6-substituted penicillanic acid 1,1-dioxide compounds

Details 6-substituted penicillanic acid 1,1-dioxide compounds 6-substituted penicillanic acid 1,1-dioxide compounds

1986-02-06

1986-09-23

Rizzo, Nicholas S.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D49900, A61K 31425

Patent

active

046134620

ABSTRACT:
A series of novel derivatives of penicillanic acid 1,1-dioxide, having a disubstituted methyl group of the formula X-CH-Y at the 6-position, and the pharmaceutically-acceptable salts thereof and the pharmaceutically-acceptable esters thereof readily hydrolyzable in vivo, wherein X is hydroxy, acylated hydroxy or amino and Y is carboxy or esterified carboxy. The compounds of the invention are inhibitors of bacterial beta-lactamases, and they will protect certain beta-lactamase-susceptible beta-lactam antibiotics, e.g. ampicillin, against inactivation by beta-lactamases. Co-administration of a compound of the invention with a beta-lactam antibiotic such as ampicillin to a mammalian subject increases the effectiveness of the beta-lactam antibiotic against infections caused by beta-lactamase-producing bacteria.

REFERENCES:
patent: 4234579 (1980-11-01), Barth
patent: 4287181 (1981-09-01), Kellogg
patent: 4452796 (1984-06-01), Barth
patent: 4536393 (1985-08-01), Barth

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