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Page 1
Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.
Bubenik M, Mader P, Mochirian P, Vallée F, Clark J, Truchon JF, Perryman AL, Pau V, Kurinov I, Zahn KE, Leclaire ME, Papp R, Mathieu MC, Hamel M, Duffy NM, Godbout C, Casas-Selves M, Falgueyret JP, Baruah PS, Nicolas O, Stocco R, Poirier H, Martino G, Fortin AB, Roulston A, Chefson A, Dorich S, St-Onge M, Patel P, Pellerin C, Ciblat S, Pinter T, Barabé F, El Bakkouri M, Parikh P, Gervais C, Sfeir A, Mamane Y, Morris SJ, Black WC, Sicheri F, Gallant M. Bubenik M, et al. Among authors: falgueyret jp. J Med Chem. 2022 Oct 13;65(19):13198-13215. doi: 10.1021/acs.jmedchem.2c00998. Epub 2022 Sep 20. J Med Chem. 2022. PMID: 36126059 Free PMC article.
Primary amides as selective inhibitors of cathepsin K.
Léger S, Bayly CI, Black WC, Desmarais S, Falgueyret JP, Massé F, Percival MD, Truchon JF. Léger S, et al. Among authors: falgueyret jp. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4328-32. doi: 10.1016/j.bmcl.2007.05.024. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17544269
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: falgueyret jp. 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
Design and synthesis of potent, isoxazole-containing renin inhibitors.
Fournier PA, Arbour M, Cauchon E, Chen A, Chefson A, Ducharme Y, Falgueyret JP, Gagné S, Grimm E, Han Y, Houle R, Lacombe P, Lévesque JF, MacDonald D, Mackay B, McKay D, Percival MD, Ramtohul Y, St-Jacques R, Toulmond S. Fournier PA, et al. Among authors: falgueyret jp. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2670-4. doi: 10.1016/j.bmcl.2012.03.014. Epub 2012 Mar 11. Bioorg Med Chem Lett. 2012. PMID: 22450130
Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
Côté B, Burch JD, Asante-Appiah E, Bayly C, Bédard L, Blouin M, Campeau LC, Cauchon E, Chan M, Chefson A, Coulombe N, Cromlish W, Debnath S, Deschênes D, Dupont-Gaudet K, Falgueyret JP, Forget R, Gagné S, Gauvreau D, Girardin M, Guiral S, Langlois E, Li CS, Nguyen N, Papp R, Plamondon S, Roy A, Roy S, Seliniotakis R, St-Onge M, Ouellet S, Tawa P, Truchon JF, Vacca J, Wrona M, Yan Y, Ducharme Y. Côté B, et al. Among authors: falgueyret jp. Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22. doi: 10.1016/j.bmcl.2013.12.070. Epub 2013 Dec 24. Bioorg Med Chem Lett. 2014. PMID: 24412110
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.
Chen A, Cauchon E, Chefson A, Dolman S, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Gallant M, Grimm E, Han Y, Houle R, Huang JQ, Hughes G, Jûteau H, Lacombe P, Lauzon S, Lévesque JF, Liu S, Macdonald D, Mackay B, McKay D, Percival MD, St-Jacques R, Toulmond S. Chen A, et al. Among authors: falgueyret jp. Bioorg Med Chem Lett. 2011 Jul 1;21(13):3976-81. doi: 10.1016/j.bmcl.2011.05.014. Epub 2011 May 14. Bioorg Med Chem Lett. 2011. PMID: 21641209
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: falgueyret jp. J Med Chem. 2008 Oct 23;51(20):6410-20. doi: 10.1021/jm800610j. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811135
Identification of a potent and selective non-basic cathepsin K inhibitor.
Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Léger S, Massé F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Thérien M, Truong VL, Wesolowski G, Zamboni R, Black WC. Li CS, et al. Among authors: falgueyret jp. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. doi: 10.1016/j.bmcl.2005.12.071. Epub 2006 Jan 18. Bioorg Med Chem Lett. 2006. PMID: 16413777
80 results