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Page 1
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ. Whitman DB, et al. Among authors: bednar ra. ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069. ChemMedChem. 2009. PMID: 19418500
Proline bis-amides as potent dual orexin receptor antagonists.
Bergman JM, Roecker AJ, Mercer SP, Bednar RA, Reiss DR, Ransom RW, Meacham Harrell C, Pettibone DJ, Lemaire W, Murphy KL, Li C, Prueksaritanont T, Winrow CJ, Renger JJ, Koblan KS, Hartman GD, Coleman PJ. Bergman JM, et al. Among authors: bednar ra. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. doi: 10.1016/j.bmcl.2008.01.001. Epub 2008 Jan 8. Bioorg Med Chem Lett. 2008. PMID: 18207395
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: bednar ra. J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c. J Med Chem. 2010. PMID: 20565075
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: bednar ra. ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3. ChemMedChem. 2012. PMID: 22307992
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: bednar ra. 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
Positive allosteric interaction of structurally diverse T-type calcium channel antagonists.
Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ. Uebele VN, et al. Among authors: bednar ra. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. Cell Biochem Biophys. 2009. PMID: 19582593
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
Egbertson MS, Bednar B, Askew BC, Bednar RA, Brashear K, Breslin MJ, Duggan ME, Fisher TE, Halczenko W, Hutchinson JH, Ihle N, Prugh JD, Wai JS, Gould RJ, Hartman GD. Egbertson MS, et al. Among authors: bednar b, bednar ra. Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8. doi: 10.1016/s0960-894x(00)00385-1. Bioorg Med Chem Lett. 2000. PMID: 10987423
Discovery of 3-substituted aminocyclopentanes as potent and orally bioavailable NR2B subtype-selective NMDA antagonists.
Layton ME, Kelly MJ 3rd, Rodzinak KJ, Sanderson PE, Young SD, Bednar RA, Dilella AG, McDonald TP, Wang H, Mosser SD, Fay JF, Cunningham ME, Reiss DR, Fandozzi C, Trainor N, Liang A, Lis EV, Seabrook GR, Urban MO, Yergey J, Koblan KS. Layton ME, et al. Among authors: bednar ra. ACS Chem Neurosci. 2011 Jul 20;2(7):352-62. doi: 10.1021/cn200013d. Epub 2011 Apr 15. ACS Chem Neurosci. 2011. PMID: 22816022 Free PMC article.
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Liverton NJ, Bednar RA, Bednar B, Butcher JW, Claiborne CF, Claremon DA, Cunningham M, DiLella AG, Gaul SL, Libby BE, Lyle EA, Lynch JJ, McCauley JA, Mosser SD, Nguyen KT, Stump GL, Sun H, Wang H, Yergey J, Koblan KS. Liverton NJ, et al. Among authors: bednar ra, bednar b. J Med Chem. 2007 Feb 22;50(4):807-19. doi: 10.1021/jm060983w. Epub 2007 Jan 24. J Med Chem. 2007. PMID: 17249648
47 results