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Page 1
Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.
Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach RJ, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A, Fan Y, Swensen AM, Vortherms T, Manelli A, Balut C, Gao W, Yong H, Schrimpf M, Tse C, Kym P, Wang X. Scanio MJC, et al. Among authors: swensen am. Bioorg Med Chem Lett. 2022 Sep 15;72:128843. doi: 10.1016/j.bmcl.2022.128843. Epub 2022 Jun 7. Bioorg Med Chem Lett. 2022. PMID: 35688367
Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis.
Wang X, Liu B, Searle X, Yeung C, Bogdan A, Greszler S, Singh A, Fan Y, Swensen AM, Vortherms T, Balut C, Jia Y, Desino K, Gao W, Yong H, Tse C, Kym P. Wang X, et al. Among authors: swensen am. J Med Chem. 2018 Feb 22;61(4):1436-1449. doi: 10.1021/acs.jmedchem.7b01339. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29251932
Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222.
Singh AK, Fan Y, Balut C, Alani S, Manelli AM, Swensen AM, Jia Y, Neelands TR, Vortherms TA, Liu B, Searle XB, Wang X, Gao W, Hwang TC, Ren HY, Cyr D, Kym PR, Conrath K, Tse C. Singh AK, et al. Among authors: swensen am. J Pharmacol Exp Ther. 2020 Jan;372(1):107-118. doi: 10.1124/jpet.119.261800. Epub 2019 Nov 15. J Pharmacol Exp Ther. 2020. PMID: 31732698 Free PMC article.
Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.
Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach R, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A, Fan Y, Swensen AM, Vortherms T, Manelli A, Balut C, Jia Y, Gao W, Yong H, Schrimpf M, Tse C, Kym P, Wang X. Scanio MJC, et al. Among authors: swensen am. ACS Med Chem Lett. 2019 Oct 31;10(11):1543-1548. doi: 10.1021/acsmedchemlett.9b00377. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749908 Free PMC article.
Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.
Beebe X, Yeung CM, Darczak D, Shekhar S, Vortherms TA, Miller L, Milicic I, Swensen AM, Zhu CZ, Banfor P, Wetter JM, Marsh KC, Jarvis MF, Scott VE, Schrimpf MR, Lee CH. Beebe X, et al. Among authors: swensen am. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074. Epub 2013 Jul 4. Bioorg Med Chem Lett. 2013. PMID: 23876987
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity.
Beebe X, Darczak D, Henry RF, Vortherms T, Janis R, Namovic M, Donnelly-Roberts D, Kage KL, Surowy C, Milicic I, Niforatos W, Swensen A, Marsh KC, Wetter JM, Franklin P, Baker S, Zhong C, Simler G, Gomez E, Boyce-Rustay JM, Zhu CZ, Stewart AO, Jarvis MF, Scott VE. Beebe X, et al. Bioorg Med Chem. 2012 Jul 1;20(13):4128-39. doi: 10.1016/j.bmc.2012.04.057. Epub 2012 May 4. Bioorg Med Chem. 2012. PMID: 22626552
Mechanistic insights into the analgesic efficacy of A-1264087, a novel neuronal Ca(2+) channel blocker that reduces nociception in rat preclinical pain models.
Zhu CZ, Vortherms TA, Zhang M, Xu J, Swensen AM, Niforatos W, Neelands T, Milicic I, Lewis LG, Zhong C, Gauvin D, Mikusa J, Zhan C, Pai M, Roderwald V, Chu KL, Cole EE, Bespalov A, Searle XB, McGaraughty S, Bitner RS, Jarvis MF, Bannon AW, Joshi SK, Scott VE, Lee CH. Zhu CZ, et al. Among authors: swensen am. J Pain. 2014 Apr;15(4):387.e1-14. doi: 10.1016/j.jpain.2013.12.002. Epub 2013 Dec 25. J Pain. 2014. PMID: 24374196 Free article.
A-1048400 is a novel, orally active, state-dependent neuronal calcium channel blocker that produces dose-dependent antinociception without altering hemodynamic function in rats.
Scott VE, Vortherms TA, Niforatos W, Swensen AM, Neelands T, Milicic I, Banfor PN, King A, Zhong C, Simler G, Zhan C, Bratcher N, Boyce-Rustay JM, Zhu CZ, Bhatia P, Doherty G, Mack H, Stewart AO, Jarvis MF. Scott VE, et al. Among authors: swensen am. Biochem Pharmacol. 2012 Feb 1;83(3):406-18. doi: 10.1016/j.bcp.2011.10.019. Epub 2011 Nov 16. Biochem Pharmacol. 2012. PMID: 22153861
39 results