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Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20.
J Med Chem. 2013.
PMID: 23713656
Identification of gamma-secretase inhibitor potency determinants on presenilin.
Zhao B, Yu M, Neitzel M, Marugg J, Jagodzinski J, Lee M, Hu K, Schenk D, Yednock T, Basi G.
Zhao B, et al.
J Biol Chem. 2008 Feb 1;283(5):2927-38. doi: 10.1074/jbc.M708870200. Epub 2007 Nov 21.
J Biol Chem. 2008.
PMID: 18032377
Free article.
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Ye XM, Konradi AW, Smith J, Xu YZ, Dressen D, Garofalo AW, Marugg J, Sham HL, Truong AP, Jagodzinski J, Pleiss M, Zhang H, Goldbach E, Sauer JM, Brigham E, Bova M, Basi GS.
Ye XM, et al.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2195-9. doi: 10.1016/j.bmcl.2010.02.039. Epub 2010 Feb 13.
Bioorg Med Chem Lett. 2010.
PMID: 20207136
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Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors (Part II).
Ye XM, Konradi AW, Smith J, Aubele DL, Garofalo AW, Marugg J, Neitzel ML, Semko CM, Sham HL, Sun M, Truong AP, Wu J, Zhang H, Goldbach E, Sauer JM, Brigham EF, Bova M, Basi GS.
Ye XM, et al.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3502-6. doi: 10.1016/j.bmcl.2010.04.148. Epub 2010 May 6.
Bioorg Med Chem Lett. 2010.
PMID: 20529683
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Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.
Dressen D, Garofalo AW, Hawkinson J, Hom D, Jagodzinski J, Marugg JL, Neitzel ML, Pleiss MA, Szoke B, Tung JS, Wone DW, Wu J, Zhang H.
Dressen D, et al. Among authors: marugg jl.
J Med Chem. 2007 Oct 18;50(21):5161-7. doi: 10.1021/jm051292n. Epub 2007 Sep 19.
J Med Chem. 2007.
PMID: 17880055
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Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.
Neitzel ML, Aubele DL, Marugg JL, Jagodzinski JJ, Konradi AW, Pleiss MA, Szoke B, Zmolek W, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Bova MP, Hemphill S, Basi G.
Neitzel ML, et al. Among authors: marugg jl.
Bioorg Med Chem Lett. 2011 Jun 15;21(12):3715-20. doi: 10.1016/j.bmcl.2011.04.079. Epub 2011 May 1.
Bioorg Med Chem Lett. 2011.
PMID: 21571529
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Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.
Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D.
Basi GS, et al. Among authors: marugg j.
Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60.
Alzheimers Res Ther. 2010.
PMID: 21190552
Free PMC article.
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