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Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxyhexanamides to reduce a cardiac safety issue: discovery of DS-8108b, an orally active renin inhibitor.
Nakamura Y, Fujimoto T, Ogawa Y, Namiki H, Suzuki S, Asano M, Sugita C, Mochizuki A, Miyazaki S, Tamaki K, Nagai Y, Inoue S, Nagayama T, Kato M, Chiba K, Takasuna K, Nishi T. Nakamura Y, et al. Among authors: nagayama t. Bioorg Med Chem. 2013 Jun 1;21(11):3175-96. doi: 10.1016/j.bmc.2013.03.022. Epub 2013 Mar 26. Bioorg Med Chem. 2013. PMID: 23598247
Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors.
Mori Y, Ogawa Y, Mochizuki A, Nakamura Y, Sugita C, Miyazaki S, Tamaki K, Matsui Y, Takahashi M, Nagayama T, Nagai Y, Inoue S, Nishi T. Mori Y, et al. Among authors: nagayama t. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7677-82. doi: 10.1016/j.bmcl.2012.09.103. Epub 2012 Oct 17. Bioorg Med Chem Lett. 2012. PMID: 23122821
Synthesis and optimization of novel (3S,5R)-5-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)piperidine-3-carboxamides as orally active renin inhibitors.
Mori Y, Ogawa Y, Mochizuki A, Nakamura Y, Fujimoto T, Sugita C, Miyazaki S, Tamaki K, Nagayama T, Nagai Y, Inoue S, Chiba K, Nishi T. Mori Y, et al. Among authors: nagayama t. Bioorg Med Chem. 2013 Sep 15;21(18):5907-22. doi: 10.1016/j.bmc.2013.06.057. Epub 2013 Jul 2. Bioorg Med Chem. 2013. PMID: 23886807
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.
Nakamura Y, Fujimoto T, Ogawa Y, Sugita C, Miyazaki S, Tamaki K, Takahashi M, Matsui Y, Nagayama T, Manabe K, Mizuno M, Masubuchi N, Chiba K, Nishi T. Nakamura Y, et al. Among authors: nagayama t. ACS Med Chem Lett. 2012 Aug 18;3(9):754-8. doi: 10.1021/ml300168e. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900544 Free PMC article.
Pharmacokinetic and Pharmacodynamic Profiles of Glyco-Modified Atrial Natriuretic Peptide Derivatives Synthesized Using Chemo-enzymatic Synthesis Approaches.
Iwamoto M, Yamaguchi T, Sekiguchi Y, Oishi S, Shiiki T, Soma M, Nakamura K, Yoshida M, Chaya H, Mori Y, Miyauchi R, Hasegawa J, Nagayama T, Honda T. Iwamoto M, et al. Among authors: nagayama t. Bioconjug Chem. 2018 Aug 15;29(8):2829-2837. doi: 10.1021/acs.bioconjchem.8b00427. Epub 2018 Aug 3. Bioconjug Chem. 2018. PMID: 30107743
512 results