PHARMACEUTICAL COMPOSITIONS OF SILICON-CONTAINING SUBSTITUTED ADENOSINE NUCLEOSIDE AMIDE ANALOGS
    2.
    发明公开
    PHARMACEUTICAL COMPOSITIONS OF SILICON-CONTAINING SUBSTITUTED ADENOSINE NUCLEOSIDE AMIDE ANALOGS 审中-公开
    药物组合物从含硅取代ADENOSINNUKLEOSID - 酰胺类似物

    公开(公告)号:EP1919929A2

    公开(公告)日:2008-05-14

    申请号:EP06800695.6

    申请日:2006-08-02

    发明人: GATELY, Stephen

    CPC分类号: C07H19/167 C07H19/173

    摘要: Novel compositions of silicon-containing anti-metabolite compounds, their preparation and use in methods for treating cancer are described. The silyl group confers lipophilicity that can enhance the penetration of the compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The triorganosilyl group provides compounds having improved pharmacokinetics and anti-tumor activity. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

    PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF HIGHLY LIPOPHILIC SULFHYDRYL COMPOUNDS
    3.
    发明公开
    PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF HIGHLY LIPOPHILIC SULFHYDRYL COMPOUNDS 审中-公开
    药物组合物的方法和使用高度亲脂性巯基化合物

    公开(公告)号:EP1968609A2

    公开(公告)日:2008-09-17

    申请号:EP06848705.7

    申请日:2006-12-20

    IPC分类号: A61K31/695

    摘要: Novel compositions of silicon-containing sulfhydryl compounds, their preparation and use in methods for treating disease are described. Silicon confers lipophilicity that can enhance the penetration of the silicon derivative sulfhydryl compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The organosilyl group provides compounds having improved pharmacokinetics. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.