DERIVATIVES OF 7-ACYLAMINO-3-HETEROARYLTHIO-3-CEPHEM CARBOXYLIC ACID AND ANTIBACTERIAL COMPOSITIONS COMPRISING THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, antibiotics. SUBSTANCE: invention relates to new (7R)-7-acylamino-3-heteroarylthio-3-cephem carboxylic acid of the formula: or its pharmaceutically acceptable salts wherein R¹ is taken among group consisting of optionally substituted thiazole and optionally substituted thiadiazole; R³ represents substituted pyridyl, and also to compound of the formula: or its pharmaceutically acceptable salt wherein R′² is taken among group consisting of: -C(O)-R⁸⁸,-C(O)-OR⁸⁹,-C(O)-CH(NHR′³)-alk₄ and wherein R⁸⁸ represents or ; R′³ is taken among group consisting of hydrogen atom, alkyl and -C(O)-CH(NH₂)-alk₄ wherein alk₄ is taken among group consisting of hydrogen atom and alkyl optionally substituted with one or more substituents taken among group consisting of -COOH, -C(O) -OR⁸⁹, -C(O)NH₂, - OH, -NH_2/ and wherein R⁸⁹ is taken among group consisting of benzhydryl, tert.-butyl, allyl, p- nitrobenzyl, benzyl, p- or o-nitrobenzyl, 2,2,2-trichloroethyl, cinnamide, 2-chloroallyl, tert. -amyl, trityl, 4- methoxytrityl, 4,4'-dimethoxytrityl, trimethylsilyl, tert.-butyldimethylsilyl, β-(trimethylsilyl)-ethyl, 4- or 2- methoxybenzyl, 2,4-dimethoxybenzyl, 3,4-dimethoxybenzyl, 2,4,6-trimethoxybenzyl, methoxymethyl and 3,3-dimethylallyl. Invention relates also to an antibacterial composition used for treatment of methicillin- resistant staphylococcus bacterial infection comprising therapeutically effective dose of (7R)-7-acylamino-3- heteroarylthio-3-cephem-4-carboxylic acid or it salt in pharmaceutically acceptable carrier. Invention provides preparing new compounds that exhibit antibiotic activity with regards to broad order of organisms including organisms resistant to β-lactam antibiotics. EFFECT: valuable medicinal properties of compounds. 17 cl, 2 tbl, 140 ex