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公开(公告)号:EP1039886A1
公开(公告)日:2000-10-04
申请号:EP98963800.2
申请日:1998-12-08
发明人: LEE, Taekyu , WONG, Chi-Huey , ELDER, John, H.
IPC分类号: A61K31/045 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/38 , A61K31/405 , A61K31/47 , A61K38/05 , C07C205/02 , C07C211/09 , C07C215/18 , C07D207/16 , C07D217/16 , C07D217/26 , C07D277/24 , C07D277/28 , C07K5/062 , C07K5/065
CPC分类号: C07D213/40 , A61K38/00 , C07D207/16 , C07D217/26 , C07D277/28 , C07D401/12 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06078
摘要: With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as FIV. Modification of existing HIV protease inhibitors by reducing the size of the P3 residue has the same effect. This finding provides a new strategy for the development of HIV protease inhibitors effective against the wild type and drug-resistant mutants and further supports that FIV protease is a useful model for drug-resistant HIV proteases, which often are developed through reduction in size of the binding region for the P3 group or the combined P3 and P1 groups.