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Page 1
A formulation strategy for gamma secretase inhibitor ELND006, a BCS class II compound: development of a nanosuspension formulation with improved oral bioavailability and reduced food effects in dogs.
Quinn K, Gullapalli RP, Merisko-Liversidge E, Goldbach E, Wong A, Liversidge GG, Hoffman W, Sauer JM, Bullock J, Tonn G. Quinn K, et al. Among authors: tonn g. J Pharm Sci. 2012 Apr;101(4):1462-74. doi: 10.1002/jps.23034. Epub 2011 Dec 28. J Pharm Sci. 2012. PMID: 22213574
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: tonn g. 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
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: tonn g. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7. Bioorg Med Chem Lett. 2011. PMID: 21813278
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.
Aubele DL, Hom RK, Adler M, Galemmo RA Jr, Bowers S, Truong AP, Pan H, Beroza P, Neitz RJ, Yao N, Lin M, Tonn G, Zhang H, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Diep L, Fitzgerald K, Hoffman J, Motter R, Fauss D, Tanaka P, Dappen M, Jagodzinski J, Chan W, Konradi AW, Latimer L, Zhu YL, Sham HL, Anderson JP, Bergeron M, Artis DR. Aubele DL, et al. Among authors: tonn g. ChemMedChem. 2013 Aug;8(8):1295-313. doi: 10.1002/cmdc.201300166. Epub 2013 Jun 21. ChemMedChem. 2013. PMID: 23794260
Tetrahydroquinoline derivatives as CRTH2 antagonists.
Liu J, Wang Y, Sun Y, Marshall D, Miao S, Tonn G, Anders P, Tocker J, Tang HL, Medina J. Liu J, et al. Among authors: tonn g. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6840-4. doi: 10.1016/j.bmcl.2009.10.094. Epub 2009 Oct 25. Bioorg Med Chem Lett. 2009. PMID: 19896843
A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Browner MF. Cushing TD, et al. Among authors: tonn g. Bioorg Med Chem Lett. 2011 Jan 1;21(1):417-22. doi: 10.1016/j.bmcl.2010.10.126. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074993
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA Jr, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M. Bowers S, et al. Among authors: tonn g. Bioorg Med Chem Lett. 2013 May 1;23(9):2743-9. doi: 10.1016/j.bmcl.2013.02.065. Epub 2013 Feb 24. Bioorg Med Chem Lett. 2013. PMID: 23522834
An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl)-4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing.
Tonn GR, Wong SG, Wong SC, Johnson MG, Ma J, Cho R, Floren LC, Kersey K, Berry K, Marcus AP, Wang X, Van Lengerich B, Medina JC, Pearson PG, Wong BK. Tonn GR, et al. Drug Metab Dispos. 2009 Mar;37(3):502-13. doi: 10.1124/dmd.108.021931. Epub 2008 Dec 16. Drug Metab Dispos. 2009. PMID: 19088267 Clinical Trial.
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