57 articles for thisTarget
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Article Title
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Synthesis of dihydroimidazole tethered imidazolinethiones and their activity as novel antagonists of the nuclear retinoic acid receptor-related orphan receptors (RORs).
Torrey Pines Institute For Molecular Studies
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists.
Galderma R & D
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.
Vitae Pharmaceuticals
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
Central Pharmaceutical Research Institute
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
The University of Tokyo
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Genentech
Discovery of novel pyrazole-containing benzamides as potent ROR¿ inverse agonists.
Biogen
Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure.
The University of Tokyo
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Genentech
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).
Genentech
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR¿)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
The University of Tokyo
Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors.
The University of Tokyo
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Genentech
Identification of New Nonsteroidal ROR? Ligands; Related Structure-Activity Relationships and Docking Studies.
Genfit
The evolution paths of some reprehensive scaffolds of ROR?t modulators, a perspective from medicinal chemistry.
Sun Yat-Sen University
Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-? (ROR?) Agonist for Use in Treating Cancer.
Lycera
AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Astrazeneca
Withanolide Derivative 2,3-Dihydro-3?-methoxy Withaferin-A Modulates the Circadian Clock via Interaction with RAR-Related Orphan Receptor ? (RORa).
National Institute of Advanced Industrial Science and Technology (Aist)
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Bristol-Myers Squibb
Tricyclic-Carbocyclic ROR?t Inverse Agonists-Discovery of BMS-986313.
Bristol Myers Squibb
Discovery of carboxyl-containing biaryl ureas as potent ROR?t inverse agonists.
Fudan University
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel ROR?t inverse agonists.
Bristol Myers Squibb
Azatricyclic Inverse Agonists of ROR?t That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
Tricyclic sulfones as potent, selective and efficacious ROR?t inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Bristol Myers Squibb
Novel Tricyclic Pyroglutamide Derivatives as Potent ROR?t Inverse Agonists Identified using a Virtual Screening Approach.
Bristol Myers Squibb
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists.
Bristol Myers Squibb
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.
Bristol Myers Squibb
Discovery of Second Generation ROR? Inhibitors Composed of an Azole Scaffold.
Kyoto Prefectural University of Medicine
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.
Genentech
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable ROR? Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.
Bristol-Myers Squibb
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions.
Advinus Therapeutics
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.
Astrazeneca
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Karo Pharma
Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (ROR?t) inhibitor, S18-000003.
Shionogi
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
The University of Tokyo
Identification of an aminothiazole series of ROR? modulators.
The Scripps Research Institute
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bristol-Myers Squibb
Potent and Orally Bioavailable Inverse Agonists of ROR?t Resulting from Structure-Based Design.
Astrazeneca
Optimizing a Weakly Binding Fragment into a Potent ROR?t Inverse Agonist with Efficacy in an in Vivo Inflammation Model.
TBA
Diversity-oriented fluorescence library approach (DOFLA) to the discovery of chymotrypsin sensor.
New York University
Synthesis of tetramic and tetronic acids as beta-secretase inhibitors.
Darmstadt Technical University