1,3,4-Oxadiazoline derivatives and drugs containing these derivatives as active ingredient
申请人:——
公开号:US20030166574A1
公开(公告)日:2003-09-04
A 1,3,4-oxadiazoline derivative of formula (I)
1
, wherein W is oxygen, sulfer; R is hydrogen, alkyl, CycA, etc.; AA
1
is a single bond, amino acid residue, etc.; AA
2
is a single bond, amino acid residue, etc.; R
7
and R
8
are hydrogen, alkyl, etc.; R
9
is hydrogen, alkyl, etc., and a non-toxic salt thereof.
The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.
公式(I)的1,3,4-噁二唑啉衍生物,其中W为氧、硫;R为氢、烷基、环烷A等;AA1为单键、氨基酸残基等;AA2为单键、氨基酸残基等;R7和R8为氢、烷基等;R9为氢、烷基等,以及其非毒性盐。
公式(I)的化合物对半胱氨酸蛋白酶具有抑制活性,因此可用作预防和/或治疗炎症性疾病、凋亡诱导的疾病、免疫反应紊乱引起的疾病、自身免疫疾病、由组成生物体的蛋白质分解引起的疾病、休克、循环系统紊乱、血液凝固系统紊乱、恶性肿瘤、获得性免疫缺陷综合症(AIDS)和AIDS相关综合症(ARC)、寄生虫病、神经退行性疾病、肺部疾病、骨吸收疾病、内分泌亢进等方面具有用途。