134 results about "Beta-Lactamase Inhibitors" patented technology

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.

Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.

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).

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.

Class A beta-lactamase may be used for reducing side-effects in the intestine associated with antibiotic therapy with a combination of beta-lactam antibiotic and beta-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.

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

A pharmaceutical composition comprising: at least one aminoglycoside antibiotic and (a) at least one ion chelating agent used for inhibiting particulate formation, or (b) at least one buffer, or (c) at least one ion chelating agents and at least one buffer simultaneously. The composition for use in controlling microbial infection can be formulated into a solution, or combined with at least one beta-lactam antibiotic, or combined with at least one of beta-lactam antibiotic and at least one beta-lactamase inhibitor into a solution in a container.

The invention provides a stable-content drug compound containing Beta-lactamases inhibitors and piperacillin sodium and the preparation method thereof. The drug compound consists of piperacillin sodium, Beta-lactamases inhibitors and pH-value regulators with the weight proportion of 1 to 100:1:0.001 to 2. Diluted and delivered in any proportion with conventional clinical transfusions, the drug compound can have a stable piperacillin sodium content, dissolve rapidly, generate no crystallization or degradation products and receive no effect from the temperature. The preparation method of the stable-content drug compound containing Beta-lactamases inhibitors and piperacillin sodium has simple preparing method and high efficiency and is fit for a large-scale industrial production.

Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Polymers (i.e. polyesters, polyamides, polythioesters, polyanhydrides, or a mixture thereof) which degrade hydrolytically to provide a combination of a beta-lactam antibiotic (e.g., amoxicillin) and a beta-lactamase inhibitor (e.g., clavulanic acid) (or a pharmaceutically acceptable salt thereof) are provided. Methods of producing these polymers, intermediates useful for preparing these polymers, and methods of using these polymers to deliver a combination of a beta-lactam antibiotic and a beta-lactamase inhibitor (or a pharmaceutically acceptable salt thereof) to a host are also provided.

Described herein are compounds and compositions that modulate the activity of beta-lactamases and methods thereof. In some embodiments, the compounds described herein are biologically hydrolyzed to a beta-lactamase inhibitor. In certain embodiments, the compounds described herein are useful for the treatment of bacterial infections.

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 discloses a novel broad-spectrum beta-lactamase inhibitor. The structure of the compound is shown in the formula I, by means of research on activity of six beta-lactamases in four types with the compound, it is found that the compound can inhibit activity of multiple beta-lactamases, when the compound is combined with beta-lactam antibiotics, the combination has powerful growth inhibiting activity on bacteria generating beta-lactamase, it can be expected that a drug which can recover antibacterial activity of the beta-lactam antibiotics to treat and prevent infection caused by bacteria of animals including human can be developed, and the novel broad-spectrum beta-lactamase inhibitor has great social and economic benefits.

A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I):wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O═, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.

The present invention relates to a slow-released preparation containing beta-lactamase inhibitor and cephalosporin. Said slow-released preparation can be made into antibiotic slow-released injection or slow-released implant preparation. Said injection is formed from slow-released microsphere and solvent, the slow-released microsphere contains slow-released auxiliary material and beta-lactamase inhibitor with antibacterial effective dose and cephalosporin, the solvent is special one containing suspension adjuvant of carboxymethyl cellulose sodium, etc. and its viscosity is 100 cp-3000 cp (20 deg.C-30 deg.C). The slow-released auxiliary material is selected from EVAc, polylactic acid copolymer, sebacic acid copolymer, albumin glue and gelatin, etc. The slow-released implant preparation is prepared by using slow-released microsphere or adopting melting process. Said invention also provides its application method. and can obtain obvious therapeutic effect for curing various infective diseases.

The invention relates to a method for synthesizing a beta-lactamase inhibitor Avibactam and belongs to the technical field of preparation of beta-lactamase inhibitors. The method disclosed by the invention comprises the following steps: (1) taking a compound 2 as a raw material, and reacting with R<1>NH2 so as to produce a compound 3; (2) enabling the compound 3 and a biocatalyst to produce a compound 4 in an organic solvent in the presence of glucose or sucrose; (3) enabling the compound 4 to react with trifluoroacetic anhydride so as to obtain a compound 5; (4) enabling the compound 5 to react with R<2>ONH2 so as to produce a compound 6; (5) hydrolyzing the compound 6 under alkaline conditions so as to produce a compound 7; (6) enabling the compound 7 to react with triphosgene so as to produce a compound 8; (7) enabling the compound 8 to react with ammonium formate in the presence of a catalyst so as to produce a compound 9 in the organic solvent, wherein the catalyst is a Pd / C system; and (8) enabling the compound 9 to react with a sulfonating agent, thereby obtaining the product 1. The method disclosed by the invention is stable in process, high in yield, simple and safe in operation and low in production cost.

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.

It is intended to provide a reagent composition for detecting beta-lactamase which contains 3-[2,4-dinitrostyryl]-7-(2-thienylacetamido)-3-cephem-4-carboxylic acid or 7-[2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-(2,4-dinitrostyryl)-3-cephem-4-carboxylic acid as a substrate for detecting beta-lactamase together with at least one beta-lactamase inhibitor selected from among clavulanic acid, aztreonam, ethylenediaminetetraacetic acid and cloxacillin and by which beta-lactamase can be quickly and easily identified at a high sensitivity. Moreover, a detection kit containing the above detection reagent composition and a method of detecting beta-lactamase comprising contacting a liquid specimen containing the subject to be analyzed with the above composition are provided.

The present invention is one kind of antiseptic medicine composition containing antibiotic cefuroxime and beta-lactamase inhibitor in the weight ratio of 0.5-20. The said medicine composition as new generation of antiseptic medicine composition has the advantages of wide antiseptic spectrum and strong antiseptic effect.

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Polymers (i.e. polyesters, polyamides, polythioesters, polyanhydrides, or a mixture thereof) which degrade hydrolytically to provide a combination of a beta-lactam antibiotic (e.g., amoxicillin) and a beta-lactamase inhibitor (e.g., clavulanic acid) (or a pharmaceutically acceptable salt thereof) are provided. Methods of producing these polymers, intermediates useful for preparing these polymers, and methods of using these polymers to deliver a combination of a beta-lactam antibiotic and a beta-lactamase inhibitor (or a pharmaceutically acceptable salt thereof) to a host are also provided.

Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Described herein are compounds and compositions that modulate the activity of beta-lactamases and methods thereof. In some embodiments, the compounds described herein are biologically hydrolyzed to a beta-lactamase inhibitor. In certain embodiments, the compounds described herein are useful for the treatment of bacterial infections.