IP Library Granted Patent US 9,932,332
Granted Patent B2
US 9,932,332 · App. 15/619,883 · Granted Apr 3, 2018

FXR (NR1H4) modulating compounds

Inventor: Christian Gege (Mauer, DE)
Assignee: GILEAD SCIENCES, INC.
C07D417/14C07D493/08
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Quick Facts
Patent No.
US 9,932,332
App. No.
15/619,883
Granted
Apr 3, 2018
Kind
B2
Abstract

The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

Claims (9)

1. A compound selected from:

or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.

2. The compound of claim 1 of the formula:

or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.

3. The compound of claim 1 of the formula:

or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof.

4. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof, and a pharmaceutically acceptable excipient.

5. A method of treating a condition selected from the group consisting of liver fibrosis, liver cirrhosis, liver steatosis, acute liver failure, Non-Alcoholic Fatty Liver Disease (NAFLD), Non-Alcoholic Steatohepatitis (NASH), Primary Biliary Cirrhosis (PBC), and Primary Sclerosing Cholangitis (PSC) comprising administering a compound of claim 1 , or a pharmaceutically acceptable salt, a stereoisomer, a mixture of stereoisomers, or a tautomer thereof, to a patient in need thereof.

6. The method according to claim 5 , wherein the condition is Non-Alcoholic Steatohepatitis (NASH).

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2017
From: GEGE, CHRISTIAN
To: PHENEX PHARMACEUTICALS AG
Reel/Frame 043134/0489 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2017
From: PHENEX PHARMACEUTICALS AG
To: GILEAD SCIENCES, INC.
Reel/Frame 043134/0503 →
Continuity (2)
Provisional Application 62349494 · Jun 13, 2016
Related Publication 20170355694A1 · Dec 14, 2017