PMID

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Article Title

Organization

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 biaryls as ROR¿ inverse agonists by using structure-based design.

Biogen

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

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.

Genentech

Discovery of biaryl carboxylamides as potent ROR¿ inverse agonists.

Biogen Idec

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

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Genentech

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

A reversed sulfonamide series of selective RORc inverse agonists.

Argenta Discovery

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

Identification of tertiary sulfonamides as RORc inverse agonists.

Genentech

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

Discovery of Biaryl Amide Derivatives as Potent, Selective, and Orally Bioavailable RORγt Agonists for Cancer Immunotherapy.

Fudan University

Discovery and Characterization of Benzimidazole Derivative XY123 as a Potent, Selective, and Orally Available RORγ Inverse Agonist.

Guangzhou Medical University

Discovery of Chromane-6-Sulfonamide Derivative as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.

Jiangsu Carefree Pharmaceutical Co.

Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists.

Pfizer

The evolution paths of some reprehensive scaffolds of RORγt modulators, a perspective from medicinal chemistry.

Sun Yat-Sen University

Defining Target Engagement Required for Efficacy

Lilly Research Laboratories

Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) 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

Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.

Bristol Myers Squibb

Discovery of carboxyl-containing biaryl ureas as potent RORγt 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 RORγt inverse agonists.

Bristol Myers Squibb

Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.

Bristol Myers Squibb

Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.

Bristol Myers Squibb

Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach.

Bristol Myers Squibb

Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (RORγt) agonists.

Bristol Myers Squibb

Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.

Phenex Pharmaceuticals

Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.

Phenex Pharmaceuticals

Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.

Bristol Myers Squibb

Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.

Genentech

Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists.

Bristol-Myers Squibb

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.

Bristol-Myers Squibb

Structure-Based and Property-Driven Optimization of

Global Discovery Chemistry

Identification of potent RORβ modulators: Scaffold variation.

The Scripps Research Institute

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 (RORγt) inhibitor, S18-000003.

Shionogi

Identification of an aminothiazole series of RORβ modulators.

The Scripps Research Institute

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/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 RORγt Resulting from Structure-Based Design.

Astrazeneca

Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.

The University of Tokyo

Identification and biological evaluation of thiazole-based inverse agonists of RORγt.

Phenex Pharmaceuticals

Pyrimidinone derivatives as SHP2 antagonists

Merck Patent

Imidazopyridazine compounds

Hoffmann-La Roche