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Page 1
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. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. J Med Chem. 2008. PMID: 19006286
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.
Grey J, Dyck B, Rowbottom MW, Tamiya J, Vickers TD, Zhang M, Zhao L, Heise CE, Schwarz D, Saunders J, Goodfellow VS. Grey J, et al. Among authors: rowbottom mw. Bioorg Med Chem Lett. 2005 Feb 15;15(4):999-1004. doi: 10.1016/j.bmcl.2004.12.036. Bioorg Med Chem Lett. 2005. PMID: 15686900
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: rowbottom mw. J Med Chem. 2005 Feb 24;48(4):1169-78. doi: 10.1021/jm049218c. J Med Chem. 2005. PMID: 15715483
Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Rowbottom MW, Vickers TD, Dyck B, Tamiya J, Zhang M, Zhao L, Grey J, Provencal D, Schwarz D, Heise CE, Mistry M, Fisher A, Dong T, Hu T, Saunders J, Goodfellow VS. Rowbottom MW, et al. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3439-45. doi: 10.1016/j.bmcl.2005.05.015. Bioorg Med Chem Lett. 2005. PMID: 15950467
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Rowbottom MW, Vickers TD, Dyck B, Grey J, Tamiya J, Zhang M, Kiankarimi M, Wu D, Dwight W, Wade WS, Schwarz D, Heise CE, Madan A, Fisher A, Petroski R, Goodfellow VS. Rowbottom MW, et al. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4450-7. doi: 10.1016/j.bmcl.2006.06.045. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16814542
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.
Hudson S, Kiankarimi M, Rowbottom MW, Vickers TD, Wu D, Pontillo J, Ching B, Dwight W, Goodfellow VS, Schwarz D, Heise CE, Madan A, Wen J, Ban W, Wang H, Wade WS. Hudson S, et al. Among authors: rowbottom mw. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4922-30. doi: 10.1016/j.bmcl.2006.06.049. Epub 2006 Jul 7. Bioorg Med Chem Lett. 2006. PMID: 16824755
23 results