PEPTIDE, ITS PRODUCTION AND USE

摘要

PURPOSE:To provide a new peptide having endothelin-receptor antagonistic action and useful as an agent for the prevention and treatment of hypertension, cardiac and cerebral circulation diseases, renal diseases, asthma, etc. CONSTITUTION:The peptide of formula I [R1 is fat-soluble group; R2 and R5 are H or lower alkyl; R3 is aliphatic group which may contain O or S; R4 is (substituted) heterocyclic-lower alkyl; R6 is H, aromatic group, etc.; X is group having aromatic ring; n is 0 or >=1; m is >=2] or its salt, e.g. the peptide of formula It. The peptide can be produced e.g. by successively condensing amino acids according to the sequence of formula I by solid-phase synthesis or liquid-phase synthesis, optionally removing protecting group from the obtained peptide and separating and purifying the peptide by column chromatography, liquid chromatography, etc.