,  ROSENQUIST, Åsa Annica Kristina, ,  SAMUELSSON, Bengt Bertil,

    IPC分类号： C07D487/04 ,  C07D245/04 ,  C07K5/078 ,  A61K38/05 ,  A61K31/33 ,  A61P31/14 ,  C07K5/06

    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 Ν, 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, polyhaloC11-6alkoxy, 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)-ΝR5a - 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是N，CH，并且其中X带有双键，它是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; 或者R1a和R1b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 - ， - OC 1-4烷烃二基 - ， - O-CO-，-O-C（= O）-NR 5a - 或-O-C（= O）-NR 5a -C 1-4链烷二基 - 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; R 4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9-12元双环杂环系统，其中所述环系统含有一个氮和任选1-3个选自O，S和N的另外的杂原子， 并且其中剩余的环成员是碳原子; 其中所述环系可以任选被取代; n是3,4,5或6; p是1或2; 芳基是苯基，萘基，茚满基或1,2,3,4-四氢萘基，它们中的每一个可以任选地被一个，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，部分不饱和或完全不饱和的杂环，其任选地与苯环稠合，并且其中Het可以任选被一个，两个或三个 三个取代基; 含有化合物（I）的药物组合物和用于制备化合物（I）的方法。