C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/4985 (2006.01) A61P 3/10 (2006.01)
Patent
CA 2536251
The present invention relates to crystalline anhydrate polymorphs of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro[1,2,4]triazolo[4,3-.alpha.]pyrazin-7(8H)-yl]-1-(2,4,5- trifluorophenyl)butan-2-amine as well as a process for their preparation, pharmaceutical compositions containing these novel forms, and methods of use of the novel forms and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure. The invention also concerns novel crystalline solvates of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3- (trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-.alpha.]pyrazin-7(8H)-yl]-1- (2,4,5-trifluorophenyl)butan-2-amine as well as a crystalline desolvated polymorph and their use for the preparation of the anhydrate polymorphs of the present invention.
L'invention se rapporte à des polymorphes anhydrates cristallins du sel de dihydrogenphosphate de (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-?]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, ainsi que sur un procédé de préparation associé, sur des compositions pharmaceutiques contenant ces nouvelles formes, et sur des procédés d'utilisation des ces nouvelles formes ainsi que sur des compositions pharmaceutiques pour le traitement de diabètes, de l'obésité, et la pression sanguine élevée. Cette invention porte aussi sur de nouveaux solvates cristallins du sel de dihydrogenphosphate de (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-?]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, ainsi que sur un polymorphe désolvaté cristallin, et sur leur utilisation pour la préparation des polymorphes anhydrates susmentionnés.
Armstrong Joseph D. III
Chen Alex M.
Cypes Stephen
Ferlita Russell R.
Hansen Karl
Gowling Lafleur Henderson Llp
Merck & Co. Inc.
Merck Sharp & Dohme Corp.
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