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 C2-4-alkylene, cis- or trans--CH2--CH= CH--CH2-, -CH2-C≡C-CH2- or
,
; A2 is C1-5-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
Authors
Dates
1998-12-27—Published
1993-01-14—Filed