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Page 1
Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study.
Chen A, Dubé D, Dubé L, Gagné S, Gallant M, Gaudreault M, Grimm E, Houle R, Lacombe P, Laliberté S, Liu S, MacDonald D, Mackay B, Martin D, McKay D, Powell D, Lévesque JF. Chen A, et al. Among authors: houle r. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5074-9. doi: 10.1016/j.bmcl.2010.07.030. Epub 2010 Jul 11. Bioorg Med Chem Lett. 2010. PMID: 20673718
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.
Chen A, Bayly C, Bezençon O, Richard-Bildstein S, Dubé D, Dubé L, Gagné S, Gallant M, Gaudreault M, Grimm E, Houle R, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, Martin D, McKay D, Powell D, Remen L, Soisson S, Toulmond S. Chen A, et al. Among authors: houle r. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2204-9. doi: 10.1016/j.bmcl.2010.02.036. Epub 2010 Feb 18. Bioorg Med Chem Lett. 2010. PMID: 20206513
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: houle r. 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
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: houle r. 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
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: houle r. 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
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: houle r. 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: houle r. 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: houle r. 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
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.
Chen A, Aspiotis R, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Falgueyret JP, Gagné S, Han Y, Houle R, Laliberté S, Larouche G, Lévesque JF, McKay D, Percival D. Chen A, et al. Among authors: houle r. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7399-404. doi: 10.1016/j.bmcl.2011.10.013. Epub 2011 Oct 19. Bioorg Med Chem Lett. 2011. PMID: 22071301
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: houle r. 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
42 results