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Sulfhydryl pyrrolidine formyl piperidine substituted penem derivant

A technology of substituents and alkyl groups is applied in the field of penem derivatives substituted by mercaptopyrrolidinecarbonyl piperidine, which can solve the problems of short half-life and low clinical availability.

Active Publication Date: 2010-12-15
XUANZHU BIOPHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the continuous increase of bacterial resistance due to the abuse of antibiotics and the limitation of digestive tract absorption, the currently marketed carbapenems can only be administered as injections in clinical practice, and the clinical utilization is not high. The half-life of penem is relatively short, which can no longer meet the clinical needs

Method used

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  • Sulfhydryl pyrrolidine formyl piperidine substituted penem derivant
  • Sulfhydryl pyrrolidine formyl piperidine substituted penem derivant
  • Sulfhydryl pyrrolidine formyl piperidine substituted penem derivant

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Abstract

The present invention belongs to the technical field of medicine, in particular to a penem derivative substituted by mercaptopyrrolidine formylpiperidine shown in the formula (I) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, an isomer, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4> and R<5> are defined in the description. The present invention also relates to preparation methods of the compounds, drug combinations and applications of the compounds in the preparation of drugs for treating and / or preventing infective diseases.

Description

1. Technical field The invention belongs to the technical field of medicine, and in particular relates to penem derivatives substituted by mercaptopyrrolidineformyl piperidine, pharmaceutically acceptable salts thereof, easily hydrolyzed esters, isomers thereof, hydrates thereof, and esters thereof or salt hydrates, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and uses of these compounds in the preparation of medicaments for treating and / or preventing infectious diseases. 2. Background technology Carbapenem antibiotics are a class of β-lactam antibiotics developed in the 1970s. It has attracted much attention because of its broad antibacterial spectrum, strong antibacterial activity, and stability to β-lactamase. Its structural feature is that the sulfur at the 1-position of the penicillane core is replaced by carbon, and the 2-position has a double bond, which combines the five-membered ring of penicillin and the conjugate...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D477/20A61K31/407A61K31/454A61K31/506A61P31/04
CPCY02P20/55
Inventor 黄振华
Owner XUANZHU BIOPHARMACEUTICAL CO LTD
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