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AMINO ACIDS AND PEPTIDES HAVING MODIFIED TYROSINE RESIDUE, PREPARATION THEREOF AND APPLICATION AS MEDICAMENTS

机译:具有修饰的酪氨酸残基的氨基酸和肽,其制备方法及作为药物的应用

摘要

These compounds are represented by formula I, wherein R 1 to R 2 = H, C 1 -C 8 alkyl, C 3 -C 7 cycloalkyl or aromatic; (When R1 = H, R2 may be amine protecting group, amino acid residue or peptide fragment, R1 and R2 may form with N a 5-7 membered ring); A = carbonyl or methylene; W = hydroxy, phenoxy, C 1 -C 8 alkoxy, phenoxy (C 1 -C 8) alkyl, amino, (C 1 -C 8) alkylamino, di (C 1 -C 8) alkylamino, (when A = carbonyl, W = amino acid residue or peptide fragment); Y = -OSO 2 OR 3 II, -OPO (OR 3) 2 III, - (CH 2) m -SO 2 OR 3 IV or - (CH 2) m -PO ( OR3) 2 V [R3 = H, C1-C8 alkyl; m = 1 to 4]; Z = cyclohexane, pyridyl or phenyl; n = 0 to 4; provided that when Y = II or III, -A-W is other than a sequence composed of natural amino acids. They have antipsychotic properties, an effect facilitating memory processes, analgesic properties; they are useful as anorectics, and they have effects stimulating the intestinal motility. BR/ (CF DRAWING IN BOPI) BR/ / P
机译:这些化合物由式I表示,其中R 1至R 2 = H,C 1 -C 8烷基,C 3 -C 7环烷基或芳族基; (当R1 = H时,R2可以是胺保护基,氨基酸残基或肽片段,R1和R2可以与N形成5-7元环); A =羰基或亚甲基; W =羟基,苯氧基,C 1 -C 8烷氧基,苯氧基(C 1 -C 8)烷基,氨基,(C 1 -C 8)烷基氨基,二(C 1 -C 8)烷基氨基(当A =羰基时, W =氨基酸残基或肽片段); Y = -OSO 2 OR 3 II,-OPO(OR 3)2 III,-(CH 2)m -SO 2 OR 3 IV或-(CH 2)m -PO(OR3)2 V [R3 = H,C1 -C 8烷基; m = 1至4]; Z =环己烷,吡啶基或苯基; n = 0至4;前提是当Y = II或III时,-A-W不是由天然氨基酸组成的序列。它们具有抗精神病特性,促进记忆过程,镇痛特性;它们可用作厌食药,并且具有刺激肠蠕动的作用。
(CF在BOPI中绘制)

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