Derivatives of clavulanic acid, a process for their preparation

Details Derivatives of clavulanic acid, a process for their preparation Derivatives of clavulanic acid, a process for their preparation

1980-09-24

1982-08-10

Berch, Mark L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

2602453, 542420, C07D49804, A61K 3142

Patent

active

043438075

ABSTRACT:
The compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and esters thereof wherein X is a C.sub.1-6 alkylene group; m is 1, 2 or 3; n is 1, 2 or 3; A is oxygen, sulphur, --CH.sub.2 -- or --NR.sup.3 -- wherein R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-6)alkyl; R.sup.1 is hydrogen, oxo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or phenyl; and R.sup.2 is hydrogen, oxo, C.sub.1-6 alkyl or phenyl: with the proviso that if m and n are both 1 then A is --CH.sub.2 -- and R.sup.2 is not oxo: have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use are described.

REFERENCES:
patent: 3926955 (1975-12-01), Burton et al.
patent: 4229443 (1980-10-01), Bendrup
patent: 4231928 (1980-11-01), Naito et al.
patent: 4237051 (1980-12-01), McCombie
patent: 4244965 (1981-01-01), Howartt
patent: 4246262 (1981-01-01), Vangedal
patent: 4252772 (1981-02-01), Melillo
patent: 4278686 (1981-07-01), Corbett
Brook et al. The Lancet, Feb. 7, 1981, p. 332.
Stirling et al. Chem Abs. 92, 163955d (1979).

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