Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success.
Dubowchik GM, Conway CM, Xin AW.
J Med Chem · review; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.9b01810 PUBLIKATIONSREGISTRET
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11 träffarCalcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
Bell IM.
J Med Chem · review; journal article · DOI 10.1021/jm500364uIdentification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
Joshi P, Anderson C, Binch H, Hadida S, Yoo S, Bergeron D, Decker C, terHaar E, Moore J, Garcia-Guzman M, Termin A.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2013.12.089[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
Bell IM, Gallicchio SN, Stump CA, Bruno JG, Fan H, Gantert LT, Hostetler ED, Kemmerer AL, McWherter M, Moore EL, Mosser SD, Purcell ML, Riffel K, Salvatore CA, Sanabria-Bohórquez S, Staas DD, White RB, Williams M, Zartman CB, Cook JJ, Hargreaves RJ, Kane SA, Graham SL, Selnick HG.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml400199pDiscovery 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.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2013.04.012MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Bell IM, Stump CA, Gallicchio SN, Staas DD, Zartman CB, Moore EL, Sain N, Urban M, Bruno JG, Calamari A, Kemmerer AL, Mosser SD, Fandozzi C, White RB, Zrada MM, Selnick HG, Graham SL, Vacca JP, Kane SA, Salvatore CA.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2012.04.105Identification of a novel RAMP-independent CGRP receptor antagonist.
Zartman CB, Bell IM, Gallicchio SN, Graham SL, Kane SA, Mallee JJ, Rutledge RZ, Salvatore CA, Vacca JP, Williams TM.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2011.09.056Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.
Paone DV, Nguyen DN, Shaw AW, Burgey CS, Potteiger CM, Deng JZ, Mosser SD, Salvatore CA, Yu S, Roller S, Kane SA, Selnick HG, Vacca JP, Williams TM.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.12.054Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
Burgey CS, Potteiger CM, Deng JZ, Mosser SD, Salvatore CA, Yu S, Roller S, Kane SA, Vacca JP, Williams TM.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2009.09.066The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Bell IM, Bednar RA, Corcoran HA, Fay JF, Gallicchio SN, Johnston VK, Hershey JC, Miller-Stein CM, Moore EL, Mosser SD, Roller SA, Salvatore CA, Theberge CR, Wong BK, Blair Zartman C, Kane SA, Williams TM, Graham SL, Vacca JP.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2009.06.057Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).
Paone DV, Shaw AW, Nguyen DN, Burgey CS, Deng JZ, Kane SA, Koblan KS, Salvatore CA, Mosser SD, Johnston VK, Wong BK, Miller-Stein CM, Hershey JC, Graham SL, Vacca JP, Williams TM.
J Med Chem · journal article · DOI 10.1021/jm070668p