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    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
    7.
    发明申请
    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase 审中-公开
    核苷衍生物作为rna依赖性rna病毒聚合酶的抑制剂

    公开(公告)号：US20060264389A1

    公开(公告)日：2006-11-23

    申请号：US10521006

    申请日：2003-07-11

    申请人： Balkrishen Bhat ,  Steven Carroll ,  Anne Eldrup ,  Malcolm MacCoss ,  David Olsen ,  Thazha Prakash

    发明人： Balkrishen Bhat ,  Steven Carroll ,  Anne Eldrup ,  Malcolm MacCoss ,  David Olsen ,  Thazha Prakash

    IPC分类号： A61K31/7076 ,  C07H19/22

    CPC分类号： C07H19/14 ,  C07H19/22

    摘要： Thee present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA via 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 nucleoside 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 creating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

    摘要翻译： 本发明提供作为RNA依赖性RNA病毒聚合酶抑制剂的核苷化合物及其某些衍生物。 这些化合物是通过复制的RNA依赖性RNA的抑制剂，并且可用于治疗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）有活性的试剂组合的药物组合物。 还公开了抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或用本发明的核苷化合物产生RNA依赖性RNA病毒感染的方法。

    Oligomeric Compounds That Facilitate Risc Loading
    10.
    发明申请
    Oligomeric Compounds That Facilitate Risc Loading 审中-公开
    促进Risc加载的低分子化合物

    公开(公告)号：US20070275921A1

    公开(公告)日：2007-11-29

    申请号：US11569929

    申请日：2005-06-02

    申请人： Eric Swayze ,  Balkrishen Bhat ,  Richard Griffey ,  Thazha Prakash ,  Charles Allerson

    发明人： Eric Swayze ,  Balkrishen Bhat ,  Richard Griffey ,  Thazha Prakash ,  Charles Allerson

    IPC分类号： A61K31/7052 ,  A61P43/00 ,  C07H21/00

    CPC分类号： A61K31/7052

    摘要： The present invention provides double stranded compositions wherein one of the strands is useful in, for example, influencing the preferential loading the opposite strand into the RISC (or cleavage) complex. In particular, the present invention provides oligomeric compounds that comprise chemical modifications in at least one of the strands to drive loading of the opposite strand into the RISC (or cleavage) complex. Such modifications can be used to increase potency of duplex constructs that have been modified to enhance stability. Examples of chemical modifications that drive loading of the second strand include, but are not limited to, MOE (2′-O(CH2)2OCH3), 2′-O-methyl, -ethyl, -propyl, and —N-methylacetamide. Such modifications can be distributed throughout the strand, or placed at the 5′ and/or 3′ ends to make a gapmer motif on the sense strand. The activity of the 4′-thio gapmer RNA antisense strand can be improved by incorporating alternating MOE or MOE gapmer motif into the sense strand.

    摘要翻译： 本发明提供双链组合物，其中一条链可用于例如影响相对链优先加载到RISC（或切割）复合物中。 特别地，本发明提供了在至少一个链中包含化学修饰以驱动相反链加载到RISC（或切割）复合物中的低聚化合物。 可以使用这些修饰来增加经修饰以增强稳定性的双链构建体的效力。 驱动第二链的负载的化学修饰的实例包括但不限于MOE（2'-O（CH 2）2 OCH 3） ，2'-O-甲基， - 乙基， - 丙基和-N-甲基乙酰胺。 这样的修饰可以分布在整个链上，或者放置在5'和/或3'末端以在有义链上形成gapmer基序。 通过将交替的MOE或MOE gapmer基序并入有义链中，可以改善4'-硫代间隔RNA反义链的活性。