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Results: 1 to 20 of 120

1.

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
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
3.

Orexin receptor antagonists: medicinal chemistry and therapeutic potential.

Roecker AJ, Coleman PJ.

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

PMID:
18673167
[PubMed - indexed for MEDLINE]
4.

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
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
6.

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
[PubMed - indexed for MEDLINE]
7.

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
[PubMed - indexed for MEDLINE]
8.

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
[PubMed - indexed for MEDLINE]
9.

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
[PubMed - indexed for MEDLINE]
10.

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.

PMID:
23552372
[PubMed - indexed for MEDLINE]
Free Article
11.

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
[PubMed - indexed for MEDLINE]
12.

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
[PubMed - indexed for MEDLINE]
13.

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.

PMID:
21034217
[PubMed - indexed for MEDLINE]
Free PMC Article
14.

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
[PubMed - indexed for MEDLINE]
15.

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.

PMID:
22759794
[PubMed - indexed for MEDLINE]
Free Article
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
[PubMed - indexed for MEDLINE]
17.

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
[PubMed - indexed for MEDLINE]
18.

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

Nishino S.

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

PMID:
17970638
[PubMed - indexed for MEDLINE]
19.

Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.

Bettica P, Nucci G, Pyke C, Squassante L, Zamuner S, Ratti E, Gomeni R, Alexander R.

J Psychopharmacol. 2012 Aug;26(8):1058-70. doi: 10.1177/0269881111408954. Epub 2011 Jul 5.

PMID:
21730017
[PubMed - indexed for MEDLINE]
20.

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
[PubMed - indexed for MEDLINE]

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