Broad spectrum beta-lactamase inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 501/18 (2006.01) A61K 31/545 (2006.01) A61K 31/546 (2006.01) A61P 31/04 (2006.01) C07D 501/24 (2006.01)

Patent

CA 2702257

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. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

L'invention concerne des inhibiteurs de bêta-lactamase à large spectre. Certains inhibiteurs présentent également une activité antibiotique puissante en plus de l'inhibition de bêta-lactamase. Les composés de l'invention sont conçus de telle sorte que lors d'un clivage du cycle bêta-lactame, des fractions réactives qui peuvent inactiver la bêta-lactamase sont générées. Sont également proposés des procédés de préparation d'inhibiteurs de bêta-lactamase et des antibiotiques bêta-lactame présentant une telle inhibition. Il est en outre proposé des compositions pharmaceutiques pour traitement ou prévention d'infections bactériennes et des procédés de traitement de telles infections.

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