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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: skene r. 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 and characterization of novel allosteric FAK inhibitors.
Iwatani M, Iwata H, Okabe A, Skene RJ, Tomita N, Hayashi Y, Aramaki Y, Hosfield DJ, Hori A, Baba A, Miki H. Iwatani M, et al. Eur J Med Chem. 2013 Mar;61:49-60. doi: 10.1016/j.ejmech.2012.06.035. Epub 2012 Jun 26. Eur J Med Chem. 2013. PMID: 22819505
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: skene r. 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, 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: skene r. 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
42 results