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    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    116.
    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。

    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    117.
    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.

    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    118.
    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。