FXR (NR1H4) modulating compounds

Patent metadata

Field	Value
Publication number	US-9932332-B2
Application number	US-201715619883-A
Country	US
Kind code	B2
Filing date	Jun 12, 2017
Priority date	Jun 13, 2016
Publication date	Apr 3, 2018
Grant date	Apr 3, 2018

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.

First claim

The invention claimed is:

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).

Assignees

• Gilead Sciences Inc

Inventors

• Gege Christian

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

• A61P35/00

  Antineoplastic agents · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P5/38

  of the suprarenal hormones · CPC title