Amino methyl imidazoles of Formula I are provided:
1
wherein R, R
1
, R
2
, R
3
, R
4
, R
5
, and R
6
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. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.
本发明提供了式I的
氨甲基
咪唑化合物:1其中R,R1,R2,R3,R4,R5和R6的定义如本文所述。此类化合物是C5a受体的
配体。式I的优选化合物具有高亲和力结合C5a受体,并在C5a受体上表现为中性拮抗剂或逆激动剂活性。本发明还涉及包含此类化合物的制药组合物。此外,本发明还涉及标记的
氨甲基
咪唑化合物,其可用作C5a受体定位的探针。本发明还提供了使用这类化合物治疗各种炎症、心血管和免疫系统疾病的方法。