Details for Patent: 9,732,116

Title:	Preparation and uses of obeticholic acid
Abstract:	The present invention relates to obeticholic acid: ##STR00001## or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
Inventor(s):	Steiner; Andre (Raubling, DE), Waenerlund Poulsen; Heidi (Koge, DK), Jolibois; Emilie (Cambridge, GB), Rewolinski; Melissa (San Diego, CA), Gross; Ralf (Raubling, DE), Sharp; Emma (Cambridge, GB), Dubas-Fisher; Fiona (Cambridge, GB), Eberlin; Alex (Cambridge, GB)
Assignee:	Intercept Pharmaceuticals, Inc. (New York, NY)
Filing Date:	Nov 20, 2015
Application Number:	14/947,492
Claims:	1. A crystalline form of obeticholic acid characterized by an X-ray powder diffraction pattern comprising peaks at 9.5, 12.5 and 16.7.+-.0.2 degrees 2-theta. 2. A crystalline form of obeticholic acid characterized by an X-ray powder diffraction pattern set forth in FIG. 5. 3. The crystalline form of claim 1 characterized by a differential scanning calorimetry thermogram having an endothermic peak at about 98.+-.2.degree. C. 4. The crystalline form of claim 1 characterized by a differential scanning calorimetry thermogram pattern set forth in FIG. 6. 5. The crystalline form of claim 1 characterized by a thermo-gravimetric analysis thermogram pattern set forth in FIG. 6. 6. The crystalline form of claim 1 having a purity of greater than about 96%. 7. The crystalline form of claim 6 having a purity of greater than about 98%. 8. The crystalline form of claim 1 having a total of less than about 4% of one or more impurities selected 6-ethylursodeoxycholic acid, 3.alpha.-hydroxy-6.alpha.-ethyl-7-cheto-5.beta.-cholan-24-oic acid, 6.beta.-ethylchenodeoxycholic acid, 3.alpha.,7.alpha.-dihydroxy-6-ethyliden-5.beta.-cholan-24-oic acid, chenodeoxycholic acid, and 3.alpha.(3.alpha.,7.alpha.-dihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oyl- oxy)-7.alpha.-hydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid. 9. The crystalline form of claim 8, wherein the total percentage of impurities is less than about 3.8%. 10. The crystalline form of claim 9, wherein the total percentage of impurities is less than about 3.6%.