Cephalosporin antibiotics

Details Cephalosporin antibiotics Cephalosporin antibiotics

C - Chemistry, Metallurgy

07

D

260/104.1

C07D 501/46 (2006.01) C07D 277/20 (2006.01)

Patent

CA 1136616

ABSTRACT Cephalosporin antibiotics of general formula Image (I) (wherein Ra and Rb, which may be the same or differ- ent, each represent a C1-4 alkyl group, or together with the carbon atom to which they are attached form a C3-7 cycloalkylidene group and R1 represents a C1-4alkyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms. Particularly effective compounds of formula (I) are (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2- carboxyprop-2-oxyimino)acetamido]-3-(2-methyl- pyrazolium-l-ylmethyl)ceph-3-em-4-carboxylate and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-[(1-carboxy- cyclobut-l-oxyimino)acetamido]-3-(2-methylpyrazolium- l-ylmethyl)ceph-3-em-4-carboxylate. The invention also ,ncludes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I), compositions containing the antibiotic compounds of the invention and processes for the preparation of the antibiotics.

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