Claims for Patent: 8,653,094

Summary for Patent: 8,653,094

Title:	Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phen- yl)-2,2,2-trifluoroethoxy)-pyrimidin-4-yl)phenyl)propanoate and methods of their use
Abstract:	Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phen- yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.
Inventor(s):	Bednarz; Mark S. (Yardley, PA), De Paul; Susan (Zurich, CH), Kanamarlapudi; Ramanaiah C. (Bridgewater, NJ), Perlberg; Anett (Gunzgen, CH), Zhang; Haiming (San Mateo, CA)
Assignee:	Lexicon Pharmaceuticals, Inc. (The Woodlands, TX)
Application Number:	13/486,103
Patent Claims:	1. A method of treating or managing a disease or disorder mediated by peripheral serotonin, which comprises administering to a patient in need of such treatment, or management a therapeutically effective amount of a compound, which is crystalline (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phen- yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate or a pharmaceutically acceptable salt thereof. 2. The method of claim 1, wherein the disease or disorder is carcinoid syndrome. 3. The method of claim 1, wherein the disease or disorder is a gastrointestinal disease or disorder. 4. The method of claim 3, wherein the disease or disorder is irritable bowel syndrome. 5. The method of claim 1, wherein the disease or disorder is Crohn's disease. 6. The method of claim 1, wherein the compound is crystalline (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phen- yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate. 7. The method of claim 6, wherein the compound has a melting point of about 104.degree. C. 8. The method of claim 6, wherein the compound has an X-ray powder diffraction pattern with peaks at one or more of about 10.7, 12.2, 12.8, 17.7 and/or 22.0 degrees 2.theta.. 9. The method of claim 6, wherein the compound has an X-ray powder diffraction pattern that is substantially the same as that shown in FIG. 1. 10. The method of claim 1, wherein the compound is a crystalline salt of (S)-ethyl 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)propanoate. 11. The method of claim 10, wherein the compound is a hippurate salt. 12. The method of claim 11, wherein the compound has a melting point of about 145.degree. C. 13. The method of claim 11, wherein the compound has an X-ray powder diffraction pattern comprising peaks at one or more of about 8.2, 9.5, 12.6, 16.9, 21.8, 22.0, 22.7, 24.3 and/or 29.1 degrees 2.theta.. 14. The method of claim 11, wherein the compound has an X-ray powder diffraction pattern that is substantially the same as that shown in FIG. 2. 15. The method of claim 11, wherein the compound has a Raman spectrum that is substantially the same as that shown in FIG. 3. 16. The method of claim 10, wherein the compound is a succinate salt. 17. The method of claim 16, wherein the compound has an X-ray powder diffraction pattern comprising peaks at one or more of about 7.7, 11.5, 11.7, 15.7, 17.9, 21.1 and/or 23.2 degrees 2.theta.. 18. The method of claim 16, wherein the compound has an X-ray powder diffraction pattern that is substantially the same as that shown in FIG. 4.