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Items: 1 to 20 of 94

1.

Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.

Kuduk SD, Skudlarek JW, Di Marco CN, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1784-9. doi: 10.1016/j.bmcl.2014.02.026. Epub 2014 Feb 19.

PMID:
24630562
2.

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23.

PMID:
25577040
3.

Unusual pyrimidine participation: efficient stereoselective synthesis of potent dual orexin receptor antagonist MK-6096.

Chung JY, Zhong YL, Maloney KM, Reamer RA, Moore JC, Strotman H, Kalinin A, Feng R, Strotman NA, Xiang B, Yasuda N.

Org Lett. 2014 Nov 21;16(22):5890-3. doi: 10.1021/ol5028249. Epub 2014 Nov 3.

PMID:
25365229
4.

Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.

Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Garson SL, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2488-92. doi: 10.1016/j.bmcl.2015.04.066. Epub 2015 Apr 29.

PMID:
25981685
5.

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.

Stump CA, Cooke AJ, Bruno J, Cabalu TD, Gotter AL, Harell CM, Kuduk SD, McDonald TP, O'Brien J, Renger JJ, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5809-5814. doi: 10.1016/j.bmcl.2016.10.019. Epub 2016 Oct 14.

PMID:
27818110
6.

Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.

Roecker AJ, Mercer SP, Harrell CM, Garson SL, Fox SV, Gotter AL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 May 1;24(9):2079-85. doi: 10.1016/j.bmcl.2014.03.052. Epub 2014 Mar 26.

PMID:
24704030
7.

Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.

Yoshida Y, Naoe Y, Terauchi T, Ozaki F, Doko T, Takemura A, Tanaka T, Sorimachi K, Beuckmann CT, Suzuki M, Ueno T, Ozaki S, Yonaga M.

J Med Chem. 2015 Jun 11;58(11):4648-64. doi: 10.1021/acs.jmedchem.5b00217. Epub 2015 May 22.

PMID:
25953512
8.

Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.

Roecker AJ, Mercer SP, Bergman JM, Gilbert KF, Kuduk SD, Harrell CM, Garson SL, Fox SV, Gotter AL, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4992-9. doi: 10.1016/j.bmcl.2014.12.081. Epub 2015 Jan 6.

PMID:
25613676
9.

Orexin in sleep, addiction and more: is the perfect insomnia drug at hand?

Hoyer D, Jacobson LH.

Neuropeptides. 2013 Dec;47(6):477-88. doi: 10.1016/j.npep.2013.10.009. Epub 2013 Oct 23. Review.

PMID:
24215799
10.

Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.

Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. doi: 10.1016/j.bmcl.2014.08.041. Epub 2014 Aug 26.

PMID:
25248679
11.

Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.

Yoshida Y, Terauchi T, Naoe Y, Kazuta Y, Ozaki F, Beuckmann CT, Nakagawa M, Suzuki M, Kushida I, Takenaka O, Ueno T, Yonaga M.

Bioorg Med Chem. 2014 Nov 1;22(21):6071-88. doi: 10.1016/j.bmc.2014.08.034. Epub 2014 Sep 8. Erratum in: Bioorg Med Chem. 2015 Jul 1;23(13):3870.

PMID:
25267004
12.

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
13.

Synthesis and biological activity of 5-aryl-4-(4-(5-methyl-1H-imidazol-4-yl)piperidin-1-yl)pyrimidine analogs as potent, highly selective, and orally bioavailable NHE-1 inhibitors.

Atwal KS, O'Neil SV, Ahmad S, Doweyko L, Kirby M, Dorso CR, Chandrasena G, Chen BC, Zhao R, Zahler R.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4796-9. Epub 2006 Jul 25.

PMID:
16870436
14.

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
15.

Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide.

Futamura A, Nozawa D, Araki Y, Tamura Y, Tokura S, Kawamoto H, Tokumaru Y, Kakihara S, Aoki T, Ohtake N.

Bioorg Med Chem. 2017 Oct 15;25(20):5203-5215. doi: 10.1016/j.bmc.2017.07.051. Epub 2017 Jul 29.

PMID:
28807572
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.

Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic stability and pharmacokinetic properties. Part 1.

Sifferlen T, Boller A, Chardonneau A, Cottreel E, Hoecker J, Aissaoui H, Williams JT, Brotschi C, Heidmann B, Siegrist R, Gatfield J, Treiber A, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1201-8. doi: 10.1016/j.bmcl.2013.12.092. Epub 2013 Dec 30.

PMID:
24447850
18.

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.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6620-4. doi: 10.1016/j.bmcl.2013.10.045. Epub 2013 Oct 30.

PMID:
24215892
19.

Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.

Sifferlen T, Koberstein R, Cottreel E, Boller A, Weller T, Gatfield J, Brisbare-Roch C, Jenck F, Boss C.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3857-63. doi: 10.1016/j.bmcl.2013.04.071. Epub 2013 May 8.

PMID:
23719231
20.

Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain.

Lan Y, Chen Y, Cao X, Zhang J, Wang J, Xu X, Qiu Y, Zhang T, Liu X, Liu BF, Zhang G.

J Med Chem. 2014 Dec 26;57(24):10404-23. doi: 10.1021/jm501207r. Epub 2014 Dec 4.

PMID:
25420090

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