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Page 1
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: santone ks. J Med Chem. 2012 Dec 13;55(23):10644-51. doi: 10.1021/jm3013147. Epub 2012 Nov 15. J Med Chem. 2012. PMID: 23153230
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: santone ks. 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
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: santone ks. 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
Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF. Kostich W, et al. Among authors: santone ks. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13. J Pharmacol Exp Ther. 2016. PMID: 27411717 Free PMC article.
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: santone ks. 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.
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: santone ks. 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.
Inhibitors of HIV-1 attachment. Part 7: indole-7-carboxamides as potent and orally bioavailable antiviral agents.
Yeung KS, Qiu Z, Xue Q, Fang H, Yang Z, Zadjura L, D'Arienzo CJ, Eggers BJ, Riccardi K, Shi PY, Gong YF, Browning MR, Gao Q, Hansel S, Santone K, Lin PF, Meanwell NA, Kadow JF. Yeung KS, et al. Among authors: santone k. Bioorg Med Chem Lett. 2013 Jan 1;23(1):198-202. doi: 10.1016/j.bmcl.2012.10.115. Epub 2012 Nov 6. Bioorg Med Chem Lett. 2013. PMID: 23200252
Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.
Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG. Belema M, et al. Among authors: santone ks. J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12. J Med Chem. 2014. PMID: 24521299
46 results