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Useful Combinations of Monobactam Antibiotics With Beta-Lactamase Inhibitors

InactiveUS20100056478A1Antibacterial agentsBiocideMedicineAztreonam

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).

Useful Combinations of Monobactam Antibiotics With Beta-Lactamase Inhibitors

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Owner:BASILEA PHARMACEUTICA AG

Beta-lactamase inhibitors

ActiveUS20110294777A1Antibacterial agentsBiocideAntibiotic YImipenem

Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.

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Owner:MERCK SHARP & DOHME LLC

1,2,4-oxadiazole and 1,2,4-thiadiazole beta-lactamase inhibitors

ActiveUS20130289012A1High binding affinityBiocideOrganic chemistryΒ lactamasesThiadiazoles

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.

1,2,4-oxadiazole and 1,2,4-thiadiazole beta-lactamase inhibitors

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Owner:MERCK SHARP & DOHME LLC

Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids

InactiveUS20120053350A1Small material requirementAvoid less flexibilityOrganic chemistryBulk chemical productionΒ lactamasesIridium

A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein PG1 is an amine protective group; k is 0, 1, or 2; and RU, R1, R2, and R3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (RU)3S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.

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Owner:MERCK SHARP & DOHME CORP

Β-lactamase inhibitors

ActiveUS8487093B2Antibacterial agentsBiocideΒ lactamasesCeftazidime

Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.

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Owner:MERCK SHARP & DOHME LLC

Therapy for Treating Resistant Bacterial Infections

InactiveUS20090275552A1Antibacterial agentsBiocideΒ lactamasesAdjuvant

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.

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Owner:PATEL MAHESH VITHALBHAI +5

Device and method for detecting antibiotic-inactivating enzymes

ActiveUS20050089947A1Facilitated releaseRobust in vitroMicrobiological testing/measurementBiological material analysisΒ lactamasesMicroorganism

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.

Device and method for detecting antibiotic-inactivating enzymes

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Owner:CREIGHTON UNIVERSITY

Isoxazole beta-lactamase inhibitors

ActiveUS20130345190A1Antibacterial agentsBiocideΒ lactamasesΒ lactamase inhibitor

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.

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Owner:MERCK SHARP & DOHME LLC

Beta-lactamase detecting reagent composition, detection kit and detection method

InactiveUS20060014230A1Quick checkOrganic chemistryMicrobiological testing/measurementΒ lactamasesNitrostyrol

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.

Beta-lactamase detecting reagent composition, detection kit and detection method

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Owner:SHOWA YAKUHIN KAKO +1

Methods of treating bacterial infections

InactiveUS20150119363A1High sensitivityAntibacterial agentsBiocideΒ lactamasesMedicine

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.

Methods of treating bacterial infections

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Owner:REMPEX PHARM INC

Boronic acid derivatives and therapeutic uses thereof

ActiveUS20180002351A1Antibacterial agentsBoron compound active ingredientsΒ lactamasesAcid derivative

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).

Boronic acid derivatives and therapeutic uses thereof

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Owner:QPEX BIOPHARMA INC

Neurotherapeutic Compositions and Method

InactiveUS20080200447A1Improve performanceEasy to learnBiocideNervous disorderΒ lactamasesCognition

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.

Neurotherapeutic Compositions and Method

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Owner:REVAAX PHARMA LLC

Neurotherapeutic compositions and method

InactiveUS7842683B2Reduce in quantityImprove latencyBiocideNervous disorderΒ lactamasesCognition

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.

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Owner:REVAAX PHARMA LLC

Device and method for detecting antibiotic-inactivating enzymes

ActiveUS7291480B2Facilitated releaseGrowth inhibitionMicrobiological testing/measurementBiological material analysisMicroorganismΒ lactamases

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.

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Owner:CREIGHTON UNIVERSITY

Bate-lactamase inhibitors

InactiveUS20110046101A1Antibacterial agentsBiocideΒ lactamasesMedicine

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.

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Owner:DMITRIENKO GARY I +4

Compositions comprising carbacephem beta-lactam antibiotics and beta-lactamase inhibitors

InactiveUS20080146535A1BiocideOrganic active ingredientsBacteroidesBeta lactam antibiotic

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.

Compositions comprising carbacephem beta-lactam antibiotics and beta-lactamase inhibitors

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Owner:BLANCA PHARMA

Antibacterial combination and its use

InactiveUS20100029604A1Good curative effectAntibacterial agentsBiocideGeometric isomerDiastereomer

The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum β-lactamase inhibitor.

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Owner:LEK PHARMA D D

Neurotherapeutic compositions

InactiveUS20080044471A1Effective neuroprotectiveAvoid problemsBiocideNervous disorderΒ lactamasesMedicine

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.

Owner:KOPPEL GAY A

SS-lactamase inhibitors and uses thereof

ActiveUS20180148448A1High activityGood effectAntibacterial agentsOrganic active ingredientsΒ lactamasesDrug resistance

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.

SS-lactamase inhibitors and uses thereof

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Owner:SHANDONG XUANZHU PHARMA TECH CO LTD

1,2,4-oxadiazole and 1,2,4-thiadiazole β-lactamase inhibitors

ActiveUS8916709B2BiocideOrganic chemistryΒ lactamasesThiadiazoles

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.

1,2,4-oxadiazole and 1,2,4-thiadiazole β-lactamase inhibitors

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Owner:MERCK SHARP & DOHME LLC

Boronic acid derivatives and therapeutic uses thereof

ActiveUS10294249B2Antibacterial agentsBoron compound active ingredientsΒ lactamasesAcid derivative

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).

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Owner:QPEX BIOPHARMA INC

Process for synthesizing beta-lactamase inhibitor intermediates

InactiveUS20080009634A1Eliminate needAntibacterial agentsOrganic chemistryΒ lactamasesAryl

There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.

Process for synthesizing beta-lactamase inhibitor intermediates

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Owner:WYETH HOLDINGS CORP

Combination therapy for treatment of resistant bacterial infections

ActiveUS9968593B2Antibacterial agentsOrganic chemistryImipenem/cilastatinCompound (substance)

The present invention is directed to combinations of a β-lactamase inhibitor with sulbactam and, optionally, imipenem / cilastatin. The combinations are useful for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant pathogens. More particularly, the invention relates to a combination of β-lactamase inhibitor compound 1: or a pharmaceutically acceptable salt thereof, with sulbactam, or a pharmaceutically acceptable salt thereof, and, optionally, imipenem / cilastatin, or a pharmaceutically acceptable salt thereof.

Combination therapy for treatment of resistant bacterial infections

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Owner:ENTASIS THERAPEUTICS

Cyclisation process for the preparation of c-2 beta-lactam compounds

InactiveUS20050070519A1BiocideOrganic active ingredientsCompound aCarboxylic acid

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.

Cyclisation process for the preparation of c-2 beta-lactam compounds

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Owner:ISIS INNOVATION LTD

Beta Lactamase Inhibitors

ActiveUS20170369433A1Antibacterial agentsOrganic chemistryAntibiotic YRhodanine

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.

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Owner:OXFORD UNIV INNOVATION LTD

Avibactam and carbapenems antibacterial agents

ActiveUS10434089B2Reduce probabilityAntibacterial agentsOrganic active ingredientsMedicineAntibacterial agent

Described are methods of treating or preventing a bacterial infection by administering an antibacterial agent comprising a β-lactamase inhibitor and one or more carbapenem to a subject.

Avibactam and carbapenems antibacterial agents

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Owner:THE JOHN HOPKINS UNIV SCHOOL OF MEDICINE

Isoxazole beta-lactamase inhibitors

InactiveUS20150038482A1BiocideOrganic active ingredientsΒ lactamasesΒ lactamase inhibitor

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.