首页> 外国专利> DERIVATIVES OF POLYPEPTIDE SHOWING INSULINOTROPIC ACTIVITY, PHARMACEUTICAL COMPOSITION, METHODS OF ENHANCEMENT OF INSULIN EFFECT, METHODS OF TREATMENT OF DIABETIC PATIENTS

DERIVATIVES OF POLYPEPTIDE SHOWING INSULINOTROPIC ACTIVITY, PHARMACEUTICAL COMPOSITION, METHODS OF ENHANCEMENT OF INSULIN EFFECT, METHODS OF TREATMENT OF DIABETIC PATIENTS

机译:展示胰岛素营养活性的多肽衍生物,药物成分,增强胰岛素作用的方法,糖尿病患者的治疗方法

摘要

FIELD: chemistry of proteins, medicine, endocrinology, pharmacy. SUBSTANCE: invention proposes a derivative of polypeptide containing primary structure H2N-R-COOH where R means amino acid sequence ID No 2: His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp- -Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala- -Trp-Leu-Val-Lys-Gly-Arg-Gly or its pharmaceutically acceptable salts. Derivative exhibits value pI 4.0 or less or pI 7.0 or above and shows insulinotropic activity. Derivative is a esterified, amidated, deamidated, alkylated or acetylated polypeptide. Polypeptide is synthesized by interaction with cyclic anhydride, additional C-terminal basic and/or neutral amino acid or connected acids, or by combination of two or more these variants. Derivative of the mentioned above primary structure at condition that the above mentioned derivative is not complex C-terminal alkylester containing (C1-C6)-alkyl of linear or branched chain of the primary structures and at condition that the mentioned above derivative is not C-terminal carboxamide of the formula CONR2R3 of the mentioned above primary structure where R2 and R3 means each means independently H or (C1-C6)-alkyl of linear or branched chain. Invention describes a pharmaceutical composition on the basis of the above indicated polypeptide derivative that can be used for treatment of diabetic patients. Invention proposes a method for enhancement of insulin effect in mammalian and a method of treatment of diabetic patients using the above indicated polypeptide. EFFECT: enhanced effectiveness of polypeptide for diabetic patients treatment. 23 cl, 1 tbl, 1 ex
机译:领域:蛋白质化学,医学,内分泌学,药学。物质:本发明提出了包含一级结构H 2 NR-COOH的多肽的衍生物,其中R表示氨基酸序列ID No 2:His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp --Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala--Trp-Leu-Val-Lys-Gly-Arg-Gly或其药学上可接受的盐。衍生物的pI值等于或小于4.0或pI值等于或大于7.0,并且具有促胰岛素活性。衍生物是酯化,酰胺化,脱酰胺基,烷基化或乙酰化的多肽。多肽是通过与环状酸酐,其他C端碱性和/或中性氨基酸或连接的氨基酸相互作用,或通过将两种或多种这些变体组合而合成的。在上述衍生物不是包含直链或支链的(C 1 -C 6 )-烷基的复杂的C末端烷基酯的条件下,上述一级结构的衍生物且在上述衍生物不是上述主要结构式CONR 2 R 3 的C末端羧酰胺的条件下,其中R 2 和R 3 表示各自独立地表示直链或支链的H或(C 1 -C 6 )-烷基。本发明基于上述指示的多肽衍生物描述了可用于治疗糖尿病患者的药物组合物。本发明提出了使用上述指示的多肽增强哺乳动物胰岛素作用的方法和治疗糖尿病患者的方法。效果:增强多肽治疗糖尿病患者的有效性。 23 cl,1 tbl,1前

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