Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...
Patent
1980-03-21
1982-02-09
Coughlan, Jr., Paul M.
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Bacterium or component thereof or substance produced by said...
544 25, A61K 31545, C07D50156
Patent
active
043150055
ABSTRACT:
Cephalosporin antibiotics of general formula ##STR1## (wherein R.sup.1 and R.sup.b, which may be the same or different, each represent a C.sub.1-2 alkyl group, or together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkylidene group and Y.sup..sym. represents a 1-carbamoylmethylpyridinium 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)acetami do]-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)acet amido]-3-[(1-carbamoylmethylpyridinium-4-yl)thiomethyl]-ceph-3-em-4-carboxy late. The invention also includes 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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Ayres Barry E.
Weir Niall G.
Coughlan, Jr. Paul M.
Glaxo Group Limited
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