53 results about "Β lactamase inhibitor" patented technology

A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

The invention relates to an improved therapy for treating resistant bacterial infections caused by extended-spectrum β-lactamase (ESBLs)-producing strains in a warm-blooded animal, adjuvant step down therapy, and pharmaceutical compositions for such therapies. The invention also relates to a method for inhibiting bacterial resistance in ESBLs-producing strains so as to have better control over the therapy; achieve reduced hospital stay and adjuvant step down therapy so as to avoid recrudescence. In particular, the therapy includes antibacterial combination of cefepime with sulbactam via parenteral route, followed by oral third generation cephalosporin with a suitable β lactamase inhibitor.

A method for determining whether a microorganism produces an AmpC β-lactamase is disclosed in which a culture of a microorganism suspected of producing a β-lactamase that inactivates a β-lactam-containing antibiotic is admixed with an effective amount of each of i) a β-lactam-containing antibiotic, ii) a β-lactamase inhibitor to which AmpC β-lactamase is resistant, and iii) a permeabilizing agent for the microorganism present in a non-growth-inhibiting microorganism-permeabilizing amount to form an assay culture. That assay culture in maintained under appropriate culture conditions and for a time period sufficient to determine the interaction of the microorganism with the AmpC β-lactamase resistant inhibitor and antibacterial compound, and thereby determine the presence of an AmpC β-lactamase, wherein a positive test indicates the presence of an AmpC β-lactamase.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

The present invention provides a reagent composition for detecting β-lactamase including as a β-lactamase detection substrate 3-[2,4-dinitrostyryl]-7-(2-thienylacetamido]-3-cephem-4-carboxylic acid, or 7-[2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxy-imino)acetamido]-3-(2,4-dinitrostyryl)-3-cephem-4-carboxylic acid, and at least one β-lactamase inhibitor selected from the group consisting of clavulanic acid, aztreonam, ethylenediaminetetraacetic acid, and cloxacillin, which composition can detect β-lactamases rapidly and easily with high sensitivity. The present invention also provides a detection kit including the detecting reagent composition. Further, the present invention provides a β-lactamase detection method where a liquid specimen containing a target substance to be analyzed is brought into contact with the composition.

The present invention relates to compounds, compositions and methods for treating bacterial infections. Embodiments of the present invention include antibiotics and β-lactamase inhibitors to treat resistant infections.

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).

Administration of β-Lactam compounds, including β-lactam antibiotics and β-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

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)

wherein

R₁ is selected from

R₂ is selected from

with 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.

The present invention relates to pharmaceutical compositions of carbocephem antibiotics with β-lactamase inhibitors useful for the treatment of bacterial infections, in particular infections caused by bacteria that express β-lactamases as a mechanism of resistance to β-lactam antibiotics.

Novel neuroprotectant compositions and methods are described. β-Lactamase inhibitors are used to prevent or reduce loss of neuronal cells and neuronal cell function in patients afflicted with or susceptible to disease states or conditions known to result in or cause neuronal tissue insult.

The present invention relates to a compound of Formula (I)-(IV) useful as β-lactamase inhibitor, a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, wherein R₁, R₂, M and ring A have definitions as those in the specification. The present invention further relates to methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and uses of these compounds. For example, the compounds of the present invention can be used as β-lactamase inhibitors, for treatment and/or prophylaxis of diseases caused by bacterial infections, solving drug-resistance problems caused by β-lactamases, especially bacterial drug-resistant diseases caused by type B metallo-β-lactamases.

A process for the preparation of a substituted C-2 β-lactam comprises incubating a 2-substituted 3-aminocarboxylic acid with a β-lactam synthetase under conditions such that the 2-substituted 3-aminocarboxylic acid is cyclised to produce a substituted C-2 β-lactam. The process can be used to produce an antibiotic or β-lactamase inhibitor.

A compound which is a thienolate of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R¹, R³, Ring A1, n and Ring A2 are as defined herein, are found to be useful in inhibiting metallo-beta-lactamase and therefore in potentiating the activity of beta lactamase antibiotics. The compound can be used alone or in combination with a rhodanine of formula (II) or a pharmaceutically acceptable salt thereof: (II) wherein R³, Ring A1, n, Ring A2, L and Ring B are as defined herein. Treatment or prevention of bacterial infection in combination with beta-lactam antibiotic agents is also provided.

β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.