Antibacterial combination and application thereof

A compound and solvent compound technology, applied in the field of medicine, can solve the problems of limited application, not showing good drug effect, short half-life, etc.

Active Publication Date: 2019-04-05
BEIJING AOHE DRUG RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with clavulanic acid, sulbactam and tazobactam, avibactam has long-acting enzyme inhibition and resolves the resistance problem partially mediated by class A β-lactamases (such as KPC) , but still cannot effectively solve the drug resistance caused by class B metalloenzymes, and its clinical application is limited
MK-7655 has a wider antibacterial spectrum, but it also does not show good efficacy against strains producing class B metalloenzymes
In addition, the half-lives of avibactam and MK-7655 (T 1 / 2 ) is short and cannot effectively coincide with the half-life of antibiotics, which limits its clinical application

Method used

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  • Antibacterial combination and application thereof
  • Antibacterial combination and application thereof
  • Antibacterial combination and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0199] The in vitro antibacterial activity of experimental example 1 compound (a)

[0200] Bacteria to be tested: standard enzyme-producing strains used in experiments were purchased from ATCC, and clinically isolated CRE strains were purchased from Southwest Hospital of Third Military Medical University.

[0201] Test product: part of compound (a) or the salt of compound (a), its chemical name and preparation method are shown in the preparation examples of each compound.

[0202] Control drugs: avibactam (AVI) sodium salt and MK-7655 were all made by Shandong Xuanzhu Pharmaceutical Technology Co., Ltd., and their structural formulas are as described in the background technology.

[0203] Experimental method: agar dilution method, refer to M100-S23: Performance Standards for Antimicrobial Susceptibility Testing; Twenty-Third Informational Supplement (Clinical And Laboratory Standards Institute, 2013), calculate the minimum inhibitory concentration (MIC, minimum inhibitory conc...

experiment example 2

[0216] In vitro enzymatic activity test of experimental example 2 compound (a)

[0217] Test product: part of compound (a) or the salt of compound (a), its chemical name and preparation method are shown in the preparation examples of each compound.

[0218]Control drugs: avibactam (AVI) sodium salt and MK-7655 were all made by Shandong Xuanzhu Pharmaceutical Technology Co., Ltd., and their structural formulas are as described in the background technology.

[0219] experimental method:

[0220] Nitrocefin (Nitrocefin, cephalosporin antibiotics) is sensitive to most β-lactamases and will change color after being hydrolyzed. The hydrolysis rate of Nitrocefin was determined by recording the corresponding absorbance in the reaction system in real time. β-lactamase inhibitors will inhibit the enzyme's hydrolysis of Nitrocefin and reduce the rate of hydrolysis. Calculate the IC of the inhibitor by measuring the reaction rate in the same reaction system under different inhibitor co...

experiment example 3

[0240] The in vitro antibacterial activity of experimental example 3 compound (a) combined with ceftazidime

[0241] Test article: part of compound (a) or the salt of compound (a), its chemical name and preparation method are as above.

[0242] Control drug: Avibactam (Avibactam, AVI) sodium salt, purchased from Jinan Xinzheng Pharmaceutical Technology Co., Ltd.; MK-7655, self-made, referring to the preparation method in WO2009091856A2 (public date 2009-07-23); ceftazidime (ceftazidime , CAZ), purchased from Nanjing Shenglide Biotechnology Co., Ltd.

[0243] Bacteria to be tested: standard enzyme-producing strains for experiments were purchased from ATCC, and clinically isolated CRE strains were purchased from Third Military Medical University

[0244] Learn Southwest Hospital.

[0245] Experimental method: agar dilution method, refer to M100-S23: Performance Standards for Antimicrobial Susceptibility Testing; Twenty-Third Informational Supplement (Clinical And Laboratory St...

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Abstract

The invention relates to the technical field of medicines, in particular to a medicine product. The medicine product comprises a compound (a), or salt or ester or a solvent compound, which can be pharmaceutically accepted, of the compound (a), or stereoisomer of the compound (a), and one or more beta-lactam antibiotics or derivatives of the beta-lactam antibiotics, wherein the compound (a) has a structure shown in a formula (I) (please see the specifications for the formula (I)). Meanwhile, the invention further relates to application of the medicine product to preparation of medicines for treating and / or preventing bacterial infectious diseases, preferably, bacteria have medicine resistance caused by the beta-lactamase.

Description

technical field [0001] The invention belongs to the technical field of medicine. In particular, the present invention relates to a pharmaceutical product, in particular to an antibacterial pharmaceutical composition comprising a diazabicyclooctone compound and a β-lactam antibiotic, and its preparation for the prevention and / or treatment of infectious diseases caused by bacteria. Use in disease medicine. Background technique [0002] The rapid development of antibiotics is of great significance in the history of modern medicine. The first β-lactam drug successfully applied clinically was penicillin G, which pointed out the direction for the clinical application of subsequent β-lactam antibiotics. β-lactam antibiotics refer to a large class of antibiotics with a β-lactam ring in their chemical structure, including the most commonly used clinical penicillins, cephalosporins, carbapenems, and monocyclic β-lactams. These several drugs are still the most widely used, safe and ...

Claims

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Application Information

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IPC IPC(8): A61K31/551A61K45/06A61K31/546A61K31/427A61P31/04
CPCA61K45/06A61K31/427A61K31/546A61K31/551A61K2300/00
Inventor 史澂空
Owner BEIJING AOHE DRUG RES INST
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