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filingDate 2000-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2004-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a1140bb7c4750ac3209e48325ac2f739
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publicationDate 2004-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2225868-C2
titleOfInvention Derivatives of 7-acylamino-3-heteroarylthio-3-cephem carboxylic acid and antibacterial compositions comprising thereof
abstract 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 R 1 is taken among group consisting of optionally substituted thiazole and optionally substituted thiadiazole; R 3 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)-R 88 ,-C(O)-OR 89 ,-C(O)-CH(NHR′ 3 )-alk 4 and wherein R 88 represents or ; R′ 3 is taken among group consisting of hydrogen atom, alkyl and -C(O)-CH(NH 2 )-alk 4 wherein alk 4 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) -OR 89 , -C(O)NH 2 , - OH, -NH 2/ and wherein R 89 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
priorityDate 1999-09-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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