申请人:Tanabe Seiyaku Co., Ltd.
公开号:US05202312A1
公开(公告)日:1993-04-13
Imidazole-containing peptide of the formula: ##STR1## wherein R.sup.1 is a branched alkyl group, a branched alkyloxy group or an aryl-substituted lower alkyloxy group, R.sup.2 and R.sup.4 are the same or different and each is hydrogen atom or a lower alkyl group, R.sup.3 and R.sup.5 are a phenyl-substituted lower alkyl group, R.sup.6 is hydrogen atom or a lower alkoxycarbonyl group, R.sup.7 is hydrogen atom or a nitrogen-containing heterocyclic group-substituted lower alkylthio group, X.sup.1 and X.sup.2 are the same or different and each is ##STR2## A is a lower alkylene group which may be substituted with a substituent selected from the group consisting of a lower alkoxy group, hydroxymethyl group and a group of the formula: ##STR3## and R.sup.8 and R.sup.9 are the same or different and each is hydrogen atom or a lower group, or a pharmaceutically acceptable salt thereof, which is useful as an immunomodulator and as an agent for the treatment and/or prophylaxis of autoimmune diseases such as rheumatoid arthritis, multiple sclerosis, systemic lupus erthematodes, glomerulonephris, rhumatic fever or type I diabetes and atopic allergy, a processes for the preparation thereof, and a pharmaceutical composition containing said compound as an active ingredient.
配方为:## STR1 ##的含咪唑肽,其中R.sup.1是支链烷基,支链烷氧基或芳基取代的低烷氧基,R.sup.2和R.sup.4相同或不同,每个都是氢原子或低烷基,R.sup.3和R.sup.5是苯基取代的低烷基,R.sup.6是氢原子或低烷氧羰基基团,R.sup.7是氢原子或氮含杂环基取代的低烷硫基团,X.sup.1和X.sup.2相同或不同,每个都是## STR2 ##,A是低烷基,可以用从羟甲氧基基团和公式为:## STR3 ##的基团中选择的取代基取代,R.sup.8和R.sup.9相同或不同,每个都是氢原子或低基团,或其药学上可接受的盐。它作为免疫调节剂和治疗/预防自身免疫性疾病,如类风湿性关节炎、多发性硬化症、系统性红斑狼疮、肾小球肾炎、风湿热或I型糖尿病和变应性过敏的药物,并提供了其制备过程以及含有该化合物作为活性成分的制药组合物。