PEPTIDE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHOD OF SYNTHESIS OF PEPTIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITION Russian patent published in 1997 - IPC

Abstract RU 2092491 C1

FIELD: chemistry of peptides. SUBSTANCE: product: peptide derivatives of the general formula (I): R1-A-CH2-(R2)-CON(R7)-CH2(R3)-CON(R6)-CO(R4)R5 where: R1 - hydrogen or acyl; R2 - lower alkyl, aryl-(lower)-alkyl; (C3-C7)-cycloalkyl-(lower)-alkyl; heterocyclic-(lower)-alkyl where heterocyclic group is the unsaturated 5,6-membered heteromonocyclic group containing 1-2 nitrogen atoms optionally substituted with imino-protective group; R3 - heterocyclic-(lower)-alkyl being heterocyclic group can be unsaturated fused 9-membered one containing one nitrogen atom and optionally substituted with a suitable substituent taken from (lower)-alkyl and imino-protective group, aryl-(lower)-alkyl; R4 - H, aryl-(lower)-alkyl, (lower)-alkyl, amino-(lower)-alkyl (free or protective one) and free or protective heterocyclic-(lower)-alkyl; heterocyclic group can be the unsaturated 5-6-membered one containing 1 or 2 nitrogen atoms or one sulfur atom and one nitrogen atom and optionally substituted imino-protective group; R5 - carboxy, protected carboxy, carboxy-(lower)-alkyl (free or protected one); R6 - H, heterocyclic-(lower)-alkyl where heterocyclic group is the saturated 6-membered heterocycle with one nitrogen atom; R7 - H or (lower)-alkyl; A - -O-, NH, (lower)-alkylimino, lower alkylene, or their pharmaceutically acceptable salts. Method of synthesis of compounds of the formula (I) involves condensation of two fragments R1ACH2(R2)-COOH and R7NHCH(R3)CON(R6)CH(R4)R8, and pharmaceutical composition containing pharmaceutically acceptable carrier and peptide derivative of the formula (I) as an active component taken at effective dose. The synthesized compounds were used in medicine for hypertension treatment and prophylaxis. EFFECT: improved method of synthesis. 8 cl

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RU 2 092 491 C1

Authors

Kejdzi Khemmi[Jp]

Masakhiro Neja[Jp]

Naoki Fukami[Jp]

Masasi Khasimoto[Jp]

Khirokazu Tanaka[Jp]

Natsuko Kajakiri[Jp]

Dates

1997-10-10Published

1991-05-13Filed