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1.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
IPC分类号： C07H19/00 , C07H19/22 , C07H19/167 , C07H19/173 , A01N43/04 , A61K31/70
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.
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2.发明公开PHARMACEUTICAL COMPOSITIONS OF SILICON-CONTAINING SUBSTITUTED ADENOSINE NUCLEOSIDE AMIDE ANALOGS 审中-公开包含硅取代的取代的腺苷核苷类似物的药物组合物
公开(公告)号：EP1919929A4
公开(公告)日：2008-08-06
申请号：EP06800695
申请日：2006-08-02
发明人： GATELY STEPHEN
IPC分类号： C07H19/167 , A01N43/04 , A61K31/7076 , C07F7/08 , C07H19/173
CPC分类号： C07H19/167 , C07H19/173
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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
发明人： GATELY, Stephen , WEST, Robert
IPC分类号： A61K31/695
CPC分类号： C07F7/0818 , C07D213/60 , C07D213/75 , C07F7/0814
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.
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