Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor

Details Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor Phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/4985 (2006.01) A61P 3/10 (2006.01)

Patent

CA 2529400

The dihydrogenphosphate salt of 4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro[1,2,4]triazolo[4,3-&agr;]pyrazin-7(8H)-yl]-1-(2,4,5- trifluorophenyl)butan-2-amine is a potent inhibitor of dipeptidyl peptidase-IV and is useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The invention also relates to a crystalline monohydrate of the dihydrogenphosphate salt as well as a process for its preparation, pharmaceutical compositions containing this novel form and methods of use for the treatment of diabetes, obesity, and high blood pressure.

Cette invention concerne un sel de dihydrogène phosphate de 4-oxo-4-[3-trifluorométhyl)-5,6-dihydro[1,2,4]triazolo[4,3-.alpha.]pyrazin-7(8<I>H</I>)-yl]-1-(2,4,5-trifluorophényl)butan-2-amine constituant un inhibiteur puissant de la dipeptidyl peptidase IV et servant à la prévention et/ou au traitement du diabète non insulino-dépendant, aussi connu sous le nom de diabète de type 2. Cette invention concerne également un monohydrate cristallin du sel de dihydrogène phosphate ainsi qu'un procédé de préparation de celui-ci, des compositions pharmaceutiques contenant cette nouvelle forme et des méthodes d'utilisation pour le traitement du diabète, de l'obésité et de l'hypertension artérielle.

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