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Page 1
Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden.
Anan K, Iso Y, Oguma T, Nakahara K, Suzuki S, Yamamoto T, Matsuoka E, Ito H, Sakaguchi G, Ando S, Morimoto K, Kanegawa N, Kido Y, Kawachi T, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Austin N, Van Den Bergh A, Verboven P, Bischoff F, Gijsen HJM, Yamano Y, Kusakabe K. Anan K, et al. Among authors: sakaguchi g. ChemMedChem. 2019 Nov 20;14(22):1894-1910. doi: 10.1002/cmdc.201900478. Epub 2019 Nov 12. ChemMedChem. 2019. PMID: 31657130
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
Koriyama Y, Hori A, Ito H, Yonezawa S, Baba Y, Tanimoto N, Ueno T, Yamamoto S, Yamamoto T, Asada N, Morimoto K, Einaru S, Sakai K, Kanazu T, Matsuda A, Yamaguchi Y, Oguma T, Timmers M, Tritsmans L, Kusakabe KI, Kato A, Sakaguchi G. Koriyama Y, et al. Among authors: sakaguchi g. J Med Chem. 2021 Feb 25;64(4):1873-1888. doi: 10.1021/acs.jmedchem.0c01917. Epub 2021 Feb 15. J Med Chem. 2021. PMID: 33588527 Clinical Trial.
Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.
Fuchino K, Mitsuoka Y, Masui M, Kurose N, Yoshida S, Komano K, Yamamoto T, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Miyajima H, Hiroyama S, Koyabu K, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Fuchino K, et al. Among authors: sakaguchi g. J Med Chem. 2018 Jun 28;61(12):5122-5137. doi: 10.1021/acs.jmedchem.8b00002. Epub 2018 May 23. J Med Chem. 2018. PMID: 29733614
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.
Nakahara K, Fuchino K, Komano K, Asada N, Tadano G, Hasegawa T, Yamamoto T, Sako Y, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Nakahara K, et al. Among authors: sakaguchi g. J Med Chem. 2018 Jul 12;61(13):5525-5546. doi: 10.1021/acs.jmedchem.8b00011. Epub 2018 Jun 14. J Med Chem. 2018. PMID: 29775538
Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Tadano G, Komano K, Yoshida S, Suzuki S, Nakahara K, Fuchino K, Fujimoto K, Matsuoka E, Yamamoto T, Asada N, Ito H, Sakaguchi G, Kanegawa N, Kido Y, Ando S, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Van Den Bergh A, Austin N, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Tadano G, et al. Among authors: sakaguchi g. J Med Chem. 2019 Oct 24;62(20):9331-9337. doi: 10.1021/acs.jmedchem.9b01140. Epub 2019 Oct 8. J Med Chem. 2019. PMID: 31549838
Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1.
Tsuno N, Yukimasa A, Yoshida O, Ichihashi Y, Inoue T, Ueno T, Yamaguchi H, Matsuda H, Funaki S, Yamanada N, Tanimura M, Nagamatsu D, Nishimura Y, Ito T, Soga M, Horita N, Yamamoto M, Hinata M, Imai M, Morioka Y, Kanemasa T, Sakaguchi G, Iso Y. Tsuno N, et al. Among authors: sakaguchi g. Bioorg Med Chem Lett. 2016 Oct 15;26(20):4930-4935. doi: 10.1016/j.bmcl.2016.09.013. Epub 2016 Sep 7. Bioorg Med Chem Lett. 2016. PMID: 27637151
Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2.
Tsuno N, Yukimasa A, Yoshida O, Suzuki S, Nakai H, Ogawa T, Fujiu M, Takaya K, Nozu A, Yamaguchi H, Matsuda H, Funaki S, Nishimura Y, Ito T, Nagamatsu D, Asaki T, Horita N, Yamamoto M, Hinata M, Soga M, Imai M, Morioka Y, Kanemasa T, Sakaguchi G, Iso Y. Tsuno N, et al. Among authors: sakaguchi g. Bioorg Med Chem Lett. 2016 Oct 15;26(20):4936-4941. doi: 10.1016/j.bmcl.2016.09.014. Epub 2016 Sep 7. Bioorg Med Chem Lett. 2016. PMID: 27634196
Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain.
Tsuno N, Yukimasa A, Yoshida O, Suzuki S, Nakai H, Ogawa T, Fujiu M, Takaya K, Nozu A, Yamaguchi H, Matsuda H, Funaki S, Yamanada N, Tanimura M, Nagamatsu D, Asaki T, Horita N, Yamamoto M, Hinata M, Soga M, Imai M, Morioka Y, Kanemasa T, Sakaguchi G, Iso Y. Tsuno N, et al. Among authors: sakaguchi g. Bioorg Med Chem. 2017 Apr 1;25(7):2177-2190. doi: 10.1016/j.bmc.2017.02.047. Epub 2017 Mar 1. Bioorg Med Chem. 2017. PMID: 28284871
BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice.
Nishitomi K, Sakaguchi G, Horikoshi Y, Gray AJ, Maeda M, Hirata-Fukae C, Becker AG, Hosono M, Sakaguchi I, Minami SS, Nakajima Y, Li HF, Takeyama C, Kihara T, Ota A, Wong PC, Aisen PS, Kato A, Kinoshita N, Matsuoka Y. Nishitomi K, et al. Among authors: sakaguchi g, sakaguchi i. J Neurochem. 2006 Dec;99(6):1555-63. doi: 10.1111/j.1471-4159.2006.04178.x. Epub 2006 Nov 2. J Neurochem. 2006. PMID: 17083447 Free article.
Destruxin E decreases Beta-amyloid generation by reducing colocalization of beta-amyloid-cleaving enzyme 1 and beta-amyloid protein precursor.
Itoh N, Okochi M, Tagami S, Nishitomi K, Nakayama T, Yanagida K, Fukumori A, Jiang J, Mori K, Hosono M, Kikuchi J, Nakano Y, Takinami Y, Dohi K, Nishigaki A, Takemoto H, Minagawa K, Katoh T, Willem M, Haass C, Morihara T, Tanaka T, Kudo T, Hasegawa H, Nishimura M, Sakaguchi G, Kato A, Takeda M. Itoh N, et al. Among authors: sakaguchi g. Neurodegener Dis. 2009;6(5-6):230-9. doi: 10.1159/000236902. Epub 2009 Sep 9. Neurodegener Dis. 2009. PMID: 19738368
299 results