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    • 2. 发明公开
    • Peptides containing an N-substituted glycine residue
    • N-取代基甘氨酸enthaltende肽
    • EP0934952A2
    • 1999-08-11
    • EP98124653.1
    • 1998-12-24
    • Nisshin Flour Milling Co., Ltd.
    • Yanai, MakotoSuzuki, MasashiOshida, NorioKawamura, KojiHiramoto, ShigeruYasuda, OrieKinoshita, NobuhiroShingai, AkikoTakasu, Masako
    • C07K7/06A61K38/08
    • C07K7/06A61K38/00
    • A depsipeptide containing N-substituted glycine residue having the formula (1) or (2):

      (wherein R 1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms; R 2 is a group of the formula -A-B-W-(D) m -(E) n , -A-B-W-(D) m -(E) n -F or -A-B-W-(D) m -(E) n -F-Z; R 3 is a hydroxyl group, a lower alkoxy group, a benzyloxy group, or a group of the formula -Z, -Z-G or -Z-G-J; A, B, D, E, F, G and J independently are an N-substituted glycine residue or a residue of an amino acid selected from the group consisting of alanine, valine, leucine, serine, etc.; Wand Z independently are a residue of an amino acid selected from the group consisting of an aspartic acid, a glutamic acid, etc.; at least one of A, B, D, E, F, G and J is an N-substituted glycine residue) or a pharmacologically acceptable salt thereof.
      The above depsipeptides have a promoting activity on the production of apolipoprotein E, and are useful as a therapeutic agent for neurologic damages, especially dementia, and hyperlipemia.
    • 含有具有式(1)或(2)的N-取代的甘氨酸残基的缩酚酸肽:其中R 1是5-20个碳原子的直链或支链烷基或5或5的直链或支链烷氧基甲基 -15的碳原子; R2是式-ABW-(D)m-(E)n,-ABW-(D)m-(E)nF或-ABW-(D)m-(E)nFZ R3是羟基,低级烷氧基,苄氧基或式-Z,-ZG或-ZGJ的基团; A,B,D,E,F,G和J独立地是N-取代的 甘氨酸残基或选自丙氨酸,缬氨酸,亮氨酸,丝氨酸等的氨基酸的残基; W和Z独立地是选自天冬氨酸,谷氨酸, A,B,D,E,F,G和J中的至少一个是N-取代的甘氨酸残基)或其药理学上可接受的盐。 上述脱脂肽对载脂蛋白E的产生具有促进作用,可用作神经损伤,特别是痴呆和高脂血症的治疗剂。