首页> 外国专利> CNS-Active N-acyl-asparagyl-glutamic acids and salts - prepd by reacting N-acyl aspartic acid with anhydride, then reaction with glutamic acid salt

CNS-Active N-acyl-asparagyl-glutamic acids and salts - prepd by reacting N-acyl aspartic acid with anhydride, then reaction with glutamic acid salt

机译:CNS活性N-酰基-天冬酰胺-谷氨酸和盐-通过将N-酰基天冬氨酸与酸酐反应,然后与谷氨酸盐反应制备

摘要

N-Acyl(alpha- andd beta-)asparaglyl-glutamic acids and salts in L- or DL-form, are of general formula (I) and (II): (in which M = a cation with n-valency which is either a metal cation of a cation of an organic substance such as amino alcohol, amino acid or a quat. ammonium cpd. e.g., a betaine or choline; R = acyl; m = 0,1,2 or 3 and varies with the number of carboxyl gps. converted to the salt form, whereby m = not 0 when R = acetyl). Specif. cpd. includes Na-salt of N-acetyl-asparagyl-glutamic acid and the K-salt of N-propionyl-asparagyl-glutamic acid both as alpha- and/or beta-isomers in L- or DL-configuration). (I) and (II) allow the introduction of an asparagyl-glutamic acid peptide into the animal and human organism. The salts increase the activity and have selective CNS-activity. They may be used in the treatment of cerebral tiredness, conditions of shock, weakness and depression, loss of memory, etc. They also have cardiovascular activity.
机译:L-或DL形式的N-酰基(α-和β-)天冬酰胺基谷氨酸及其盐具有通式(I)和(II):(其中M =具有n价的阳离子有机物质(如氨基醇,氨基酸或季铵基cpd,例如甜菜碱或胆碱)的阳离子的金属阳离子; R =酰基; m = 0,1,2或3,并随羧基转化为盐形式,其中当R =乙酰基时,m =不为0。规格。 cpd。包括N-乙酰基-天冬酰胺基-谷氨酸的Na-盐和N-丙酰-天冬酰胺基-谷氨酸的K-盐,均为L-或DL-构型的α-和/或β-异构体。 (I)和(II)允许将天冬酰胺基谷氨酸肽引入动物和人类有机体。盐增加了活性并具有选择性的CNS活性。它们可用于治疗脑疲劳,休克,虚弱和沮丧,记忆力减退等。它们还具有心血管活性。

著录项

  • 公开/公告号JPS5827263B2

    专利类型

  • 公开/公告日1983-06-08

    原文格式PDF

  • 申请/专利权人 TEA TERAPUTEIIKU E APURIKASHION SA;ORUSAN;

    申请/专利号JP19750005878

  • 发明设计人 JORUJU SHIBURE;GUEN KON DATSUKU;

    申请日1975-01-10

  • 分类号A61K38/00;A61P25/00;C07C237/12;C07C237/22;C07K5/06;C07K5/072;

  • 国家 JP

  • 入库时间 2022-08-22 12:05:34

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