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For: 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. 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. J Med Chem 2015;58:4648-64. [PMID: 25953512 DOI: 10.1021/acs.jmedchem.5b00217] [Cited by in Crossref: 43] [Cited by in F6Publishing: 36] [Article Influence: 6.1] [Reference Citation Analysis]
Number Citing Articles
1 Beuckmann CT, Suzuki H, Musiek ES, Ueno T, Sato T, Bando M, Osada Y, Moline M. Evaluation of SAMP8 Mice as a Model for Sleep-Wake and Rhythm Disturbances Associated with Alzheimer's Disease: Impact of Treatment with the Dual Orexin (Hypocretin) Receptor Antagonist Lemborexant. J Alzheimers Dis 2021;81:1151-67. [PMID: 33843668 DOI: 10.3233/JAD-201054] [Reference Citation Analysis]
2 Boss C, Roch C. Orexin research: patent news from 2016. Expert Opinion on Therapeutic Patents 2017;27:1123-33. [DOI: 10.1080/13543776.2017.1344221] [Cited by in Crossref: 7] [Cited by in F6Publishing: 6] [Article Influence: 1.4] [Reference Citation Analysis]
3 Jacobson LH, Chen S, Mir S, Hoyer D. Orexin OX2 Receptor Antagonists as Sleep Aids. In: Lawrence AJ, de Lecea L, editors. Behavioral Neuroscience of Orexin/Hypocretin. Cham: Springer International Publishing; 2017. pp. 105-36. [DOI: 10.1007/7854_2016_47] [Cited by in Crossref: 17] [Cited by in F6Publishing: 15] [Article Influence: 2.8] [Reference Citation Analysis]
4 Jacobson LH, Hoyer D, de Lecea L. Hypocretins (orexins): The ultimate translational neuropeptides. J Intern Med 2022. [PMID: 35043499 DOI: 10.1111/joim.13406] [Reference Citation Analysis]
5 Jana S, Sarkar S, Morris SA. Recent developments towards the synthesis of paroxetine: A 3,4-disubstituted piperidine. Tetrahedron 2020. [DOI: 10.1016/j.tet.2020.131215] [Cited by in Crossref: 3] [Cited by in F6Publishing: 1] [Article Influence: 1.5] [Reference Citation Analysis]
6 Landry I, Aluri J, Nakai K, Hall N, Miyajima Y, Ueno T, Dayal S, Filippov G, Lalovic B, Moline M, Reyderman L. Evaluation of the CYP3A and CYP2B6 Drug-Drug Interaction Potential of Lemborexant. Clin Pharmacol Drug Dev 2021;10:681-90. [PMID: 33455055 DOI: 10.1002/cpdd.915] [Cited by in Crossref: 3] [Cited by in F6Publishing: 4] [Article Influence: 3.0] [Reference Citation Analysis]
7 Takada S, Saito T, Iwata K, Nishii Y. Copper-Catalyzed 1,5-Addition of Grignard reagents to Enantioenriched Donor-Acceptor Cyclopropanes with Inversion. Asian J Org Chem 2016;5:1225-9. [DOI: 10.1002/ajoc.201600313] [Cited by in Crossref: 7] [Cited by in F6Publishing: 3] [Article Influence: 1.2] [Reference Citation Analysis]
8 Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K. Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation. Nat Commun 2021;12:815. [PMID: 33547286 DOI: 10.1038/s41467-021-21087-6] [Cited by in Crossref: 6] [Cited by in F6Publishing: 4] [Article Influence: 6.0] [Reference Citation Analysis]
9 Han Y, Yuan K, Zheng Y, Lu L. Orexin Receptor Antagonists as Emerging Treatments for Psychiatric Disorders. Neurosci Bull 2020;36:432-48. [PMID: 31782044 DOI: 10.1007/s12264-019-00447-9] [Cited by in Crossref: 14] [Cited by in F6Publishing: 11] [Article Influence: 4.7] [Reference Citation Analysis]
10 Ueno T, Ishida T, Aluri J, Suzuki M, Beuckmann CT, Kameyama T, Asakura S, Kusano K. Disposition and Metabolism of [ 14 C]Lemborexant in Healthy Human Subjects and Characterization of Its Circulating Metabolites. Drug Metab Dispos 2020;49:31-8. [DOI: 10.1124/dmd.120.000229] [Cited by in Crossref: 5] [Cited by in F6Publishing: 5] [Article Influence: 2.5] [Reference Citation Analysis]
11 Beuckmann CT, Ueno T, Nakagawa M, Suzuki M, Akasofu S. Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation. Sleep 2019;42:zsz076. [PMID: 30923834 DOI: 10.1093/sleep/zsz076] [Cited by in Crossref: 14] [Cited by in F6Publishing: 14] [Article Influence: 7.0] [Reference Citation Analysis]
12 Dale NC, Hoyer D, Jacobson LH, Pfleger KDG, Johnstone EKM. Orexin Signaling: A Complex, Multifaceted Process. Front Cell Neurosci 2022;16:812359. [DOI: 10.3389/fncel.2022.812359] [Reference Citation Analysis]
13 Hoyer D, Jacobson LH. Orexin Receptor Antagonists. Curr Sleep Medicine Rep 2017;3:342-53. [DOI: 10.1007/s40675-017-0099-7] [Cited by in Crossref: 1] [Cited by in F6Publishing: 1] [Article Influence: 0.2] [Reference Citation Analysis]
14 Yuan S, Yu B, Liu H. New drug approvals for 2019: Synthesis and clinical applications. European Journal of Medicinal Chemistry 2020;205:112667. [DOI: 10.1016/j.ejmech.2020.112667] [Cited by in Crossref: 6] [Cited by in F6Publishing: 3] [Article Influence: 3.0] [Reference Citation Analysis]
15 Landry I, Nakai K, Ferry J, Aluri J, Hall N, Lalovic B, Moline ML. Pharmacokinetics, Pharmacodynamics, and Safety of the Dual Orexin Receptor Antagonist Lemborexant: Findings From Single-Dose and Multiple-Ascending-Dose Phase 1 Studies in Healthy Adults. Clin Pharmacol Drug Dev 2021;10:153-65. [PMID: 32468649 DOI: 10.1002/cpdd.817] [Cited by in Crossref: 11] [Cited by in F6Publishing: 12] [Article Influence: 5.5] [Reference Citation Analysis]
16 Boof M, Alatrach A, Ufer M, Dingemanse J. Interaction potential of the dual orexin receptor antagonist ACT-541468 with CYP3A4 and food: results from two interaction studies. Eur J Clin Pharmacol 2019;75:195-205. [DOI: 10.1007/s00228-018-2559-5] [Cited by in Crossref: 12] [Cited by in F6Publishing: 12] [Article Influence: 3.0] [Reference Citation Analysis]
17 Biernacki K, Daśko M, Ciupak O, Kubiński K, Rachon J, Demkowicz S. Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery. Pharmaceuticals (Basel) 2020;13:E111. [PMID: 32485996 DOI: 10.3390/ph13060111] [Cited by in Crossref: 19] [Cited by in F6Publishing: 12] [Article Influence: 9.5] [Reference Citation Analysis]
18 Hoyer D, Allen A, Jacobson LH. Hypnotics with novel modes of action. Br J Clin Pharmacol 2020;86:244-9. [PMID: 31756268 DOI: 10.1111/bcp.14180] [Cited by in Crossref: 11] [Cited by in F6Publishing: 7] [Article Influence: 5.5] [Reference Citation Analysis]
19 Brotschi C, Roch C, Gatfield J, Treiber A, Williams JT, Sifferlen T, Heidmann B, Jenck F, Bolli MH, Boss C. Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep‐Promoting Properties in Rats. ChemMedChem 2019;14:1257-70. [DOI: 10.1002/cmdc.201900242] [Cited by in Crossref: 3] [Cited by in F6Publishing: 3] [Article Influence: 1.0] [Reference Citation Analysis]
20 Clemenceau A, Thesmar P, Gicquel M, Le Flohic A, Baudoin O. Direct Synthesis of Cyclopropanes from gem -Dialkyl Groups through Double C–H Activation. J Am Chem Soc 2020;142:15355-61. [DOI: 10.1021/jacs.0c05887] [Cited by in Crossref: 13] [Cited by in F6Publishing: 5] [Article Influence: 6.5] [Reference Citation Analysis]
21 Herring WJ, Roth T, Krystal AD, Michelson D. Orexin receptor antagonists for the treatment of insomnia and potential treatment of other neuropsychiatric indications. J Sleep Res 2018;28. [DOI: 10.1111/jsr.12782] [Cited by in Crossref: 17] [Cited by in F6Publishing: 13] [Article Influence: 4.3] [Reference Citation Analysis]
22 Talele TT. The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules. J Med Chem 2016;59:8712-56. [PMID: 27299736 DOI: 10.1021/acs.jmedchem.6b00472] [Cited by in Crossref: 314] [Cited by in F6Publishing: 222] [Article Influence: 52.3] [Reference Citation Analysis]
23 Hino T, Saitoh T, Nagumo Y, Yamamoto N, Kutsumura N, Irukayama-Tomobe Y, Ishikawa Y, Tanimura R, Yanagisawa M, Nagase H. Design and synthesis of novel orexin 2 receptor agonists based on naphthalene skeleton. Bioorg Med Chem Lett 2022;:128530. [PMID: 35007725 DOI: 10.1016/j.bmcl.2022.128530] [Reference Citation Analysis]
24 Boss C, Gatfield J, Brotschi C, Heidmann B, Sifferlen T, von Raumer M, Schmidt G, Williams JT, Treiber A, Roch C. The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders. ChemMedChem 2020;15:2286-305. [PMID: 32937014 DOI: 10.1002/cmdc.202000453] [Cited by in Crossref: 4] [Cited by in F6Publishing: 3] [Article Influence: 2.0] [Reference Citation Analysis]
25 Thomasy HE, Opp MR. Hypocretin Mediates Sleep and Wake Disturbances in a Mouse Model of Traumatic Brain Injury. J Neurotrauma 2019;36:802-14. [PMID: 30136622 DOI: 10.1089/neu.2018.5810] [Cited by in Crossref: 15] [Cited by in F6Publishing: 12] [Article Influence: 3.8] [Reference Citation Analysis]
26 Mei H, Remete AM, Zou Y, Moriwaki H, Fustero S, Kiss L, Soloshonok VA, Han J. Fluorine-containing drugs approved by the FDA in 2019. Chinese Chemical Letters 2020;31:2401-13. [DOI: 10.1016/j.cclet.2020.03.050] [Cited by in Crossref: 49] [Cited by in F6Publishing: 19] [Article Influence: 24.5] [Reference Citation Analysis]
27 Scott LJ. Lemborexant: First Approval. Drugs 2020;80:425-32. [PMID: 32096020 DOI: 10.1007/s40265-020-01276-1] [Cited by in Crossref: 17] [Cited by in F6Publishing: 18] [Article Influence: 8.5] [Reference Citation Analysis]
28 Landry I, Aluri J, Hall N, Kumar D, Dayal S, Moline M, Reyderman L. Effect of gastric acid-reducing agents on the pharmacokinetics and efficacy of lemborexant. Pharmacol Res Perspect 2020;8:e00678. [PMID: 33135390 DOI: 10.1002/prp2.678] [Cited by in Crossref: 3] [Cited by in F6Publishing: 2] [Article Influence: 3.0] [Reference Citation Analysis]
29 Treiber A, de Kanter R, Roch C, Gatfield J, Boss C, von Raumer M, Schindelholz B, Muehlan C, van Gerven J, Jenck F. The Use of Physiology-Based Pharmacokinetic and Pharmacodynamic Modeling in the Discovery of the Dual Orexin Receptor Antagonist ACT-541468. J Pharmacol Exp Ther 2017;362:489-503. [DOI: 10.1124/jpet.117.241596] [Cited by in Crossref: 25] [Cited by in F6Publishing: 26] [Article Influence: 5.0] [Reference Citation Analysis]
30 Boss C, Roch C. Substituted cyclopentanes, tetrahydrofurans and pyrrolidines as orexin-1-receptor antagonists for treatment of various CNS disorders (WO2015/055994; WO2015/124932; WO2015/124934). Expert Opin Ther Pat 2016;26:409-15. [PMID: 26593218 DOI: 10.1517/13543776.2016.1124087] [Cited by in Crossref: 1] [Cited by in F6Publishing: 1] [Article Influence: 0.1] [Reference Citation Analysis]
31 Futamura A, Suzuki R, Tamura Y, Kawamoto H, Ohmichi M, Hino N, Tokumaru Y, Kirinuki S, Hiyoshi T, Aoki T, Kambe D, Nozawa D. Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia. Bioorganic & Medicinal Chemistry 2020;28:115489. [DOI: 10.1016/j.bmc.2020.115489] [Cited by in Crossref: 1] [Cited by in F6Publishing: 1] [Article Influence: 0.5] [Reference Citation Analysis]
32 Roecker AJ, Cox CD, Coleman PJ. Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. J Med Chem 2016;59:504-30. [PMID: 26317591 DOI: 10.1021/acs.jmedchem.5b00832] [Cited by in Crossref: 62] [Cited by in F6Publishing: 55] [Article Influence: 8.9] [Reference Citation Analysis]
33 Zammit G, Krystal A. Evaluating lemborexant for the treatment of insomnia. Expert Opin Pharmacother 2021;22:1235-43. [PMID: 33711243 DOI: 10.1080/14656566.2021.1902987] [Reference Citation Analysis]
34 Vermeeren A, Jongen S, Murphy P, Moline M, Filippov G, Pinner K, Perdomo C, Landry I, Majid O, Van Oers ACM, Van Leeuwen CJ, Ramaekers JG, Vuurman EFPM. On-the-road driving performance the morning after bedtime administration of lemborexant in healthy adult and elderly volunteers. Sleep 2019;42:zsy260. [PMID: 30597112 DOI: 10.1093/sleep/zsy260] [Cited by in Crossref: 24] [Cited by in F6Publishing: 19] [Article Influence: 12.0] [Reference Citation Analysis]
35 Brotschi C, Bolli MH, Gatfield J, Heidmann B, Jenck F, Roch C, Sifferlen T, Treiber A, Williams JT, Boss C. From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs. ChemMedChem 2020;15:430-48. [DOI: 10.1002/cmdc.201900618] [Cited by in Crossref: 1] [Cited by in F6Publishing: 1] [Article Influence: 0.5] [Reference Citation Analysis]
36 Bhagat KK, Biswas JP, Dutta S, Maiti D. Catalytic C−H Activation via Four‐Membered Metallacycle Intermediate. Helvetica Chimica Acta. [DOI: 10.1002/hlca.202100192] [Reference Citation Analysis]
37 Mieda M. The roles of orexins in sleep/wake regulation. Neuroscience Research 2017;118:56-65. [DOI: 10.1016/j.neures.2017.03.015] [Cited by in Crossref: 42] [Cited by in F6Publishing: 39] [Article Influence: 8.4] [Reference Citation Analysis]
38 Flick AC, Leverett CA, Ding HX, McInturff E, Fink SJ, Mahapatra S, Carney DW, Lindsey EA, DeForest JC, France SP, Berritt S, Bigi-Botterill SV, Gibson TS, Liu Y, O'Donnell CJ. Synthetic Approaches to the New Drugs Approved during 2019. J Med Chem 2021;64:3604-57. [PMID: 33783211 DOI: 10.1021/acs.jmedchem.1c00208] [Cited by in Crossref: 2] [Cited by in F6Publishing: 1] [Article Influence: 2.0] [Reference Citation Analysis]
39 Lindsay-scott PJ, Gallagher PT. Synthesis of heterocycles from arylacetonitriles: Powerful tools for medicinal chemists. Tetrahedron Letters 2017;58:2629-35. [DOI: 10.1016/j.tetlet.2017.05.089] [Cited by in Crossref: 11] [Article Influence: 2.2] [Reference Citation Analysis]
40 Rappas M, Ali AAE, Bennett KA, Brown JD, Bucknell SJ, Congreve M, Cooke RM, Cseke G, de Graaf C, Doré AS, Errey JC, Jazayeri A, Marshall FH, Mason JS, Mould R, Patel JC, Tehan BG, Weir M, Christopher JA. Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis. J Med Chem 2020;63:1528-43. [PMID: 31860301 DOI: 10.1021/acs.jmedchem.9b01787] [Cited by in Crossref: 16] [Cited by in F6Publishing: 14] [Article Influence: 8.0] [Reference Citation Analysis]
41 Yang D, Zhou Q, Labroska V, Qin S, Darbalaei S, Wu Y, Yuliantie E, Xie L, Tao H, Cheng J, Liu Q, Zhao S, Shui W, Jiang Y, Wang MW. G protein-coupled receptors: structure- and function-based drug discovery. Signal Transduct Target Ther 2021;6:7. [PMID: 33414387 DOI: 10.1038/s41392-020-00435-w] [Cited by in Crossref: 11] [Cited by in F6Publishing: 10] [Article Influence: 11.0] [Reference Citation Analysis]
42 Beuckmann CT, Suzuki M, Ueno T, Nagaoka K, Arai T, Higashiyama H. In Vitro and In Silico Characterization of Lemborexant (E2006), a Novel Dual Orexin Receptor Antagonist. J Pharmacol Exp Ther 2017;362:287-95. [PMID: 28559480 DOI: 10.1124/jpet.117.241422] [Cited by in Crossref: 26] [Cited by in F6Publishing: 26] [Article Influence: 5.2] [Reference Citation Analysis]
43 Ueno T, Ishida T, Kusano K. Disposition and metabolism of [ 14 C]lemborexant, a novel dual orexin receptor antagonist, in rats and monkeys. Xenobiotica 2019;49:688-97. [DOI: 10.1080/00498254.2018.1482509] [Cited by in Crossref: 7] [Cited by in F6Publishing: 7] [Article Influence: 1.8] [Reference Citation Analysis]