Carbon substituted penems antibiotics

Abstract

The present invention belongs to the technical field of medicine, in particular to a carbapenem antibiotic with antibiotic activity shown in the formula (I) and a pharmaceutically acceptable salt, an easily hydrolyzed ester, a hydrate and a hydrate of the ester or the salt thereof: wherein, R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are defined in the description. Moreover, the present invention also provides preparation methods of the compounds, drug combinations containing the compounds 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 carbapenem antibiotics, pharmaceutically acceptable salts thereof, easily hydrolyzed esters, isomers thereof, hydrates thereof, and hydrates of esters or salts thereof. The preparation method of the compounds, the pharmaceutical composition containing these compounds, and the use of these compounds in the preparation of medicines 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 conjugated double bond of cephalosporin to acti...

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Problems solved by technology

Patent document JP1999071277 discloses the compound shown below. This compound has good antibacterial activity against Pseudomonas aeruginosa, but it has poor activity against other bacterial species, and its half-life is very short, so it cannot be administered orally

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

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