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17 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: berthelette c. 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: berthelette c. 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. Among authors: berthelette c. 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
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: berthelette c. 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: berthelette c. 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
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: berthelette c. 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 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: berthelette c. 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
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: berthelette c. 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
17 results