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Claims for Patent: 9,238,673

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Claims for Patent: 9,238,673

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)
Application Number:13/919,734
Patent Claims: 1. A pharmaceutical composition comprising obeticholic acid Form 1 and a pharmaceutically acceptable carrier, wherein the obeticholic acid Form 1 comprises less than 1% of chenodeoxycholic acid.

2. The pharmaceutical composition of claim 1, wherein the obeticholic acid Form 1 further comprises not more than 0.15% of 6.beta.-ethylchenodeoxycholic acid.

3. The pharmaceutical composition of claim 2, wherein the obeticholic acid Form 1 comprises less than about 0.07% of 6.beta.-ethylchenodeoxycholic acid.

4. The pharmaceutical composition of claim 3, wherein the obeticholic acid Form 1 comprises less than about 0.06% of 6.beta.-ethylchenodeoxycholic acid.

5. The pharmaceutical composition of claim 4, wherein the obeticholic acid Form 1 comprises less than about 0.05% of 6.beta.-ethylchenodeoxycholic acid.

6. The pharmaceutical composition of claim 1, wherein the obeticholic acid Form 1 comprises less than about 0.5% of chenodeoxycholic acid.

7. The pharmaceutical composition of claim 6, wherein the obeticholic acid Form 1 comprises less than about 0.3% of chenodeoxycholic acid.

8. The pharmaceutical composition of claim 7, wherein the obeticholic acid Form 1 comprises less than about 0.2% of chenodeoxycholic acid.

9. The pharmaceutical composition of claim 1, wherein the obeticholic acid Form 1 further comprises not more than 0.15% of 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.

10. The pharmaceutical composition of claim 9, wherein the obeticholic acid Form 1 comprises less than about 0.07% of 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.

11. The pharmaceutical composition of claim 10, wherein the obeticholic acid Form 1 comprises less than about 0.06% of 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.

12. The pharmaceutical composition of claim 11, wherein the obeticholic acid Form 1 comprises less than about 0.05% of 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.

13. The pharmaceutical composition of claim 1, wherein the obeticholic acid Form 1 further comprises not more than 0.15% of 6.beta.-ethylchenodeoxycholic acid and not more than 0.15% of 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.

14. The pharmaceutical composition of claim 13, wherein the obeticholic acid Form 1 comprises less than about 0.07% of 6.beta.-ethylchenodeoxycholic acid.

15. The pharmaceutical composition of claim 13, wherein the obeticholic acid Form 1 comprises less than about 0.05% of 6.beta.-ethylchenodeoxycholic acid.

16. The pharmaceutical composition of claim 13, wherein the obeticholic acid Form 1 comprises less than about 0.5% of chenodeoxycholic acid.

17. The pharmaceutical composition of claim 16, wherein the obeticholic acid Form 1 comprises less than about 0.3% of chenodeoxycholic acid.

18. The pharmaceutical composition of claim 17, wherein the obeticholic acid Form 1 comprises less than about 0.2% of chenodeoxycholic acid.

19. The pharmaceutical composition of claim 1, wherein the obeticholic acid Form 1 comprises less than about 0.05% of 6.beta.-ethylchenodeoxycholic acid, and less than about 0.05% of 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.

20. The pharmaceutical composition of claim 19, wherein the obeticholic acid Form 1 comprises less than about 0.3% of chenodeoxycholic acid.

21. The pharmaceutical composition of claim 20, wherein the obeticholic acid Form 1 comprises less than about 0.2% of chenodeoxycholic acid.

22. The pharmaceutical composition of claim 1, wherein the obeticholic acid Form 1 further comprises less than about 2% of water.

23. A pharmaceutical composition comprising obeticholic acid Form 1 and a pharmaceutically acceptable carrier, wherein the obeticholic acid Form 1 comprises one or more compound selected from 6.beta.-ethylchenodeoxycholic 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, wherein 6.beta.-ethylchenodeoxycholic acid is present in an amount between about 0% and not more than 0.05%, chenodeoxycholic acid is present in an amount between about 0% and not more than 0.2%, 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 is present in an amount between about 0% and not more than 0.05%.
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