IP Library Granted Patent US 9,650,409
Granted Patent B2
US 9,650,409 · App. 13/871,492 · Granted May 16, 2017

TGR5 modulators and methods of use thereof

Inventor: Roberto Pellicciari (Perugia, IT)
Assignee: Intercept Pharmaceuticals, Inc.
C07J9/005C07J9/00C07J31/00C07J41/00
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Quick Facts
Patent No.
US 9,650,409
App. No.
13/871,492
Granted
May 16, 2017
Kind
B2
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.

Claims (9)

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.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded Jan 4, 2024
From: U.S. BANK TRUST COMPANY, NATIONAL ASSOCIATION
To: INTERCEPT PHARMACEUTICALS, INC.
Reel/Frame 066662/0210 →
CHANGE OF ADDRESS Recorded Aug 22, 2022
From: INTERCEPT PHARMACEUTICALS, INC.
To: INTERCEPT PHARMACEUTICALS, INC.
Reel/Frame 061297/0856 →
SECURITY INTEREST Recorded Aug 18, 2021
From: INTERCEPT PHARMACEUTICALS, INC.
To: U.S. BANK NATIONAL ASSOCIATION
Reel/Frame 057650/0772 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 7, 2013
From: PELLICCIARI, ROBERTO
To: INTERCEPT PHARMACEUTICALS, INC.
Reel/Frame 030567/0257 →
Priority Claims (1)
EP 08169462 · Nov 19, 2008 · regional
Continuity (3)
Continuation 13313689 · Dec 7, 2011
Continuation 12622123 · Nov 19, 2009
Related Publication 20140100209A1 · Apr 10, 2014