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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: gallant m. 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.
Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
Szychowski J, Papp R, Dietrich E, Liu B, Vallée F, Leclaire ME, Fourtounis J, Martino G, Perryman AL, Pau V, Yin SY, Mader P, Roulston A, Truchon JF, Marshall CG, Diallo M, Duffy NM, Stocco R, Godbout C, Bonneau-Fortin A, Kryczka R, Bhaskaran V, Mao D, Orlicky S, Beaulieu P, Turcotte P, Kurinov I, Sicheri F, Mamane Y, Gallant M, Black WC. Szychowski J, et al. Among authors: gallant m. J Med Chem. 2022 Aug 11;65(15):10251-10284. doi: 10.1021/acs.jmedchem.2c00552. Epub 2022 Jul 26. J Med Chem. 2022. PMID: 35880755 Free PMC article.
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: gallant m. 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
Azaindoles as potent CRTH2 receptor antagonists.
Simard D, Leblanc Y, Berthelette C, Zaghdane MH, Molinaro C, Wang Z, Gallant M, Lau S, Thao T, Hamel M, Stocco R, Sawyer N, Sillaots S, Gervais F, Houle R, Lévesque JF. Simard D, et al. Among authors: gallant m. Bioorg Med Chem Lett. 2011 Jan 15;21(2):841-5. doi: 10.1016/j.bmcl.2010.11.084. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21185722
New indole amide derivatives as potent CRTH2 receptor antagonists.
Zaghdane H, Boyd M, Colucci J, Simard D, Berthelette C, Leblanc Y, Wang Z, Houle R, Lévesque JF, Molinaro C, Hamel M, Stocco R, Sawyer N, Sillaots S, Gervais F, Gallant M. Zaghdane H, et al. Among authors: gallant m. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3471-4. doi: 10.1016/j.bmcl.2011.03.085. Epub 2011 Mar 30. Bioorg Med Chem Lett. 2011. PMID: 21515053
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: gallant m. 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
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: gallant m. 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
The discovery and synthesis of potent zwitterionic inhibitors of renin.
Aspiotis R, Chen A, Cauchon E, Dubé D, Falgueyret JP, Gagné S, Gallant M, Grimm EL, Houle R, Juteau H, Lacombe P, Laliberté S, Lévesque JF, MacDonald D, McKay D, Percival MD, Roy P, Soisson SM, Wu T. Aspiotis R, et al. Among authors: gallant m. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2430-6. doi: 10.1016/j.bmcl.2011.02.067. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21429746
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. 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
190 results