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3,096 results

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Page 1
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.
Roecker AJ, Mercer SP, Harrell CM, Garson SL, Fox SV, Gotter AL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ. Roecker AJ, et al. Among authors: cui d. Bioorg Med Chem Lett. 2014 May 1;24(9):2079-85. doi: 10.1016/j.bmcl.2014.03.052. Epub 2014 Mar 26. Bioorg Med Chem Lett. 2014. PMID: 24704030
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Cox CD, Breslin MJ, Whitman DB, Schreier JD, McGaughey GB, Bogusky MJ, Roecker AJ, Mercer SP, Bednar RA, Lemaire W, Bruno JG, Reiss DR, Harrell CM, Murphy KL, Garson SL, Doran SM, Prueksaritanont T, Anderson WB, Tang C, Roller S, Cabalu TD, Cui D, Hartman GD, Young SD, Koblan KS, Winrow CJ, Renger JJ, Coleman PJ. Cox CD, et al. Among authors: cui d. J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c. J Med Chem. 2010. PMID: 20565075
Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.
Winrow CJ, Gotter AL, Cox CD, Doran SM, Tannenbaum PL, Breslin MJ, Garson SL, Fox SV, Harrell CM, Stevens J, Reiss DR, Cui D, Coleman PJ, Renger JJ. Winrow CJ, et al. Among authors: cui d. J Neurogenet. 2011 Mar;25(1-2):52-61. doi: 10.3109/01677063.2011.566953. Epub 2011 Apr 8. J Neurogenet. 2011. PMID: 21473737
Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia.
Winrow CJ, Gotter AL, Cox CD, Tannenbaum PL, Garson SL, Doran SM, Breslin MJ, Schreier JD, Fox SV, Harrell CM, Stevens J, Reiss DR, Cui D, Coleman PJ, Renger JJ. Winrow CJ, et al. Among authors: cui d. Neuropharmacology. 2012 Feb;62(2):978-87. doi: 10.1016/j.neuropharm.2011.10.003. Epub 2011 Oct 18. Neuropharmacology. 2012. PMID: 22019562
Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.
Coleman PJ, Schreier JD, Cox CD, Breslin MJ, Whitman DB, Bogusky MJ, McGaughey GB, Bednar RA, Lemaire W, Doran SM, Fox SV, Garson SL, Gotter AL, Harrell CM, Reiss DR, Cabalu TD, Cui D, Prueksaritanont T, Stevens J, Tannenbaum PL, Ball RG, Stellabott J, Young SD, Hartman GD, Winrow CJ, Renger JJ. Coleman PJ, et al. Among authors: cui d. ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3. ChemMedChem. 2012. PMID: 22307992
The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold.
Gotter AL, Winrow CJ, Brunner J, Garson SL, Fox SV, Binns J, Harrell CM, Cui D, Yee KL, Stiteler M, Stevens J, Savitz A, Tannenbaum PL, Tye SJ, McDonald T, Yao L, Kuduk SD, Uslaner J, Coleman PJ, Renger JJ. Gotter AL, et al. Among authors: cui d. BMC Neurosci. 2013 Aug 28;14:90. doi: 10.1186/1471-2202-14-90. BMC Neurosci. 2013. PMID: 23981345 Free PMC article.
Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).
Mercer SP, Roecker AJ, Garson S, Reiss DR, Meacham Harrell C, Murphy KL, Bruno JG, Bednar RA, Lemaire W, Cui D, Cabalu TD, Tang C, Prueksaritanont T, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ. Mercer SP, et al. Among authors: cui d. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6620-4. doi: 10.1016/j.bmcl.2013.10.045. Epub 2013 Oct 30. Bioorg Med Chem Lett. 2013. PMID: 24215892
Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ. Roecker AJ, et al. Among authors: cui d. ChemMedChem. 2014 Feb;9(2):311-22. doi: 10.1002/cmdc.201300447. Epub 2013 Dec 27. ChemMedChem. 2014. PMID: 24376006
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ. Roecker AJ, et al. Among authors: cui d. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. doi: 10.1016/j.bmcl.2014.08.041. Epub 2014 Aug 26. Bioorg Med Chem Lett. 2014. PMID: 25248679
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ. Raheem IT, et al. Among authors: cui d. Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23. Bioorg Med Chem Lett. 2015. PMID: 25577040
3,096 results