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Page 1
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. Among authors: tong x. 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
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
Debenham JS, Madsen-Duggan CB, Wang J, Tong X, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CC, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Euan Macintyre D, Hale JJ, Walsh TF. Debenham JS, et al. Among authors: tong x. Bioorg Med Chem Lett. 2009 May 1;19(9):2591-4. doi: 10.1016/j.bmcl.2009.03.005. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19328684
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: tong x. J Med Chem. 2010 May 27;53(10):4028-37. doi: 10.1021/jm100023j. J Med Chem. 2010. PMID: 20423086
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ. Vachal P, et al. Among authors: tong x. J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27. J Med Chem. 2012. PMID: 22364528
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. Among authors: tong x. 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
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: tong x. 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: tong x. 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
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: tong x. 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
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Vachal P, Fletcher JM, Fong TM, Huang CC, Lao J, Xiao JC, Shen CP, Strack AM, Shearman L, Stribling S, Chen RZ, Frassetto A, Tong X, Wang J, Ball RG, Tsou NN, Hickey GJ, Thompson DF, Faidley TD, Nicolich S, Achanfuo-Yeboah J, Hora DF, Hale JJ, Hagmann WK. Vachal P, et al. Among authors: tong x. J Med Chem. 2009 Apr 23;52(8):2550-8. doi: 10.1021/jm900063x. J Med Chem. 2009. PMID: 19320488
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. Among authors: tong x. 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
4,901 results