PEPTIDE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF PROPHYLAXIS AND ELIMINATION OF THROMBOSIS Russian patent published in 1998 - IPC

FIELD: organic chemistry, peptides. SUBSTANCE: product: peptide derivatives of the general formula (I): where: R¹ - aryl that can contain 1-3 substituents taken from amidino- and protected amidine group; R² - carboxy(lower)alkyl or protected carboxy(lower)alkyl; R³ - carboxy or protected carboxy-group; A¹ - alkylene that can contain 1-3 substituents taken from amino- and protected amino-group; A² - -N(R⁴)CH₂CO- where R⁴ - lower alkyl; or group A²: -NHCH₂CH₂CO-; A³ - lower alkylene containing 1-3 substituents taken from: lower alkyl, mono-, di- or triphenyl(lower)alkyl containing 1-3 substituents taken from the group: hydroxy, lower alkoxy, protected hydroxy, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, [cyclo(lower)alkyl]-(lower)alkyl, pyridyl(lower)alkyl; l, m and n are similar or different and mean whole number 0 or 1 at condition that A² can not be group -NHCH₂CH₂CO- if l = 0, or pharmaceutical salts. Peptides can be synthesized by two ways: a) by interaction of compounds of the formula (II): or their reactive derivatives with compounds of the formula (III): and protected groups were split off from the condensation product; or b) by interaction of compounds of the formula (IV): with compounds of the formula (V): H₂NCHR²CONHA³R³, or their reactive derivatives by amino-group. Pharmaceutical composition has peptide derivatives of the formula (I) as an active component taken at effective amount. The synthesized compounds were used in medicine for prophylaxis and elimination of thrombosis in mammals by administration of derivatives of the formula (I) at daily dose 0.001-200 mg/kg mass for 2-4 doses. EFFECT: improved method of synthesis. 12 cl, 3 tbl