Cephalosporin antibiotics

Details Cephalosporin antibiotics Cephalosporin antibiotics

C - Chemistry, Metallurgy

07

D

260/104.1

C07D 501/46 (2006.01) A61K 31/545 (2006.01) A61K 31/55 (2006.01) C07D 501/38 (2006.01) C07D 501/56 (2006.01)

Patent

CA 1144156

ABSTRACT Processes for the preparation of cephalosporin antibiotics of general formula Image (I) (wherein Ra and Rb, which may be the same or different, each represent a C1-4 alkyl group, or together with the carbon atom to which they are attached form a C3- 7 cycloalkylidene group). These compounds 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-(pyridazinium-1-ylmethyl)ceph- 3-em-4-carboxylate and (6R,7R)-7- (Z)-2-(2-aminothiazol- 4-yl)-2- (1l-carboxycyclobut-l-oxyimino)acetamido -3- (pyridazinium-1-ylmethyl)ceph-3-em-4-carboxylate. The invention also includes processes for the preparation of the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I).

346275

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