发明申请
US20050148548A1 Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
有权
磺酰胺衍生物作为天冬氨酰蛋白酶抑制剂的前药
- 专利标题： Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
- 专利标题（中）： 磺酰胺衍生物作为天冬氨酰蛋白酶抑制剂的前药
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申请号： US10958223申请日： 2004-10-04
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公开(公告)号： US20050148548A1公开(公告)日： 2005-07-07
- 发明人: Roger Tung , Michael Hale , Christopher Baker , Eric Furfine , Istvan Kaldor , Wieslaw Kazmierski , Andrew Spaltenstein
- 申请人： Roger Tung , Michael Hale , Christopher Baker , Eric Furfine , Istvan Kaldor , Wieslaw Kazmierski , Andrew Spaltenstein
- 专利权人： Vertex Pharmaceuticals Inc.
- 当前专利权人： Vertex Pharmaceuticals Inc.
- 主分类号： A61K31/18
- IPC分类号： A61K31/18 ; A61K31/215 ; A61K31/265 ; A61K31/27 ; A61K31/34 ; A61K31/341 ; A61K31/4025 ; A61K31/496 ; A61K31/66 ; A61K31/661 ; A61K31/664 ; A61K31/7048 ; A61K45/00 ; A61P31/12 ; A61P31/18 ; A61P43/00 ; C07C311/15 ; C07C311/18 ; C07C311/37 ; C07D277/30 ; C07D307/20 ; C07D405/12 ; C07D407/12 ; C07D417/12 ; C07F9/655 ; C07F9/6584 ; C07H15/04 ; C07H15/26 ; A61K31/675 ; A61K31/443 ; A61K31/4709 ; A61K31/551
摘要：
The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
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