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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: vortherms t. 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: vortherms t. 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
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: vortherms t. 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.
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: vortherms ta. 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.
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: vortherms ta. 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. Among authors: vortherms t. 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
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD. Liu H, et al. J Med Chem. 2008 Nov 27;51(22):7094-8. doi: 10.1021/jm8007618. J Med Chem. 2008. PMID: 18983139
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: vortherms ta. 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.
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.
Altenbach RJ, Adair RM, Bettencourt BM, Black LA, Fix-Stenzel SR, Gopalakrishnan SM, Hsieh GC, Liu H, Marsh KC, McPherson MJ, Milicic I, Miller TR, Vortherms TA, Warrior U, Wetter JM, Wishart N, Witte DG, Honore P, Esbenshade TA, Hancock AA, Brioni JD, Cowart MD. Altenbach RJ, et al. J Med Chem. 2008 Oct 23;51(20):6571-80. doi: 10.1021/jm8005959. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811133
37 results