Steroid agonist for FXR
View Patent ↗The invention relates to a FXR agonist of formula (I) and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
1. A compound of formula (I):
and pharmaceutically acceptable salts or amino acid conjugates thereof.
2. The glycine conjugate of the compound of formula (I):
3. The taurine conjugate of the compound of formula (I):
4. The compound of claim 1 , wherein said compound is radiolabeled.
5. The compound of claim 4 , wherein said compound is tritiated.
6. A pharmaceutical formulation comprising a compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.
7. A method for the treatment of an FXR mediated disease or condition in a mammal comprising administering to a mammal suffering from an FXR mediated disease or condition a therapeutically effective amount of a compound according to claim 1 , wherein said FXR mediated disease or condition is selected from the group consisting of hypercholesteremia, hyperlipidemia, low HDL-cholesterol, and high triglycerides.
8. A method for the treatment of cardiovascular disease in a mammal comprising administering to a mammal suffering from a cardiovascular disease a therapeutically effective amount of a compound according to claim 1 , wherein said cardiovascular disease is selected from the group consisting of artherosclerosis and hypercholesteremia.
9. The method according to claim 8 , wherein said cardiovascular disease is artherosclerosis.
10. A method for increasing HDL cholesterol in a mammal, said method comprising administering to a mammal whose HDL cholesterol is to be increased a therapeutically effective amount of a compound according to claim 1 .
11. A method for lowering triglycerides in a mammal, said method comprising administering to a mammal whose triglycerides are to be lowered a therapeutically effective amount of a compound according to claim 1 .