15 results about "Avibactam" patented technology

The application relates to a compound cefoperazone and avibactam powder injection and a preparation method thereof. The compound powder injection is obtained by uniformly mixing cefoperazone hydrochloride and avibactam sodium, tabletting and crushing. When the powder injection is prepared into an injection solution, the powder injection is easy to disperse and dissolve, is convenient to use, ensures the content of cefoperazone, is not prone to produce beta-lactamase bacterial drug resistance, and has a good market application prospect.

The present application relates to a kind of recycling method of avibactam intermediate production waste liquid, belong to pharmaceutical chemical technology field;The present application will be in the 5-benzyloxyamine piperidin-2S-formic acid ethyl ester oxalate in avibactam intermediate production waste liquid by desalination into free state, under the condition of ethyl acetate as solvent, using the dilute solution of m-chloroperbenzoic acid drop, homogeneous reaction in organic solvent, effectively improve the utilization of raw material, with the advantage of less by-product, and have higher recovery rate than prior art, in addition, the present application also prepares a kind of activated carbon loaded sodium triacetoxyborohydride, can play the role of catalytic sodium triacetoxyborohydride reduction amination reaction, improve the utilization of sodium triacetoxyborohydride, and prevent sodium triacetoxyborohydride from contacting with water.

The utility model discloses a reaction kettle for producing avibactam, which comprises a reaction kettle body, supporting feet are arranged at the bottom of the reaction kettle body, a second motor is arranged at the bottom in the reaction kettle body, a rotary reaction cylinder is arranged on the second motor, the interior of the rotary reaction cylinder is divided into a liquid collecting cavity and a reaction cavity through a partition plate, and the liquid collecting cavity is communicated with the reaction cavity. An inner heating and stirring assembly and a temperature sensor are arranged in the reaction cavity, pressurizing boxes are arranged on the two sides of the inner wall of the reaction kettle, a cover plate is arranged on the reaction kettle, a heat conduction oil circulating box and a control box are arranged on the cover plate, and the second motor and the temperature sensor are electrically connected with the control box. According to the utility model, the heating speed and efficiency are improved through two heating modes of internal heating and external heating of the reaction cavity, so that the temperature in the reaction cavity can be quickly increased to a set value when being lower than the set value, the production stability is ensured, and the production quality and efficiency are improved.

The invention provides an avibactam / ceftazidime blood concentration rapid joint detection test strip and a preparation method, system and application thereof. The system comprises an immunochromatography test strip and a time-resolved fluorescence detection system. The immunochromatography test strip comprises a sample pad, a combination pad, a nitrocellulose membrane detection area and an absorption pad; the sample pad is made of glass fibers treated by cane sugar or a surfactant; the combination pad is loaded with a time-resolved fluorescent microsphere coupled monoclonal antibody probe; an avibactam detection line T1, a ceftazidime detection line T2 and a quality control line C are arranged in the nitrocellulose membrane detection area according to the flowing direction; the absorption pad is made of cellulose materials. Compared with the prior art, rapid combined detection of the avibactam / ceftazidime blood concentration can be realized within 15 minutes, and the method has the advantages of high sensitivity, wide linear range, strong anti-interference capability and simplicity and convenience in operation, and can meet the bedside rapid detection requirement.

The present invention is directed to improved processes for making the avibactam prodrug known as avibactam tomilopil or ethyl 3-[((1R,2S,5R)-2-carbamoyl-7-oxo-1,6- diazabicyclo[32.1]oct-6-yl)oxysulfonyloxy]-2,2-dimethylpropanoate of formula (I) and the spherical agglomerate particles resulting from said processes that are useful in large scale manufacturing.

The application discloses a combined drug sensitivity test method for rapidly detecting the synergistic effect of amikacin and ceftazidime-avibactam, and the method comprises the following steps: uniformly coating a to-be-detected bacterial suspension on an MH agar plate, firstly pasting two ATM paper sheets and two CZA paper sheets respectively, and ensuring that the four paper sheets are uniformly distributed on the plate; secondly, pasting a to-be-detected ATM drug sensitivity paper sheet on a to-be-detected CZA paper sheet, and indicating the CZA ATM ; thirdly, pasting a to-be-detected CZA drug sensitivity paper sheet on a to-be-detected ATM paper sheet, and indicating the ATM CZA ; fourthly, respectively dropping 20 μL of sterile normal saline on the CZA ATM and ATM CZA ; and finally, placing the plate in a 35℃ incubator for 8 hours, measuring the diameters of the bacteriostatic rings of ATM, CZA, ATM CZA and CZA ATM , and determining the synergistic effect according to the diameters of the bacteriostatic rings and the drug sensitivity breakpoint standard. The application has the advantages of simple operation, rapidness, accuracy, low cost and the like.

The application relates to the technical field of medicine synthesis, and discloses a preparation method of an avibactam intermediate, which comprises the following steps: taking AVI-SM-0 as a starting material, and sequentially performing esterification reaction, Boc protection, ring-opening addition reaction, imidization reaction, deprotection ring closure reaction, reduction reaction and salt formation to obtain the avibactam intermediate. The process is simple in operation, low in cost, high in stability, and the product quality meets the registration declaration requirements of avibactam.

The application discloses a beta-lactamase inhibitor selected from a compound shown in a structure as shown in formula I or a pharmaceutically acceptable salt, isomer or deuterated product thereof. The application discloses application of the beta-lactamase inhibitor in preparation of a beta-lactamase inhibitor. The application also discloses application of the beta-lactamase inhibitor in preparation of a drug for treating diseases related to bacterial infection. The bacteria are bacteria capable of producing beta-lactamase. The beta-lactamase inhibitor of the application can rapidly and completely release an active metabolite such as avibactam, dorobactam, relebactam, nacubactam and other dinitrogen heterocyclic beta-lactamase inhibitors in the body, can rapidly take effect, effectively improves oral bioavailability of the beta-lactamase inhibitor, enables oral administration of the beta-lactamase inhibitor and solves the problem of low oral bioavailability of the dinitrogen heterocyclic beta-lactamase inhibitor.

The invention belongs to the technical field of medicines, and particularly relates to a cefmenoxime-avibactam injection as well as a preparation method and application thereof. A novel beta-lactamase antibiotic / beta-lactamase inhibitor cefmenoxime-avibactam compound antibiotic product for injection is developed, bacterial drug resistance can be remarkably improved, and the injection is stable in prescription process, good in reproducibility and high in dissolving speed and has a good application prospect.

The invention discloses a pharmaceutical composition for inhibiting CRE and application, and relates to the technical field of drug research and development, and the key points of the technical scheme are as follows: the effect of aztreonam combined with four beta-lactamase inhibitors (avibactam, clavulanic acid, tazobactam and sulbactam) on 77 CRE isolates in Shenzhen children hospitals is evaluated. It is found that most of CRE isolates, resistant to aztreonam, in CRE isolates collected in Shenzhen children hospitals carry MBL and other beta-lactamase genes at the same time. And aztreonam / avibactam has good antibacterial activity on all the tested strains. For isolates which carry MBL genes but do not have AmpC enzyme coding genes, aztreonam / clavulanic acid can be used as a more economical and potential combination therapy regimen than aztreonam / avibactam, but is not suitable for CRE isolates carrying AmpC enzyme genes.

The invention belongs to the technical field of drug synthesis, and particularly relates to a deprotection preparation method of an avibactam intermediate, which comprises the following steps: reacting a compound I with formate in a solvent under the catalysis of palladium carbon and the existence of acid to prepare a product, and post-treating the product to obtain an avibactam intermediate compound II, the method is mild in condition, high in safety, simple and convenient to operate, high in reaction purity, few in impurity and easy for industrial production.

Disclosed in the present application is a β-lactamase inhibitor, selected from a compound represented by formula (I) or a pharmaceutically acceptable salt, isomer, or deuterated derivative thereof. Disclosed in the present application is a use of the β-lactamase inhibitor in the preparation of a diazabicyclooctane β-lactamase inhibitor. Also disclosed in the present application is a use of the β-lactamase inhibitor in the preparation of a medicament for treating diseases related to bacterial infections, the bacteria being capable of producing β-lactamase. The β-lactamase inhibitor of the present application can rapidly and completely release active metabolites in vivo, such as avibactam, durlobactam, relebactam, nacubactam, and other diazabicyclooctane β-lactamase inhibitors, and can act quickly, effectively improving the oral bioavailability of diazabicyclooctane β-lactamase inhibitors, enabling oral administration and solving the problem of low oral bioavailability of diazabicyclooctane β-lactamase inhibitors.

The present invention relates to combinations of meropenem and one or more antibiotic resistance disrupting agents, pharmaceutical compositions comprising said combinations, and methods for treating bacterial infections comprising administering said combinations. In particular, the present invention relates to a pharmaceutical composition comprising (a) meropenem, (b) avibactam and (c) EDTA.

The invention discloses a beta-lactamase inhibitor, which is selected from a compound with a structure shown as a formula I or pharmaceutically acceptable salts, isomers or deuterated substances of the compound. The invention discloses an application of the beta-lactamase inhibitor in preparation of the beta-lactamase inhibitor. The invention also discloses application of the beta-lactamase inhibitor in preparation of medicines for treating diseases related to bacterial infection. The bacteria are bacteria capable of producing beta-lactamase. The beta-lactamase inhibitor disclosed by the invention can quickly and completely release active metabolites such as avibactam, dulobactam, relebactam, nacchabactam and other diazabicyclo beta-lactamase inhibitors in vivo, and can quickly take effect, so that the oral bioavailability of the beta-lactamase inhibitor is effectively improved, the bioavailability of the beta-lactamase inhibitor is improved, and the bioavailability of the beta-lactamase inhibitor is improved. Therefore, the diazabicyclo beta-lactamase inhibitor can be orally taken, and the problem of low oral bioavailability of the diazabicyclo beta-lactamase inhibitor is solved.

Provided are a β-lactamase inhibitor and the use thereof. The β-lactamase inhibitor has a structure as represented by the below formula (I), or a pharmaceutically acceptable salt thereof, or an isomer thereof or a deuterated substance thereof. A group of the β-lactamase inhibitor capable of enhancing the lipid solubility of the compound binds to the amide and sulfonic acid groups in an avibactam structure, thereby increasing the lipid solubility of the structure. Under the action of biological enzymes, the β-lactamase inhibitor can rapidly and completely release an active metabolite, i.e. avibactam, and enabling the rapid onset of action thereof, which effectively improves the oral bioavailability of avibactam, and enables oral administration of avibactam, thereby solving the problem whereby avibactam cannot be be administered orally.