Crystalline Forms of 1-[(3R,4S)-4-Cyanotetrahydropyran-3-YL]-3-[(2-Fluoro-6-Methoxy-4-Pyridyl)Amino]Pyrazole-4-Carboxamide
AssigneeIntervet Inc.
InventorsChristophe Pierre Alain Chassaing, Xiaoling Jin, Rositza Iordanova Petrova, Richard J. Varsolona, Lorenzo Codan, Edward Cleator, Adrian Goodyear, Jonathan Simmons, Tanja Schweisel
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Abstract
The present application relates to crystalline forms of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide and processes for the preparation thereof. The compound is useful for the treatment of JAK-mediated diseases or conditions such as atopic dermatitis.
Claims15
A crystalline form (Form 1) of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide having at least one of the following characteristics:
- an X-ray powder diffraction (XRPD) pattern having at least one peak in terms of ° 2θ(±0.2) selected from the group consisting of 6.9, 13.9, 17.8, 19.6, 20.4, 20.9, 24.7, 25.0, 26.6 and 29.1;
- a carbon-13 cross-polarization magic-angle spinning (CPMAS) nuclear magnetic resonance (NMR) spectrum having at least one peak selected from the group consisting of 30.61, 32.60, 53.40, 59.59, 67.21, 71.93, 88.50, 96.35, 104.47, 120.39, 121.95, 131.45, 153.31, 161.41, 163.36, and 166.70 ppm;
- or
- a differential scanning calorimetry (DSC) thermogram comprising an endothermic peak at about 257° C.
A crystalline hydrate form of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide having at least one of the following characteristics:
- an X-ray powder diffraction (XRPD) spectrum having at least one peak in terms of ° 2θ(±0.2) selected from the group consisting of 7.3, 12.6, 12.9, 13.1, 16.2, 17.4, 21.8, 27.8 and 28.4;
- a carbon-13 cross-polarization magic-angle spinning (CPMAS) nuclear magnetic resonance (NMR) spectrum having at least one peak selected from the group consisting of 29.80, 30.52, 54.35, 60.67, 65.45, 70.62, 89.08, 92.52, 102.17, 121.96, 123.48, 131.05, 152.21, 163.46, 164.53, and 168.40 ppm;
- or
- a differential scanning calorimetry (DSC) thermogram comprising a first endothermic peak with an onset temperature of about 27° C. and a second endothermic peak at about 254° C.
Dependencies are inferred from the claim text.