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

C - Chemistry – Metallurgy – 07 – D

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260/266.4, 260/2

C07D 498/04 (2006.01) C07D 503/00 (2006.01)

Patent

CA 1132548

ABSTRACT This invention provides the compounds of the formula (II) (II) Image and pharmaceutically acceptable salts and esters thereof, wherein A is an oxygen or sulphur atom or is a group NR5, wherein R5 is a hydrogen atom or a C1-6 alkyl, C1-6 alkanoyl, C1-6 alkoxycarbonyl, arylcarbonyl or aralkylcarbonyl group. any of such groups being optionally substituted by C1-3 alkyl, C1-3 alkoxy, hydroxy, C1-3 alkanoyloxy, or esterified or salified carboxy; or R5 is a group of the sub-formula (i): Image (i) wherein X is a bond or a -CH2- moiety; R6 is hydrogen, fluorine. chlorine. bromine. C1-3 alkyl, C1-3 alkoxy or hydroxy, R7 is hydrogen or C1-3 alkyl, and R8 is hydrogen or C1-3 alkyl, and R3 and R4 are independently hydrogen or C1-6 alkyl; these compounds are useful as antibacterial agents and as .beta.-lactamase inhibitors. Their preparation and use are described.

362824

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