TGR5 modulators and methods of use thereof

Patent metadata

Field	Value
Publication number	US-9650409-B2
Application number	US-201313871492-A
Country	US
Kind code	B2
Filing date	Apr 26, 2013
Priority date	Nov 19, 2008
Publication date	May 16, 2017
Grant date	May 16, 2017

Abstract

The invention relates to compounds of Formula A:

or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

First claim

What is claimed:

1. A method of ameliorating a disease in a subject in need thereof, comprising administering compound Ih3e:

or a pharmaceutically acceptable salt or glycine or taurine amino acid conjugate wherein the disease is selected from a metabolic disease, wherein the metabolic disease is selected from metabolic syndrome, insulin resistance, pre-diabetic insulin resistance, hypertension, and dyslipidemia.

2. The method of claim 1 , wherein the disease is metabolic syndrome.

3. The method of claim 1 , wherein the disease is insulin resistance.

4. The method of claim 1 , wherein the compound is a free acid.

5. The method of claim 1 , wherein the compound is a pharmaceutically acceptable salt.

6. The method of claim 1 , wherein the compound is a glycine amino acid conjugate.

7. The method of claim 1 , wherein the compound is a taurine amino acid conjugate.

8. The method of claim 1 , further comprising administering at least one pharmaceutically acceptable excipient.

Assignees

• Intercept Pharmaceuticals Inc

Inventors

• Pellicciari Roberto

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

• A61P43/00

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

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P37/02

  Immunomodulators · CPC title