FXR (NR1H4) binding and activity modulating compounds

Patent metadata

Field	Value
Publication number	US-9820979-B2
Application number	US-201615369521-A
Country	US
Kind code	B2
Filing date	Dec 5, 2016
Priority date	Jul 13, 2011
Publication date	Nov 21, 2017
Grant date	Nov 21, 2017

Abstract

The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention 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 method of treating primary biliary cirrhosis comprising administering to a patient in need thereof a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein a compound having the following structure, or a pharmaceutically acceptable salt thereof, is administered to the patient in need thereof:

3. The method of claim 1 , wherein a compound having the following structure, or a pharmaceutically acceptable salt thereof, is administered to the patient in need thereof:

4. A method of treating primary sclerosing cholangitis cirrhosis comprising administering to a patient in need thereof a compound selected from the group consisting of

or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 , wherein a compound having the following structure, or a pharmaceutically acceptable salt thereof, is administered to the patient in need thereof:

6. The method of claim 4 , wherein a compound having the following structure, or a pharmaceutically acceptable salt thereof, is administered to the patient in need thereof:

Assignees

• Gilead Sciences Inc

Inventors

• Kinzel Olaf
• Steeneck Christoph
• Kremoser Claus

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

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title