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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: sawyer n. 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
Identification of an indole series of prostaglandin D2 receptor antagonists.
Sturino CF, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Brideau C, Cauchon E, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, O'Neill G, Wang Z, Zamboni R, Metters KM, Young RN. Sturino CF, et al. Among authors: sawyer n. Bioorg Med Chem Lett. 2006 Jun 1;16(11):3043-8. doi: 10.1016/j.bmcl.2006.02.062. Epub 2006 Mar 10. Bioorg Med Chem Lett. 2006. PMID: 16529930
Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Leblanc Y, Roy P, Dufresne C, Lachance N, Wang Z, O'Neill G, Greig G, Denis D, Mathieu MC, Slipetz D, Sawyer N, Tsou N. Leblanc Y, et al. Among authors: sawyer n. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2125-8. doi: 10.1016/j.bmcl.2009.03.010. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19307115
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: sawyer n. 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: sawyer n. 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
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Belley M, Gallant M, Roy B, Houde K, Lachance N, Labelle M, Trimble LA, Chauret N, Li C, Sawyer N, Tremblay N, Lamontagne S, Carrière MC, Denis D, Greig GM, Slipetz D, Metters KM, Gordon R, Chan CC, Zamboni RJ. Belley M, et al. Among authors: sawyer n. Bioorg Med Chem Lett. 2005 Feb 1;15(3):527-30. doi: 10.1016/j.bmcl.2004.11.051. Bioorg Med Chem Lett. 2005. PMID: 15664806
The C3a receptor antagonist SB 290157 has agonist activity.
Mathieu MC, Sawyer N, Greig GM, Hamel M, Kargman S, Ducharme Y, Lau CK, Friesen RW, O'Neill GP, Gervais FG, Therien AG. Mathieu MC, et al. Among authors: sawyer n. Immunol Lett. 2005 Sep 15;100(2):139-45. doi: 10.1016/j.imlet.2005.03.003. Epub 2005 Mar 25. Immunol Lett. 2005. PMID: 16154494
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: sawyer n. J Med Chem. 2007 Feb 22;50(4):794-806. doi: 10.1021/jm0603668. J Med Chem. 2007. PMID: 17300164
Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist.
Gervais FG, Sawyer N, Stocco R, Hamel M, Krawczyk C, Sillaots S, Denis D, Wong E, Wang Z, Gallant M, Abraham WM, Slipetz D, Crackower MA, O'Neill GP. Gervais FG, et al. Among authors: sawyer n. Mol Pharmacol. 2011 Jan;79(1):69-76. doi: 10.1124/mol.110.068585. Epub 2010 Oct 13. Mol Pharmacol. 2011. PMID: 20943773
122 results