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    NOVEL IMINOSUGARS AND THEIR APPLICATIONS
    1.
    发明公开
    NOVEL IMINOSUGARS AND THEIR APPLICATIONS 审中-公开
    NEUARTIGE IMINOZUCKER UND DEREN ANWENDUNGEN

    公开(公告)号：EP2858642A1

    公开(公告)日：2015-04-15

    申请号：EP13800188.8

    申请日：2013-06-05

    申请人： Unither Virology, LLC ,  The Chancellor, Masters and Scholars of The University of Oxford

    发明人： KIAPPES, J. L. ,  LAING, Peter ,  DWEK, Raymond ,  ZITZMANN, Nicole ,  POLLOCK, Stephanie

    IPC分类号： A61K31/355 ,  A61K31/445 ,  A61K31/575 ,  A61P31/12

    CPC分类号： C07D405/12 ,  C07D211/46 ,  C07D401/12 ,  C07J43/003

    摘要： Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogs of tocopherol or select analogs of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals.

    摘要翻译： 描述了通过共价引入生育酚部分或作为生育酚类型或胆固醇的选择性类似物或其拮抗剂“依泽替米贝”的替代部分具有内含递送特征的亚氨基缩寡核苷酸化合物; 并且可能具有广谱抗病毒活性。 这些化合物与以前的亚氨基硫糖化合物不同，甚至是脂肪细胞的化合物，更疏水，并且类似于脂肪和油在其体内分泌行为脂蛋白，细胞脂滴细胞器和生物膜的脂质相中的作用。 这些特征在体内赋予许多独特的递送属性，特别是有利于涉及淋巴系统和肝细胞的病毒感染的治疗，但是这些特征对于治疗人和动物的病毒感染通常也是有利的 。