| 摘要 |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of amidine of the formula (I) <EMI ID=0.311 HE=21 WI=60 TI=CHI> where R<SB>1</SB> and R<SB>2</SB> are similar or distinct and mean hydrogen, halide, alkyl, phenyl possibly substituted with halogen, alkyl, alkoxyl or acyl, OR<SB>5</SB> where R<SB>5</SB> - H, alkyl, phenyl possibly substituted with halogen, alkyl, alkoxyl or acyl, group SO<SB>2</SB>R<SB>6</SB> where R<SB>6</SB> - alkyl, phenyl, COR<SB>6</SB>; or R<SB>1</SB> and R<SB>2</SB> together mean groups -CR<SB>8</SB>=CR<SB>9</SB>-CH= CH-, -CH=CR<SB>8</SB>-CR<SB>9</SB>=CH- or -CR<SB>8</SB>=CH--CR<SB>9</SB>=CH- bound with adjacent carbon atoms of benzene ring where R<SB>8</SB> and R<SB>9</SB> mean H, OH, alkyl, alkoxy, acyl or -O--CHR<SB>10</SB>-CH<SB>2</SB> where R<SB>10</SB> - H, alkyl or -CO--CH<SB>2</SB>-CH<SB>2</SB>-O-; R<SB>3</SB> - hydroxyl, H, alkyl, alkoxy or acyl, phenyl; R<SB>4</SB> - H or alkoxy; A - one of group X<SB>1</SB>-A-X<SB>2</SB> (a) or X<SB>2</SB>-A<SB>2</SB>-X<SB>3</SB> (b) where A<SB>1</SB> is C<SB>2-4</SB>-alkylene, cis- or trans--CH<SB>2</SB>--CH= CH--CH<SB>2</SB>-, <EMI ID=0.312 HE=6 WI=27 TI=CHI> or <EMI ID=0.313 HE=15 WI=27 TI=CHI>, <EMI ID=0.314 HE=15 WI=27 TI=CHI>; A<SB>2</SB> is C<SB>1-5</SB>-alkylene; X<SB>1</SB> - O, imino, sulfur, sulfinyl, carbonyl, methylene; X<SB>2</SB> - oxygen or sulfur atom, imino-group or <EMI ID=0.315 HE=12 WI=21 TI=CHI>; X<SB>3</SB> is NH-CO, CO-NH or SO<SB>2</SB>-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-B<SB>4</SB> 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
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