Crystalline forms of a dipeptidyl peptidase-IV inhibitor
AssigneeMerck Sharp & Dohme Corp.
InventorsItzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Abstract
Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
Claims12
Crystalline (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine of Compound I:
- characterized by having at least four peaks in its powder X-ray diffraction pattern selected from the group consisting of 10.3±0.1 2θ, 12.7±0.1 2θ, 14.6±0.1 2θ, 16.1±0.1 2θ, 17.8±0.1 2θ, 19.2±0.1 2θ, 22.2±0.1 2θ, 24.1±0.1 2θ and 26.9±0.1 2θ.
Crystalline (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine of Compound I:
- characterized by having at least four peaks in its powder X-ray diffraction pattern selected from the group consisting of 7.5±0.1 2θ, 15.0±0.1 2θ, 16.2±0.1 2θ, 20.9±0.1 2θ, 22.0±0.1 2θ, 27.0±0.1 2θ, 27.6±0.1 2θ, 33.3+0.1 2θ.
Crystalline (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine of Compound I:
- characterized by having at least four peaks in its powder X-ray diffraction pattern selected from the group consisting of 14.5±0.1 2θ, 15.9±0.1 2θ, 17.3±0.1 2θ, 18.7±0.1 2θ, 19.5±0.1 2θ, 19.5±0.1 2θ, 21.2±0.1 2θ, 22.0±0.1 2θ and 23.2±0.1 2θ.
Crystalline (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine of Compound I:
- characterized by having at least four peaks in its powder X-ray diffraction pattern selected from the group consisting of 8.1±0.1 2θ, 10.6±0.1 2θ, 16.0±0.1 2θ, 16.9±0.1 2θ, 19.5±0.1 2θ, 21.3±0.1 2θ, 23.3±0.1 2θ and 25.4±0.1 2θ.
Dependencies are inferred from the claim text.