发明申请
- 专利标题: 3-SUBSTITUTED-6-ARYL PYRIDINES
- 专利标题(中): 3-取代的6-芳基吡啶
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申请号: US12983661申请日: 2011-01-03
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公开(公告)号: US20110281837A1公开(公告)日: 2011-11-17
- 发明人: Alan J. Hutchinson , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
- 申请人: Alan J. Hutchinson , Jun Yuan , Kyungae Lee , George D. Maynard , Bertrand L. Chenard , Nian Liu , Qin Guo , Zihong Guo , Peter Hrnciar
- 主分类号: A61K31/397
- IPC分类号: A61K31/397 ; A61K31/5377 ; A61K31/4439 ; A61K31/4709 ; C12N5/078 ; A61P19/02 ; A61P17/06 ; A61P9/00 ; A61P11/06 ; C12N5/071 ; A61K31/4418 ; A61K31/4545
摘要:
3-substituted-6-aryl pyridines of Formula I 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 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 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
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