Pharmaceutical forms of diazabicyclooctane derivatives and process for producing the same

Abstract

The present invention relates to a pharmaceutical composition and a lyophilisate of a diazabicyclooctane derivative represented by Compound I, a process for producing the same and methods for using the same.

Description

Background technique [0001] Penicillins and cephalosporins are widely and commonly used β-lactam antibiotics in clinic. However, acquired resistance to β-lactam antibiotics by various pathogens has a damaging effect on maintaining effective treatment of bacterial infections. The most important known mechanism associated with the acquisition of bacterial resistance is the production of class A, C and D beta-lactamases with a serine residue in the active center. These enzymes break down β-lactam antibiotics, resulting in loss of antimicrobial activity. Class A β-lactamases preferentially hydrolyze penicillins, whereas class C β-lactamases have substrate characteristics that facilitate the hydrolysis of cephalosporins. [0002] Commercially available β-lactamase inhibitors (e.g., clavulanic acid, sulbactam, and tazobactam) are known, and these inhibitors are mainly effective against class A β-lactamase producing bacteria, And it is used as a mixture with the penicillin antibio...

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Problems solved by technology

[0005] Although other crystalline forms have been previously characterized, a large-scale manufacturing process that provides good reproducibility, high stability, and high yield has not yet been achieved

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