Search Results - "Kono, Mitsunori"
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Discovery of the First Potent and Orally Available Agonist of the Orphan G‑Protein-Coupled Receptor 52
Published in Journal of medicinal chemistry (26-06-2014)“…G-protein-coupled receptor 52 (GPR52) is an orphan Gs-coupled G-protein-coupled receptor. GPR52 inhibits dopamine D2 receptor signaling and activates dopamine…”
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Pharmacological inhibitory profile of TAK-828F, a potent and selective orally available RORγt inverse agonist
Published in Biochemical pharmacology (01-04-2018)“…[Display omitted] Retinoic acid-related orphan receptor γt (RORγt) is a key master regulator of the differentiation and activation of IL-17 producing CD4+…”
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Discovery of [cis-3-({(5R)‑5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro‑1H‑inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5H)‑yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist
Published in Journal of medicinal chemistry (12-04-2018)“…A series of tetrahydronaphthyridine derivatives as novel RORγt inverse agonists were designed and synthesized. We reduced the lipophilicity of…”
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Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist
Published in Journal of medicinal chemistry (14-02-2019)“…Retinoic acid receptor-related orphan receptor γt (RORγt) agonists are expected to provide a novel class of immune-activating anticancer drugs via activation…”
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Identification of novel quinazolinedione derivatives as RORγt inverse agonist
Published in Bioorganic & medicinal chemistry (01-02-2018)“…[Display omitted] Novel small molecules were synthesized and evaluated as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for…”
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Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives
Published in Bioorganic & medicinal chemistry (15-01-2018)“…[Display omitted] A series of tetrahydroisoquinoline derivatives were designed, synthesized, and evaluated for their potential as novel orally efficacious…”
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Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
Published in Bioorganic & medicinal chemistry (15-01-2018)“…[Display omitted] A series of novel phenylglycinamides as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists were discovered…”
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Biochemical Properties of TAK-828F, a Potent and Selective Retinoid-Related Orphan Receptor Gamma t Inverse Agonist
Published in Pharmacology (01-11-2018)“…Retinoid-related orphan receptor gamma t (RORγt) is a master regulator of T helper 17 cells that plays a pivotal role in the production of inflammatory…”
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Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors
Published in Bioorganic & medicinal chemistry (01-01-2013)“…A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH)…”
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Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists
Published in ChemMedChem (20-11-2019)“…Retinoic‐acid‐related orphan receptor γt (RORγt) inverse agonists could be used for the treatment of autoimmune diseases. Previously, we reported a novel…”
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Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors
Published in Bioorganic & medicinal chemistry (15-02-2014)“…A series of piperazine ureas were designed, synthesized, and evaluated for their potential as novel orally efficacious fatty acid amide hydrolase (FAAH)…”
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Discovery of a 7-arylaminobenzimidazole series as novel CRF1 receptor antagonists
Published in Bioorganic & medicinal chemistry (01-10-2016)“…[Display omitted] A promising lead compound 1 of a benzimidazole series has been identified as a corticotropin-releasing factor 1 (CRF1) receptor antagonist…”
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