Sulfhydryl pyrrolidine formamido pyridine substituted penem derivant

A formyl, representative technology, applied in the field of penem derivatives substituted by mercaptopyrrolidinecarboxamidopyridine, can solve the problems of low clinical utilization and short half-life

Active Publication Date: 2011-01-12
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 formamido pyridine substituted penem derivant
  • Sulfhydryl pyrrolidine formamido pyridine substituted penem derivant
  • Sulfhydryl pyrrolidine formamido pyridine substituted penem derivant

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Abstract

The present invention belongs to the technical field of medicine, and in particular relates to a penem derivative substituted by sulfhydryl pyrrolidine carbamoyl pyridine as shown in Formula (I), an acceptable salt thereof in pharmacy, an easily hydrolyzed ester thereof, an isomer thereof, a hydrate thereof, and a hydrate of ester or salt thereof; wherein, R<1>, R<2>, R<3>, R<4> , R<5> and R<6> are defined as in the specification. The present invention also relates to the preparation methods of the compounds, drug compositions of the compounds, and the application of the compounds in preparation of medicine which is used for treating and / or preventing infectious diseases.

Description

1. Technical field The present invention belongs to the technical field of medicine, and specifically relates to penem derivatives substituted by mercaptopyrrolidincarboxamidopyridine, pharmaceutically acceptable salts thereof, easily hydrolyzed esters, isomers, hydrates, and esters thereof Or salt hydrates, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in the preparation of drugs for the treatment and / or prevention of infectious diseases. 2. Background technology Carbapenem antibiotics are a class of β-lactam antibiotics developed in the 1970s. Because of its wide antibacterial spectrum, strong antibacterial activity, and stability to β-lactamase, it has attracted much attention. Its structural feature is that the sulfur at position 1 of the penicillin nucleus is replaced by carbon, and there is a double bond at position 2, compounding the five-membered ring of penicillin and the conjugated doubl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D477/20A61K31/4439A61K31/407A61P31/04
CPCY02P20/55
Inventor 黄振华
Owner XUANZHU BIOPHARMACEUTICAL CO LTD
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