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Page 1
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.
Isabel E, Aspiotis R, Black WC, Colucci J, Fortin R, Giroux A, Grimm EL, Han Y, Mellon C, Nicholson DW, Rasper DM, Renaud J, Roy S, Tam J, Tawa P, Vaillancourt JP, Xanthoudakis S, Zamboni RJ. Isabel E, et al. Among authors: mellon c. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1671-4. doi: 10.1016/j.bmcl.2006.12.110. Epub 2007 Jan 11. Bioorg Med Chem Lett. 2007. PMID: 17251019
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Robichaud J, Black WC, Thérien M, Paquet J, Oballa RM, Bayly CI, McKay DJ, Wang Q, Isabel E, Léger S, Mellon C, Kimmel DB, Wesolowski G, Percival MD, Massé F, Desmarais S, Falgueyret JP, Crane SN. Robichaud J, et al. Among authors: mellon c. J Med Chem. 2008 Oct 23;51(20):6410-20. doi: 10.1021/jm800610j. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811135
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Isabel E, Bateman KP, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Gauthier JY, Lamontagne S, Lau CK, Léger S, LeRiche T, Lévesque JF, Li CS, Massé F, McKay DJ, Mellon C, Nicoll-Griffith DA, Oballa RM, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC. Isabel E, et al. Among authors: mellon c. Bioorg Med Chem Lett. 2010 Feb 1;20(3):887-92. doi: 10.1016/j.bmcl.2009.12.083. Epub 2009 Dec 28. Bioorg Med Chem Lett. 2010. PMID: 20061146
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
Isabel E, Mellon C, Boyd MJ, Chauret N, Deschênes D, Desmarais S, Falgueyret JP, Gauthier JY, Khougaz K, Lau CK, Léger S, Levorse DA, Li CS, Massé F, Percival MD, Roy B, Scheigetz J, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC. Isabel E, et al. Among authors: mellon c. Bioorg Med Chem Lett. 2011 Feb 1;21(3):920-3. doi: 10.1016/j.bmcl.2010.12.070. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21232956
3,4-Diarylpiperidines as potent renin inhibitors.
Lacombe P, Arbour M, Aspiotis R, Cauchon E, Chen A, Dubé D, Falgueyret JP, Fournier PA, Gallant M, Grimm E, Han Y, Juteau H, Liu S, Mellon C, Ramtohul Y, Simard D, St-Jacques R, Tsui GC. Lacombe P, et al. Among authors: mellon c. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1953-7. doi: 10.1016/j.bmcl.2012.01.044. Epub 2012 Jan 26. Bioorg Med Chem Lett. 2012. PMID: 22325946
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.
Gallant M, Beaulieu C, Berthelette C, Colucci J, Crackower MA, Dalton C, Denis D, Ducharme Y, Friesen RW, Guay D, Gervais FG, Hamel M, Houle R, Krawczyk CM, Kosjek B, Lau S, Leblanc Y, Lee EE, Levesque JF, Mellon C, Molinaro C, Mullet W, O'Neill GP, O'Shea P, Sawyer N, Sillaots S, Simard D, Slipetz D, Stocco R, Sørensen D, Truong VL, Wong E, Wu J, Zaghdane H, Wang Z. Gallant M, et al. Among authors: mellon c. Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93. doi: 10.1016/j.bmcl.2010.11.015. Epub 2010 Nov 5. Bioorg Med Chem Lett. 2011. PMID: 21106375
31 results