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170 results

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Page 1
In vitro biotransformations of the prostaglandin D2 (DP) antagonist MK-0524 and synthesis of metabolites.
Nicoll-Griffith DA, Seto C, Aubin Y, Lévesque JF, Chauret N, Day S, Silva JM, Trimble LA, Truchon JF, Berthelette C, Lachance N, Wang Z, Sturino C, Braun M, Zamboni R, Young RN. Nicoll-Griffith DA, et al. Among authors: levesque jf. Bioorg Med Chem Lett. 2007 Jan 15;17(2):301-4. doi: 10.1016/j.bmcl.2006.10.055. Epub 2006 Oct 25. Bioorg Med Chem Lett. 2007. PMID: 17095220
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Aubin Y, Bateman KP, Chauret N, Day SH, Lévesque JF, Seto C, Silva JH, Trimble LA, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, Abraham WM, Jones T, McAuliffe M, Piechuta H, Nicoll-Griffith DA, Wang Z, Zamboni R, Young RN, Metters KM. Sturino CF, et al. Among authors: levesque jf. J Med Chem. 2007 Feb 22;50(4):794-806. doi: 10.1021/jm0603668. J Med Chem. 2007. PMID: 17300164
Metabolic activation of indole-containing prostaglandin D2 receptor 1 antagonists: impacts of glutathione trapping and glucuronide conjugation on covalent binding.
Lévesque JF, Day SH, Chauret N, Seto C, Trimble L, Bateman KP, Silva JM, Berthelette C, Lachance N, Boyd M, Li L, Sturino CF, Wang Z, Zamboni R, Young RN, Nicoll-Griffith DA. Lévesque JF, et al. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3038-43. doi: 10.1016/j.bmcl.2007.03.058. Epub 2007 Mar 23. Bioorg Med Chem Lett. 2007. PMID: 17418572
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: levesque jf. 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
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: levesque jf. 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
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. Among authors: levesque jf. 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
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
Colucci J, Boyd M, Berthelette C, Chiasson JF, Wang Z, Ducharme Y, Friesen R, Wrona M, Levesque JF, Denis D, Mathieu MC, Stocco R, Therien AG, Clarke P, Rowland S, Xu D, Han Y. Colucci J, et al. Among authors: levesque jf. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3760-3. doi: 10.1016/j.bmcl.2010.04.065. Epub 2010 Apr 18. Bioorg Med Chem Lett. 2010. PMID: 20471829
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: levesque jf. 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
170 results