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209 results

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Page 1
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP. Hanan EJ, et al. Among authors: siu m. J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23061660
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.
Staben ST, Siu M, Goldsmith R, Olivero AG, Do S, Burdick DJ, Heffron TP, Dotson J, Sutherlin DP, Zhu BY, Tsui V, Le H, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Sideris S, Wiesmann C, Wu P. Staben ST, et al. Among authors: siu m. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4054-8. doi: 10.1016/j.bmcl.2011.04.124. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21636270
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.
Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D. Nair SK, et al. Among authors: siu m. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24. Bioorg Med Chem Lett. 2013. PMID: 23489629
Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.
Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP. Hunt KW, et al. Among authors: siu m. J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16. J Med Chem. 2013. PMID: 23537249
Mechanistic pharmacokinetic-pharmacodynamic modeling of BACE1 inhibition in monkeys: development of a predictive model for amyloid precursor protein processing.
Liu X, Wong H, Scearce-Levie K, Watts RJ, Coraggio M, Shin YG, Peng K, Wildsmith KR, Atwal JK, Mango J, Schauer SP, Regal K, Hunt KW, Thomas AA, Siu M, Lyssikatos J, Deshmukh G, Hop CE. Liu X, et al. Among authors: siu m. Drug Metab Dispos. 2013 Jul;41(7):1319-28. doi: 10.1124/dmd.112.050864. Epub 2013 Apr 12. Drug Metab Dispos. 2013. PMID: 23584887
2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.
Siu M, Pastor R, Liu W, Barrett K, Berry M, Blair WS, Chang C, Chen JZ, Eigenbrot C, Ghilardi N, Gibbons P, He H, Hurley CA, Kenny JR, Cyrus Khojasteh S, Le H, Lee L, Lyssikatos JP, Magnuson S, Pulk R, Tsui V, Ultsch M, Xiao Y, Zhu BY, Sampath D. Siu M, et al. Bioorg Med Chem Lett. 2013 Sep 1;23(17):5014-21. doi: 10.1016/j.bmcl.2013.06.008. Epub 2013 Jun 15. Bioorg Med Chem Lett. 2013. PMID: 23870430
Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.
Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP, Gunawardana IW. Thomas AA, et al. Among authors: siu m. J Med Chem. 2014 Feb 13;57(3):878-902. doi: 10.1021/jm401635n. Epub 2014 Jan 22. J Med Chem. 2014. PMID: 24397738
209 results