AMIDINE DERIVATIVES, MIXTURE OF THEIR ISOMERS OR SEPARATE ISOMERS AND SALTS, PHARMACEUTICAL COMPOSITION SHOWING ANTAGONISTIC EFFECT WITH RESPECT TO LEUKOTRIENE-B Russian patent published in 1998 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of amidine of the formula (I) where R₁ and R₂ are similar or distinct and mean hydrogen, halide, alkyl, phenyl possibly substituted with halogen, alkyl, alkoxyl or acyl, OR₅ where R₅ - H, alkyl, phenyl possibly substituted with halogen, alkyl, alkoxyl or acyl, group SO₂R₆ where R₆ - alkyl, phenyl, COR₆; or R₁ and R₂ together mean groups -CR₈=CR₉-CH= CH-, -CH=CR₈-CR₉=CH- or -CR₈=CH--CR₉=CH- bound with adjacent carbon atoms of benzene ring where R₈ and R₉ mean H, OH, alkyl, alkoxy, acyl or -O--CHR₁₀-CH₂ where R₁₀ - H, alkyl or -CO--CH₂-CH₂-O-; R₃ - hydroxyl, H, alkyl, alkoxy or acyl, phenyl; R₄ - H or alkoxy; A - one of group X₁-A-X₂ (a) or X₂-A₂-X₃ (b) where A₁ is C_2-4-alkylene, cis- or trans--CH₂--CH= CH--CH₂-, -CH₂-C≡C-CH₂- or , ; A₂ is C_1-5-alkylene; X₁ - O, imino, sulfur, sulfinyl, carbonyl, methylene; X₂ - oxygen or sulfur atom, imino-group or ; X₃ is NH-CO, CO-NH or SO₂-NH; B - a group CH=CH or CH=N, a mixture of their isomers, or separate isomers and their salts. Pharmaceutical composition has compounds of the formula (I) as an active component and shows antagonistic effect with respect to leukotriene-B₄ and can be used, in part, for treatment of patients with asthma and ulcer colitis. EFFECT: improved method of synthesis. 11 cl, 5 tbl, 29 ex