IP Library Granted Patent US 8,772,483
Granted Patent B2
US 8,772,483 · App. 13/288,366 · Granted Jul 8, 2014

Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid

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Quick Facts
Patent No.
US 8,772,483
App. No.
13/288,366
Granted
Jul 8, 2014
Kind
B2
Abstract

Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed.

Claims (12)

1. A crystalline compound, which is (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid besylate.

2. The crystalline compound of claim 1 , which is anhydrous.

3. The crystalline compound of claim 2 , which has a melting point of about 234° C. and/or a DSC peak at about 238° C.

4. The crystalline compound of claim 3 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 9.2, 15.9, 16.8, 18.4, 19.8, and/or 20.8 degrees 2θ.

5. The crystalline compound of claim 1 , which is a hydrate.

6. The crystalline compound of claim 5 , which has a melting point of about 218° C.

7. The compound of claim 5 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 8.7, 9.1, 13.4, 18.3, and/or 20.2 degrees 2θ.

8. The crystalline compound of claim 2 , which has a melting point of about 228° C. and/or a DSC peak at about 233° C.

9. The crystalline compound of claim 2 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 8.7, 9.5, 16.9, 17.5, 19.1, 19.7, 20.1, 20.4, 21.8, 22.1, and/or 26.4 degrees 2θ.

10. The crystalline compound of claim 2 , which has an X-ray powder diffraction pattern substantially the same as that shown in FIG. 1 .

11. The crystalline compound of claim 3 , which has an X-ray powder diffraction pattern comprising a peak at one or more of about 7.6, 8.6, 12.9, 15.0, 15.3, 17.3, 19.2, 19.5, 20.2, and/or 23.1 degrees 2θ.

12. A pharmaceutical dosage form comprising the crystalline compound of claim 1 .