PYRROLIDINYL GROUPS FOR ATTACHING CONJUGATES TO OLIGOMERIC COMPOUNDS
    32.
    发明申请
    PYRROLIDINYL GROUPS FOR ATTACHING CONJUGATES TO OLIGOMERIC COMPOUNDS 审中-公开
    连接到低分子化合物的吡咯烷基

    公开(公告)号:US20090203132A1

    公开(公告)日:2009-08-13

    申请号:US11574396

    申请日:2005-09-01

    IPC分类号: C12N5/06 C07H21/02

    CPC分类号: C07D207/12

    摘要: The present invention provides pyrrolidinyl compounds that are useful for preparing conjugated oligomeric compounds. The conjugated pyrrolidinyl compounds can be attached to support medium and provide a free hydroxyl for oligomer synthesis to prepare an oligmeric compound having a 3′-conjugate. Alternatively, the pyrrolidinyl compound can be prepared as a phosphoramidite which can be placed internally or at the 5′-position of an oligomeric compound. These two strategies can be used together to prepare oligomeric compounds having 2 or more conjugates at any selected positions. The present invention also provides methods for modulating gene expression using the conjugated oligomeric compounds.

    摘要翻译: 本发明提供可用于制备共轭低聚化合物的吡咯烷基化合物。 缀合的吡咯烷基化合物可以连接到载体介质上并提供用于低聚物合成的游离羟基以制备具有3'-缀合物的寡聚化合物。 或者,可以制备吡咯烷基化合物作为亚磷酰胺,其可以位于低聚化合物的内部或5'-位。 这两种策略可一起使用以制备在任何选定位置具有2个或更多个缀合物的低聚化合物。 本发明还提供了使用共轭低聚化合物调节基因表达的方法。

    Chimeric oligomeric compounds and their use in gene modulation
    33.
    发明申请
    Chimeric oligomeric compounds and their use in gene modulation 审中-公开
    嵌合寡聚化合物及其在基因调控中的应用

    公开(公告)号:US20050053976A1

    公开(公告)日:2005-03-10

    申请号:US10859825

    申请日:2004-06-03

    IPC分类号: A61K48/00 C07H21/02 C12Q1/68

    CPC分类号: A61K31/713

    摘要: Oligomer compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capble of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes at least one nucleotide comprising a chimeric organic composition. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide comprising a chimeric organic composition.

    摘要翻译: 提供包含第一和第二寡聚物的低聚物组合物,其中至少一部分第一寡聚体能够与至少一部分第二寡聚物杂交,至少一部分第一寡聚体与所选择的寡核苷酸杂交互补和杂交 靶核酸,并且所述第一或第二寡聚体中的至少一个包含至少一个包含嵌合有机组合物的核苷酸。 还提供寡聚物/蛋白质组合物,其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡聚体和至少一种包含至少一部分RNA诱导的沉默复合物(RISC)的蛋白质,其中至少一个核苷酸包含 嵌合有机组合物。

    Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
    38.
    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:US20070004669A1

    公开(公告)日:2007-01-04

    申请号:US10517295

    申请日:2003-06-17

    摘要: The 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 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 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 treating 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)有活性的试剂组合的药物组合物。 还公开了本发明的核苷化合物抑制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。