THROMBIN INHIBITORS Russian patent published in 2002 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel inhibitors of thrombin of the formula (I): A-B-C-Lys-D where A means H, 2- hydroxy-3-cyclohexylpropionyl-group, R₁, R₁-CO-, R₁-SO₂-,-(CHR₂)_nCOOR₃- where R₁ is taken among -(1-6C)-alkylene-COOH, (1-12C)-alkyl, (6-14C)-aryl, (7-15C)-aralkyl and (8-16C)-aralkenyl and this aryl-group can be substituted with (1-6C)-alkyl, (2-12C)-alkoxy-group or halogen atom; R₂ means H or (1-12C)-alkyl; R₃ means H or (1-12C)-alkyl; n = 1-3; B means a bond L-Asp, Leu, norLeu, -N-(benzyl)-CH₂-CO-, -N- (2-indane)-CH₂-CO-, D-1-Piq, D-Tiq, Atc or D-amino acid having hydrophobic aromatic side chain; C means Pro, norLeu(cyclo)Gly, amino acid of one of formulas -N-[(3-8-C)-cycloalkyl] - CH₂-CO- or -N-(benzyl)-CH₂-CO-; D is taken among COOH, tetrazole, oxazole, thiazole and benzothiazole; or A and C have the above indicated values; B means D-(3-8C)-cycloalkylalanine and D means tetrazole, oxazole, thiazole or benzothiazole; or its prodrug; or its pharmaceutically acceptable salt with exception of the compound Me-D-Phe-Pro-Lys-COOH. The above indicated compounds can be used as antithrombotic agents. EFFECT: new thrombin inhibitors indicated above, valuable medicinal properties. 9 cl