Heterocyclic esters of phenoxybenzoic acids

C - Chemistry – Metallurgy – 07 – D

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C07D 307/20 (2006.01) A01N 43/04 (2006.01) A01N 43/08 (2006.01) A01N 43/16 (2006.01) C07C 205/59 (2006.01) C07D 309/12 (2006.01)

Patent

CA 1175849

ABSTRACT The compounds of the formula: Image and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof wherein R1 is a hydrogen atom or a group selected from OH, OSO3H or a pharmaceutically acceptable salt or C1-4 alkyl ester thereof, OR2, SR3, OCOR2, OCO2R3 or OCONHR3, where R2 is a C1-6 alkyl group or an optionally substituted benzyl group and R3 is a C1-6 alkyl group or an optionally substituted benzyl or an optionally substituted phenyl group; and R22 is a hydrogen atom, C1-6 alkyl, C2-6 alkenyl, C3-6 alkynyl wherein the triple bond is not present on the carbon adjacent to the sulphur atom, aralkyl, C1-6 alkanoyl, aralkanoyl, aryloxyalkanoyl or arylcarbonyl, any of such R22 groups being optionally substituted; with the proviso that when R22 is 2-aminoethyl R1 must be SR3 or OSO3H or a pharmaceutically acceptable salt or C1-4 alkyl ester thereof; have been found to be antibacterially active. Their use is described as are processes for their preparation.

419935

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