SUBSTITUTED NUCLEOSIDE DERIVATIVES WITH ANTIVIRAL AND ANTIMICROBIAL PROPERTIES
    3.
    发明申请
    SUBSTITUTED NUCLEOSIDE DERIVATIVES WITH ANTIVIRAL AND ANTIMICROBIAL PROPERTIES 有权
    取代的具有抗病毒和抗微生物特性的核苷酸衍生物

    公开(公告)号:US20110039798A1

    公开(公告)日:2011-02-17

    申请号:US12668262

    申请日:2008-07-09

    CPC classification number: C07H19/06 C07D411/04 C07H19/10 C07H19/16 C07H19/20

    Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.

    Abstract translation: 本发明涉及脂肪酸和脂肪醇取代的核苷衍生物以及在多价支架(例如,聚合物,肽,多羧酸取代的化合物,含有多环维生素基团的化合物)上取代的核苷和核苷衍生物,其显示有效的抗HIV活性。 此外,它们显示增强的抗多药耐药性,R5和细胞相关病毒的活性。 其中一些还显示针对其他性传播病原体和精子的活动。 本发明提供了它们的合成方法,物质组成和使用方法。 强调其作为局部杀微生物剂的应用,以治疗或预防疾病,特别是艾滋病毒/艾滋病的性传播。

    Substituted nucleoside derivatives with antiviral and antimicrobial properties
    4.
    发明授权
    Substituted nucleoside derivatives with antiviral and antimicrobial properties 有权
    取代的具有抗病毒和抗微生物特性的核苷衍生物

    公开(公告)号:US09296776B2

    公开(公告)日:2016-03-29

    申请号:US12668262

    申请日:2008-07-09

    CPC classification number: C07H19/06 C07D411/04 C07H19/10 C07H19/16 C07H19/20

    Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.

    Abstract translation: 本发明涉及脂肪酸和脂肪醇取代的核苷衍生物以及在多价支架(例如,聚合物,肽,多羧酸取代的化合物,含有多环维生素基团的化合物)上取代的核苷和核苷衍生物,其显示有效的抗HIV活性。 此外,它们显示增强的抗多药耐药性,R5和细胞相关病毒的活性。 其中一些还显示针对其他性传播病原体和精子的活动。 本发明提供了它们的合成方法,物质组成和使用方法。 强调其作为局部杀微生物剂的应用,以治疗或预防疾病,特别是艾滋病毒/艾滋病的性传播。

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