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Items: 1 to 20 of 153

1.

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
2.

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
3.

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
4.

Orexin receptor antagonists: medicinal chemistry and therapeutic potential.

Roecker AJ, Coleman PJ.

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

PMID:
18673167
5.

Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia.

Betschart C, Hintermann S, Behnke D, Cotesta S, Fendt M, Gee CE, Jacobson LH, Laue G, Ofner S, Chaudhari V, Badiger S, Pandit C, Wagner J, Hoyer D.

J Med Chem. 2013 Oct 10;56(19):7590-607. doi: 10.1021/jm4007627. Epub 2013 Sep 18.

PMID:
23964859
6.

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
7.

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

Nishino S.

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

PMID:
17970638
8.

Orexin receptors: pharmacology and therapeutic opportunities.

Scammell TE, Winrow CJ.

Annu Rev Pharmacol Toxicol. 2011;51:243-66. doi: 10.1146/annurev-pharmtox-010510-100528. Review.

9.

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
10.

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
11.

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
12.

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
13.

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
14.

N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.

Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, Hata M, Fukami T, Kanatani A, Yamada K.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4497-9.

PMID:
14643355
15.

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
16.

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
17.

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.

18.

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
19.

Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.

Coleman PJ, Schreier JD, Roecker AJ, Mercer SP, McGaughey GB, Cox CD, Hartman GD, Harrell CM, Reiss DR, Doran SM, Garson SL, Anderson WB, Tang C, Prueksaritanont T, Winrow CJ, Renger JJ.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4201-5. doi: 10.1016/j.bmcl.2010.05.047. Epub 2010 May 25.

PMID:
20610153
20.

Orexins and orexin receptors: from molecules to integrative physiology.

Matsuki T, Sakurai T.

Results Probl Cell Differ. 2008;46:27-55. doi: 10.1007/400_2007_047. Review.

PMID:
18204827

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