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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: goto m. 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: goto m. J Med Chem. 2011 Mar 10;54(5):1430-40. doi: 10.1021/jm101452x. Epub 2011 Feb 9. J Med Chem. 2011. PMID: 21306167