Cephalosporin antibiotics

Details Cephalosporin antibiotics Cephalosporin antibiotics

C - Chemistry, Metallurgy

07

D

260/104.1

C07D 501/36 (2006.01) C07D 213/20 (2006.01)

Patent

CA 1144920

ABSTRACT "Cephalosporin antibiotics" Cephalosporin antibiotics of general formula Image (I) (wherein Ra and Rb, which may be the same or different, each represent a C1-2 alkyl group, or together with the carbon atom to which they are attached form a C3-6 cycloalkylidene group and Y ? represents a 1-carbamoyl- methylpyridinium 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-carboxy- prop-2-oxyimino)acetamido]-3-[(1-carbamoylmethylpyridinium- 4-yl)thiomethyl]ceph-3-em-4-carboxylate and (6R,7R)- [(Z)-2-(2-aminothiazol-4-yl)-2-[(1-carboxycyclobut- 1-oxyimino)acetamido]-3-[(1-carbamoylmethylpyridinium- 4-yl)thiomethyl]-ceph-3-em-4-carboxylate. The invention also includes the non-toxic salts and non-toxic metabol- ically labile esters of compounds of formula (I), com- positions containing the antibiotic compounds of the invention and processes for the preparation of the antibiotics.

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