Substituted ketone derivatives as inhibitors of interleukin-1.beta.
申请人:Merck & Co., Inc.
公开号:US05866545A1
公开(公告)日:1999-02-02
This invention relates to substituted ketone derivatives of formula (I) useful in the treatment of inflammation in lung, central nervous system, kidney, joints, endocardium, pericardium, eyes, ears, skin, gastrointestinal tract and urogenital system. More particularly, this invention relates to substituted ketone drivatives that are useful inhibitors of interleukin-1.beta. converting enzyme (ICE). Interleukin-1.beta. converting enzyme (ICE) has been identified as the enzyme responsible for converting precursor interleukin-1.beta. (IL-1.beta.) to biologically active IL-1.beta..
本发明涉及式(I)的取代酮衍生物,其在治疗肺部、中枢神经系统、肾脏、关节、心内膜、心包、眼、耳、皮肤、胃肠道和泌尿生殖系统的炎症中有用。更具体地说,本发明涉及取代酮衍生物,其是有用的白细胞介素-1β转化酶(ICE)抑制剂。已经确定白细胞介素-1β转化酶(ICE)是将前体白细胞介素-1β(IL-1β)转化为生物活性IL-1β的酶。