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Page 1
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.
Lacombe P, Deschênes D, Dubé D, Dubé L, Gallant M, Macdonald D, Mastracchio A, Perrier H, Charleson S, Huang Z, Laliberté F, Liu S, Mancini JA, Masson P, Salem M, Styhler A, Girard Y. Lacombe P, et al. Bioorg Med Chem Lett. 2006 May 15;16(10):2608-12. doi: 10.1016/j.bmcl.2006.02.043. Epub 2006 Mar 3. Bioorg Med Chem Lett. 2006. PMID: 16516471
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Macdonald D, Mastracchio A, Perrier H, Dubé D, Gallant M, Lacombe P, Deschênes D, Roy B, Scheigetz J, Bateman K, Li C, Trimble LA, Day S, Chauret N, Nicoll-Griffith DA, Silva JM, Huang Z, Laliberté F, Liu S, Ethier D, Pon D, Muise E, Boulet L, Chan CC, Styhler A, Charleson S, Mancini J, Masson P, Claveau D, Nicholson D, Turner M, Young RN, Girard Y. Macdonald D, et al. Among authors: lacombe p. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. doi: 10.1016/j.bmcl.2005.08.036. Epub 2005 Sep 15. Bioorg Med Chem Lett. 2005. PMID: 16168647
Design, synthesis, and biological evaluation of 8-biarylquinolines: a novel class of PDE4 inhibitors.
Gallant M, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Huang Z, Lacombe P, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini J, Masson P, Mastracchio A, Nicholson D, Nicoll-Griffith DA, Perrier H, Salem M, Styhler A, Young RN, Girard Y. Gallant M, et al. Among authors: lacombe p. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1407-12. doi: 10.1016/j.bmcl.2008.01.004. Epub 2008 Jan 8. Bioorg Med Chem Lett. 2008. PMID: 18207397
Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors.
Lacombe P, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Gallant M, Girard Y, Huang Z, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini JA, Masson P, Nicholson DW, Nicoll-Griffith DA, Salem M, Styhler A, Young RN. Lacombe P, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5266-9. doi: 10.1016/j.bmcl.2009.03.105. Epub 2009 Mar 26. Bioorg Med Chem Lett. 2009. PMID: 19640717
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: lacombe p. 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
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: lacombe p. 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
Identification of a new biaryl scaffold generating potent renin inhibitors.
Lacombe P, Aspiotis R, Bayly C, Chen A, Dubé D, Fortin R, Gallant M, Juteau H, Liu S, McKay D, Roy P, Wu T. Lacombe P, et al. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5822-6. doi: 10.1016/j.bmcl.2010.07.127. Epub 2010 Aug 3. Bioorg Med Chem Lett. 2010. PMID: 20728350
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Gallant M, Aspiotis R, Day S, Dias R, Dubé D, Dubé L, Friesen RW, Girard M, Guay D, Hamel P, Huang Z, Lacombe P, Laliberté S, Lévesque JF, Liu S, Macdonald D, Mancini J, Nicholson DW, Styhler A, Townson K, Waters K, Young RN, Girard Y. Gallant M, et al. Among authors: lacombe p. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6387-93. doi: 10.1016/j.bmcl.2010.09.087. Epub 2010 Sep 21. Bioorg Med Chem Lett. 2010. PMID: 20933411
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: lacombe p. 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
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. 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
326 results