Novel polymorphs of racemic, dextrorotatory, and...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 401/04 (2006.01) A61K 31/4545 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2546039

A polymorphic forms of the hydrochloride salt and mesylate salt of racemic (.plusmn.)-1-cyclopropyl-6-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1- yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid, dextrorotatory R-(+)-1- cyclopropyl-ó-fluoro-8-methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4- dihydro-4-oxo-quinoline-3-carboxylic acid and S-(-)-1-cyclopropyl-6-fluoro-8- methoxy-7-(4-amino-3,3-dimethylpiperidin-1-yl)-1,4-dihydro-4-oxo-quinoline-3- carboxylic acid having formula (I) and (II) respectively are described. Processes for their preparation are also described. The invention further relates to methods of using, and pharmaceutical compositions comprising the compounds of the invention for treatment of bacterial infections in mammals.

L'invention concerne des formes polymorphes du sel de chlorhydrate et du sel de mésylate d'un acide (.plusmn.)-1-cyclopropyl-6-fluoro-8-méthoxy-7-(4-amino-3,3-diméthylpipéridin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylique racémique, d'un acide R-(+)-1-cyclopropyl-6-fluoro-8-méthoxy-7-(4-amino-3,3-diméthylpipéridin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylique dextrogyre, et d'un acide S-(-)-1-cyclopropyl-6-fluoro-8-méthoxy-7-(4-amino-3,3-diméthylpipéridin-1-yl)-1,4-dihydro-4-oxo-quinoline-3-carboxylique lévogyre de formules (I) et (II). L'invention se rapporte en outre à leurs procédés de préparation. Elle concerne également des méthodes d'utilisation et des compositions pharmaceutiques renfermant les composés susmentionnés pour le traitement d'infections bactériennes chez des mammifères.

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