IP Library Granted Patent US 7,138,390
Granted Patent B2
US 7,138,390 · App. 10/471,549 · Granted Nov 21, 2006

Steroids as agonists for FXR

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Quick Facts
Patent No.
US 7,138,390
App. No.
10/471,549
Granted
Nov 21, 2006
Kind
B2
Abstract

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.

Claims (14)

1. A compound of 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 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.

Assignments (3)
CHANGE OF ADDRESS Recorded Jul 22, 2022
From: INTERCEPT PHARMACEUTICALS, INC.
To: INTERCEPT PHARMACEUTICALS, INC.
Reel/Frame 060814/0757 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 29, 2010
From: PELLICCIARI, ROBERTO
To: INTERCEPT PHARMACEUTICALS, INC.
Reel/Frame 024153/0749 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 19, 2004
From: PELLICCIARI, ROBERTO
To: INTERCEPT PHARMACEUTICALS
Reel/Frame 015693/0870 →