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    • 5. 发明申请
    • NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION
    • 用于治疗RNA依赖性RNA病毒感染的核苷类ARYL磷酸酯
    • WO2006012078A2
    • 2006-02-02
    • PCT/US2005021684
    • 2005-06-20
    • MERCK & CO INCMACCOSS MALCOLMOLSEN DAVID B
    • MACCOSS MALCOLMOLSEN DAVID B
    • C12Q1/68
    • C07H19/20C07H19/14C07H19/16
    • The present invention provides nucleoside aryl phosphoramidates which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to 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 pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 nucleoside aryl phosphoramidates of the present invention.
    • 本发明提供核苷芳基氨基磷酸酯,其是RNA依赖性RNA病毒聚合酶抑制剂的前体。 这些化合物是RNA依赖性RNA病毒复制抑制剂的前体,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。 本发明还描述了单独含有这种核苷芳基氨基磷酸酯或与其它对RNA依赖性RNA病毒感染,特别是HCV感染有活性的试剂组合的药物组合物。 还公开了本发明的核苷芳基氨基磷酸酯抑制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。