Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
View Patent ↗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 compound 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 or amino acid conjugates thereof.
2. A compound of formula (I):
wherein the hydroxy group in position 7 is in the alpha position and R is hydrogen.
3. A compound of formula (I):
wherein the hydroxy group in position 7 is in the beta position and R is hydrogen.
4. A compound of formula (I):
wherein the hydroxy group in position 7 is in the alpha position and R is alpha-hydroxy.
5. A compound of formula (I) according to claim 1 wherein the pharmaceutically acceptable salt is:
6. A compound of formula (I) according to claim 1 wherein the pharmaceutically acceptable salt is:
7. A method for the treatment of cholestasis in a mammal comprising administering to the mammal suffering from cholestasis a therapeutically effective amount of a compound of formula (I) according to any one of claims 1 - 4 .
8. A pharmaceutical composition comprising a compound of formula (I) according to any one of claims 1 - 4 and a pharmaceutically acceptable carrier or diluent.