95 results about "Β lactamases" patented technology

This invention discloses and claims methods for inhibiting bacterial β-lactamases and treating bacterial infections by inhibiting bacterial β-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a β-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a β-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.

Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

Drug delivery systems for delivering agents capable of reducing the quantity of residual antibiotics reaching the colon following oral or parenteral antibiotic therapy, and for delivering metallo-dependent enzymes, and methods of using the drug delivery systems, are disclosed. The drug delivery systems include pectin beads that encapsulate the active agent (which can be a metallo-dependent enzyme), where the pectin is crosslinked with zinc or any divalent cation of interest and the pectin beads are coated with Eudragit®-type polymers. The drug delivery systems are orally administrable, but can deliver the active agents to the colon. In some embodiments, they can administer the agents to various positions in the gastro-intestinal tract, including the colon. One metallo-dependent enzyme is the β-lactamase L1 from Stenotrophomonas maltophilia, and agents that inactivate macrolide, quinolone, fluoroquinolone or glycopeptide antibiotics can also be used. The delivery of the active agent can be modulated to occur at various pre-selected sites of delivery within the intestinal tract by gelling / crosslinking a mixture of the active agent, such as a metallo-dependent enzyme, and pectin, with divalent metallic cations such as Ca+2 or Zn+2. A stable metallo-dependent enzyme formulation can be delivered to the lower intestine or colon. The use of zinc cations to crosslink the pectin is particularly preferred when specific metallo-dependent enzymes, which are Zn2+ dependent, could interact with other cationic species if they were used to gel the pectin beads and thus adversely affect the activity of such metallo-dependent enzymes.

The present invention relates to broad spectrum β-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) β-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I)whereinR1 is selected fromR2 is selected fromwith certain provisos as herein defined;in combination with a pharmaceutically acceptable β-lactam antibiotic in an amount which is effective for treating the bacterial infection.

This invention relates to certain tricyclic 6-alkylidene penems which act as a inhibitor of class-D enzymes. β-Lactamases hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. In accordance with the present invention there are provided compounds of formula I which are useful for treatment of bacterial infections having class-D enzymes associated therewith: wherein: One of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S or O.