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Efficient and scalable enantioselective synthesis of a CGRP antagonist.
Leahy DK, Fan Y, Desai LV, Chan C, Zhu J, Luo G, Chen L, Hanson RL, Sugiyama M, Rosner T, Cuniere N, Guo Z, Hsiao Y, Gao Q. Leahy DK, et al. Among authors: chen l. Org Lett. 2012 Sep 21;14(18):4938-41. doi: 10.1021/ol302262q. Epub 2012 Sep 6. Org Lett. 2012. PMID: 22954228
Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.
Luo G, Chen L, Conway CM, Denton R, Keavy D, Signor L, Kostich W, Lentz KA, Santone KS, Schartman R, Browning M, Tong G, Houston JG, Dubowchik GM, Macor JE. Luo G, et al. Among authors: chen l. J Med Chem. 2012 Dec 13;55(23):10644-51. doi: 10.1021/jm3013147. Epub 2012 Nov 15. J Med Chem. 2012. PMID: 23153230
Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.
Hu S, Huang Y, Deshpande M, Luo G, Bruce MA, Chen L, Mattson G, Iben LG, Zhang J, Russell JW, Clarke WJ, Hogan JB, Ortiz A, Flint O, Henwood A, Gao Q, Antal-Zimanyi I, Poindexter GS. Hu S, et al. Among authors: chen l. ACS Med Chem Lett. 2012 Jan 4;3(3):222-6. doi: 10.1021/ml200265m. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900458 Free PMC article.
Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.
Luo G, Chen L, Conway CM, Denton R, Keavy D, Gulianello M, Huang Y, Kostich W, Lentz KA, Mercer SE, Schartman R, Signor L, Browning M, Macor JE, Dubowchik GM. Luo G, et al. Among authors: chen l. ACS Med Chem Lett. 2012 Feb 27;3(4):337-41. doi: 10.1021/ml300021s. eCollection 2012 Apr 12. ACS Med Chem Lett. 2012. PMID: 24900474 Free PMC article.
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