发明公开
- 专利标题： 4,5-DISUBSTITUTED-2-ARYL PYRIMIDINES
- 专利标题（中）： 4,5-DISUBSTITUIERTE 2-ARYL-PYRIMIDINE
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申请号： EP05746687.2申请日： 2005-05-06
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公开(公告)号： EP1745033A2公开(公告)日： 2007-01-24
- 发明人: MAYNARD, George, D. , GHOSH, Manuka , YUAN, Jun , CURRIE, Kevin, S. , MITCHELL, Scott , GUO, Qin , ZHAO, He
- 申请人： NEUROGEN CORPORATION
- 申请人地址： 35 N.E. Industrial Road Branford, CT 06405 US
- 专利权人： NEUROGEN CORPORATION
- 当前专利权人： NEUROGEN CORPORATION
- 当前专利权人地址： 35 N.E. Industrial Road Branford, CT 06405 US
- 代理机构： Forstmeyer, Dietmar
- 优先权： US569222P 20040508; US649973P 20050204
- 国际公布： WO2005110416 20051124
- 主分类号： C07D401/04
- IPC分类号： C07D401/04 ; A61K31/506
摘要：
4,5-disubstituted-2-arylpyrimidines of Formula (I) and Formula (II) are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 4,5-disubstituted-2-arylpyrimidines, which are useful as probes for the localization of C5a receptors.
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