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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: kondo m. 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 a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB).
Arikawa Y, Nishida H, Kurasawa O, Hasuoka A, Hirase K, Inatomi N, Hori Y, Matsukawa J, Imanishi A, Kondo M, Tarui N, Hamada T, Takagi T, Takeuchi T, Kajino M. Arikawa Y, et al. Among authors: kondo m. J Med Chem. 2012 May 10;55(9):4446-56. doi: 10.1021/jm300318t. Epub 2012 Apr 30. J Med Chem. 2012. PMID: 22512618
Novel approach of fragment-based lead discovery applied to renin inhibitors.
Tawada M, Suzuki S, Imaeda Y, Oki H, Snell G, Behnke CA, Kondo M, Tarui N, Tanaka T, Kuroita T, Tomimoto M. Tawada M, et al. Among authors: kondo m. Bioorg Med Chem. 2016 Nov 15;24(22):6066-6074. doi: 10.1016/j.bmc.2016.09.065. Epub 2016 Sep 28. Bioorg Med Chem. 2016. PMID: 27720325
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.
Imaeda Y, Tokuhara H, Fukase Y, Kanagawa R, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T. Imaeda Y, et al. Among authors: kondo m. ACS Med Chem Lett. 2016 Sep 12;7(10):933-938. doi: 10.1021/acsmedchemlett.6b00251. eCollection 2016 Oct 13. ACS Med Chem Lett. 2016. PMID: 27774132 Free PMC article.
Discovery, synthesis, and structure-activity relations of 3,4-dihydro-1H-spiro(naphthalene-2,2'-piperidin)-1-ones as potassium-competitive acid blockers.
Imaeda T, Ono K, Nakai K, Hori Y, Matsukawa J, Takagi T, Fujioka Y, Tarui N, Kondo M, Imanishi A, Inatomi N, Kajino M, Itoh F, Nishida H. Imaeda T, et al. Among authors: kondo m. Bioorg Med Chem. 2017 Jul 15;25(14):3719-3735. doi: 10.1016/j.bmc.2017.05.012. Epub 2017 May 6. Bioorg Med Chem. 2017. PMID: 28522264
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Tokuhara H, Imaeda Y, Fukase Y, Iwanaga K, Taya N, Watanabe K, Kanagawa R, Matsuda K, Kajimoto Y, Kusumoto K, Kondo M, Snell G, Behnke CA, Kuroita T. Tokuhara H, et al. Among authors: kondo m. Bioorg Med Chem. 2018 Jul 23;26(12):3261-3286. doi: 10.1016/j.bmc.2018.04.051. Epub 2018 Apr 27. Bioorg Med Chem. 2018. PMID: 29754833
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: kondo m. 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 a Novel Series of Potent, Selective, Orally Available, and Brain-Penetrable C1s Inhibitors for Modulation of the Complement Pathway.
Ikeda Z, Kamei T, Sasaki Y, Reynolds M, Sakai N, Yoshikawa M, Tawada M, Morishita N, Dougan DR, Chen CH, Levin I, Zou H, Kuno M, Arimura N, Kikukawa Y, Kondo M, Tohyama K, Sato K. Ikeda Z, et al. Among authors: kondo m. J Med Chem. 2023 May 11;66(9):6354-6371. doi: 10.1021/acs.jmedchem.3c00348. Epub 2023 Apr 25. J Med Chem. 2023. PMID: 37120845 Free PMC article.
4,464 results