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Exploration of pyrrole derivatives to find an effective potassium-competitive acid blocker with moderately long-lasting suppression of gastric acid secretion.
Nishida H, Fujimori I, Arikawa Y, Hirase K, Ono K, Nakai K, Inatomi N, Hori Y, Matsukawa J, Fujioka Y, Imanishi A, Fukui H, Itoh F. Nishida H, et al. Among authors: matsukawa j. Bioorg Med Chem. 2017 Jul 1;25(13):3447-3460. doi: 10.1016/j.bmc.2017.04.034. Epub 2017 Apr 27. Bioorg Med Chem. 2017. PMID: 28483454
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: matsukawa j. 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
1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases.
Hori Y, Imanishi A, Matsukawa J, Tsukimi Y, Nishida H, Arikawa Y, Hirase K, Kajino M, Inatomi N. Hori Y, et al. Among authors: matsukawa j. J Pharmacol Exp Ther. 2010 Oct;335(1):231-8. doi: 10.1124/jpet.110.170274. Epub 2010 Jul 12. J Pharmacol Exp Ther. 2010. PMID: 20624992
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: matsukawa j. J Med Chem. 2012 May 10;55(9):4446-56. doi: 10.1021/jm300318t. Epub 2012 Apr 30. J Med Chem. 2012. PMID: 22512618
45 results