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    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    1.
    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
    2.
    发明公开
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒大环抑制剂

    公开(公告)号：EP1912996A1

    公开(公告)日：2008-04-23

    申请号：EP06764265.2

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd. ,  Medivir Aktiebolag

    发明人： DE KOCK, Herman, Augustinus ,  RABOISSON, Pierre, Jean-Marie, Bernard ,  TAHRI, Abdellah ,  SIMMEN, Kenneth, Alan ,  NILSSON, Karl Magnus, Medivir AB ,  SAMUELSSON, Bengt Bertil, Medivir AB ,  ROSENQUIST, Åsa Annica Kristina, Medivir AB ,  ANTONOV, Dmitry, Medivir AB

    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.

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    5.
    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。

    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    6.
    发明公开
    MACROCYLIC 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：EP1912995A1

    公开(公告)日：2008-04-23

    申请号：EP06764264.5

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals Ltd.

    发明人： RABOISSON, Pierre, Jean-Marie, Bernard ,  DE KOCK, Herman, Augustinus ,  VENDEVILLE, Sandrine, Marie, Helene ,  HU, Lili ,  VAN DE VREKEN, Wim ,  MC GOWAN, David, Craig ,  TAHRI, Abdellah ,  SURLERAUX, Dominique, Louis, Nestor, Ghislain ,  SIMMEN, Kenneth, Alan

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

    CPC分类号： C07D487/04 ,  C07K5/06165

    摘要： Inhibitors of HCV of formula (I), and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 8 to 12 membered bicyclic heterocyclic ring system containing one nitrogen, and optionally one to three oxygen, sulfur or nitrogen, wherein said ring system may be optionally substituted; L is a direct bond, -O-. -O-C1-4alkanediyl-, -O-CO-, -O-C(=O)-NR5a- or -O-C(=O)-NR5a-C1-4alkanediyl-; R2 is hydrogen, -OR6, -C(O)OR6, -C(=O)R7, -C(=O)NR5aR5b, -C(=O)NHR5c, -NR5aR5b, -NHR5c, -NHSOpNR5aR5b, -NR5aSOpR8, or -B(OR6)2; R3 and R4 are hydrogen or C1-6alkyl; or R3 and R4 taken together may form a C3-7cycloalkyl ring; 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 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 ; 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抑制剂及其N-氧化物，盐和立体化学异构体形式，其中R1为芳基或饱和的，部分不饱和或完全不饱和的5或6元单环或8-12元双环杂环 含有一个氮和任选1-3个氧，硫或氮的体系，其中所述环体系可以任选被取代; L是直接键，-O-。 -O-C（= O）-NR5a-或-O-C（= O）-NR5a-C1-4烷二基 - （= O）R7，-C（= O）NR5aR5b，-C（= O）NHR5c，-NR5aR5b，-NHR5c，-NHSOpNR5aR5b，-NR5aSOpR8， 或-B（OR 6）2; R3和R4是氢或C1-6烷基; 或者R3和R4一起形成C3-7环烷基环; n是3,4,5或6; p是1或2; 芳基是苯基，萘基，2,3-二氢化茚基或1,2,3,4-四氢萘基，它们中的每一个可以任选地被取代.Het是5或6元饱和，部分不饱和或完全不饱和的含有1至4个各自独立选择的杂原子的杂环 由氮，氧和硫任选地与苯环稠合，并且其中基团Het作为整体可以任选被取代; 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。

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    7.
    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.

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    8.
    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。