公开(公告)号：US5411985A

公开(公告)日：1995-05-02

申请号：US62881

申请日：1993-05-17

申请人： Gerald F. Bills ,  Otto D. Hensens ,  Jerrold M. Liesch ,  Russel B. Lingham ,  Jon D. Polishook ,  Michael J. Salvatore ,  Susan L. Raghoobar

发明人： Gerald F. Bills ,  Otto D. Hensens ,  Jerrold M. Liesch ,  Russel B. Lingham ,  Jon D. Polishook ,  Michael J. Salvatore ,  Susan L. Raghoobar

IPC分类号： A61K31/35 ,  C07D309/38 ,  C12P17/06

CPC分类号： C12R1/645 ,  A61K31/35 ,  C07D309/38 ,  C12P17/06

摘要： Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia. ##STR1##

摘要翻译： 发现式I的新型肽基衍生物是白细胞介素-1β转换酶（ICE）的有效抑制剂。 式I化合物可用于治疗肺和气道炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵 关节，骨骼和结缔组织; 包括心包的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 式I化合物也可用于治疗感染（例如，革兰氏阴性休克）的并发症和其中IL1作为自分泌生长因子或作为恶病质介质的肿瘤。