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Page 1
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: neitzel ml. 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 and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1838-43. doi: 10.1016/j.bmcl.2011.01.046. Epub 2011 Jan 20. Bioorg Med Chem Lett. 2011. PMID: 21316234
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: neitzel ml. 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
Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.
Mattson MN, Neitzel ML, Quincy DA, Semko CM, Garofalo AW, Keim PS, Konradi AW, Pleiss MA, Sham HL, Brigham EF, Goldbach EG, Zhang H, Sauer JM, Basi GS. Mattson MN, et al. Among authors: neitzel ml. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14. Bioorg Med Chem Lett. 2010. PMID: 20206516
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Hom RK, Bowers S, Sealy JM, Truong AP, Probst GD, Neitzel ML, Neitz RJ, Fang L, Brogley L, Wu J, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Quinn K, Sauer JM, Powell K, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Hom RK, et al. Among authors: neitzel ml. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7303-7. doi: 10.1016/j.bmcl.2010.10.066. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 21071223
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: neitzel ml. Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60. Alzheimers Res Ther. 2010. PMID: 21190552 Free PMC article.
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: neitzel ml. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
11 results