Gilead Sciences, Inc.

Phenex Pharmaceuticals Ag

Orsobio, Inc.

Phenix Pharmaceuticals Ag

Claus Kremoser

Olaf Kinzel

Christoph Steeneck

Ulrich Deuschle

Christian Gege

John S Kiely

Ronnie C Hanecak

Elena Dneprovskaia

Kerstin Otte

Manfred Birkel

Eva Hambruch

Manish Sud

Carlton Sage

Matthew Lee

Harald Kranz

Manfred Kögl

Ingo Kober

Normand Hébert

Kristina Giegrich

Tim Gahman

Zach Cheruvallath

Ulrike Bauer

Aaron C Schmitt

Ulrich Abel

William John Watkins

Kevin S Currie

Peter A Blomgren

Jeffrey E Kropf

Jianjun Xu

Gerald Kleymann

Thomas Hoffmann

Andreas Schulz

Thomas Schlüter

Michael Albers

Sanja Perovic-Ottstadt

The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXRa and/or LXKJ3) and act preferably as inverse agonists of LXR.

LXR modulators with bicyclic core moiety

The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXRα and/or LXKβ) and act preferably as inverse agonists of LXR.

The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXR&#x3b1; and/or LXK&#x3b2;) and act preferably as inverse agonists of LXR. 

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.

FXR (NR1H4) binding and activity modulating compounds

FXR (NR1H4) modulating compounds

Hydroxy containing FXR (NR1H4) modulating compounds

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.

The invention provides modulators for the orphan nuclear receptor ROR&#x3b3; and methods for treating ROR&#x3b3; mediated diseases by administrating these novel ROR&#x3b3; modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof. 

Compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR&#x3b3;, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune disease

The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists or partial 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.

Heterocyclic FXR binding compounds

The invention provides compounds according to the general formula () which bind to the NRHreceptor and act as agonists, antagonists or mixed agonists/antagonists of the NRHreceptor. The invention further provides methods of treating diseases and/or conditions through binding of the nuclear receptor by the compounds and the production of medicaments using the compounds.

FXR NR1H4 nuclear receptor binding compounds

The present invention relates to compounds according to the general formula (I) which bind to the nuclear receptor, NR1H4, and act as agonists and antagonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear receptor by the compounds.

NR1H4 nuclear receptor binding compounds

Growing community of inventors

Heidelberg, Germany

Claus Kremoser