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Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Kono M, Ochida A, Oda T, Imada T, Banno Y, Taya N, Masada S, Kawamoto T, Yonemori K, Nara Y, Fukase Y, Yukawa T, Tokuhara H, Skene R, Sang BC, Hoffman ID, Snell GP, Uga K, Shibata A, Igaki K, Nakamura Y, Nakagawa H, Tsuchimori N, Yamasaki M, Shirai J, Yamamoto S. Kono M, et al. Among authors: sang bc. J Med Chem. 2018 Apr 12;61(7):2973-2988. doi: 10.1021/acs.jmedchem.8b00061. Epub 2018 Mar 14. J Med Chem. 2018. PMID: 29510038
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.
Yukawa T, Nara Y, Kono M, Sato A, Oda T, Takagi T, Sato T, Banno Y, Taya N, Imada T, Shiokawa Z, Negoro N, Kawamoto T, Koyama R, Uchiyama N, Skene R, Hoffman I, Chen CH, Sang B, Snell G, Katsuyama R, Yamamoto S, Shirai J. Yukawa T, et al. J Med Chem. 2019 Feb 14;62(3):1167-1179. doi: 10.1021/acs.jmedchem.8b01181. Epub 2019 Feb 4. J Med Chem. 2019. PMID: 30652849
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, Masada S, Kawamoto T, Yonemori K, Koyama R, Nakagawa H, Nakayama M, Uga K, Shibata A, Koga K, Okui T, Shirasaki M, Skene R, Sang B, Hoffman I, Lane W, Fujitani Y, Yamasaki M, Yamamoto S. Shirai J, et al. Bioorg Med Chem. 2018 Jan 15;26(2):483-500. doi: 10.1016/j.bmc.2017.12.006. Epub 2017 Dec 9. Bioorg Med Chem. 2018. PMID: 29262987
Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Fukase Y, Sato A, Tomata Y, Ochida A, Kono M, Yonemori K, Koga K, Okui T, Yamasaki M, Fujitani Y, Nakagawa H, Koyama R, Nakayama M, Skene R, Sang BC, Hoffman I, Shirai J, Yamamoto S. Fukase Y, et al. Among authors: sang bc. Bioorg Med Chem. 2018 Feb 1;26(3):721-736. doi: 10.1016/j.bmc.2017.12.039. Epub 2017 Dec 28. Bioorg Med Chem. 2018. PMID: 29342416
Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists.
Sato A, Fukase Y, Kono M, Ochida A, Oda T, Sasaki Y, Ishii N, Tomata Y, Fukumoto S, Imai YN, Uga K, Shibata A, Yamasaki M, Nakagawa H, Shirasaki M, Skene R, Hoffman I, Sang BC, Snell G, Shirai J, Yamamoto S. Sato A, et al. Among authors: sang bc. ChemMedChem. 2019 Nov 20;14(22):1917-1932. doi: 10.1002/cmdc.201900416. Epub 2019 Nov 5. ChemMedChem. 2019. PMID: 31659845
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
Okawa T, Aramaki Y, Yamamoto M, Kobayashi T, Fukumoto S, Toyoda Y, Henta T, Hata A, Ikeda S, Kaneko M, Hoffman ID, Sang BC, Zou H, Kawamoto T. Okawa T, et al. Among authors: sang bc. J Med Chem. 2017 Aug 24;60(16):6942-6990. doi: 10.1021/acs.jmedchem.7b00443. Epub 2017 Aug 3. J Med Chem. 2017. PMID: 28699740
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Fujimoto J, Kurasawa O, Takagi T, Liu X, Banno H, Kojima T, Asano Y, Nakamura A, Nambu T, Hata A, Ishii T, Sameshima T, Debori Y, Miyamoto M, Klein MG, Tjhen R, Sang BC, Levin I, Lane SW, Snell GP, Li K, Kefala G, Hoffman ID, Ding SC, Cary DR, Mizojiri R. Fujimoto J, et al. Among authors: sang bc. ACS Med Chem Lett. 2019 Sep 19;10(10):1498-1503. doi: 10.1021/acsmedchemlett.9b00400. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620240 Free PMC article.
A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR) γ agonists: design and synthesis of benzylpyrazole acylsulfonamides.
Rikimaru K, Wakabayashi T, Abe H, Imoto H, Maekawa T, Ujikawa O, Murase K, Matsuo T, Matsumoto M, Nomura C, Tsuge H, Arimura N, Kawakami K, Sakamoto J, Funami M, Mol CD, Snell GP, Bragstad KA, Sang BC, Dougan DR, Tanaka T, Katayama N, Horiguchi Y, Momose Y. Rikimaru K, et al. Among authors: sang bc. Bioorg Med Chem. 2012 Jan 15;20(2):714-33. doi: 10.1016/j.bmc.2011.12.008. Epub 2011 Dec 13. Bioorg Med Chem. 2012. PMID: 22209730
47 results