申请人:Nisshin Flour Milling Co., Ltd.
                            
                            
                                公开号:EP0960885A1
                            
                            
                                公开(公告)日:1999-12-01
                            
                            
Depsipeptides represented by the formula (1):
 (wherein:
R1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; R2 is -A-B, -A-B-W, -A-B-W-D or -A-B-W-D-E, R3 is a hydroxyl group, a lower alkoxy group, a benzyloxy group, -Z, -Z-G or -Z-G-J, the above A, B, D, E, G and J independently each other are a residue of an amino acid selected from alanine, valine, leucine, isoleucine, serine, threonine, lysine, hydroxylysine, arginine, cysteine, methionine, phenylalanine, tyrosine, aspartic acid, asparagine, glutamic acid, glutamine and the like or an N-(C1-C4) alkyl derivative of these amino acid residues; the above W and Z independently each other are a residue of an amino acid selected from aspartic acid, asparagine, glutamic acid, glutamine, alanine, serine or lysine) or pharmacologically acceptable salts thereof.
The depsipeptides have an activity of promoting the production of apolipoprotein E and are useful as a therapeutic agent for neurologic damages, especially for dementia, and further as a therapeutic agent for hyperlipemia.
                            由式(1)代表的去肽类化合物:
 其中
R1 是 5-20 个碳原子的直链或支链烷基,或 5-15 个碳原子的直链或支链烷氧基甲基;R2是-A-B、-A-B-W、-A-B-W-D或-A-B-W-D-E,R3是羟基、低级烷氧基、苄氧基、-Z、-Z-G或-Z-G-J,上述A、B、D、E、G和J各自独立地是选自丙
氨酸、缬
氨酸、亮
氨酸、
异亮氨酸的
氨基酸残基、
氨基酸残基,或这些
氨基酸残基的 N-(C1-C4) 烷基衍
生物;上述 W 和 Z 相互独立地为选自
天冬氨酸、天冬酰胺、谷
氨酸、谷
氨酰胺、丙
氨酸、
丝氨酸或赖
氨酸的
氨基酸残基或其药理上可接受的盐。
去肽类化合物具有促进脂蛋白 E 生成的活性,可作为神经损伤,特别是痴呆症的治疗剂,还可作为高脂血症的治疗剂。