发明授权
- 专利标题： 4,5-disubstituted-2-aryl pyrimidines
- 专利标题（中）： 4,5-二取代-2-芳基嘧啶
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申请号： US12320539申请日： 2009-01-26
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公开(公告)号： US08129395B2公开(公告)日： 2012-03-06
- 发明人: George D. Maynard , Manuka Ghosh , Jun Yuan , Kevin S. Currie , Scott Mitchell , Qin Guo , He Zhao
- 申请人： George D. Maynard , Manuka Ghosh , Jun Yuan , Kevin S. Currie , Scott Mitchell , Qin Guo , He Zhao
- 申请人地址： BM Hamilton
- 专利权人： Novartis International Pharmaceutical Ltd.
- 当前专利权人： Novartis International Pharmaceutical Ltd.
- 当前专利权人地址： BM Hamilton
- 代理机构： Edwards Wildman Palmer LLP
- 代理商 Peter F. Corless; Dwight K. Kim
- 主分类号： A01N43/54
- IPC分类号： A01N43/54 ; C07D239/42 ; C07D401/04 ; C07D403/00
摘要：
4,5-disubstituted-2-arypyrimidines 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 agonist 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.
公开/授权文献
- US20100022516A1 4,5-Disubstituted-2-aryl pyrimidines 公开/授权日：2010-01-28
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