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Thiophene substituted acylguanidines as BACE1 inhibitors.
Fobare WF, Solvibile WR, Robichaud AJ, Malamas MS, Manas E, Turner J, Hu Y, Wagner E, Chopra R, Cowling R, Jin G, Bard J. Fobare WF, et al. Among authors: Hu Y. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5353-6. doi: 10.1016/j.bmcl.2007.08.010. Epub 2007 Aug 11. Bioorg Med Chem Lett. 2007. PMID: 17761418
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: Hu Y. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.
Malamas MS, Barnes K, Hui Y, Johnson M, Lovering F, Condon J, Fobare W, Solvibile W, Turner J, Hu Y, Manas ES, Fan K, Olland A, Chopra R, Bard J, Pangalos MN, Reinhart P, Robichaud AJ. Malamas MS, et al. Among authors: Hu Y. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2068-73. doi: 10.1016/j.bmcl.2010.02.075. Epub 2010 Feb 23. Bioorg Med Chem Lett. 2010. PMID: 20223661
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Zhou P, Li Y, Fan Y, Wang Z, Chopra R, Olland A, Hu Y, Magolda RL, Pangalos M, Reinhart PH, Turner MJ, Bard J, Malamas MS, Robichaud AJ. Zhou P, et al. Among authors: Hu Y. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2326-9. doi: 10.1016/j.bmcl.2010.01.136. Epub 2010 Feb 12. Bioorg Med Chem Lett. 2010. PMID: 20202842
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.
Malamas MS, Barnes K, Johnson M, Hui Y, Zhou P, Turner J, Hu Y, Wagner E, Fan K, Chopra R, Olland A, Bard J, Pangalos M, Reinhart P, Robichaud AJ. Malamas MS, et al. Among authors: Hu Y. Bioorg Med Chem. 2010 Jan 15;18(2):630-9. doi: 10.1016/j.bmc.2009.12.007. Epub 2009 Dec 6. Bioorg Med Chem. 2010. PMID: 20045648
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.
Malamas MS, Erdei J, Gunawan I, Barnes K, Johnson M, Hui Y, Turner J, Hu Y, Wagner E, Fan K, Olland A, Bard J, Robichaud AJ. Malamas MS, et al. Among authors: Hu Y. J Med Chem. 2009 Oct 22;52(20):6314-23. doi: 10.1021/jm9006752. J Med Chem. 2009. PMID: 19757823
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Pu J, Kreft AF, Aschmies SH, Atchison KP, Berkowitz J, Caggiano TJ, Chlenov M, Diamantidis G, Harrison BL, Hu Y, Huryn D, Steven Jacobsen J, Jin M, Lipinski K, Lu P, Martone RL, Morris K, Sonnenberg-Reines J, Riddell DR, Sabalski J, Sun SC, Wagner E, Wang Y, Xu Z, Zhou H, Resnick L. Pu J, et al. Among authors: Hu Y. Bioorg Med Chem. 2009 Jul 1;17(13):4708-17. doi: 10.1016/j.bmc.2009.04.052. Epub 2009 May 3. Bioorg Med Chem. 2009. PMID: 19443228
(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.
Cole DC, Stock JR, Kreft AF, Antane M, Aschmies SH, Atchison KP, Casebier DS, Comery TA, Diamantidis G, Ellingboe JW, Harrison BL, Hu Y, Jin M, Kubrak DM, Lu P, Mann CW, Martone RL, Moore WJ, Oganesian A, Riddell DR, Sonnenberg-Reines J, Sun SC, Wagner E, Wang Z, Woller KR, Xu Z, Zhou H, Jacobsen JS. Cole DC, et al. Among authors: Hu Y. Bioorg Med Chem Lett. 2009 Feb 1;19(3):926-9. doi: 10.1016/j.bmcl.2008.11.116. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097890
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
Kreft A, Harrison B, Aschmies S, Atchison K, Casebier D, Cole DC, Diamantidis G, Ellingboe J, Hauze D, Hu Y, Huryn D, Jin M, Kubrak D, Lu P, Lundquist J, Mann C, Martone R, Moore W, Oganesian A, Porte A, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Woller K, Xu Z, Zhou H, Steven Jacobsen J. Kreft A, et al. Among authors: Hu Y. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18556202
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