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Page 1
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: tokuhara h. 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 [ 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: tokuhara h. 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
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Tokuhara H, Imaeda Y, Fukase Y, Iwanaga K, Taya N, Watanabe K, Kanagawa R, Matsuda K, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T. Tokuhara H, et al. Bioorg Med Chem. 2018 Jul 23;26(12):3261-3286. doi: 10.1016/j.bmc.2018.04.051. Epub 2018 Apr 27. Bioorg Med Chem. 2018. PMID: 29754833
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.
Imaeda Y, Tokuhara H, Fukase Y, Kanagawa R, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T. Imaeda Y, et al. Among authors: tokuhara h. ACS Med Chem Lett. 2016 Sep 12;7(10):933-938. doi: 10.1021/acsmedchemlett.6b00251. eCollection 2016 Oct 13. ACS Med Chem Lett. 2016. PMID: 27774132 Free PMC article.
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.
Sasaki Y, Tokuhara H, Ohba Y, Okabe A, Nakayama M, Nakagawa H, Skene R, Hoffman I, Zou H, Yoshida M. Sasaki Y, et al. Among authors: tokuhara h. Bioorg Med Chem Lett. 2020 Mar 1;30(5):126963. doi: 10.1016/j.bmcl.2020.126963. Epub 2020 Jan 13. Bioorg Med Chem Lett. 2020. PMID: 31980341
Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl Moiety.
Ikeda S, Sugiyama H, Tokuhara H, Murakami M, Nakamura M, Oguro Y, Aida J, Morishita N, Sogabe S, Dougan DR, Gay SC, Qin L, Arimura N, Takahashi Y, Sasaki M, Kamada Y, Aoyama K, Kimoto K, Kamata M. Ikeda S, et al. Among authors: tokuhara h. J Med Chem. 2021 Aug 12;64(15):11014-11044. doi: 10.1021/acs.jmedchem.1c00432. Epub 2021 Jul 30. J Med Chem. 2021. PMID: 34328319
Antimalarial activity of 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251) and its carboxylic acid derivatives.
Sato A, Kawai S, Hiramoto A, Morita M, Tanigawa N, Nakase Y, Komichi Y, Matsumoto M, Hiraoka O, Hiramoto K, Tokuhara H, Masuyama A, Nojima M, Higaki K, Hayatsu H, Wataya Y, Kim HS. Sato A, et al. Among authors: tokuhara h. Parasitol Int. 2011 Dec;60(4):488-92. doi: 10.1016/j.parint.2011.08.017. Epub 2011 Sep 8. Parasitol Int. 2011. PMID: 21924377
New approaches to the synthesis of spiro-peroxylactones.
McCullough KJ, Tokuhara H, Masuyama A, Nojima M. McCullough KJ, et al. Among authors: tokuhara h. Org Biomol Chem. 2003 May 7;1(9):1522-7. doi: 10.1039/b300342f. Org Biomol Chem. 2003. PMID: 12926282