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Items: 1 to 20 of 102

1.

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
2.

Orexin receptor antagonists: medicinal chemistry and therapeutic potential.

Roecker AJ, Coleman PJ.

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

PMID:
18673167
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.

Orexin receptor antagonists differ from standard sleep drugs by promoting sleep at doses that do not disrupt cognition.

Uslaner JM, Tye SJ, Eddins DM, Wang X, Fox SV, Savitz AT, Binns J, Cannon CE, Garson SL, Yao L, Hodgson R, Stevens J, Bowlby MR, Tannenbaum PL, Brunner J, Mcdonald TP, Gotter AL, Kuduk SD, Coleman PJ, Winrow CJ, Renger JJ.

Sci Transl Med. 2013 Apr 3;5(179):179ra44. doi: 10.1126/scitranslmed.3005213.

6.

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
7.

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
8.

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
9.

Orexin receptor antagonists: a review of promising compounds patented since 2006.

Coleman PJ, Renger JJ.

Expert Opin Ther Pat. 2010 Mar;20(3):307-24. doi: 10.1517/13543770903567085. Review.

PMID:
20180618
10.

Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.

Sifferlen T, Boss C, Cottreel E, Koberstein R, Gude M, Aissaoui H, Weller T, Gatfield J, Brisbare-Roch C, Jenck F.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1539-42. doi: 10.1016/j.bmcl.2010.01.070. Epub 2010 Jan 22.

PMID:
20144866
11.

Almorexant, a dual orexin receptor antagonist for the treatment of insomnia.

Neubauer DN.

Curr Opin Investig Drugs. 2010 Jan;11(1):101-10. Review.

PMID:
20047164
12.

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
13.

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
14.

International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology.

Gotter AL, Webber AL, Coleman PJ, Renger JJ, Winrow CJ.

Pharmacol Rev. 2012 Jul;64(3):389-420. doi: 10.1124/pr.111.005546. Review.

15.

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

Nishino S.

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

PMID:
17970638
16.

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
17.

Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.

Malherbe P, Borroni E, Pinard E, Wettstein JG, Knoflach F.

Mol Pharmacol. 2009 Sep;76(3):618-31. doi: 10.1124/mol.109.055152. Epub 2009 Jun 19.

18.

Discovery, synthesis, selectivity modulation and DMPK characterization of 5-azaspiro[2.4]heptanes as potent orexin receptor antagonists.

Stasi LP, Artusi R, Bovino C, Buzzi B, Canciani L, Caselli G, Colace F, Garofalo P, Giambuzzi S, Larger P, Letari O, Mandelli S, Perugini L, Pucci S, Salvi M, Toro P.

Bioorg Med Chem Lett. 2013 May 1;23(9):2653-8. doi: 10.1016/j.bmcl.2013.02.093. Epub 2013 Mar 1.

PMID:
23535328
19.

Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists.

Tran DT, Bonaventure P, Hack M, Mirzadegan T, Dvorak C, Letavic M, Carruthers N, Lovenberg T, Sutton SW.

Eur J Pharmacol. 2011 Sep 30;667(1-3):120-8. doi: 10.1016/j.ejphar.2011.05.074. Epub 2011 Jun 12.

PMID:
21679703
20.

Discovery and development of orexin receptor antagonists as therapeutics for insomnia.

Winrow CJ, Renger JJ.

Br J Pharmacol. 2014 Jan;171(2):283-93. doi: 10.1111/bph.12261. Review.

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