Gilead Sciences, Inc.

Phenex Pharmaceuticals Ag

Janssen Pharmaceutica Nv

Orsobio, Inc.

Phenex Discovery Verwaltungs-gmbh

Olaf Kinzel

Christoph Steeneck

Christian Gege

Claus Kremoser

Gerald Kleymann

Thomas Hoffmann

Steven D Goldberg

Hariharan Venkatesan

Xiaohua Xue

Anne Fourie

Ulrich Deuschle

Eva Hambruch

Manfred Birkel

Aaron C Schmitt

Virginia M Tanis

David A Kummer

William John Watkins

Kevin S Currie

Peter A Blomgren

Aihua Wang

Jeffrey E Kropf

Jianjun Xu

Maud J Urbanski

Ulrich Abel

Thomas Schlüter

Michael Albers

Simon Anderhub

Martin Hornberger

Sanja Perovic-Ottstadt

Anne M Fourie

Barbara MORSCHHÄUSER

Sheena Pinto

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 invention provides modulators of indoleamine 2,3-dioxygenase (IDO1) and their use in the prophylaxis and/or treatment of IDO1-mediated diseases. Specifically, the present invention provides compounds according to Formula (I) an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof. 

Substituted N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase

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

The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide or sulfonamide containing cyclic compounds of Formula (1), (1'), (100), (100&#x2032;), (200) and (200&#x2032;) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof. 

Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ROR[&#x3b3;]

The present invention comprises methods of making 5-(2,3-dichloro-4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2-hydroxy-2-methylpropyl)-4-(R-1-carbonyl)thiazole-2-carboxamide, wherein Ris defined in the specification.

Trifluoromethyl alcohols as modulators of ROR&#x3b3;t

The present invention comprises compounds of Formula I wherein:R, R, R, R, R, R, R, and {circle around (A)} are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR&#x3b3;t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Thiazoles as modulators of ROR&#x3b3;t

FXR (NR1H4) modulating compounds

The present invention comprises compounds of Formula I wherein:R, R, R, R, R, R, R, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR&#x3b3;t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

The present invention comprises compounds of Formula I. wherein:X, A, A, A, A, R, R, and Rare defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR&#x3b3;t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim

The present invention comprises compounds of Formula I. wherein:R, R, R, R, A, A, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR&#x3b3;t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Amide substituted thiazoles as modulators of RORyt

The invention provides modulators for the orphan nuclear receptor RORand methods for treating RORmediated diseases by administrating these novel RORmodulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof. 

Pyrrolo carboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (ROR&#x3b3;, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases

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Heidelberg, Germany

Olaf Kinzel