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Novel and potent calcium-sensing receptor antagonists: discovery of (5R)-N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide monotosylate (TAK-075) as an orally active bone anabolic agent.
Yoshida M, Mori A, Morimoto S, Kotani E, Oka M, Notoya K, Makino H, Ono M, Shirasaki M, Tada N, Fujita H, Ban J, Ikeda Y, Kawamoto T, Goto M, Kimura H, Baba A, Yasuma T. Yoshida M, et al. Among authors: fujita h. Bioorg Med Chem. 2011 Mar 15;19(6):1881-94. doi: 10.1016/j.bmc.2011.02.001. Epub 2011 Feb 24. Bioorg Med Chem. 2011. PMID: 21353570
Discovery of novel and potent orally active calcium-sensing receptor antagonists that stimulate pulselike parathyroid hormone secretion: synthesis and structure-activity relationships of tetrahydropyrazolopyrimidine derivatives.
Yoshida M, Mori A, Kotani E, Oka M, Makino H, Fujita H, Ban J, Ikeda Y, Kawamoto T, Goto M, Kimura H, Baba A, Yasuma T. Yoshida M, et al. Among authors: fujita h. J Med Chem. 2011 Mar 10;54(5):1430-40. doi: 10.1021/jm101452x. Epub 2011 Feb 9. J Med Chem. 2011. PMID: 21306167
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.
Sakauchi N, Kohara Y, Sato A, Suzaki T, Imai Y, Okabe Y, Imai S, Saikawa R, Nagabukuro H, Kuno H, Fujita H, Kamo I, Yoshida M. Sakauchi N, et al. Among authors: fujita h. J Med Chem. 2016 Apr 14;59(7):2989-3002. doi: 10.1021/acs.jmedchem.5b01528. Epub 2016 Mar 17. J Med Chem. 2016. PMID: 26954848
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.
Asano M, Hitaka T, Imada T, Yamada M, Morimoto M, Shinohara H, Hara T, Yamaoka M, Santou T, Nakayama M, Imai Y, Habuka N, Yano J, Wilson K, Fujita H, Hasuoka A. Asano M, et al. Among authors: fujita h. Bioorg Med Chem Lett. 2017 May 1;27(9):1897-1901. doi: 10.1016/j.bmcl.2017.03.038. Epub 2017 Mar 21. Bioorg Med Chem Lett. 2017. PMID: 28363748
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
Aikawa K, Asano M, Ono K, Habuka N, Yano J, Wilson K, Fujita H, Kandori H, Hara T, Morimoto M, Santou T, Yamaoka M, Nakayama M, Hasuoka A. Aikawa K, et al. Among authors: fujita h. Bioorg Med Chem. 2017 Jul 1;25(13):3330-3349. doi: 10.1016/j.bmc.2017.04.018. Epub 2017 Apr 13. Bioorg Med Chem. 2017. PMID: 28454849
Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
Kanematsu-Yamaki Y, Nishizawa N, Kaisho T, Nagai H, Mochida T, Asakawa T, Inooka H, Dote K, Fujita H, Matsumiya K, Hirabayashi H, Sakamoto J, Ohtaki T, Takekawa S, Asami T. Kanematsu-Yamaki Y, et al. Among authors: fujita h. J Med Chem. 2017 Jul 27;60(14):6089-6097. doi: 10.1021/acs.jmedchem.7b00330. Epub 2017 Jul 18. J Med Chem. 2017. PMID: 28657315
A potent neuromedin U receptor 2-selective alkylated peptide.
Nishizawa N, Kanematsu-Yamaki Y, Funata M, Nagai H, Shimizu A, Fujita H, Sakamoto J, Takekawa S, Asami T. Nishizawa N, et al. Among authors: fujita h. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4626-4629. doi: 10.1016/j.bmcl.2017.09.019. Epub 2017 Sep 9. Bioorg Med Chem Lett. 2017. PMID: 28935264
4,088 results