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1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
Epple R, Azimioara M, Russo R, Bursulaya B, Tian SS, Gerken A, Iskandar M. Epple R, et al. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. doi: 10.1016/j.bmcl.2006.02.079. Epub 2006 Mar 20. Bioorg Med Chem Lett. 2006. PMID: 16546385
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.
Epple R, Russo R, Azimioara M, Cow C, Xie Y, Wang X, Wityak J, Karanewsky D, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS. Epple R, et al. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4376-80. doi: 10.1016/j.bmcl.2006.05.055. Epub 2006 Jun 5. Bioorg Med Chem Lett. 2006. PMID: 16750626
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Epple R, Azimioara M, Russo R, Xie Y, Wang X, Cow C, Wityak J, Karanewsky D, Bursulaya B, Kreusch A, Tuntland T, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS. Epple R, et al. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5488-92. doi: 10.1016/j.bmcl.2006.08.052. Epub 2006 Aug 22. Bioorg Med Chem Lett. 2006. PMID: 16931011
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
Epple R, Urbina HD, Russo R, Liu H, Mason D, Bursulaya B, Tumanut C, Li J, Harris JL. Epple R, et al. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1254-9. doi: 10.1016/j.bmcl.2006.12.014. Epub 2006 Dec 9. Bioorg Med Chem Lett. 2007. PMID: 17196818
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Alper P, et al. Among authors: epple r. Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023. Epub 2014 Mar 27. Bioorg Med Chem Lett. 2014. PMID: 24751443
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S.
Chatterjee AK, Liu H, Tully DC, Guo J, Epple R, Russo R, Williams J, Roberts M, Tuntland T, Chang J, Gordon P, Hollenbeck T, Tumanut C, Li J, Harris JL. Chatterjee AK, et al. Among authors: epple r. Bioorg Med Chem Lett. 2007 May 15;17(10):2899-903. doi: 10.1016/j.bmcl.2007.02.049. Epub 2007 Feb 27. Bioorg Med Chem Lett. 2007. PMID: 17382545
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Azimioara M, et al. Among authors: epple r. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13. Bioorg Med Chem Lett. 2014. PMID: 25455488
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Lelais G, et al. Among authors: epple r. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19. J Med Chem. 2016. PMID: 27433829
42 results