Broad spectrum beta-lactamase inhibitors
AssigneeGladius Pharmaceuticals Corporation
InventorsLarry Sutton, Sophia Yu
Life of this patent
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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. 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.
Claims21
A method of treating bacterial infection, the method comprising:
- administering to an individual in need of treatment a therapeutically effective amount of a beta-lactam antibiotic;
- wherein the beta-lactam antibiotic is also a beta-lactamase inhibitor that inhibits a beta-lactamase enzyme and
- which comprises a leaving group that is in conjugation with the lactam nitrogen of the beta-lactam ring through a styryl moiety such that, when the beta-lactam ring is opened by the beta-lactamase enzyme to form a ring-opened compound, the leaving group is expelled to form a reactive moiety on the ring-opened compound, and the reactive moiety covalently binds to the beta-lactamase enzyme, wherein the reactive moiety is a substituted or unsubstituted cyclohexadienyl methide.
Dependencies are inferred from the claim text.