Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1982-09-27
1986-11-04
Rizzo, Nicholas S.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540225, 540227, C07D50136, A61K 31545
Patent
active
046210814
ABSTRACT:
Cephalosporin antibiotics of general formula: ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group, and Y.sup..sym. represents a C-linked 5- or 6-membered heterocyclic ring containing at least one C.sub.1-4 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-aminothiazol-4-yl)-2-(1-carboxycyclobut-1-oxyimino)ace tamido]-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.
REFERENCES:
patent: 4095021 (1978-06-01), Bradshaw et al.
patent: 4237128 (1980-12-01), Cimarusti et al.
patent: 4278793 (1981-07-01), Durckheimer et al.
patent: 4315005 (1982-02-01), Ayres et al.
patent: 4504477 (1985-03-01), O'Callaghan et al.
Ayres Barry E.
Livermore David G. H.
Newall Christopher E.
O'Callaghan Cynthia H.
Weir Niall G.
Glaxo Group Limited
Rizzo Nicholas S.
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