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    Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
    42.
    发明授权
    Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase 失效
    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：US07323449B2

    公开(公告)日：2008-01-29

    申请号：US10520925

    申请日：2003-07-18

    申请人： David B. Olsen ,  Balkrishen Bhat ,  Phillip Dan Cook

    发明人： David B. Olsen ,  Balkrishen Bhat ,  Phillip Dan Cook

    IPC分类号： C07D487/04 ,  A61K31/52 ,  A61K31/675 ,  C07F9/6561 ,  A61P31/14

    CPC分类号： A61K45/06 ,  C07H19/14

    摘要： 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.

    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。

    Nucleosidic and non-nucleosidic folate conjugates
    47.
    发明授权
    Nucleosidic and non-nucleosidic folate conjugates 有权
    核苷和非核苷酸叶酸偶联物

    公开(公告)号：US06335434B1

    公开(公告)日：2002-01-01

    申请号：US09275505

    申请日：1999-03-24

    申请人： Andrei P. Guzaev ,  Phillip Dan Cook ,  Muthiah Manoharan ,  Balkrishen Bhat

    发明人： Andrei P. Guzaev ,  Phillip Dan Cook ,  Muthiah Manoharan ,  Balkrishen Bhat

    IPC分类号： C12Q168

    CPC分类号： C07H15/26 ,  C07D475/04

    摘要： Oligonucleotide-folate conjugates are described wherein folates are conjugated to one or more sites on an oligonucleotide including the 2′-, 3′-, 5′-, nucleobase and internucleotide linkage sites. The folate can be attached via the &agr;- or &ggr;-carboxylate, optionally through a linking group. Methods for the regiospecific synthesis of the conjugates are diclosed. Also disclosed are nucleosidic and non-nucleosidic linkers conjugated to folic acid and related folates.

    摘要翻译： 描述了寡核苷酸 - 叶酸盐缀合物，其中叶酸酯与包含2'，3'，5'，核碱基和核苷酸间位点的寡核苷酸上的一个或多个位点缀合。 叶酸可以通过α-或γ-羧酸盐，任选地通过连接基团连接。 缀合物区域特异性合成的方法是分开的。 还公开了与叶酸和相关叶酸缀合的核苷和非核苷酸接头。