Cephalosporin antibiotics

Details Cephalosporin antibiotics Cephalosporin antibiotics

C - Chemistry, Metallurgy

07

D

260/104.1

C07D 501/36 (2006.01)

Patent

CA 1129408

ABSTRACT OF THE DISCLOSURE Cephalosporin antibiotics of general formula: (I) Image (wherein Ra and Rb, which may be the same or different, each represent a C1-4 alkyl group or Ra and Rb together with the carbon atom to which they are attached form a C3-7 cycloalkylidene group, and Y? represents a C-linked 5- or 6-membered heterocyclic ring containing at least one C1-4 alkyl-substituted quaternary nitrogen atom, which ring may also contain one or more sulphur atoms) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms. A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties is (6R,7R)-7-[(Z)-2-(2-amino- thiazo1-4-yl)-2-(1-carboxycyclobut-1-oxyimino)acetamido] -3-[(1-methylpyridinium-4-yl)-thiomethyl]ceph-3-em-4- carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of the antibiotics.

328416

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