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Page 1
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: levesque jf. 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
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
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.
Burch JD, Belley M, Fortin R, Deschênes D, Girard M, Colucci J, Farand J, Therien AG, Mathieu MC, Denis D, Vigneault E, Lévesque JF, Gagné S, Wrona M, Xu D, Clark P, Rowland S, Han Y. Burch JD, et al. Among authors: levesque jf. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2048-54. doi: 10.1016/j.bmcl.2008.01.103. Epub 2008 Jan 31. Bioorg Med Chem Lett. 2008. PMID: 18291643
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Blouin M, Han Y, Burch J, Farand J, Mellon C, Gaudreault M, Wrona M, Lévesque JF, Denis D, Mathieu MC, Stocco R, Vigneault E, Therien A, Clark P, Rowland S, Xu D, O'Neill G, Ducharme Y, Friesen R. Blouin M, et al. Among authors: levesque jf. J Med Chem. 2010 Mar 11;53(5):2227-38. doi: 10.1021/jm901771h. J Med Chem. 2010. PMID: 20163116
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-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: levesque jf. 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: levesque jf. 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
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.
Burch JD, Farand J, Colucci J, Sturino C, Ducharme Y, Friesen RW, Lévesque JF, Gagné S, Wrona M, Therien AG, Mathieu MC, Denis D, Vigneault E, Xu D, Clark P, Rowland S, Han Y. Burch JD, et al. Among authors: levesque jf. Bioorg Med Chem Lett. 2011 Feb 1;21(3):1041-6. doi: 10.1016/j.bmcl.2010.12.014. Epub 2010 Dec 8. Bioorg Med Chem Lett. 2011. PMID: 21215624
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
167 results