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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: chauret n. 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
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. Gauthier JY, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15. Bioorg Med Chem Lett. 2008. PMID: 18226527
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: chauret n. 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
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: chauret 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
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Macdonald D, Mastracchio A, Perrier H, Dubé D, Gallant M, Lacombe P, Deschênes D, Roy B, Scheigetz J, Bateman K, Li C, Trimble LA, Day S, Chauret N, Nicoll-Griffith DA, Silva JM, Huang Z, Laliberté F, Liu S, Ethier D, Pon D, Muise E, Boulet L, Chan CC, Styhler A, Charleson S, Mancini J, Masson P, Claveau D, Nicholson D, Turner M, Young RN, Girard Y. Macdonald D, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5241-6. doi: 10.1016/j.bmcl.2005.08.036. Epub 2005 Sep 15. Bioorg Med Chem Lett. 2005. PMID: 16168647
Substituted coumarins as potent 5-lipoxygenase inhibitors.
Grimm EL, Brideau C, Chauret N, Chan CC, Delorme D, Ducharme Y, Ethier D, Falgueyret JP, Friesen RW, Guay J, Hamel P, Riendeau D, Soucy-Breau C, Tagari P, Girard Y. Grimm EL, et al. Among authors: chauret n. Bioorg Med Chem Lett. 2006 May 1;16(9):2528-31. doi: 10.1016/j.bmcl.2006.01.085. Epub 2006 Feb 7. Bioorg Med Chem Lett. 2006. PMID: 16464579
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: chauret n. 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: chauret n. 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: chauret n. 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
61 results