Anti-bacterial agents

A - Human Necessities – 61 – K

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A61K 31/545 (2006.01)

Patent

CA 1118349

ABSTRACT A synergistic pharmaceutical composition which comprises a penicillin or a cephalosporin and a compound of the formula (II): Image (II) or an ester thereof or a pharmaceutically acceptable acid addition salt of such an ester wherein R1 is a hydrogen atom, an alkyl group of up to 5 carbon atoms, a cycloalkyl group of 5 or 6 carbon atoms, a hydroxylalkyl group of up to 5 carbon atoms or a moiety of the sub-formula (a): Image wherein R2 is a hydrogen, fluorine, chlorine or bromine atom or an alkyl group of 1-3 carbon atoms, an alkoxy group of 1-3 carbon atoms, an acyloxyl group of 1-3 carbon atoms, hydroxyl group, an alkoxycarbonyl group containing 1-3 carbon atoms in the alkoxy part, or a group -N(R5)CO.R6, -N(R5)SO2R6, -CO-NR5R6 where R5 is a hydrogen atom or an alkyl group of 1-3 carbon atoms or a phenyl or benzyl group and R6 is an alkyl group of 1-3 carbon atoms or a phenyl or benzyl group; R3 is a hydrogen, fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms, an alkoxy group of 1-3 carbon atoms or an acyloxy group of 1-3 carbon atoms; and R4 is a hydrogen fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms or an alkoxy group of 1-3 carbon atoms and when required a pharmaceutically acceptable carrier therefor. The compounds of the formula (II) have antibacterial activity which is enhanced in the presence of the penicillin or cephalosporin.

368440

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