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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: taniguchi t. 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: taniguchi t. 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: taniguchi t. Chem Pharm Bull (Tokyo). 2017;65(11):1058-1077. doi: 10.1248/cpb.c17-00564. Chem Pharm Bull (Tokyo). 2017. PMID: 29093293 Free article.
Development of a series of novel carbon-11 labeled PDE10A inhibitors.
Stepanov V, Miura S, Takano A, Amini N, Nakao R, Hasui T, Nakashima K, Taniguchi T, Kimura H, Kuroita T, Halldin C. Stepanov V, et al. Among authors: taniguchi t. J Labelled Comp Radiopharm. 2015 May 15;58(5):202-8. doi: 10.1002/jlcr.3284. Epub 2015 Apr 19. J Labelled Comp Radiopharm. 2015. PMID: 25891816
4,534 results