Aminothiazoles with terminal aminocarboxylic acid grouping

C - Chemistry – Metallurgy – 07 – D

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C07D 501/20 (2006.01) C07D 277/20 (2006.01) C07D 277/48 (2006.01) C07D 501/00 (2006.01) C07D 501/59 (2006.01)

Patent

CA 1146535

ABSTRACT The invention relates to aminothiazolacetamido0 3-cephem-4-carboxylic acid compounds of the formula Image (I), in which the index n represents an integer of 1 to 4, X represents oxygen, sulphur, an -NH- group or the direct bond, Y represents oxygen or sulphur, A represents methylene or methylene substituted by amino, hydroxy, carboxyl, sulpho, oxo, or the group =N-O-R? in which R? repre- sents hydrogen or optionally substituted lower alkyl, R1 represents hydrogen, lower alkyl, an esterified or ehterified hydroxy or mercapto group, halogen, formyl or a group of the formula -CH2-R2 in which R2 represents an esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, and R3 represents hydrogen or methoxy, in which functional groups are optionally present in protected form, salts of such compounds with acidic and/or basic groups, processes for the manufacture fo these compounds, pharmaceutical agents containing such substances and their therapeutic use. The compounds have an antibiotic activity and can be used for combating infections. The invention also relates to new intermediates for the manufacture of the afore-mentioned compounds, processes for their manufacture and their use.

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