Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and pharmaceutical compositions containing same
申请人:Sigma-Tau Industrie
Farmaceutiche Riunite S.p.A.
公开号:EP0464009A2
公开(公告)日:1992-01-02
Ipoxantine derivatives of general formula (I):
both as racemate and chiral forms and the salts thereof with pharmacologically acceptable cations, wherein n is an integer comprised between 2 and 6, and A is the residue of a dipeptide, tripeptide, tetrapeptide and pentapeptide selected, respectively, from the groups consisting of:
(a) glycyl-aspartate, alanyl-glycine, glycyl-glycine, aspartyl-arginine, leucyl-arginine;
(b) arginyl-lysyl-aspartate, aspartyl-lysyl-arginine, lysyl-prolyl-arginine, prolyl-prolyl-arginine, lysyl-histidyl-glycinamide, prolyl-phenilalanyl-arginine, phenylalanyl-prolyl-arginine;
(c) arginyl-lysyl-aspartyl-valine, valyl-aspartyl-lysyl-arginine, threonylvalyl-leucyl-histidyne; and
(d) arginyl-lysyl-aspartyl-valyl-tyrosine; are endowed with immunomodulating activity and can be formulated in orally or parenterally administrable pharmaceutical compositions.
通式(I)的
次黄嘌呤衍
生物:
外消旋体和手性体及其与药理学上可接受的阳离子的盐类,其中 n 是介于 2 和 6 之间的整数,A 是二肽、三肽、四肽和五肽的残基,分别选自由下列组成的组
(a) 甘
氨酰-
天冬氨酸、丙
氨酰-甘
氨酸、甘
氨酰-甘
氨酸、天冬
氨酰-精
氨酸、
亮氨酰-精氨酸;
(b) 精
氨酰-赖
氨酰-
天冬氨酸、天冬
氨酰-赖
氨酰-精
氨酸、赖
氨酰-脯
氨酰-精
氨酸、脯
氨酰-脯
氨酰-精
氨酸、赖
氨酰-组
氨酰-甘
氨酰胺、脯
氨酰-
苯丙
氨酰-精
氨酸、
苯丙
氨酰-脯
氨酰-精
氨酸;
(c) 精
氨酰-赖
氨酰-天冬
氨酰-缬
氨酸、缬
氨酰-天冬
氨酰-赖
氨酰-精
氨酰、苏
氨酰-缬
氨酰-亮
氨酰-组
氨酰;以及
(d) 精
氨酰-赖
氨酰-天冬
氨酰-缬
氨酰-
酪氨酸;具有免疫调节活性,可配制成口服或肠外给药的药物组合物。