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    • 4. 发明授权
    • Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
    • 用于治疗RNA依赖性RNA病毒感染的核苷芳基氨基磷酸酯
    • US08071568B2
    • 2011-12-06
    • US12520738
    • 2007-12-28
    • Frank NarjesCristina GardelliMonica DonghiBarbara AttenniPhilippe L. Durette
    • Frank NarjesCristina GardelliMonica DonghiBarbara AttenniPhilippe L. Durette
    • A61K31/70C07H19/10
    • C07H19/04C07H19/048C07H19/10C07H19/20
    • The present invention provides nucleoside aryl phosphoramidates of structural formula (I) 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. (I)
    • 本发明提供结构式(I)的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含有这种核苷芳基氨基磷酸酯的药物组合物。 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。 (一世)