Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
1. A method of treating an FXR-mediated gastrointestinal disease or condition in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula (I):
or a pharmaceutically acceptable salt or amino acid conjugate thereof; wherein R is H, and the hydroxyl group in the 7 position is in the alpha position; and wherein the gastrointestinal disease or condition is selected from Crohn's disease, ulcerative colitis, post-radiation colitis, microscopic colitis, and colorectal cancer.
2. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is Crohn's disease.
3. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is ulcerative colitis.
4. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is post-radiation colitis or microscopic colitis.
5. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is colorectal cancer.
6. The method of claim 1 , wherein the pharmaceutically acceptable salt is
7. The method of claim 1 , wherein the pharmaceutically acceptable salt is