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Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Chen C, et al. Among authors: huang cq. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. J Med Chem. 2008. PMID: 19006286
Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.
Chen C, Wilcoxen KM, Huang CQ, Xie YF, McCarthy JR, Webb TR, Zhu YF, Saunders J, Liu XJ, Chen TK, Bozigian H, Grigoriadis DE. Chen C, et al. Among authors: huang cq. J Med Chem. 2004 Sep 9;47(19):4787-98. doi: 10.1021/jm040058e. J Med Chem. 2004. PMID: 15341493
Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.
Chen M, Guo Z, Lanier MC, Zhao L, Betz SF, Huang CQ, Loweth CJ, Ashweek NJ, Liu XJ, Struthers RS, Bradbury MJ, Behan JW, Wen J, O'Brien Z, Saunders J, Zhu YF. Chen M, et al. Among authors: huang cq. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3845-50. doi: 10.1016/j.bmcl.2007.05.009. Epub 2007 May 10. Bioorg Med Chem Lett. 2007. PMID: 17521908
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
Moree WJ, Li BF, Zamani-Kord S, Yu J, Coon T, Huang C, Marinkovic D, Tucci FC, Malany S, Bradbury MJ, Hernandez LM, Wen J, Wang H, Hoare SR, Petroski RE, Jalali K, Yang C, Sacaan A, Madan A, Crowe PD, Beaton G. Moree WJ, et al. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5874-8. doi: 10.1016/j.bmcl.2010.07.117. Epub 2010 Aug 3. Bioorg Med Chem Lett. 2010. PMID: 20800486
194 results