DERIVATIVES OF DIPEPTIDE P-AMIDINOBENZYLAMIDES WITH N-TERMINAL SULFONYL RESIDUES AND THEIR SALTS WITH PHYSIOLOGICALLY ACCEPTABLE ACIDS Russian patent published in 2000 - IPC

FIELD: organic chemistry, peptide derivatives. SUBSTANCE: invention describes the novel derivatives of dipeptide p-amidinobenzylamides with N-terminal residues of the general formula (I) where R is alkyl with 1-20 carbon atoms, fluoroalkyl with 1-3 carbon atoms, arylalkyl with 1-10 carbon atoms in alkyl moiety, aryl, heteroaryl that is five- or six-membered aromatic cycle containing one nitrogen or sulfur as heteroatom, hydroxyl or R²R³N where R² and R³ are similar or different and mean hydrogen atom, alkyl with 1-10 carbon atoms; A means residue of α-amino acid of the formula (II) where R⁴ means hydrogen atom, cycloalkyl with 3-7 carbon atoms or aryl; R⁵ means hydrogen atom, cycloalkylalkyl with 3-7 carbon atoms in cycloalkyl moiety and 1-3 carbon atoms in alkyl moiety, arylalkyl with 1-3 carbon atoms in alkyl moiety; B means residue of cyclic α-amino acid of the formula (III) where m = 2, 3 or 4 and if m = 3 or 4 then two adjacent hydrogen atoms can be replaced with double bond, or their salt with physiologically acceptable acids. Compounds of the formula (I) show biological activity, in part, they inhibit activity of thrombin. EFFECT: new compounds indicated above, valuable pharmacological activity. 2 cl, 1 tbl, 22 ex