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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. J Med Chem. 2008 Aug 28;51(16):4858-61. doi: 10.1021/jm800546t. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665579
Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.
Gillman KW, Parker MF, Silva M, Degnan AP, Tora GO, Lodge NJ, Li YW, Lelas S, Taber M, Krause RG, Bertekap RL, Newton AE, Pieschl RL, Lengyel KD, Johnson KA, Taylor SJ, Bronson JJ, Macor JE. Gillman KW, et al. Among authors: degnan ap. Bioorg Med Chem Lett. 2013 Jan 15;23(2):407-11. doi: 10.1016/j.bmcl.2012.11.094. Epub 2012 Nov 30. Bioorg Med Chem Lett. 2013. PMID: 23253443
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: degnan ap. 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
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.
Degnan AP, Tora GO, Han Y, Rajamani R, Bertekap R, Krause R, Davis CD, Hu J, Morgan D, Taylor SJ, Krause K, Li YW, Mattson G, Cunningham MA, Taber MT, Lodge NJ, Bronson JJ, Gillman KW, Macor JE. Degnan AP, et al. Bioorg Med Chem Lett. 2015 Aug 1;25(15):3039-43. doi: 10.1016/j.bmcl.2015.04.098. Epub 2015 Jun 2. Bioorg Med Chem Lett. 2015. PMID: 26048800
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.
Yang F, Snyder LB, Balakrishnan A, Brown JM, Sivarao DV, Easton A, Fernandes A, Gulianello M, Hanumegowda UM, Huang H, Huang Y, Jones KM, Li YW, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Simutis FJ, Westphal R, Whiterock VJ, Bronson JJ, Macor JE, Degnan AP. Yang F, et al. Among authors: degnan ap. ACS Med Chem Lett. 2016 Jan 4;7(3):289-93. doi: 10.1021/acsmedchemlett.5b00450. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985317 Free PMC article.
Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.
Huang H, Degnan AP, Balakrishnan A, Easton A, Gulianello M, Huang Y, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Snyder LB, Westphal R, Whiterock VJ, Yang F, Bronson JJ, Macor JE. Huang H, et al. Among authors: degnan ap. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9. doi: 10.1016/j.bmcl.2016.07.065. Epub 2016 Jul 28. Bioorg Med Chem Lett. 2016. PMID: 27496211
Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression.
Degnan AP, Tora GO, Huang H, Conlon DA, Davis CD, Hanumegowda UM, Hou X, Hsiao Y, Hu J, Krause R, Li YW, Newton AE, Pieschl RL, Raybon J, Rosner T, Sun JH, Taber MT, Taylor SJ, Wong MK, Zhang H, Lodge NJ, Bronson JJ, Macor JE, Gillman KW. Degnan AP, et al. ACS Chem Neurosci. 2016 Dec 21;7(12):1635-1640. doi: 10.1021/acschemneuro.6b00337. Epub 2016 Oct 18. ACS Chem Neurosci. 2016. PMID: 27744678
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