Steroids as agonists for FXR
The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
1. A compound of formula I formula (I):
wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
2. The glycine conjugate of a compound of formula (I):
wherein R is ethyl.
3. The taurine conjugate of a compound of formula (I):
wherein R is ethyl.
4. A pharmaceutical formulation comprising a compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.
5. 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.
6. 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 desease disease is selected from the group consisting of artherosclerosis atherosclerosis and hypercholesteremia.
7. The method according to claim 6 , wherein said cardiovascular disease is atherosclerosis.
8. 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 .
9. A method for lowering triglycerides in a mammal, said method comprising administering to a mammal whose triglycerides are to be decreased a therapeutically effective amount of a compound according to claim 1 .
10. The compound of claim 1 , wherein said compound is radiolabeled.
11. The compound of claim 10 , wherein said compound is tritiated.
12. The compound of claim 1, which is the compound of formula (I)
wherein R is ethyl.
13. A pharmaceutically acceptable salt of the compound of claim 1.
14. A solvate of the compound of claim 1.