Broad spectrum beta-lactamase inhibitors
US8883772B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 9, 2008 |
| Grant date | Nov 11, 2014 |
| Priority date | — |
| Expiry date | Mar 4, 2031 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D501/60
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Compounds of the invention include those of formula:and pharmacologically acceptable salts thereof where variables Z, Y, M, y, n, R, R4, R5, R1 and R2 are as defined in the specification. M most generally represents a chemical moiety which is in conjugation with the nitrogen of the core beta-lactam ring system of the compound, such that one or more reactive species, e.g., electrophilic or nucleophilic sites are generated on modification of M which is initiated by cleavage of the beta-lactam ring. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions containing compounds of the invention for treatment or prevention of bacterial infections and methods of treatment of such infections employing such compounds.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.