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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: iwashita 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.
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: iwashita 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
A novel glycogen synthase kinase-3 inhibitor 2-methyl-5-(3-{4-[(S )-methylsulfinyl]phenyl}-1-benzofuran-5-yl)-1,3,4-oxadiazole decreases tau phosphorylation and ameliorates cognitive deficits in a transgenic model of Alzheimer's disease.
Onishi T, Iwashita H, Uno Y, Kunitomo J, Saitoh M, Kimura E, Fujita H, Uchiyama N, Kori M, Takizawa M. Onishi T, et al. Among authors: iwashita h. J Neurochem. 2011 Dec;119(6):1330-40. doi: 10.1111/j.1471-4159.2011.07532.x. Epub 2011 Nov 2. J Neurochem. 2011. PMID: 21992552 Free article.
2-{3-[4-(Alkylsulfinyl)phenyl]-1-benzofuran-5-yl}-5-methyl-1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta with good brain permeability.
Saitoh M, Kunitomo J, Kimura E, Iwashita H, Uno Y, Onishi T, Uchiyama N, Kawamoto T, Tanaka T, Mol CD, Dougan DR, Textor GP, Snell GP, Takizawa M, Itoh F, Kori M. Saitoh M, et al. Among authors: iwashita h. J Med Chem. 2009 Oct 22;52(20):6270-86. doi: 10.1021/jm900647e. J Med Chem. 2009. PMID: 19775160
228 results