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Erythromycin derivatives as antibacterial agents

A technology of solvates and halogens, applied in the field of new antibiotics, can solve the problems of not having a direct bonded benzene ring, not disclosing, etc.

Inactive Publication Date: 2008-01-09
ALPHARMA AS
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, none of these patent documents discloses macrolides having a substituted benzene ring directly bonded to the nitrogen atom of the oxazolidinone structure, and neither discloses macrolides having a substituted benzene ring directly bonded to a nitrogen atom containing at least one Macrolides of saturated benzene rings with nitrogen atoms

Method used

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  • Erythromycin derivatives as antibacterial agents
  • Erythromycin derivatives as antibacterial agents
  • Erythromycin derivatives as antibacterial agents

Examples

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Embodiment Construction

[0144] 4″-O-(allyloxycarbonyl)-N-demethyl clarithromycin 11,12-carbonate-2′,3′-aminomethyl Ethyl acetate (5)

[0145] Clarithromycin (4, 5.00 g, 6.69 mmol) was dissolved in dichloromethane (100 mL), and pyridine (6.30 mL, 77.9 mmol) and phosgene (20.0 mL, 38.0 mmol in 20% toluene) were added. The reaction mixture was stirred at room temperature for 5 hours. Allyl alcohol (9.00ml, 132mmol) was added and stirring continued for an additional 30 minutes (yellow solution). Aqueous sodium hydroxide solution was added, and the product was extracted with dichloromethane. The combined organic layers were washed with water and brine, dried over magnesium sulfate and filtered. Evaporation of the filtrate and chasing toluene gave a pale yellow solid which was recrystallized from toluene; 5.07 g (87%) of allyl carbonate 5 was obtained as a white solid; mp.: 307-310° C. (toluene). (C 43 h 67 NO 17 Calculated: C, 59.36; H, 7.76. Found: C, 60.01; H, 7.36%). HRMS, ESIpos.: M+Na + =...

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Abstract

This invention relates to a novel class of antibiotic agents, more specifically to macrolides comprising an oxazolidinone structure, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them.

Description

field of invention [0001] The present invention relates to a new class of antibiotics (antibiotic agent), more specifically to macrolides containing oxazolidinone structures, their preparation, pharmaceutical compositions containing them, their uses and methods of using them treatment method. Background of the invention [0002] Bacterial resistance to currently available antimicrobial agents is a growing global health problem. Therefore, a great deal of work is being done to discover new classes of new antimicrobial agents with new mechanisms of action. Such agents will exhibit no cross-resistance with existing antimicrobial drugs. [0003] The binding site for macrolides in bacteria has been shown to be within the 50S ribosomal subunit within the protein egress channel, close to the peptidyltransferase site. Among them, once the peptide chain reaches a certain length, macrolides constitute a molecular block for the growing chain to be used for protein production. 1 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/08A61K31/7048
Inventor H·艾于顿U·谢尔
Owner ALPHARMA AS
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