Compounds with terminal aminocarboxylic acid grouping

C - Chemistry – Metallurgy – 07 – D

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C07D 501/20 (2006.01) C07D 307/52 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01)

Patent

CA 1113453

Compounds with terminal aminocarboxylic acid grouping Abstract of the Disclosure Acylamido-3-cephem-4-carboxylic acid compounds of the formula Image (I) in which the index n represents an integer of from 1 to 4, the index m represents 0 or 1, X represents oxygen, sulphur or an -NH- group, W represents a -CO-, -CO-NHSO2- or -SO2NH-CO- group, or X-W together represent a -CO- or -CO-NHSO2- group, A represents optionally substituted phenylene, thienylene or furylene, Y represents hydrogen, hydroxyl, formyloxy, amino or sulpho optionally present in salt form, and Z represents hydrogen, or Y and Z together represent an oxo group or an =N-O-Ro group in which Ro represents hydrogen or optionally substituted lower alkyl, R1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula -CH2-R2 in which R2 is a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, and R3 represents hydrogen or methoxy, wherein the carboxyl groups are optionally esterified in a form that can be split under physiological conditions, and the salts thereof, are obtained by liberating the functional group(s) in a starting compound of the formula I in which at least one of the functional groups present is protected. The compounds are effective in vitro and in vivo against gram-positive and gram-negative bacteria and cocci.

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