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    • 6. 发明申请
    • THIONUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE
    • 作为RNA依赖性RNA病毒聚合酶抑制剂的硫代胞苷衍生物
    • WO2004009020A2
    • 2004-01-29
    • PCT/US0322556
    • 2003-07-18
    • MERCK & CO INCISIS PHARMACEUTICALS INCOLSEN DAVID BBHAT BALKRISHENCOOK PHILLIP DAN
    • OLSEN DAVID BBHAT BALKRISHENCOOK PHILLIP DAN
    • A61K45/06A61P31/12A61P31/14C07H19/14A61K
    • A61K45/06C07H19/14
    • The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such thionucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the thionucleoside compounds of the present invention.
    • 本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷类化合物及其某些衍生物。 这些化合物是RNA依赖性RNA病毒复制的抑制剂,可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒(HCV)NS5B聚合酶的抑制剂,作为HCV复制的抑制剂和/或用于治疗丙型肝炎感染。 本发明还描述了单独或与其它对RNA依赖性RNA病毒感染(特别是HCV感染)有活性的试剂组合含有这样的硫代核苷化合物的药物组合物。 还公开了用本发明的硫代核苷化合物抑制RNA依赖性RNA聚合酶,抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。
    • 7. 发明申请
    • FLUORINATED PYRROLO[2,3-D]PYRIMIDINE NUCLEOSIDES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION
    • 用于治疗RNA依赖性RNA病毒感染的氟化吡咯烷[2,3-D]嘧啶核苷
    • WO2006065335A3
    • 2006-09-14
    • PCT/US2005037224
    • 2005-10-17
    • MERCK & CO INCMACCOSS MALCOLMOLSEN DAVID BLEONE JOSEPHDURETTE PHILIPPE L
    • MACCOSS MALCOLMOLSEN DAVID BLEONE JOSEPHDURETTE PHILIPPE L
    • A61K31/7052A61K31/7042C07H19/14
    • C07H19/14
    • The present invention provides fluorinated pyrrolo[2,3,d]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaeutical compositions containing such fluorinated pyrrolo[2,3-d]pyrimidine nucleoside alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the fluorinated pyrrolo[2,3-d]pyrimidine nucleoside of the present invention.
    • 本发明提供了作为RNA依赖性RNA病毒聚合酶抑制剂的氟化吡咯并[2,3,d]嘧啶核苷化合物。 这些化合物是RNA依赖性RNA病毒复制的抑制剂,可用于治疗RNA依赖性RNA病毒感染。 它们特别可用作丙型肝炎病毒(HCV)NS5B聚合酶抑制剂的前体,作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。 本发明还描述了含有这种氟化吡咯并[2,3-d]嘧啶核苷的药物组合物,或者与其它对RNA依赖性RNA病毒感染,特别是HCV感染有活性的试剂组合。 还公开了本发明的氟化吡咯并[2,3-d]嘧啶核苷抑制RNA依赖性RNA聚合酶,抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。