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Page 1
Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease.
Chen JJ, Qian W, Biswas K, Yuan C, Amegadzie A, Liu Q, Nixey T, Zhu J, Ncube M, Rzasa RM, Chavez F Jr, Chen N, DeMorin F, Rumfelt S, Tegley CM, Allen JR, Hitchcock S, Hungate R, Bartberger MD, Zalameda L, Liu Y, McCarter JD, Zhang J, Zhu L, Babu-Khan S, Luo Y, Bradley J, Wen PH, Reid DL, Koegler F, Dean C Jr, Hickman D, Correll TL, Williamson T, Wood S. Chen JJ, et al. Among authors: zhu j, zhu l. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6447-54. doi: 10.1016/j.bmcl.2013.09.041. Epub 2013 Sep 29. Bioorg Med Chem Lett. 2013. PMID: 24139583
Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors.
Wood S, Wen PH, Zhang J, Zhu L, Luo Y, Babu-Khan S, Chen K, Pham R, Esmay J, Dineen TA, Kaller MR, Weiss MM, Hitchcock SA, Citron M, Zhong W, Hickman D, Williamson T. Wood S, et al. Among authors: zhu l. J Pharmacol Exp Ther. 2012 Nov;343(2):460-7. doi: 10.1124/jpet.112.197954. Epub 2012 Aug 21. J Pharmacol Exp Ther. 2012. PMID: 22911925
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Chai L, Chaffee SC, Deak HL, Epstein LF, Faust T, Gallant P, Gore A, Gu Y, Henkle B, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, Zhao H, Zhu L, Zhu X. DiMauro EF, et al. Among authors: zhu x, zhu l. J Med Chem. 2008 Mar 27;51(6):1681-94. doi: 10.1021/jm7010996. Epub 2008 Mar 6. J Med Chem. 2008. PMID: 18321037
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG. Martin MW, et al. Among authors: zhu x, zhu l. J Med Chem. 2008 Mar 27;51(6):1637-48. doi: 10.1021/jm701095m. Epub 2008 Feb 16. J Med Chem. 2008. PMID: 18278858
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Martin MW, Newcomb J, Nunes JJ, McGowan DC, Armistead DM, Boucher C, Buchanan JL, Buckner W, Chai L, Elbaum D, Epstein LF, Faust T, Flynn S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Lee JH, Metz D, Middleton S, Mohn D, Morgenstern K, Morrison MJ, Novak PM, Oliveira-dos-Santos A, Powers D, Rose P, Schneider S, Sell S, Tudor Y, Turci SM, Welcher AA, White RD, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Amouzegh P, Ermann M, Jenkins J, Johnston D, Napier S, Power E. Martin MW, et al. Among authors: zhu x, zhu l. J Med Chem. 2006 Aug 10;49(16):4981-91. doi: 10.1021/jm060435i. J Med Chem. 2006. PMID: 16884310
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cee VJ, Chai L, Deak HL, Epstein LF, Faust T, Gallant P, Geuns-Meyer SD, Gore A, Gu Y, Henkle B, Hodous BL, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, Masse CE, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, White RD, Zhao H, Zhu L, Zhu X. DiMauro EF, et al. Among authors: zhu x, zhu l. J Med Chem. 2006 Sep 21;49(19):5671-86. doi: 10.1021/jm0605482. J Med Chem. 2006. PMID: 16970394
Safety monitoring in clinical trials.
Yao B, Zhu L, Jiang Q, Xia HA. Yao B, et al. Among authors: zhu l. Pharmaceutics. 2013 Jan 17;5(1):94-106. doi: 10.3390/pharmaceutics5010094. Pharmaceutics. 2013. PMID: 24300399 Free PMC article.
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