申请人:Merck & Co., Inc.
公开号:US05955480A1
公开(公告)日:1999-09-21
2,4-Diaryl-5-pyridylimidazoles are glucagon antagonists and inhibitors of the biosynthesis and/or action of TNF-.alpha. and IL-1. The compounds block the action of glucagon at its receptor and thereby decrease the levels of plasma glucose. The instant imidazoles are also inhibitors of TNF-.alpha. and IL-1. Compounds of the present invention may be used for glucagon-mediated as well as cytokine mediated diseases. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production of one or more cytokines occurs. Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) are cytokines produced by a variety of cells, which are involved in immunoregulation and other physiological conditions, such as inflammation.
2,4-二芳基-5-吡啶基咪唑是胰高血糖素拮抗剂,可抑制TNF-α和IL-1的生物合成和/或作用。这些化合物阻断了胰高血糖素在其受体上的作用,从而降低了血浆葡萄糖水平。这些咪唑也是TNF-α和IL-1的抑制剂。本发明的化合物可用于胰高血糖素介导的疾病以及细胞因子介导的疾病。细胞因子介导的疾病是指发生一种或多种细胞因子过度或失调产生的疾病或症状。白细胞介素-1(IL-1)和肿瘤坏死因子(TNF)是多种细胞产生的细胞因子,参与免疫调节和其他生理条件,如炎症。