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Page 1
Discovery of 2-(6-{[(1R,2R)-2-hydroxycyclohexyl]amino}-4,5-dimethylpyridazin-3-yl)-5-(trifluoromethyl)phenol (ASP0965): A potent, orally active and brain-penetrable NLRP3 inflammasome inhibitor with a novel scaffold for the treatment of α-synucleinopathy.
Inagaki Y, Kamikubo T, Kuriwaki I, Watanabe J, Yamaki S, Iida M, Tomita K, Kakefuda K, Kurokawa J, Kiso T, Saba K, Koike T. Inagaki Y, et al. Among authors: kuriwaki i. Bioorg Med Chem. 2024 Dec 12;118:118042. doi: 10.1016/j.bmc.2024.118042. Online ahead of print. Bioorg Med Chem. 2024. PMID: 39742857
Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity.
Kuriwaki I, Kameda M, Iikubo K, Hisamichi H, Kawamoto Y, Kikuchi S, Moritomo H, Terasaka T, Iwai Y, Noda A, Tomiyama H, Kikuchi A, Hirano M. Kuriwaki I, et al. Bioorg Med Chem. 2022 Apr 1;59:116657. doi: 10.1016/j.bmc.2022.116657. Epub 2022 Feb 11. Bioorg Med Chem. 2022. PMID: 35219181
Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.
Kuriwaki I, Kameda M, Iikubo K, Hisamichi H, Kawamoto Y, Kikuchi S, Moritomo H, Kondoh Y, Terasaka T, Amano Y, Tateishi Y, Echizen Y, Iwai Y, Noda A, Tomiyama H, Nakazawa T, Hirano M. Kuriwaki I, et al. Bioorg Med Chem. 2021 Mar 1;33:116019. doi: 10.1016/j.bmc.2021.116019. Epub 2021 Jan 16. Bioorg Med Chem. 2021. PMID: 33486159