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Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.
Chaturvedula PV, Mercer SE, Pin SS, Thalody G, Xu C, Conway CM, Keavy D, Signor L, Cantor GH, Mathias N, Moench P, Denton R, Macci R, Schartman R, Whiterock V, Davis C, Macor JE, Dubowchik GM. Chaturvedula PV, et al. Among authors: conway cm. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3157-61. doi: 10.1016/j.bmcl.2013.04.012. Epub 2013 Apr 12. Bioorg Med Chem Lett. 2013. PMID: 23632269
Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.
Dasgupta B, Kozlowski E, Schroeder DR, Torrente JR, Xu C, Pin S, Conway CM, Dubowchik GM, Macor JE, Vrudhula VM. Dasgupta B, et al. Among authors: conway cm. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2744-8. doi: 10.1016/j.bmcl.2014.04.033. Epub 2014 Apr 18. Bioorg Med Chem Lett. 2014. PMID: 24794104
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure.
Degnan AP, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Denton R, Han X, Macci R, Mathias NR, Moench P, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Macor JE, Dubowchik GM. Degnan AP, et al. Among authors: conway cm. J Med Chem. 2008 Aug 28;51(16):4858-61. doi: 10.1021/jm800546t. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665579
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Macci R, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Chaturvedula PV, Macor JE, Dubowchik GM. Han X, et al. Among authors: conway cm. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4723-7. doi: 10.1016/j.bmcl.2012.05.074. Epub 2012 Jun 1. Bioorg Med Chem Lett. 2012. PMID: 22727645
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: conway cm. J Med Chem. 2012 Dec 13;55(23):10644-51. doi: 10.1021/jm3013147. Epub 2012 Nov 15. J Med Chem. 2012. PMID: 23153230
164 results