FXR (NR1H4) binding and activity modulating compounds

US8952042B2 · kind B2 · utility

Assignee

• PHENEX PHARMACEUTICALS AG · DE

Inventors

• Claus Kremoser · Heidelberg, DE
• Ulrich Abel · Schifferstadt, DE
• Christoph Steeneck · Dossenheim, DE
• Olaf Kinzel · Heidelberg, DE

Key dates

• Filing date: Aug 19, 2010
• Grant date: Feb 10, 2015
• Expiry date: Aug 21, 2031

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to compounds of formula (1):where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (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.