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Page 1
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.
Probst G, Aubele DL, Bowers S, Dressen D, Garofalo AW, Hom RK, Konradi AW, Marugg JL, Mattson MN, Neitzel ML, Semko CM, Sham HL, Smith J, Sun M, Truong AP, Ye XM, Xu YZ, Dappen MS, Jagodzinski JJ, Keim PS, Peterson B, Latimer LH, Quincy D, Wu J, Goldbach E, Ness DK, Quinn KP, Sauer JM, Wong K, Zhang H, Zmolek W, Brigham EF, Kholodenko D, Hu K, Kwong GT, Lee M, Liao A, Motter RN, Sacayon P, Santiago P, Willits C, Bard F, Bova MP, Hemphill SS, Nguyen L, Ruslim L, Tanaka K, Tanaka P, Wallace W, Yednock TA, Basi GS. Probst G, et al. Among authors: goldbach e. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Truong AP, Aubele DL, Probst GD, Neitzel ML, Semko CM, Bowers S, Dressen D, Hom RK, Konradi AW, Sham HL, Garofalo AW, Keim PS, Wu J, Dappen MS, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Hemphill SS, Bova MP, Bard F, Yednock TA, Basi G. Truong AP, et al. Among authors: goldbach e. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4920-3. doi: 10.1016/j.bmcl.2009.07.092. Epub 2009 Jul 23. Bioorg Med Chem Lett. 2009. PMID: 19660943
N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.
Bowers S, Probst GD, Truong AP, Hom RK, Konradi AW, Sham HL, Garofalo AW, Wong K, Goldbach E, Quinn KP, Sauer JM, Wallace W, Nguyen L, Hemphill SS, Bova MP, Basi GS. Bowers S, et al. Among authors: goldbach e. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6952-6. doi: 10.1016/j.bmcl.2009.10.060. Epub 2009 Oct 30. Bioorg Med Chem Lett. 2009. PMID: 19879755
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. Among authors: goldbach e. 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
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. Among authors: goldbach e. 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
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Truong AP, Tóth G, Probst GD, Sealy JM, Bowers S, Wone DW, Dressen D, Hom RK, Konradi AW, Sham HL, Wu J, Peterson BT, Ruslim L, Bova MP, Kholodenko D, Motter RN, Bard F, Santiago P, Ni H, Chian D, Soriano F, Cole T, Brigham EF, Wong K, Zmolek W, Goldbach E, Samant B, Chen L, Zhang H, Nakamura DF, Quinn KP, Yednock TA, Sauer JM. Truong AP, et al. Among authors: goldbach e. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6231-6. doi: 10.1016/j.bmcl.2010.08.102. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20833041
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: goldbach e. 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
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: goldbach e. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7. Bioorg Med Chem Lett. 2011. PMID: 21813278
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.
Aubele DL, Truong AP, Dressen DB, Probst GD, Bowers S, Mattson MN, Semko CM, Sun M, Garofalo AW, Konradi AW, Sham HL, Zmolek W, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Bova MP, Hemphill SS, Basi G. Aubele DL, et al. Among authors: goldbach e. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5791-4. doi: 10.1016/j.bmcl.2011.08.008. Epub 2011 Aug 9. Bioorg Med Chem Lett. 2011. PMID: 21885276
Novel cinnoline-based inhibitors of LRRK2 kinase activity.
Garofalo AW, Adler M, Aubele DL, Bowers S, Franzini M, Goldbach E, Lorentzen C, Neitz RJ, Probst GD, Quinn KP, Santiago P, Sham HL, Tam D, Truong AP, Ye XM, Ren Z. Garofalo AW, et al. Among authors: goldbach e. Bioorg Med Chem Lett. 2013 Jan 1;23(1):71-4. doi: 10.1016/j.bmcl.2012.11.021. Epub 2012 Nov 16. Bioorg Med Chem Lett. 2013. PMID: 23219325
24 results