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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: chefson a. 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.
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Chen A, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Grimm E, Han Y, Houle R, Huang JQ, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, McKay D, Percival MD, Regan C, Regan H, St-Jacques R, Toulmond S. Chen A, et al. Among authors: chefson a. Bioorg Med Chem Lett. 2011 Jul 1;21(13):3970-5. doi: 10.1016/j.bmcl.2011.05.013. Epub 2011 May 14. Bioorg Med Chem Lett. 2011. PMID: 21621998
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: chefson a. 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
Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents.
Lévesque JF, Bleasby K, Chefson A, Chen A, Dubé D, Ducharme Y, Fournier PA, Gagné S, Gallant M, Grimm E, Hafey M, Han Y, Houle R, Lacombe P, Laliberté S, MacDonald D, Mackay B, Papp R, Tschirret-Guth R. Lévesque JF, et al. Among authors: chefson a. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5547-51. doi: 10.1016/j.bmcl.2011.06.095. Epub 2011 Jun 28. Bioorg Med Chem Lett. 2011. PMID: 21784634
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: chefson a. 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: chefson a. 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
RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors.
Roulston A, Zimmermann M, Papp R, Skeldon A, Pellerin C, Dumas-Bérube É, Dumais V, Dorich S, Fader LD, Fournier S, Li L, Leclaire ME, Yin SY, Chefson A, Alam H, Yang W, Fugère-Desjardins C, Vignini-Hammond S, Skorey K, Mulani A, Rimkunas V, Veloso A, Hamel M, Stocco R, Mamane Y, Li Z, Young JTF, Zinda M, Black WC. Roulston A, et al. Among authors: chefson a. Mol Cancer Ther. 2022 Feb;21(2):245-256. doi: 10.1158/1535-7163.MCT-21-0615. Epub 2021 Dec 15. Mol Cancer Ther. 2022. PMID: 34911817 Free PMC article.
15 results