Crystalline form of...

C - Chemistry – Metallurgy – 07 – D

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C07D 413/14 (2006.01) A61K 31/675 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2751392

A crystalline form of crystalline (i?)-3-(4-(2-(2-methyltetrazol-5-yl)- pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.

L'invention concerne une forme cristalline du dihydrogénophosphate de (R)-3-(4-(2-(2-méthyltétrazol-5-yl)-pyridin-5-yl)-3-fluorophényl)-5-hydroxyméthyl oxazolidin-2-one, des procédés de préparation de la forme cristalline et des compositions contenant la forme cristalline utiles comme antibiotiques. En outre, les dérivés de la présente invention peuvent exercer une puissante activité antibactérienne sur divers pathogènes humains et animaux, notamment sur les bactéries Gram-positives telles que les staphylocoques, les entérocoques et les streptocoques, les micro-organismes anaérobies tels que les bactéroides et les Clostridia, et les micro-organismes acido-résistants tels que Mycobacterium tuberculosis et Mycobacterium avium. Les compositions contenant la forme cristalline peuvent donc être utilisées comme antibiotiques.

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