Phenex Pharmaceuticals Ag

Janssen Pharmaceutica Nv

Phenex Discovery Verwaltungs-Gmbh

Thomas Hoffmann

Christoph Steeneck

Olaf Kinzel

Gerald Kleymann

Christian Gege

Steven D Goldberg

Hariharan Venkatesan

Xiaohua Xue

Anne Fourie

Michael Albers

Virginia M Tanis

Ulrich Deuschle

David A Kummer

Aihua Wang

Maud J Urbanski

Claus Kremoser

Thomas Schlüter

Simon Anderhub

Sanja Perovic-Ottstadt

Martin Hornberger

Sheena Pinto

Anne M Fourie

Barbara MORSCHHÄUSER

The present invention relates to compounds which can act as aryl hydrocarbon receptor (AhR) modulators and, in particular, as AhR antagonists. The invention further relates to the use of the compounds for the treatment and/or prophylaxis of diseases and/or conditions through binding of said aryl hydrocarbon receptor by said compounds. 

Aryl hydrocarbon receptor (AhR) modulator compounds

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

Aryl hydrocarbon receptor (AHR) modulator 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

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

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 containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof. 

Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor ROR&#x3b3;

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

Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-&#x3b3; (ROR-&#x3b3;, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases

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

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Speyer, Germany

Thomas Hoffmann