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Page 1
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: yukawa t. 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 a novel series of peripheral-selective noradrenaline reuptake inhibitor.
Fujimori I, Yukawa T, Kamei T, Nakada Y, Sakauchi N, Yamada M, Ohba Y, Takiguchi M, Kuno M, Kamo I, Nakagawa H, Hamada T, Igari T, Okuda T, Yamamoto S, Tsukamoto T, Ishichi Y, Ueno H. Fujimori I, et al. Among authors: yukawa t. Bioorg Med Chem. 2015 Aug 1;23(15):5000-5014. doi: 10.1016/j.bmc.2015.05.017. Epub 2015 May 15. Bioorg Med Chem. 2015. PMID: 26051602
Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives.
Kono M, Oda T, Tawada M, Imada T, Banno Y, Taya N, Kawamoto T, Tokuhara H, Tomata Y, Ishii N, Ochida A, Fukase Y, Yukawa T, Fukumoto S, Watanabe H, Uga K, Shibata A, Nakagawa H, Shirasaki M, Fujitani Y, Yamasaki M, Shirai J, Yamamoto S. Kono M, et al. Among authors: yukawa t. Bioorg Med Chem. 2018 Jan 15;26(2):470-482. doi: 10.1016/j.bmc.2017.12.008. Epub 2017 Dec 11. Bioorg Med Chem. 2018. PMID: 29258712
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
239 results