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    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    1.
    发明授权
    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权

    公开(公告)号：EP1912995B1

    公开(公告)日：2011-07-27

    申请号：EP06764264.5

    申请日：2006-07-28

    申请人： Tibotec Pharmaceuticals

    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.

    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    3.
    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。