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Items: 1 to 20 of 179

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.

ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069.

PMID:
19418500
2.

Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.

Coleman PJ, Schreier JD, McGaughey GB, Bogusky MJ, Cox CD, Hartman GD, Ball RG, Harrell CM, Reiss DR, Prueksaritanont T, Winrow CJ, Renger JJ.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2311-5. doi: 10.1016/j.bmcl.2010.01.138. Epub 2010 Feb 8.

PMID:
20207138
3.

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.

Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30.

PMID:
21831639
4.

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.

ChemMedChem. 2012 Mar 5;7(3):415-24, 337. doi: 10.1002/cmdc.201200025. Epub 2012 Feb 3.

PMID:
22307992
5.

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.

J Med Chem. 2010 Jul 22;53(14):5320-32. doi: 10.1021/jm100541c.

PMID:
20565075
6.

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.

J Neurogenet. 2011 Mar;25(1-2):52-61. doi: 10.3109/01677063.2011.566953. Epub 2011 Apr 8.

PMID:
21473737
7.

Orexin receptor antagonists: medicinal chemistry and therapeutic potential.

Roecker AJ, Coleman PJ.

Curr Top Med Chem. 2008;8(11):977-87. Review.

PMID:
18673167
8.

Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure.

Winrow CJ, Tanis KQ, Reiss DR, Rigby AM, Uslaner JM, Uebele VN, Doran SM, Fox SV, Garson SL, Gotter AL, Levine DM, Roecker AJ, Coleman PJ, Koblan KS, Renger JJ.

Neuropharmacology. 2010 Jan;58(1):185-94. doi: 10.1016/j.neuropharm.2009.07.008. Epub 2009 Jul 14.

PMID:
19596018
9.

The hypocretin/orexin receptor: therapeutic prospective in sleep disorders.

Nishino S.

Expert Opin Investig Drugs. 2007 Nov;16(11):1785-97. Review.

PMID:
17970638
10.

Intracerebroventricular injection of orexin-2 receptor antagonist promotes REM sleep.

Kummangal BA, Kumar D, Mallick HN.

Behav Brain Res. 2013 Jan 15;237:59-62. doi: 10.1016/j.bbr.2012.09.015. Epub 2012 Sep 16.

PMID:
22989413
11.

N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Aissaoui H, Koberstein R, Zumbrunn C, Gatfield J, Brisbare-Roch C, Jenck F, Treiber A, Boss C.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5729-33. doi: 10.1016/j.bmcl.2008.09.079. Epub 2008 Sep 26.

PMID:
18845436
12.

Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.

McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK, Dvorak CA, Lovenberg TW, Carruthers NI, Jones TK.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9.

PMID:
15261275
13.

Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists.

Fujimoto T, Kunitomo J, Tomata Y, Nishiyama K, Nakashima M, Hirozane M, Yoshikubo S, Hirai K, Marui S.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6414-6. doi: 10.1016/j.bmcl.2011.08.093. Epub 2011 Aug 30.

PMID:
21917455
14.

Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia.

Coleman PJ, Cox CD, Roecker AJ.

Curr Top Med Chem. 2011;11(6):696-725. Review.

PMID:
21261591
15.

Conformational analysis of N,N-disubstituted-1,4-diazepane orexin receptor antagonists and implications for receptor binding.

Cox CD, McGaughey GB, Bogusky MJ, Whitman DB, Ball RG, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2997-3001. doi: 10.1016/j.bmcl.2009.04.026. Epub 2009 Apr 14.

PMID:
19406641
16.

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.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30. doi: 10.1016/j.bmcl.2008.01.001. Epub 2008 Jan 8.

PMID:
18207395
17.

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.

Neuropharmacology. 2012 Feb;62(2):978-87. doi: 10.1016/j.neuropharm.2011.10.003. Epub 2011 Oct 18.

PMID:
22019562
18.

Inhibitory effects of an orexin-2 receptor antagonist on orexin A- and stress-induced ACTH responses in conscious rats.

Chang H, Saito T, Ohiwa N, Tateoka M, Deocaris CC, Fujikawa T, Soya H.

Neurosci Res. 2007 Mar;57(3):462-6. Epub 2006 Dec 22.

PMID:
17188385
19.

Hypocretin/orexin type 1 receptor in brain: role in cardiovascular control and the neuroendocrine response to immobilization stress.

Samson WK, Bagley SL, Ferguson AV, White MM.

Am J Physiol Regul Integr Comp Physiol. 2007 Jan;292(1):R382-7. Epub 2006 Aug 10.

20.

Treatment and prevention of various therapeutic conditions using OX receptor antagonistic activity (WO2012081692).

Christopher JA, Congreve MS.

Expert Opin Ther Pat. 2013 Feb;23(2):273-7. doi: 10.1517/13543776.2013.749240. Epub 2013 Jan 3.

PMID:
23282091

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