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Page 1
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.
Mercer SE, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Pin SS, Macci R, Schartman R, Signor LJ, Widmann KA, Whiterock VJ, Chen P, Xu C, Herbst JJ, Kostich WA, Thalody G, Macor JE, Dubowchik GM. Mercer SE, et al. Among authors: signor lj. Bioorg Med Chem Lett. 2021 Jan 1;31:127624. doi: 10.1016/j.bmcl.2020.127624. Epub 2020 Oct 21. Bioorg Med Chem Lett. 2021. PMID: 33096162
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Degnan AP, Jiang XJ, Macci R, Mathias NR, Moench P, Pin SS, Schartman R, Signor LJ, Thalody G, Tora G, Whiterock V, Xu C, Macor JE, Dubowchik GM. Han X, et al. Among authors: signor lj. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1870-3. doi: 10.1016/j.bmcl.2013.01.011. Epub 2013 Jan 24. Bioorg Med Chem Lett. 2013. PMID: 23402880
Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels.
Gribkoff VK, Starrett JE Jr, Dworetzky SI, Hewawasam P, Boissard CG, Cook DA, Frantz SW, Heman K, Hibbard JR, Huston K, Johnson G, Krishnan BS, Kinney GG, Lombardo LA, Meanwell NA, Molinoff PB, Myers RA, Moon SL, Ortiz A, Pajor L, Pieschl RL, Post-Munson DJ, Signor LJ, Srinivas N, Taber MT, Thalody G, Trojnacki JT, Wiener H, Yeleswaram K, Yeola SW. Gribkoff VK, et al. Among authors: signor lj. Nat Med. 2001 Apr;7(4):471-7. doi: 10.1038/86546. Nat Med. 2001. PMID: 11283675
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: signor lj. 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 (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: signor lj. J Med Chem. 2008 Aug 28;51(16):4858-61. doi: 10.1021/jm800546t. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665579