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Page 1
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. 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
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: debenham js. 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
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: debenham js. 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
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Debenham JS, Madsen-Duggan CB, Toupence RB, Walsh TF, Wang J, Tong X, Kumar S, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, Goulet MT. Debenham JS, et al. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1448-52. doi: 10.1016/j.bmcl.2009.12.065. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20096577
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
Yan L, Huo P, Debenham JS, Madsen-Duggan CB, Lao J, Chen RZ, Xiao JC, Shen CP, Stribling DS, Shearman LP, Strack AM, Tsou N, Ball RG, Wang J, Tong X, Bateman TJ, Reddy VB, Fong TM, Hale JJ. Yan L, et al. Among authors: debenham js. J Med Chem. 2010 May 27;53(10):4028-37. doi: 10.1021/jm100023j. J Med Chem. 2010. PMID: 20423086
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.
Madsen-Duggan CB, Debenham JS, Walsh TF, Yan L, Huo P, Wang J, Tong X, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, Goulet MT, Hale JJ. Madsen-Duggan CB, et al. Among authors: debenham js. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. doi: 10.1016/j.bmcl.2010.04.071. Epub 2010 Apr 21. Bioorg Med Chem Lett. 2010. PMID: 20483606
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Debenham JS, Graham TH, Verras A, Zhang Y, Clements MJ, Kuethe JT, Madsen-Duggan C, Liu W, Bhatt UR, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Li X, Lisnock J, Shen Z, Tong X, Tung EC, Wiltsie J, Xu S, Hale JJ, Pinto S, Shen DM. Debenham JS, et al. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6228-33. doi: 10.1016/j.bmcl.2013.09.094. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24157366
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.
Debenham JS, Madsen-Duggan C, Clements MJ, Walsh TF, Kuethe JT, Reibarkh M, Salowe SP, Sonatore LM, Hajdu R, Milligan JA, Visco DM, Zhou D, Lingham RB, Stickens D, DeMartino JA, Tong X, Wolff M, Pang J, Miller RR, Sherer EC, Hale JJ. Debenham JS, et al. J Med Chem. 2016 Dec 22;59(24):11039-11049. doi: 10.1021/acs.jmedchem.6b01242. Epub 2016 Nov 30. J Med Chem. 2016. PMID: 28002958
19 results