Publications
Neurocrine's R & D programs are presented at medical congresses and through major peer-reviewed publications.
Most Recent Publications
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. J Med Chem. 2008 Nov 12. [Epub ahead of print]
The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies
Feher M; Gao Y; Baber JC; Shirley WA; Saunders J, Bioorganic & Medicinal Chemistry [Bioorg Med Chem] 2008 Jan 1; Vol. 16 (1), pp. 422-7. Date of Electronic Publication: 2007 Sep 18
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Regan CF, Guo Z, Chen Y, Huang CQ, Chen M, Jiang W, Rueter JK, Coon T, Chen C, Saunders J, Brown MS, Betz SF, Struthers RS, Yang C, Wen J, Madan A, Zhu YF. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4503-7. Epub 2008 Jul 17.
See also Bioorganic & Medicinal Chemistry Letters
Non-peptide gonadotropin-releasing hormone receptor antagonists.
Betz SF, Zhu YF, Chen C, Struthers RS. J Med Chem. 2008 Jun 26;51(12):3331-48. Review. No abstract available.
Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Chen C, Chen Y, Pontillo J, Guo Z, Huang CQ, Wu D, Madan A, Chen T, Wen J, Xie Q, Tucci FC, Rowbottom M, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3301-5. Epub 2008 Apr 26.
See also Bioorganic & Medicinal Chemistry Letters
5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Zhao L, Guo Z, Chen Y, Hu T, Wu D, Zhu YF, Rowbottom M, Gross TD, Tucci FC, Struthers RS, Xie Q, Chen C. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3344-9. Epub 2008 Apr 15.
See also Bioorganic & Medicinal Chemistry Letters
Small molecule antagonists of the corticotropin releasing factor (CRF) receptor: recent medicinal chemistry developments.
Tellew JE, Luo Z. Curr Top Med Chem. 2008;8(6):506-20. Review. |
