abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes derivatives of [1,2,4]-triazolo-[4,3-a] of the general formula (I) where R 1 means linear or branched C 1-6 -alkyl, substituted COX' or POX'X'' where X' and X'' means independently hydroxyl- or alkoxy-group; R 6 and R 9 mean hydrogen atom; R 7 means CF 3 and R 8 means imidazolyl, piperidino- or morpholino-group being their rings are optionally substituted with one or two substituents taken among phenyl and C 1-6 -alkyl, or their pharmaceutically acceptable salts. Compounds of the formula (I) show antagonistic activity with respect to AMPA-receptors and are useful for treatment of patients with symptoms of hyperactivity of exciting neuromediators. Invention proposes also method of synthesis of compounds of the formula (I), pharmaceutical composition based on said and method of inhibition of AMPA-receptors activity. EFFECT: improved method of synthesis, valuable pharmacological properties. 8 cl, 1 tbl, 13 ex |