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Antibacterial composition and uses thereof

A composition and compound technology, applied in the direction of antibacterial drugs, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems of inconsistent half-life of antibiotics, restrictions, etc.

Active Publication Date: 2018-10-09
SHANDONG XUANZHU PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, avibactam and MK-7655 in clinical T 1 / 2 It is short and cannot be effectively matched with the half-life of antibiotics, which limits its clinical application

Method used

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  • Antibacterial composition and uses thereof
  • Antibacterial composition and uses thereof
  • Antibacterial composition and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0196] Compound Synthesis Preparation Example 1 Preparation of (2S,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid

[0197]

[0198] (1) Ethyl (S)-2-((tert-butoxycarbonyl)amino-6-(dimethyl (oxo)-λ 6 Preparation of -thioylide)-5-oxohexanoic acid ester

[0199]

[0200] Dissolve trimethylsulfoxide iodide (343.2g, 1.56mol) into N,N-dimethylformamide (2300mL), add potassium tert-butoxide (156.9g, 1.40mol) in batches, and stir at room temperature for 1 Hour. Add 1-tert-butyl 2-ethyl (S)-5-oxopyrrolidine-1,2-dicarboxylate (350g, 1.36mol) in batches, stir at room temperature for 2 hours after the addition, add water (4000mL ), extracted with ethyl acetate (3000mL × 5), the organic phases were combined, washed with saturated brine (3000mL), dried over anhydrous sodium sulfate, concentrated, and the crude product was subjected to silica gel column chromatography (dichloromethane:methanol=10: 1) Purification gave the title compound (280 g, yield 59%) as ...

preparation example 2

[0224] Preparation Example 2 Preparation of tert-butyl 6-hydroxyl-2-azaspiro[3.3]heptane-2-carboxylate

[0225]

[0226] Add tert-butyl 6-oxo-2-azaspiro[3.3]heptane-2-carboxylate (4.22g, 20mmol) into methanol (30mL), lower the temperature to 0°C under nitrogen protection, add hydroboration Sodium (1.52g, 40mmol), after the addition was completed, the temperature was raised to 25°C and stirred for 1 hour. LC-MS detected that the reaction was complete, and water (1mL) was added to quench the reaction. The solvent was evaporated under reduced pressure, and water (100mL) and ethyl acetate ( 100 mL), liquid separation, the organic phase was washed with hydrochloric acid (1mol / L, 50 mL), dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated to give the white title compound (4.0 g, yield 93.7%).

preparation example 3

[0227] Preparation Example 3 Preparation of tert-butyl 6-(1,3-dioxoisoindoline-2-yl)-2-azaspiro[3.3]heptane-2-carboxylate

[0228]

[0229] Under nitrogen protection, tert-butyl 6-hydroxyl-2-azaspiro[3.3]heptane-2-carboxylate (4.0g, 18.8mmol), phthalimide (3.86g, 26.2mmol) and triphenylphosphine (5.92g, 22.6mmol) were added to tetrahydrofuran (100mL), the temperature was lowered to 0°C, diethyl azodicarboxylate (3.93g, 22.6mmol) was slowly added dropwise, and the temperature was raised to 25 °C and stirred for 16 hours. LC-MS detected that the reaction was complete, adding water (1mL) to quench the reaction, concentrating the solvent under reduced pressure, adding water (150mL) and ethyl acetate (150mL), separating the layers, extracting the aqueous phase with ethyl acetate (100mL×2), combining the organic phase, concentrated, and the crude product was purified by silica gel column chromatography (petroleum ether: ethyl acetate = 10:1) to obtain the white title compound (6...

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Abstract

The present invention relates to the technical field of medicine, specifically to a composition, which contains a compound (a), a pharmaceutically acceptable salt, an ester, a solvate or a stereoisomer thereof, and at least a carbapenem antibiotic or a derivative thereof, wherein the compound (a) has a structure represented by a formula (I) defined in the specification. The invention further relates to uses of the composition in preparation of drugs for prevention and / or treatment of infectious diseases caused by bacteria, wherein preferably the bacteria have drug resistance caused by beta-lactamase.

Description

technical field [0001] The present invention relates to a composition and its pharmaceutical use, in particular to an antibacterial composition comprising a diazabicyclooctone compound and a carbapenem antibiotic, and the antibacterial composition is used in the preparation of treatment and / or prevention of bacterial infection use in infectious diseases. Background technique [0002] The rapid development of antibiotics is of great significance in the history of modern medicine. However, antibiotic resistance, especially the resistance of Gram-negative bacteria, is becoming more and more serious, which has seriously threatened human health. Worryingly, the current bacterial drug resistance shows a trend of multidrug resistance (MDR) and pan-drug resistance (PDR), which makes patients lack effective treatment options when facing severe bacterial infections, Thereby endangering the life safety of the patient. In Europe, the number of deaths caused by antibiotic resistance i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61K31/407A61P31/04
CPCA61K31/407A61K31/439A61K2300/00
Inventor 盛泽娟张宝成高聪范秀君王田园
Owner SHANDONG XUANZHU PHARMA TECH CO LTD
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