Derivatives of clavulanic acid, a process for their...

A - Human Necessities – 61 – K

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A61K 31/545 (2006.01) A61K 31/43 (2006.01)

Patent

CA 1177400

A B S T R A C T Synergistic compositions comprising compounds of the formula (II): Image (II) or pharmaceutically acceptable salts or esters thereof wherein A is a hydrogen atom or an esterifying radical; X is an alkyl group of 1-12 carbon atoms optionally substituted by a hydroxy, amino, acylamino of C1-6 alkoxy group, which substituents are not on the carbon atom adjacent to the nitrogen atom; or a C5-7 cyclo- alkyl group; or a phenylalkyl group wherein the carbon atom content of the alkyl part is 1-6 and the phenyl part is optionally substituted with a fluorine, bromine, chlorine, C1-6 alkyl, or C1-6 alkoxy; with the proviso that when X represents an optionally substituted phenyl- alkyl group and A represents C1-3 alkyl, then the -CO2A group is attached to the alkyl part of the phenyl- alkyl group; in admixture with penicillins and/or cephalosporins in pharmaceutically acceptable form. These compositions have enhanced activity as .beta.-lactamase inhibitors and antibacterial agents.

443122

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