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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: kawamoto 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 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: kawamoto t. 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
Discovery of 3,5-Diphenyl-4-methyl-1,3-oxazolidin-2-ones as Novel, Potent, and Orally Available Δ-5 Desaturase (D5D) Inhibitors.
Fujimoto J, Okamoto R, Noguchi N, Hara R, Masada S, Kawamoto T, Nagase H, Tamura YO, Imanishi M, Takagahara S, Kubo K, Tohyama K, Iida K, Andou T, Miyahisa I, Matsui J, Hayashi R, Maekawa T, Matsunaga N. Fujimoto J, et al. Among authors: kawamoto t. J Med Chem. 2017 Nov 9;60(21):8963-8981. doi: 10.1021/acs.jmedchem.7b01210. Epub 2017 Oct 31. J Med Chem. 2017. PMID: 29023121
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: kawamoto 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
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. Among authors: kawamoto t. 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
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. Among authors: kawamoto t. 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 TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.
Fujimoto T, Rikimaru K, Fukuda K, Sugimoto H, Masuda K, Ohyabu N, Banno Y, Tokunaga N, Kawamoto T, Tomata Y, Kumagai Y, Iida M, Nagano Y, Yoneyama-Hirozane M, Shimizu Y, Sasa K, Ishikawa T, Yukitake H, Ito M, Aoyama K, Matsumoto T. Fujimoto T, et al. Among authors: kawamoto t. ACS Med Chem Lett. 2022 Feb 4;13(3):457-462. doi: 10.1021/acsmedchemlett.1c00626. eCollection 2022 Mar 10. ACS Med Chem Lett. 2022. PMID: 35295087 Free PMC article.
Discovery of a novel series of medium-sized cyclic enteropeptidase inhibitors.
Kikuchi F, Ikeda Z, Kakegawa K, Nishikawa Y, Sasaki S, Fukuda K, Takami K, Banno Y, Nishikawa H, Taya N, Nakahata T, Itono S, Yashiro H, Tsuchimori K, Hiyoshi H, Sasaki M, Tohyama K, Matsumiya K, Ishihara Y, Kawamoto T, Kamaura M, Watanabe M, Kitazaki T, Maekawa T, Sasaki M. Kikuchi F, et al. Among authors: kawamoto t. Bioorg Med Chem. 2023 Oct 1;93:117462. doi: 10.1016/j.bmc.2023.117462. Epub 2023 Aug 29. Bioorg Med Chem. 2023. PMID: 37683572 Free article.
1,720 results