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3-SUBSTITUTED-6-ARYL PYRIDINES AS LIGANDS OF C5A RECEPTORS

机译:3取代6芳基吡啶作为C5A受体的配体

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.
机译:提供了式I的3-取代的6-芳基吡啶:其中R 1,R 2,R 3,R 8,R 9,A和Ar在本文中定义。这样的化合物是C5a受体的配体。优选的式I化合物以高亲和力结合C5a受体,并对C5a受体表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含此类化合物的药物组合物,以及此类化​​合物在治疗各种炎性,心血管和免疫系统疾病中的用途。另外,本发明提供了标记的3-取代的6-芳基吡啶,其可用作C5a受体定位的探针。

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