Preparation and uses of obeticholic acid
AssigneeIntercept Pharmaceuticals, Inc.
InventorsAndré STEINER, Heidi WAENERLUND POULSEN, Emilie JOLIBOIS, Melissa REWOLINSKI, Ralf GROSS, Emma SHARP, Fiona DUBAS-FISCHER, Alex EBERLIN
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Abstract
The present invention relates to obeticholic acid: 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.
Claims21
An oral formulation comprising:
- obeticholic acid Form 1 that is pharmaceutically acceptable for administration to a human;
- and
- a pharmaceutically acceptable excipient,
- wherein chenodeoxycholic acid is present as an impurity in the obeticholic acid Form 1 that is pharmaceutically acceptable for administration to a human and the amount of the chenodeoxycholic acid is less than 1%.
A composition comprising:
- obeticholic acid Form 1;
- and
- a pharmaceutically acceptable excipient,
- wherein chenodeoxycholic acid is present as an impurity in the obeticholic acid Form 1 and the amount of the chenodeoxycholic acid is less than 1%,
- wherein obeticholic acid Form 1 is pharmaceutically acceptable for administration to a human, and
- wherein the obeticholic acid Form 1 contains an organic solvent at a residual level suitable for human pharmaceutical use.
A composition comprising:
- obeticholic acid Form 1 that is pharmaceutically acceptable for administration to a human obtained by converting crystalline obeticholic acid or by converting a pharmaceutically acceptable salt of crystalline obeticholic acid;
- and
- a pharmaceutically acceptable excipient,
- wherein chenodeoxycholic acid is present as an impurity in the obeticholic acid Form 1 that is pharmaceutically acceptable for administration to a human obtained by converting crystalline obeticholic acid or by converting a pharmaceutically acceptable salt of crystalline obeticholic acid and the amount of the chenodeoxycholic acid is less than 1%.
21-29. (canceled)
Dependencies are inferred from the claim text.