6-substituted penicillanic acid 1,1-dioxide compounds
US4590073A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Jul 2, 1985 |
| Grant date | May 20, 1986 |
| Priority date | — |
| Expiry date | Jul 2, 2005 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.