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Formyl aniline substituted sulfhydryl pyrrolidine carbpenem compounds

A compound, methyl technology, applied in the field of matter, can solve the problems of not meeting clinical needs, weak antibacterial activity of MRSA, and low clinical availability.

Active Publication Date: 2010-11-17
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 and the limitation of digestive tract absorption due to the abuse of antibiotics, the carbapenems currently on the market can only be administered as injections in clinical practice, and the clinical utilization is not high, and the antibacterial activity against MRSA Weak, can no longer meet clinical needs

Method used

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  • Formyl aniline substituted sulfhydryl pyrrolidine carbpenem compounds
  • Formyl aniline substituted sulfhydryl pyrrolidine carbpenem compounds
  • Formyl aniline substituted sulfhydryl pyrrolidine carbpenem compounds

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Abstract

The present invention relates to a formanilide substituted sulfhydryl pyrrolidine carbapenems compound as shown in Formula (I), easily hydrolyzed ester thereof, acceptable non-toxicity salt thereof in pharmacy, isomer thereof, hydrate thereof, and hydrate of ester or salt thereof. The present invention also relates to a preparation method of the compound as shown in Formula (I), application of the compounds as active substances for medicine, in particular to the application for preparing the medicine used for treating and / or preventing infectious diseases. The R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, R<8> and X are defined in details in the specification.

Description

1. Technical field The present invention relates to mercaptopyrrolidine carbapenems substituted by formanilide, their easily hydrolyzed esters, their pharmaceutically acceptable non-toxic salts, their isomers, their hydrates, and the hydration of their esters or salts Compounds, preparation methods of these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds for the preparation of drugs for treating and / or preventing infectious diseases belong to the field of medical technology. 2. Background technology Carbapenems are new broad-spectrum, enzyme-resistant and highly effective β-lactam antibiotics developed in the 1970s. In 1976, Thiamycin, the first carbapenem antibiotic, was discovered, but it was not used clinically due to its poor chemical stability. Later, the chemical structure modification of thiamycin produced a series of carbapenem derivatives. At present, such drugs that have been marketed include imipenem, panipenem, ...

Claims

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Application Information

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