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603 results

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Page 1
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent.
Kurasawa O, Miyazaki T, Homma M, Oguro Y, Imada T, Uchiyama N, Iwai K, Yamamoto Y, Ohori M, Hara H, Sugimoto H, Iwata K, Skene R, Hoffman I, Ohashi A, Nomura T, Cho N. Kurasawa O, et al. Among authors: hoffman i. J Med Chem. 2020 Feb 13;63(3):1084-1104. doi: 10.1021/acs.jmedchem.9b01427. Epub 2020 Jan 14. J Med Chem. 2020. PMID: 31895562
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.
Kurasawa O, Oguro Y, Miyazaki T, Homma M, Mori K, Iwai K, Hara H, Skene R, Hoffman I, Ohashi A, Yoshida S, Ishikawa T, Cho N. Kurasawa O, et al. Among authors: hoffman i. Bioorg Med Chem. 2017 Apr 1;25(7):2133-2147. doi: 10.1016/j.bmc.2017.02.021. Epub 2017 Feb 16. Bioorg Med Chem. 2017. PMID: 28284870
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: hoffman i. 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 [ 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. 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
Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.
Keung W, Boloor A, Brown J, Kiryanov A, Gangloff A, Lawson JD, Skene R, Hoffman I, Atienza J, Kahana J, De Jong R, Farrell P, Balakrishna D, Halkowycz P. Keung W, et al. Among authors: hoffman i. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1099-1104. doi: 10.1016/j.bmcl.2016.12.024. Epub 2016 Dec 20. Bioorg Med Chem Lett. 2017. PMID: 28082036
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: hoffman i. 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: hoffman i. 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
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: hoffman i. 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
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
Mikami S, Nakamura S, Ashizawa T, Nomura I, Kawasaki M, Sasaki S, Oki H, Kokubo H, Hoffman ID, Zou H, Uchiyama N, Nakashima K, Kamiguchi N, Imada H, Suzuki N, Iwashita H, Taniguchi T. Mikami S, et al. Among authors: hoffman id. J Med Chem. 2017 Sep 28;60(18):7677-7702. doi: 10.1021/acs.jmedchem.7b00807. Epub 2017 Sep 5. J Med Chem. 2017. PMID: 28796496
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: hoffman id. 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.
603 results