Ludwigshafen Am Rhein-oggersheim, Germany
Ludwigshafen Am Rhein-oggersheim, Germany

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The invention provides modulators for the orphan nuclear receptor ROR and methods for treating ROR mediated diseases by administering these novel ROR modulators to a human or a mammal in need thereof. Specifically, the present invention relates to compounds for use ROR modulators, wherein the compounds are carboxamide containing cyclic compounds of Formula (6) to Formula (9)


Grant
Agency: Cordis | Branch: FP7 | Program: MC-ITN | Phase: FP7-PEOPLE-2012-ITN | Award Amount: 3.54M | Year: 2013

Neuroinflammatory disease, in particular multiple sclerosis affects more than 700.000 people within Europe alone. European countries are at the forefront of neuroimmunological research and students in medicine and biology are greatly attracted by the field. Neuroimmunology research further impacts our understanding of the ethiopathology of other CNS-disorders including Alzheimers Dementia and Morbus Parkinson. The ability of inflammatory immune cells to cause tissue damage within the nervous system is largely governed by soluble mediators including cytokines/chemokines, cytolytic molecules and growth factors. The therapeutic targeting of such mediators has proven successful for the treatment of a number of inflammatory diseases, yet is failing for the treatment of neuroinflammatory disorders. Clearly, the rules and regulatory elements, which govern inflammation and tissue injury within the CNS, differ significantly from those of other tissues and a unique CNS-focused research approach to unravel these rules is required. In this ITN proposal, we will train ESRs and ERs specifically in Neuroimmunology by combining prominent laboratories in academia and industry on the task to study the communication networks between immune and CNS-resident cells. Scientifically, we focus particularly on the soluble factors mediating cell-cell communication at the immune-CNS interface. To this end, we combine expertise in molecular and cellular Neuroimmunology with Neuropathology of human and animal models of CNS inflammation. In addition, our goal is to further utilize inflammatory processes for neuroprotection.


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), (200) and (200) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.


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.


The invention provides modulators for the orphan nuclear receptor ROR and methods for treating ROR mediated diseases by administrating these novel ROR 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.


Patent
Phenex Pharmaceuticals | Date: 2012-07-12

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.


The invention provides modulators for the orphan nuclear receptor ROR_() and methods for treating ROR_() mediated diseases by administrating these novel ROR_() modulators 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.


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.


Patent
Phenex Pharmaceuticals | Date: 2013-01-16

The present invention relates to compounds which 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.R is selected from the group consisting of COOR_(6), CONR_(7)R_(8), tetrazolyl, SO_(2)NR_(7)R_(8), C_(1-6) alkyl, SO_(2)-C_(1-6) alkyl and H, with R_(6) independently selected from the group consisting of H or C_(1-6) alkyl, and R_(7) and R_(8) independently from each other selected from the group consisting of H, C_(1-6) alkyl, halo-C_(1-6) alkyl, C_(1-6) alkylene-R_(9), SO_(2)-C_(1-6) alkyl, wherein R_(9) is selected from the group consisting of COOH, OH and SO_(3)H;A is selected from the group consisting of phenyl, pyridyl, pyrimidyl, pyrazolyl, indolyl, thienyl, benzothienyl, indazolyl, benzisoxazolyl, benzofuranyl, benzotriazolyl, furanyl, benzothiazolyl, thiazolyl, oxadiazolyl, each optionally substituted with one or two groups independently selected from the group consisting of OH, O-C_(1-6) alkyl, O-halo-C_(1-6) alkyl, C_(1-6) alkyl, halo-C_(1-6) alkyl, C_(3-6) cycloalkyl and halogen;Q is selected from the group consisting of phenyl, pyridyl, thiazolyl, thiophenyl, pyrimidyl, each optionally substituted with one or two groups independently selected from the group consisting of C_(1-6) alkyl, halo-C_(1-6) alkyl, halogen and CF_(3);Y is selected from N or CH;Z is selected fromX= CH, N, NO.


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

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