-
1
-
-
84874732424
-
-
Merck & Co. Inc., CN 101880276, EP 2089382, EP 2392572, JP 201051121, JP 2011068665, JP 2011079848, US 2008132490, US 7951797, US 2011195957, WO 2008069997
-
Bergman, J.M., Breslin, M.J., Coleman, P.J., Cox, C.D., Mercer, S.P., Roecker, A.J. (Merck & Co., Inc.) Substituted diazepan compounds as orexin receptor antagonists. CN 101880276, EP 2089382, EP 2392572, JP 201051121, JP 2011068665, JP 2011079848, US 2008132490, US 7951797, US 2011195957, WO 2008069997.
-
Substituted Diazepan Compounds As Orexin Receptor Antagonists
-
-
Bergman, J.M.1
Breslin, M.J.2
Coleman, P.J.3
Cox, C.D.4
Mercer, S.P.5
Roecker, A.J.6
-
2
-
-
77954731181
-
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, C.D., Breslin, M.J., Whitman, D.B. et al. 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. J Med Chem 2010, 53(14): 5320-32.
-
(2010)
J Med Chem
, vol.53
, Issue.14
, pp. 5320-5332
-
-
Cox, C.D.1
Breslin, M.J.2
Whitman, D.B.3
-
3
-
-
84863633075
-
Enantioselective synthesis of a dual orexin receptor antagonist
-
Mangion, I.K., Sherry, B.D., Yin, J., Fleitz, F.J. Enantioselective synthesis of a dual orexin receptor antagonist. Org Lett 2012, 14(13): 3458-61.
-
(2012)
Org Lett
, vol.14
, Issue.13
, pp. 3458-3461
-
-
Mangion, I.K.1
Sherry, B.D.2
Yin, J.3
Fleitz, F.J.4
-
4
-
-
79952834243
-
The first large-scale synthesis of MK-4305: A dual orexin receptor antagonist for the treatment of sleep disorder
-
Baxter, C.A., Cleator, E., Brands, K.M.J. et al. The first large-scale synthesis of MK-4305: A dual orexin receptor antagonist for the treatment of sleep disorder. Org Proc Res Dev 2011, 15(2): 367-75.
-
(2011)
Org Proc Res Dev
, vol.15
, Issue.2
, pp. 367-375
-
-
Baxter, C.A.1
Cleator, E.2
Brands, K.M.J.3
-
5
-
-
84874755401
-
Development of the manufacturing route for suvorexant - A dual orexin antagonist for sleep disorder
-
Aug 19-23, Philadelphia) , Abst ORGN-271
-
Wallace, D.J. Development of the manufacturing route for suvorexant - A dual orexin antagonist for sleep disorder. 244th ACS Natl Meet Exp (Aug 19-23, Philadelphia) 2012, Abst ORGN-271.
-
(2012)
244th ACS Natl Meet Exp
-
-
Wallace, D.J.1
-
6
-
-
84874701643
-
Development of the manufacturing route for suvorexant - A dual orexin antagonist for sleep disorder
-
July 1-4, Tallinn
-
Baxter, C.A. Development of the manufacturing route for suvorexant - A dual orexin antagonist for sleep disorder. Balticum Organicum Syntheticum - Intl Conf Org Synth (July 1-4, Tallinn) 2012, p 16.
-
(2012)
Balticum Organicum Syntheticum - Intl Conf Org Synth
, pp. 16
-
-
Baxter, C.A.1
-
7
-
-
79957733667
-
Reaction development and mechanistic study of a ruthenium catalyzed intramolecular asymmetric reductive amination en route to the dual orexin inhibitor suvorexant (MK-4305)
-
Strotman, N.A., Baxter, C.A., Brands, K.M.J. et al. Reaction development and mechanistic study of a ruthenium catalyzed intramolecular asymmetric reductive amination en route to the dual orexin inhibitor suvorexant (MK-4305). J Am Chem Soc 2011, 133(21): 8362-71.
-
(2011)
J Am Chem Soc
, vol.133
, Issue.21
, pp. 8362-8371
-
-
Strotman, N.A.1
Baxter, C.A.2
Brands, K.M.J.3
-
8
-
-
84874673769
-
Discovery of an asymmetric synthesis of suvorexant
-
Aug 19-23, Philadelphia, Abst ORGN-13
-
Cleator, E. Discovery of an asymmetric synthesis of suvorexant. 244th ACS Natl Meet Exp (Aug 19-23, Philadelphia) 2012, Abst ORGN-13.
-
(2012)
244th ACS Natl Meet Exp
-
-
Cleator, E.1
-
9
-
-
84930538921
-
Synthesis of suvorexant
-
Kocienski, P. Synthesis of suvorexant. Synfacts 2011, (8): 822.
-
(2011)
Synfacts
, vol.8
, pp. 822
-
-
Kocienski, P.1
-
10
-
-
81755163019
-
Amination of benzoxazoles and 1,3,4-oxadiazoles using 2,2,6,6-tetramethylpiperidine-N-oxoammonium tetrafluoroborate as an organic oxidant
-
Wertz, S., Kodama, S., Studer, A. Amination of benzoxazoles and 1,3,4- oxadiazoles using 2,2,6,6-tetramethylpiperidine-N-oxoammonium tetrafluoroborate as an organic oxidant. Angew Chem Int Ed 2011, 50(48): 11511-5.
-
(2011)
Angew Chem Int Ed
, vol.50
, Issue.48
, pp. 11511-11515
-
-
Wertz, S.1
Kodama, S.2
Studer, A.3
-
11
-
-
1342322672
-
Characterisation of the binding of 3H-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor
-
Langmead, C.J., Jerman, J.C., Brough, S.J., Scott, C., Porter, R.A., Herdon, H.J. Characterisation of the binding of 3H-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol 2004, 141(2): 340-6.
-
(2004)
Br J Pharmacol
, vol.141
, Issue.2
, pp. 340-346
-
-
Langmead, C.J.1
Jerman, J.C.2
Brough, S.J.3
Scott, C.4
Porter, R.A.5
Herdon, H.J.6
-
12
-
-
79951994324
-
Orexin receptors: Pharmacology and therapeutic opportunities
-
Scammell, T.E., Winrow, C.J. Orexin receptors: Pharmacology and therapeutic opportunities. Annu Rev Pharmacol Toxicol 2011, 51: 243-66.
-
(2011)
Annu Rev Pharmacol Toxicol
, vol.51
, pp. 243-266
-
-
Scammell, T.E.1
Winrow, C.J.2
-
13
-
-
0036016118
-
The physiology and pharmacology of the orexins
-
Smart, D., Jerman, J. The physiology and pharmacology of the orexins. Pharmacol Ther 2002, 94(1-2): 51-61.
-
(2002)
Pharmacol Ther
, vol.94
, Issue.1-2
, pp. 51-61
-
-
Smart, D.1
Jerman, J.2
-
14
-
-
0037066586
-
Orexins and the treatment of obesity
-
Smart, D., Haynes, A.C, Williams, G., Arch, J.R. Orexins and the treatment of obesity. Eur J Pharmacol 2002, 440(2-3): 199-212.
-
(2002)
Eur J Pharmacol
, vol.440
, Issue.2-3
, pp. 199-212
-
-
Smart, D.1
Haynes, A.C.2
Williams, G.3
Arch, J.R.4
-
15
-
-
84863866948
-
Multiple roles for orexin/hypocretin in addiction
-
Mahler, S.V., Smith, R.J., Moorman, D.E., Sartor, G.C., Aston-Jones, G. Multiple roles for orexin/hypocretin in addiction. Prog Brain Res 2012, 198: 79-121.
-
(2012)
Prog Brain Res
, vol.198
, pp. 79-121
-
-
Mahler, S.V.1
Smith, R.J.2
Moorman, D.E.3
Sartor, G.C.4
Aston-Jones, G.5
-
16
-
-
68249099216
-
-
Owen, R.T., Castaner, R., Bolós, J., Estivill, C. Almorexant. Drugs Fut 2009, 34(1): 5-10.
-
(2009)
Almorexant. Drugs Fut
, vol.34
, Issue.1
, pp. 5-10
-
-
Owen, R.T.1
Castaner, R.2
Bolós, J.3
Estivill, C.4
-
17
-
-
84865603296
-
Update on emerging drugs for insomnia
-
Sullivan, S. Update on emerging drugs for insomnia. Expert Opin Emerg Drugs 2012, 17(3): 295-8.
-
(2012)
Expert Opin Emerg Drugs
, vol.17
, Issue.3
, pp. 295-298
-
-
Sullivan, S.1
-
18
-
-
84866431931
-
Molecule spotlight on suvorexant
-
Hopkins, C.R. Molecule spotlight on suvorexant. ACS Chem Neurosci 2012, 3(9): 647-8.
-
(2012)
ACS Chem Neurosci
, vol.3
, Issue.9
, pp. 647-648
-
-
Hopkins, C.R.1
-
19
-
-
84857757413
-
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, P.J., Schreier, J.D., Cox, C.D. et al. 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. ChemMedChem 2012, 7(3): 415-24
-
(2012)
ChemMedChem
, vol.7
, Issue.3
, pp. 415-424
-
-
Coleman, P.J.1
Schreier, J.D.2
Cox, C.D.3
-
20
-
-
84872713609
-
Convergent kilogram scale synthesis of dual orexin receptor antagonist
-
in print
-
Girardin, M., Ouellet, S.G., Gauvreau, D. et al. Convergent kilogram scale synthesis of dual orexin receptor antagonist. Org Process Res Dev 2012, 17: in print.
-
(2012)
Org Process Res Dev
, pp. 17
-
-
Girardin, M.1
Ouellet, S.G.2
Gauvreau, D.3
-
21
-
-
84930536781
-
Preclinical characterization of MK-4305 - A novel dual orexin receptor antagonist for insomnia
-
Winrow, C., Coleman, P., Cox, C. et al. Preclinical characterization of MK- 4305 - A novel dual orexin receptor antagonist for insomnia. J Sleep Res 2010, 19(Suppl. 2): 195.
-
(2010)
J Sleep Res
, vol.19
, Issue.SUPPL. 2
, pp. 195
-
-
Winrow, C.1
Coleman, P.2
Cox, C.3
-
22
-
-
84930537027
-
Preclinical efficacy of suvorexant and other orexin receptor antagonists
-
Winrow, C.J., Kuduk, S., Doran, S.M. et al. Preclinical efficacy of suvorexant and other orexin receptor antagonists. Sleep Biol Rhythms 2011, 9(4): 332.
-
(2011)
Sleep Biol Rhythms
, vol.9
, Issue.4
, pp. 332
-
-
Winrow, C.J.1
Kuduk, S.2
Doran, S.M.3
-
23
-
-
79951991696
-
Discovery of MK-4305: A novel orexin receptor antagonist for the treatment of insomnia
-
March 21-25, San Francisco , Abst MEDI 37
-
Coleman, P.J., Cox, C.D., Breslin, M.J. et al. Discovery of MK-4305: A novel orexin receptor antagonist for the treatment of insomnia. 239th ACS Natl Meet (March 21-25, San Francisco) 2010, Abst MEDI 37.
-
(2010)
239th ACS Natl Meet
-
-
Coleman, P.J.1
Cox, C.D.2
Breslin, M.J.3
-
24
-
-
79956003278
-
Promotion of sleep by suvorexant - A novel dual orexin receptor antagonist
-
Winrow, C.J., Gotter, A.L., Cox, C.D. et al. Promotion of sleep by suvorexant - A novel dual orexin receptor antagonist. J Neurogenet 2011, 25(1-2): 52-61.
-
(2011)
J Neurogenet
, vol.25
, Issue.1-2
, pp. 52-61
-
-
Winrow, C.J.1
Gotter, A.L.2
Cox, C.D.3
-
25
-
-
84869777944
-
The single dose pharmacokinetic (PK) and pharmacodynamic (PD) profiles of suvorexant (MK-4305), a dual orexin receptor antagonist, in healthy male subjects
-
March 12-17, National Harbor
-
Sun, H., Kennedy, D., Lewis, N. et al. The single dose pharmacokinetic (PK) and pharmacodynamic (PD) profiles of suvorexant (MK-4305), a dual orexin receptor antagonist, in healthy male subjects. 113th Annu Meet Am Soc Clin Pharmacol Ther (ASCPT) (March 12-17, National Harbor) 2012, Abst PI-59
-
(2012)
113th Annu Meet Am Soc Clin Pharmacol Ther (ASCPT)
-
-
Sun, H.1
Kennedy, D.2
Lewis, N.3
-
26
-
-
84871314496
-
The single dose pharmacokinetic and pharmacodynamic profiles of suvorexant (MK-4305), a dual orexin receptor antagonist, in healthy male subjects
-
Sun, H., Kennedy, W.D., Lewis, N. et al. The single dose pharmacokinetic and pharmacodynamic profiles of suvorexant (MK-4305), a dual orexin receptor antagonist, in healthy male subjects. Sleep Biol Rhythms 2011, 9(4): 332.
-
(2011)
Sleep Biol Rhythms
, vol.9
, Issue.4
, pp. 332
-
-
Sun, H.1
Kennedy, W.D.2
Lewis, N.3
-
27
-
-
84871293418
-
Dose effects of MK-4305, a dual orexin receptor antagonist for insomnia, in healthy male subjects
-
Sun, H., Kennedy, W., Lewis, N. et al. Dose effects of MK-4305, a dual orexin receptor antagonist for insomnia, in healthy male subjects. J Sleep Res 2010, 19(Suppl. 2): 199-200.
-
(2010)
J Sleep Res
, vol.19
, Issue.SUPPL. 2
, pp. 199-200
-
-
Sun, H.1
Kennedy, W.2
Lewis, N.3
-
28
-
-
84855935700
-
Efficacy and tolerability of the dual orexin receptor antagonist MK-4305 in patients with primary insomnia: Randomized, controlled, adaptive crossover polysomnography study
-
June 5-9, San Antonio, Abst 0591
-
Herring, W.J., Budd, K.S., Hutzelmann, J. et al. Efficacy and tolerability of the dual orexin receptor antagonist MK-4305 in patients with primary insomnia: Randomized, controlled, adaptive crossover polysomnography study. 24th Annu Meet Assoc Sleep Soc (June 5-9, San Antonio) 2010, Abst 0591.
-
(2010)
24th Annu Meet Assoc Sleep Soc
-
-
Herring, W.J.1
Budd, K.S.2
Hutzelmann, J.3
-
29
-
-
84930542922
-
Efficacy and tolerability of the dual orexin receptor antagonist MK-4305 in patients with primary insomnia: A randomized, controlled, adaptive crossover polysomnography study
-
Herring, W.J., Budd, K., Hutzelmann, J. et al. Efficacy and tolerability of the dual orexin receptor antagonist MK-4305 in patients with primary insomnia: A randomized, controlled, adaptive crossover polysomnography study. J Sleep Res 2010, 19(Suppl. 2): 44-5.
-
(2010)
J Sleep Res
, vol.19
, Issue.SUPPL. 2
, pp. 44-45
-
-
Herring, W.J.1
Budd, K.2
Hutzelmann, J.3
-
30
-
-
84871323368
-
Orexin receptor antagonism for treatment of insomnia: A randomized clinical trial of suvorexant
-
Herring, W.J., Snyder, E., Budd, K. et al. Orexin receptor antagonism for treatment of insomnia: A randomized clinical trial of suvorexant. Neurology 2012, 79(23): 2265-74.
-
(2012)
Neurology
, vol.79
, Issue.23
, pp. 2265-2274
-
-
Herring, W.J.1
Snyder, E.2
Budd, K.3
-
31
-
-
84883554497
-
Efficacy and safety of suvorexant, an orexin receptor antagonist, in patients with primary insomnia: A 3- month phase 3 trial (trial #1)
-
Sept 4-8, Paris, Abst O-324
-
Connor, K., Budd, K., Snavely, D. et al. Efficacy and safety of suvorexant, an orexin receptor antagonist, in patients with primary insomnia: A 3- month phase 3 trial (trial #1). 21st Congr Eur Sleep Res Soc (ESRS) (Sept 4-8, Paris) 2012, Abst O-324.
-
(2012)
21st Congr Eur Sleep Res Soc (ESRS)
-
-
Connor, K.1
Budd, K.2
Snavely, D.3
-
32
-
-
84888008390
-
Efficacy and safety of suvorexant, an orexin receptor antagonist, in patients with primary insomnia: A 3-month phase 3 trial (trial #2)
-
Sept 4-8, Paris, Abst P-988
-
Ivgy-May, N., Liebensperger, H., Froman, S. et al. Efficacy and safety of suvorexant, an orexin receptor antagonist, in patients with primary insomnia: A 3-month phase 3 trial (trial #2). 21st Congr Eur Sleep Res Soc (ESRS) (Sept 4-8, Paris) 2012, Abst P-988.
-
(2012)
21st Congr Eur Sleep Res Soc (ESRS)
-
-
Ivgy-May, N.1
Liebensperger, H.2
Froman, S.3
-
33
-
-
84874673284
-
Efficacy and safety of suvorexant, a dual orexin receptor antagonist, in patients with primary insomnia: Results from two pivotal trials
-
June 9-16, Boston, Abst LBA4
-
Herring, W.J., Connor, K., Ivgy-May, N. et al. Efficacy and safety of suvorexant, a dual orexin receptor antagonist, in patients with primary insomnia: Results from two pivotal trials. 26th Annu Meet Assoc Profess Sleep Soc (June 9-16, Boston) 2012, Abst LBA4.
-
(2012)
26th Annu Meet Assoc Profess Sleep Soc
-
-
Herring, W.J.1
Connor, K.2
Ivgy-May, N.3
-
34
-
-
84887993171
-
Suvorexant, an orexin receptor antagonist, in preventing symptom return in patients with insomnia after 1 year of treatment: A randomised, double-blind, placebo-controlled study
-
Sept 4-8, Paris, Abst P-987
-
Herring, W.J., Snyder, E., Paradis, E. et al. Suvorexant, an orexin receptor antagonist, in preventing symptom return in patients with insomnia after 1 year of treatment: A randomised, double-blind, placebo-controlled study. 21st Congr Eur Sleep Res Soc (ESRS) (Sept 4-8, Paris) 2012, Abst P-987.
-
(2012)
21st Congr Eur Sleep Res Soc (ESRS)
-
-
Herring, W.J.1
Snyder, E.2
Paradis, E.3
-
35
-
-
84883554920
-
Long term safety and efficacy of suvorexant in patients with primary insomnia
-
June 9-16, Boston, Abst 0641
-
Herring, W.J, Snyder, E., Paradis, E., Liu, M., Snavely, D., Roth, T., Michelson, D. Long term safety and efficacy of suvorexant in patients with primary insomnia. 26th Annu Meet Assoc Profess Sleep Soc (June 9-16, Boston) 2012, Abst 0641.
-
(2012)
26th Annu Meet Assoc Profess Sleep Soc
-
-
Herring, W.J.1
Snyder, E.2
Paradis, E.3
Liu, M.4
Snavely, D.5
Roth, T.6
Michelson, D.7
-
36
-
-
84869794468
-
Power spectral profile of the orexin receptor antagonist suvorexant (MK-4305) in primary insomnia patients and healthy-subjects
-
Herring, W.J., Ma, J.S., Snyder, E. et al. Power spectral profile of the orexin receptor antagonist suvorexant (MK-4305) in primary insomnia patients and healthy-subjects. Biol Psychiatry 2012, 74(8): A942.
-
(2012)
Biol Psychiatry
, vol.74
, Issue.8
-
-
Herring, W.J.1
Ma, J.S.2
Snyder, E.3
-
39
-
-
84930541676
-
Hypocretin/orexin receptor antagonism and the promise of anticraving medications: Myth or panacea?
-
Boutrel, B. Hypocretin/orexin receptor antagonism and the promise of anticraving medications: Myth or panacea? J Addict Res Ther 2011, S4: 5-10.
-
(2011)
J Addict Res Ther
, pp. 5-10
-
-
Boutrel, B.1
-
40
-
-
79959292812
-
Orexin receptor targets for anti-relapse medication development in drug addiction
-
Zhou, L., Sun, W.-L., See, R.E. Orexin receptor targets for anti-relapse medication development in drug addiction. Pharmaceuticals 2011, (4): 804-21.
-
(2011)
Pharmaceuticals
, vol.4
, pp. 804-821
-
-
Zhou, L.1
Sun, W.-L.2
See, R.E.3
|