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Page 1
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
Isabel E, Mellon C, Boyd MJ, Chauret N, Deschênes D, Desmarais S, Falgueyret JP, Gauthier JY, Khougaz K, Lau CK, Léger S, Levorse DA, Li CS, Massé F, Percival MD, Roy B, Scheigetz J, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC. Isabel E, et al. Among authors: boyd mj. Bioorg Med Chem Lett. 2011 Feb 1;21(3):920-3. doi: 10.1016/j.bmcl.2010.12.070. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21232956
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. 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 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. 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
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. 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 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. 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
Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Boyd MJ, Bandarage UK, Bennett H, Byrn RR, Davies I, Gu W, Jacobs M, Ledeboer MW, Ledford B, Leeman JR, Perola E, Wang T, Bennani Y, Clark MP, Charifson PS. Boyd MJ, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1990-4. doi: 10.1016/j.bmcl.2015.03.013. Epub 2015 Mar 14. Bioorg Med Chem Lett. 2015. PMID: 25827523
Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.
Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS. Clark MP, et al. Among authors: boyd mj. J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24. J Med Chem. 2014. PMID: 25019388
72 results