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539 results

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Page 1
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.
Probst GD, Bowers S, Sealy JM, Stupi B, Dressen D, Jagodzinska BM, Aquino J, Gailunas A, Truong AP, Tso L, Xu YZ, Hom RK, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Sham HL, Jagodzinski J, Toth G, Brecht E, Yao N, Pan H, Lin M, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Gauby S, Zmolek W, Quinn KP, Sauer JM. Probst GD, et al. Among authors: xu yz. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6034-9. doi: 10.1016/j.bmcl.2010.08.070. Epub 2010 Aug 19. Bioorg Med Chem Lett. 2010. PMID: 20822903
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: xu yz. 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 [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Ye XM, Konradi AW, Sun M, Yuan S, Aubele DL, Dappen M, Dressen D, Garofalo AW, Jagodzinski JJ, Latimer L, Probst GD, Sham HL, Wone D, Xu YZ, Ness D, Brigham E, Kwong GT, Willtis C, Tonn G, Goldbach E, Quinn KP, Zhang HH, Sauer JM, Bova M, Basi GS. Ye XM, et al. Among authors: xu yz. Bioorg Med Chem Lett. 2013 Feb 15;23(4):996-1000. doi: 10.1016/j.bmcl.2012.12.039. Epub 2012 Dec 21. Bioorg Med Chem Lett. 2013. PMID: 23312944
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.
Bowers S, Xu YZ, Yuan S, Probst GD, Hom RK, Chan W, Konradi AW, Sham HL, Zhu YL, Beroza P, Pan H, Brecht E, Yao N, Lougheed J, Tam D, Ren Z, Ruslim L, Bova MP, Artis DR. Bowers S, et al. Among authors: xu yz. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2181-6. doi: 10.1016/j.bmcl.2013.01.103. Epub 2013 Feb 4. Bioorg Med Chem Lett. 2013. PMID: 23465612
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.
Xu YZ, Yuan S, Bowers S, Hom RK, Chan W, Sham HL, Zhu YL, Beroza P, Pan H, Brecht E, Yao N, Lougheed J, Yan J, Tam D, Ren Z, Ruslim L, Bova MP, Artis DR. Xu YZ, et al. Bioorg Med Chem Lett. 2013 May 15;23(10):3075-80. doi: 10.1016/j.bmcl.2013.03.009. Epub 2013 Mar 21. Bioorg Med Chem Lett. 2013. PMID: 23570791
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: xu yz. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.
Semko CM, Chen L, Dressen DB, Dreyer ML, Dunn W, Farouz FS, Freedman SB, Holsztynska EJ, Jefferies M, Konradi AW, Liao A, Lugar J, Mutter L, Pleiss MA, Quinn KP, Thompson T, Thorsett ED, Vandevert C, Xu YZ, Yednock TA. Semko CM, et al. Among authors: xu yz. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1741-3. doi: 10.1016/j.bmcl.2011.01.075. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316228
539 results