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Page 1
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.
Meurer LC, Finke PE, Mills SG, Walsh TF, Toupence RB, Debenham JS, Goulet MT, Wang J, Tong X, Fong TM, Lao J, Schaeffer MT, Chen J, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Van der Ploeg LH. Meurer LC, et al. Among authors: goulet mt. Bioorg Med Chem Lett. 2005 Feb 1;15(3):645-51. doi: 10.1016/j.bmcl.2004.11.031. Bioorg Med Chem Lett. 2005. PMID: 15664830
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Debenham JS, Madsen-Duggan CB, Walsh TF, Wang J, Tong X, Doss GA, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, MacIntyre DE, Van der Ploeg LH, Goulet MT. Debenham JS, et al. Among authors: goulet mt. Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. doi: 10.1016/j.bmcl.2005.10.028. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263284
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
Jiang J, Hoang M, Young JR, Chaung D, Eid R, Turner C, Lin P, Tong X, Wang J, Tan C, Feighner S, Palyha O, Hreniuk DL, Pan J, Sailer AW, MacNeil DJ, Howard A, Shearman L, Stribling S, Camacho R, Strack A, Van der Ploeg LH, Goulet MT, DeVita RJ. Jiang J, et al. Among authors: goulet mt. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5270-4. doi: 10.1016/j.bmcl.2006.08.006. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919456
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Fong TM, Shen CP, Lao J, Xiao JC, Shearman LP, Stribling DS, Rosko K, Strack A, Marsh DJ, Feng Y, Kumar S, Samuel K, Yin W, Van der Ploeg LH, Goulet MT, Hagmann WK. Lin LS, et al. Among authors: goulet mt. J Med Chem. 2006 Dec 28;49(26):7584-7. doi: 10.1021/jm060996+. J Med Chem. 2006. PMID: 17181138
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.
Madsen-Duggan CB, Debenham JS, Walsh TF, Toupence RB, Huang SX, Wang J, Tong X, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, MacIntyre DE, Van der Ploeg LH, Goulet MT. Madsen-Duggan CB, et al. Among authors: goulet mt. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2031-5. doi: 10.1016/j.bmcl.2007.01.005. Epub 2007 Jan 13. Bioorg Med Chem Lett. 2007. PMID: 17270441
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, Guthikonda R, Truong Q, Chang LL, Quaker G, Colandrea VJ, Tong X, Wang J, Xu S, Fong TM, Shen CP, Lao J, Chen J, Shearman LP, Stribling DS, Rosko K, Strack A, Ha S, Van der Ploeg L, Goulet MT, Hagmann WK. Armstrong HE, et al. Among authors: goulet mt. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. doi: 10.1016/j.bmcl.2007.01.087. Epub 2007 Feb 2. Bioorg Med Chem Lett. 2007. PMID: 17293109
Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents.
Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, Lao J, Yu H, Feng Y, Xiao JC, Van der Ploeg LH, Goulet MT, Hagmann WK, Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Francis B, Strack AM, MacIntyre DE, Shearman LP. Fong TM, et al. Among authors: goulet mt. J Pharmacol Exp Ther. 2007 Jun;321(3):1013-22. doi: 10.1124/jpet.106.118737. Epub 2007 Feb 27. J Pharmacol Exp Ther. 2007. PMID: 17327489
Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents.
Shearman LP, Stribling DS, Camacho RE, Rosko KM, Wang J, Tong S, Feng Y, Marsh DJ, Yu H, Guan X, Spann SK, Macneil DJ, Fong TM, Metzger JM, Goulet MT, Hagmann WK, Plummer CW, Finke PE, Mills SG, Shah SK, Truong Q, Van der Ploeg LH, Macintyre DE, Strack AM. Shearman LP, et al. Among authors: goulet mt. Eur J Pharmacol. 2008 Jan 28;579(1-3):215-24. doi: 10.1016/j.ejphar.2007.10.033. Epub 2007 Oct 25. Eur J Pharmacol. 2008. PMID: 18021763
50 results