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Page 1
Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia.
Higgins MA, Marcin LR, Christopher Zusi F, Gentles R, Ding M, Pearce BC, Easton A, Kostich WA, Seager MA, Bourin C, Bristow LJ, Johnson KA, Miller R, Hogan J, Whiterock V, Gulianello M, Ferrante M, Huang Y, Hendricson A, Alt A, Macor JE, Bronson JJ. Higgins MA, et al. Among authors: whiterock v. Bioorg Med Chem. 2017 Jan 15;25(2):496-513. doi: 10.1016/j.bmc.2016.11.018. Epub 2016 Nov 14. Bioorg Med Chem. 2017. PMID: 27914948
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: whiterock vj. 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: whiterock vj. 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
Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Degnan AP, Maxwell D, Balakrishnan A, Brown JM, Easton A, Gulianello M, Hanumegowda U, Hill-Drzewi M, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Westphal R, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE. Degnan AP, et al. Among authors: whiterock vj. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5871-5876. doi: 10.1016/j.bmcl.2016.11.014. Epub 2016 Nov 9. Bioorg Med Chem Lett. 2016. PMID: 27856084
Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.
Hill MD, Fang H, Brown JM, Molski T, Easton A, Han X, Miller R, Hill-Drzewi M, Gallagher L, Matchett M, Gulianello M, Balakrishnan A, Bertekap RL, Santone KS, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE, Degnan AP. Hill MD, et al. Among authors: whiterock vj. ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086. doi: 10.1021/acsmedchemlett.6b00292. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994742 Free PMC article.
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: whiterock vj. 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: whiterock v. 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
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: whiterock v. 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
19 results