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3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
Tucci FC, Zhu YF, Struthers RS, Guo Z, Gross TD, Rowbottom MW, Acevedo O, Gao Y, Saunders J, Xie Q, Reinhart GJ, Liu XJ, Ling N, Bonneville AK, Chen T, Bozigian H, Chen C. Tucci FC, et al. Among authors: bozigian h. J Med Chem. 2005 Feb 24;48(4):1169-78. doi: 10.1021/jm049218c. J Med Chem. 2005. PMID: 15715483
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.
Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ Jr, Gao Y, Rowbottom MW, Struthers RS, Reinhart GJ, Xie Q, Chen TK, Bozigian H, Killam Bonneville AL, Fisher A, Jin L, Saunders J, Chen C. Tucci FC, et al. Among authors: bozigian h. J Med Chem. 2004 Jul 1;47(14):3483-6. doi: 10.1021/jm049791w. J Med Chem. 2004. PMID: 15214774
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: bozigian h. J Med Chem. 2004 Sep 9;47(19):4787-98. doi: 10.1021/jm040058e. J Med Chem. 2004. PMID: 15341493
Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
Dyck B, Grigoriadis DE, Gross RS, Guo Z, Haddach M, Marinkovic D, McCarthy JR, Moorjani M, Regan CF, Saunders J, Schwaebe MK, Szabo T, Williams JP, Zhang X, Bozigian H, Chen TK. Dyck B, et al. Among authors: bozigian h. J Med Chem. 2005 Jun 16;48(12):4100-10. doi: 10.1021/jm050070m. J Med Chem. 2005. PMID: 15943483
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Tran JA, Jiang W, Tucci FC, Fleck BA, Wen J, Sai Y, Madan A, Chen TK, Markison S, Foster AC, Hoare SR, Marks D, Harman J, Chen CW, Arellano M, Marinkovic D, Bozigian H, Saunders J, Chen C. Tran JA, et al. Among authors: bozigian h. J Med Chem. 2007 Dec 13;50(25):6356-66. doi: 10.1021/jm701137s. Epub 2007 Nov 10. J Med Chem. 2007. PMID: 17994683
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen C, Tucci FC, Jiang W, Tran JA, Fleck BA, Hoare SR, Wen J, Chen T, Johns M, Markison S, Foster AC, Marinkovic D, Chen CW, Arellano M, Harman J, Saunders J, Bozigian H, Marks D. Chen C, et al. Among authors: bozigian h. Bioorg Med Chem. 2008 May 15;16(10):5606-18. doi: 10.1016/j.bmc.2008.03.072. Epub 2008 Apr 1. Bioorg Med Chem. 2008. PMID: 18417348
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: bozigian h. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. J Med Chem. 2008. PMID: 19006286
32 results