| abstract |
FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of barbituric acid and pharmaceutical composition with inhibitory effect on activity of metalloproteases. New derivatives of barbituric acid corresponds to the general formula (I) where X, Y, Z are oxygen; R 1 means the group W-V where W is a valent bond or means direct or branched C 1 -C 4 -alkyl group; V is a monocycle taken among the optionally substituted phenyl, pyridyl, piperidyl, thiophenyl, imidazolyl or a bicycle taken among naphthyl, quinolinyl, tetrahydroquinolyl, tetrahydroisoquinolyl, benzimidazolyl or indolyl being each of that can be substituted or W-V means optionally substituted C 1 -C 20 -alkyl group; R 2 ,R 3 both are hydrogen atom; R 4 ,R 5 mean independently each of other A-D where A and D have different values indicated in the claim of invention, or R 4 ,R 5 in common with nitrogen atom with which they are bound form a ring that can be broken additionally by N atom and can be substituted as indicated in the claim of invention. Pharmaceutical composition includes at least one compound of the formula (I) and usual substance-carriers and accessory substances additionally. EFFECT: new compound indicated above, valuable biochemical properties. 8 cl, 2 tbl |