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Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor.
Kunitomo J, Yoshikawa M, Fushimi M, Kawada A, Quinn JF, Oki H, Kokubo H, Kondo M, Nakashima K, Kamiguchi N, Suzuki K, Kimura H, Taniguchi T. Kunitomo J, et al. Among authors: oki h. J Med Chem. 2014 Nov 26;57(22):9627-43. doi: 10.1021/jm5013648. Epub 2014 Nov 10. J Med Chem. 2014. PMID: 25384088
Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Hattori Y, Matsumoto S, Morimoto S, Daini M, Toyofuku M, Matsuda S, Baba R, Murakami K, Iwatani M, Oki H, Iwasaki S, Matsumiya K, Tominari Y, Kimura H, Ito M. Hattori Y, et al. Among authors: oki h. Eur J Med Chem. 2022 Sep 5;239:114522. doi: 10.1016/j.ejmech.2022.114522. Epub 2022 Jun 7. Eur J Med Chem. 2022. PMID: 35749987 Free article.
T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice.
Matsuda S, Baba R, Oki H, Morimoto S, Toyofuku M, Igaki S, Kamada Y, Iwasaki S, Matsumiya K, Hibino R, Kamada H, Hirakawa T, Iwatani M, Tsuchida K, Hara R, Ito M, Kimura H. Matsuda S, et al. Among authors: oki h. Neuropsychopharmacology. 2019 Jul;44(8):1505-1512. doi: 10.1038/s41386-018-0300-9. Epub 2018 Dec 22. Neuropsychopharmacology. 2019. PMID: 30580376 Free PMC article.
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
Nara H, Kaieda A, Sato K, Naito T, Mototani H, Oki H, Yamamoto Y, Kuno H, Santou T, Kanzaki N, Terauchi J, Uchikawa O, Kori M. Nara H, et al. Among authors: oki h. J Med Chem. 2017 Jan 26;60(2):608-626. doi: 10.1021/acs.jmedchem.6b01007. Epub 2017 Jan 9. J Med Chem. 2017. PMID: 27966948
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Nara H, Sato K, Naito T, Mototani H, Oki H, Yamamoto Y, Kuno H, Santou T, Kanzaki N, Terauchi J, Uchikawa O, Kori M. Nara H, et al. Among authors: oki h. J Med Chem. 2014 Nov 13;57(21):8886-902. doi: 10.1021/jm500981k. Epub 2014 Oct 15. J Med Chem. 2014. PMID: 25264600
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
Nara H, Sato K, Naito T, Mototani H, Oki H, Yamamoto Y, Kuno H, Santou T, Kanzaki N, Terauchi J, Uchikawa O, Kori M. Nara H, et al. Among authors: oki h. Bioorg Med Chem. 2014 Oct 1;22(19):5487-505. doi: 10.1016/j.bmc.2014.07.025. Epub 2014 Aug 7. Bioorg Med Chem. 2014. PMID: 25192810
202 results