发明名称 4,5-Disubstituted-2-aryl pyrimidines
摘要 4,5-disubstituted-2-arylpyrimidines of Formula I and Formula II are provided: wherein R<SUB>1</SUB>, R<SUB>2</SUB>, R<SUB>3</SUB>, R<SUB>8</SUB>, R<SUB>9</SUB>, 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.
申请公布号 US2005277654(A1) 申请公布日期 2005.12.15
申请号 US20050123755 申请日期 2005.05.06
申请人 MAYNARD GEORGE D;GHOSH MANUKA;YUAN JUN;CURRIE KEVIN S;MITCHELL SCOTT;GUO QIN;ZHAO HE 发明人 MAYNARD GEORGE D.;GHOSH MANUKA;YUAN JUN;CURRIE KEVIN S.;MITCHELL SCOTT;GUO QIN;ZHAO HE
分类号 A61K31/505;C07D239/26;C07D239/28;C07D239/34;C07D239/42;C07D239/47;C07D239/48;C07D401/04;C07D401/06;C07D401/12;C07D403/04;C07D403/12;C07D405/04;C07D405/12;C07D417/04;C07D471/04;C07D498/04;(IPC1-7):A61K31/505 主分类号 A61K31/505
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