Crystalline and amorphous forms of tiagabine

Details Crystalline and amorphous forms of tiagabine Crystalline and amorphous forms of tiagabine

C - Chemistry, Metallurgy

07

D

C07D 409/14 (2006.01) A61K 31/4535 (2006.01)

Patent

CA 2661006

The present invention provides 24 new forms of tiagabine, including 22 new crystalline forms of tiagabine and its salts, an amorphous form of tiagabine free base, and a cocrystal form of tiagabine hydrochloride with 2-furancarboxylic acid. The present invention further provides a process for preparing each of the new tiagabine forms. The present invention further provides a pharmaceutical composition containing at least one of the new tiagabine forms, and a process for the preparation thereof. The present invention further provides a method of treating a disease related to GABA uptake in a mammal, comprising the step of administering to the mammal a therapeutically effective amount of at least one of the new tiagabine forms.

La présente invention concerne 24 nouvelles formes de tiagabine comportant 22 nouvelles formes cristallines de tiagabine et de ses sels, une forme amorphe de base libre de tiagabine et une forme de co-cristal d'hydrochlorure de tiagabine avec de l'acide 2-furane carboxylique. Cette invention concerne également un procédé permettant de préparer chacune des nouvelles formes de tiagabine. Elle concerne aussi une composition pharmaceutique contenant au moins une des nouvelles formes de tiagabine, ainsi qu'un procédé permettant de la préparer. En outre, cette invention concerne un procédé permettant de traiter une maladie liée à l'absorption de GABA chez un mammifère, lequel procédé consiste à administrer au mammifère une quantité efficace d'un point de vue thérapeutique d'au moins une des nouvelles formes de tiagabine.

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