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Generated: December 15, 2017

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Claims for Patent: 7,138,390

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Claims for Patent: 7,138,390

Title:Steroids as agonists for FXR
Abstract: The invention relates to compounds of formula (I): ##STR00001## wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Inventor(s): Pellicciari; Roberto (Perugia, IT)
Assignee: Intercept Pharmaceuticals (New York, NY)
Application Number:10/471,549
Patent Claims: 1. A compound of formula I: ##STR00007## wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.

2. The glycine conjugate of a compound of formula (I): ##STR00008## wherein R is ethyl.

3. The taurine conjugate of a compound of formula (I): ##STR00009## 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 is selected from the group consisting of artherosclerosis 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 increased 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.
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