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Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.
Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M, Sameshima T, Araki S, Endo S, Kawamoto T, Morin GB, Aparicio SA, Nakanishi A, Maezaki H, Imaeda Y. Ito M, et al. Among authors: kokubo h. J Med Chem. 2018 Sep 13;61(17):7710-7728. doi: 10.1021/acs.jmedchem.8b00683. Epub 2018 Aug 20. J Med Chem. 2018. PMID: 30067358
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: kokubo 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
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: kokubo h. 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
Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from 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), for the Treatment of Cognitive Disorders.
Mikami S, Kawasaki M, Ikeda S, Negoro N, Nakamura S, Nomura I, Ashizawa T, Kokubo H, Hoffman ID, Zou H, Oki H, Uchiyama N, Hiura Y, Miyamoto M, Itou Y, Nakashima M, Iwashita H, Taniguchi T. Mikami S, et al. Among authors: kokubo h. Chem Pharm Bull (Tokyo). 2017;65(11):1058-1077. doi: 10.1248/cpb.c17-00564. Chem Pharm Bull (Tokyo). 2017. PMID: 29093293 Free article.
143 results