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Page 1
The identification of potent, selective, and bioavailable cathepsin S inhibitors.
Gauthier JY, Black WC, Courchesne I, Cromlish W, Desmarais S, Houle R, Lamontagne S, Li CS, Massé F, McKay DJ, Ouellet M, Robichaud J, Truchon JF, Truong VL, Wang Q, Percival MD. Gauthier JY, et al. Among authors: masse f. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. doi: 10.1016/j.bmcl.2007.06.023. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17590332
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. Gauthier JY, et al. Among authors: masse f. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15. Bioorg Med Chem Lett. 2008. PMID: 18226527
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: masse f. 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: masse f. 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: masse f. 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
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Black WC, Bayly CI, Davis DE, Desmarais S, Falgueyret JP, Léger S, Li CS, Massé F, McKay DJ, Palmer JT, Percival MD, Robichaud J, Tsou N, Zamboni R. Black WC, et al. Among authors: masse f. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4741-4. doi: 10.1016/j.bmcl.2005.07.071. Bioorg Med Chem Lett. 2005. PMID: 16154747
78 results