Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions

Patent metadata

Field	Value
Publication number	US-9763964-B2
Application number	US-201514743295-A
Country	US
Kind code	B2
Filing date	Jun 18, 2015
Priority date	Jun 27, 2006
Publication date	Sep 19, 2017
Grant date	Sep 19, 2017

Abstract

The present invention relates to compounds of formula (I):

wherein R is hydrogen or alpha-hydroxy,
the hydroxyl group in position 7 is in the alpha or beta position;
and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.

First claim

The invention claimed is:

1. A method of treating an FXR-mediated gastrointestinal disease or condition in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula (I):

or a pharmaceutically acceptable salt or amino acid conjugate thereof; wherein R is H, and the hydroxyl group in the 7 position is in the alpha position; and wherein the gastrointestinal disease or condition is selected from Crohn's disease, ulcerative colitis, post-radiation colitis, microscopic colitis, and colorectal cancer.

2. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is Crohn's disease.

3. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is ulcerative colitis.

4. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is post-radiation colitis or microscopic colitis.

5. The method of claim 1 , wherein the FXR-mediated gastrointestinal disease or condition is colorectal cancer.

6. The method of claim 1 , wherein the pharmaceutically acceptable salt is

7. The method of claim 1 , wherein the pharmaceutically acceptable salt is

Assignees

• Intercept Pharmaceuticals Inc

Inventors

• Pellicciari Roberto
• Fiorucci Stefano
• Pruzanski Mark

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title