Steroids as agonists for FXR
The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
1. A method for treating an FXR-mediated disease or condition in a mammal comprising administering a therapeutically effective amount of an amino acid conjugate of compound of formula (I)
wherein a compound of formula (I) can be optionally radiolabeled, to the mammal, wherein said mammal is in need of treatment of the FXR-mediated disease or condition, and wherein the disease or condition is selected from a cholestatic liver disease, atherosclerosis, arteriosclerosis, hypercholesteremia, or hyperlipidemia.
2. The method of claim 1 , wherein the amino acid conjugate of compound of formula (I) is administered orally.
3. The method of claim 1 , wherein the amino acid conjugate of compound of formula (I) is administered intravenously.
4. The method of claim 1 , wherein the amino acid conjugate of compound of formula (I) is a glycine conjugate of the compound of formula (I).
5. The method of claim 1 , wherein the amino acid conjugate of compound of formula (I) is a taurine conjugate of the compound of formula (I).
6. The method of claim 1 , wherein the compound of formula (I) is radiolabeled.
7. The method of claim 6 , wherein the compound of formula (I) is tritiated.
8. The method of claim 1 , wherein the mammal is human.