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Volumn 8, Issue 11, 2008, Pages 977-987

Orexin receptor antagonists: Medicinal chemistry and therapeutic potential

Author keywords

Almorexant; Cataplexy; GPCR; Hypocretin; Insomnia; Orexin; OX1R; OX2R

Indexed keywords

1 (2 METHYL 6 BENZOXAZOLYL) 3 (1,5 NAPHTHYRIDIN 4 YL)UREA; 4 PHENYL 1,3 DIOXANE UREA DERIVATIVE; ACT 078573; ALMOREXANT; BENZAZEPINE DERIVATIVE; BENZIMIDAZOLE DERIVATIVE; GW 649898; NEUROPEPTIDE; OREXIN; OREXIN 1 RECEPTOR; OREXIN 2 RECEPTOR; OREXIN A; OREXIN B; OREXIN RECEPTOR ANTAGONIST; PYRAZOLE DERIVATIVE; RECEPTOR BLOCKING AGENT; SB 649868; SB 674042; SEDATIVE AGENT; TETRAHYDROISOQUINOLINE DERIVATIVE; UREA DERIVATIVE; ZOLPIDEM;

EID: 48249109864     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/156802608784936746     Document Type: Review
Times cited : (81)

References (45)
  • 1
    • 37549065569 scopus 로고    scopus 로고
    • Orexin neuronal circuitry: Role of the regulation of sleep and wakefulness
    • Ohno, K.; Sakurai, T. Orexin neuronal circuitry: Role of the regulation of sleep and wakefulness. Frontiers in Neuroendocrinology 2009, 29, 70-87.
    • (2009) Frontiers in Neuroendocrinology , vol.29 , pp. 70-87
    • Ohno, K.1    Sakurai, T.2
  • 6
    • 25644432796 scopus 로고    scopus 로고
    • A role for lateral hypothalamic orexin neurons in reward seeking
    • (b) Harris, G. C. Wimmer, M.; Aston-Jones, G. A role for lateral hypothalamic orexin neurons in reward seeking. Nature 2005, 437, 556-559.
    • (2005) Nature , vol.437 , pp. 556-559
    • Harris, G.C.1    Wimmer, M.2    Aston-Jones, G.3
  • 11
    • 48249112686 scopus 로고    scopus 로고
    • Actelion presentations, World Sleep Congress, Cairns, Australia, September 3-6, 2007.
    • Actelion presentations, World Sleep Congress, Cairns, Australia, September 3-6, 2007.
  • 12
    • 48249110039 scopus 로고    scopus 로고
    • Investor update
    • see
    • Ratti, E. GlaxoSmithKline: Investor update 2007, see: http://www.gsk.com/investors/presentations_webcasts07.htm.
    • (2007)
    • Ratti1    GlaxoSmithKline, E.2
  • 13
    • 33646543700 scopus 로고    scopus 로고
    • Antagoinsts of the orexin receptor
    • For reviews concerning setective orexin ligand, see: a
    • For reviews concerning setective orexin ligand, see: (a) Cai, J.; Cooke, F. E.; Sherborne, B. S. Antagoinsts of the orexin receptor. Expert Opin. Ther. Patents 2006, 16, 631-646
    • (2006) Expert Opin. Ther. Patents , vol.16 , pp. 631-646
    • Cai, J.1    Cooke, F.E.2    Sherborne, B.S.3
  • 14
    • 33748597939 scopus 로고    scopus 로고
    • Eating, sleeping and rewarding: Orexin receptors and their antagonists
    • (b) Bingham, M. J.; Cai, J.; Dechan, M. R. Eating, sleeping and rewarding: Orexin receptors and their antagonists. Curr. Opin. Disc. Dev. 2006, 9, 551-559.
    • (2006) Curr. Opin. Disc. Dev , vol.9 , pp. 551-559
    • Bingham, M.J.1    Cai, J.2    Dechan, M.R.3
  • 15
    • 48249115274 scopus 로고    scopus 로고
    • Compounds described in figures and tables of this manuscript were selected on the basis of data reported either in the primary literature or in patent publications.
    • Compounds described in figures and tables of this manuscript were selected on the basis of data reported either in the primary literature or in patent publications.
  • 16
    • 48249090150 scopus 로고    scopus 로고
    • Aissoui, H, Clozel, M, Weller, T, Koberstein, R, Sifferlen, T, Fischli, W, Actelion Pharmaceuticals Ltd, The sulfonylamino-acetic acid derivatives, WO-2004033418 2004
    • (a) Aissoui, H.; Clozel, M.; Weller, T.; Koberstein, R.; Sifferlen, T.; Fischli, W. (Actelion Pharmaceuticals Ltd.) The sulfonylamino-acetic acid derivatives, WO-2004033418 (2004).
  • 17
    • 48249114134 scopus 로고    scopus 로고
    • Aissaoui, H, Boss, C, Gude, M, Koberstein, R, Sifferlen, T, Zumbrunn Ackline, C, Actelion Pharmaceuticals Ltd, Novel sulfonamide compounds, WO-2007116374 2007
    • (b) Aissaoui, H.; Boss, C.; Gude, M.; Koberstein, R.; Sifferlen, T.; Zumbrunn Ackline, C. (Actelion Pharmaceuticals Ltd.) Novel sulfonamide compounds, WO-2007116374 (2007).
  • 18
    • 48249092384 scopus 로고    scopus 로고
    • Aissaoui, H.; Clozel, M.; Fischli, W.; Koberstein, R.; Sifferlen, T. (Actelion Pharmaceuticals Ltd.) 7,8,9,10-Tetrahydro-6H-azepino, 6,7,8,9-letrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-B]- quinazolinone derivatives, WO-2004004733 (2004)
    • Aissaoui, H.; Clozel, M.; Fischli, W.; Koberstein, R.; Sifferlen, T. (Actelion Pharmaceuticals Ltd.) 7,8,9,10-Tetrahydro-6H-azepino, 6,7,8,9-letrahydro-pyrido and 2,3-dihydro-2H-pyrrolo[2,1-B]- quinazolinone derivatives, WO-2004004733 (2004)
  • 19
    • 48249133348 scopus 로고    scopus 로고
    • Aissoui, H, Clozel, M, Welter, T, Koberstien, R, Sifferlen, T, Fischli, W, Actelion Pharmaceuticals Ltd, Novel benzazepines and related heterocyclic derivatives which are useful as orexin receptor antagonists, WO-02051838 2002
    • Aissoui, H.; Clozel, M.; Welter, T.; Koberstien, R.; Sifferlen, T.; Fischli, W. (Actelion Pharmaceuticals Ltd.) Novel benzazepines and related heterocyclic derivatives which are useful as orexin receptor antagonists, WO-02051838 (2002).
  • 23
    • 34249695940 scopus 로고    scopus 로고
    • Tafti, M. Reply to Promotion of sleep by targeting the orexin system in rats, dogs, and humans. Nat. Med. 2007, 13, 525-526.
    • Tafti, M. Reply to "Promotion of sleep by targeting the orexin system in rats, dogs, and humans". Nat. Med. 2007, 13, 525-526.
  • 24
    • 48249101375 scopus 로고    scopus 로고
    • Entry-into-humans study with almorexant (ACT-078573), a dual orexin receptor antagonist: Tolerability, safety, and pharmacokineties
    • Cairns, Australia, September 3-6
    • (a) Hoever, P.; de Haas, S.; Winkler, J.; Cavallaro, M.; van Gerven, J.; Dingemanse, J. Entry-into-humans study with almorexant (ACT-078573), a dual orexin receptor antagonist: Tolerability, safety, and pharmacokineties, World Sleep Congress Poster Presentation, Cairns, Australia, September 3-6, 2007.
    • (2007) World Sleep Congress Poster Presentation
    • Hoever, P.1    de Haas, S.2    Winkler, J.3    Cavallaro, M.4    van Gerven, J.5    Dingemanse, J.6
  • 25
    • 48249101375 scopus 로고    scopus 로고
    • Entry-nito-humans study with almorexant (ACT-078573), a dual orexin receptor antagonist: Pharmacodynamics
    • Cairns, Australia, September 3-6
    • (b) Hoever, P.; de Haas, S.; Choissi, E.; van Gerven, J.; Dingemanse, J. Entry-nito-humans study with almorexant (ACT-078573), a dual orexin receptor antagonist: Pharmacodynamics, World Sleep Congress Poster Presentation, Cairns, Australia, September 3-6, 2007.
    • (2007) World Sleep Congress Poster Presentation
    • Hoever, P.1    de Haas, S.2    Choissi, E.3    van Gerven, J.4    Dingemanse, J.5
  • 27
    • 48249139154 scopus 로고    scopus 로고
    • Chan, G, Johns, A, Jurewicz, A, Porter, R. A, Widdowson, K, SmithKline Beecham PLC) Phenyl urea and phenyl thiourea derivatives as HFGAN72 antagonists, WO-199909024 1999
    • (a) Chan, G.; Johns, A.; Jurewicz, A.; Porter, R. A.; Widdowson, K. (SmithKline Beecham PLC) Phenyl urea and phenyl thiourea derivatives as HFGAN72 antagonists, WO-199909024 (1999)
  • 28
    • 48249088584 scopus 로고    scopus 로고
    • Johns, A, Porter, R. A, SmithKline Beecham PLC) Phenyl urea and phenyl thiourea derivatives, WO-199958533 1999
    • (b) Johns, A.; Porter, R. A. (SmithKline Beecham PLC) Phenyl urea and phenyl thiourea derivatives, WO-199958533 (1999).
  • 29
    • 48249142482 scopus 로고    scopus 로고
    • For representative GSK patents, see: (a) Coulton, S, Johns, A, Porter, R. A, SmithKline Beecham PLC) Preparation of phenyl urea and phenyl thiourea derivatives as orexin receptor antagonist, WO-2000047577 2000
    • For representative GSK patents, see: (a) Coulton, S.; Johns, A.; Porter, R. A. (SmithKline Beecham PLC) Preparation of phenyl urea and phenyl thiourea derivatives as orexin receptor antagonist, WO-2000047577 (2000);
  • 30
    • 48249131753 scopus 로고    scopus 로고
    • Coulton, S, Johns, A, Porter, R. A, SmithKline Beecham PLC) Preparation of ethylene diamine derivatives as orexin receptor antagonists, WO-2003051872 (2003, c) Branch, C. L, Johnson, C. N, Stemp, G, Thewlis, K, SmithKline Beecham PLC) Preparation of piperidines as orexin receptor antagonists, WO-2001096302 2001
    • (b) Coulton, S.; Johns, A.; Porter, R. A. (SmithKline Beecham PLC) Preparation of ethylene diamine derivatives as orexin receptor antagonists, WO-2003051872 (2003); (c) Branch, C. L.; Johnson, C. N.; Stemp, G.; Thewlis, K. (SmithKline Beecham PLC) Preparation of piperidines as orexin receptor antagonists, WO-2001096302 (2001).
  • 32
    • 0034704445 scopus 로고    scopus 로고
    • Haynes, A. C-; Jackson, B.; Chapman, H.; Tadyyon, M.; Johns, A.; Porter, R. A.; Arch, J. R. A selective orexin-1 receptor antagonist reduces food consumption in male and female rats. Regul. Pept. 2000, 96, 45-51;
    • (a) Haynes, A. C-; Jackson, B.; Chapman, H.; Tadyyon, M.; Johns, A.; Porter, R. A.; Arch, J. R. A selective orexin-1 receptor antagonist reduces food consumption in male and female rats. Regul. Pept. 2000, 96, 45-51;
  • 34
    • 11444255624 scopus 로고    scopus 로고
    • Anorexia and weight loss in male rats 24 hours following single dose treatment with orexin-1 receptor antagonist SB-334867
    • (c) Ishii, Y.; Blundell, J. E.; Halford, J. C.; Upton, N.; Porter, R.; Johns, A.; Summerfield, S.; Rogers, R. J. Anorexia and weight loss in male rats 24 hours following single dose treatment with orexin-1 receptor antagonist SB-334867. Behav. Brain Res. 2005, 157, 331-341.
    • (2005) Behav. Brain Res , vol.157 , pp. 331-341
    • Ishii, Y.1    Blundell, J.E.2    Halford, J.C.3    Upton, N.4    Porter, R.5    Johns, A.6    Summerfield, S.7    Rogers, R.J.8
  • 36
    • 48249106752 scopus 로고    scopus 로고
    • Ratti, E. GlaxoSmithKline, Investor update 2004, see: Http://www.gsk.com/investors/presentations_webcasts04.htm.
    • Ratti, E. GlaxoSmithKline, Investor update 2004, see: Http://www.gsk.com/investors/presentations_webcasts04.htm.
  • 38
    • 0035987203 scopus 로고    scopus 로고
    • Evaluation of drug interactions with P-glycoprotein in drug discovery: In vitro assessment of the potential for drug-drug interactions with P-glycoprotein
    • For reviews on the relevance of Pgp to drug discovery, see: a
    • For reviews on the relevance of Pgp to drug discovery, see: (a) Hochman, J. H.; Yamazaki, M.; Ohe, T.; Lin, J. H. Evaluation of drug interactions with P-glycoprotein in drug discovery: In vitro assessment of the potential for drug-drug interactions with P-glycoprotein. Curr. Drug Metab. 2002, 3, 257-273;
    • (2002) Curr. Drug Metab , vol.3 , pp. 257-273
    • Hochman, J.H.1    Yamazaki, M.2    Ohe, T.3    Lin, J.H.4
  • 39
    • 0347623323 scopus 로고    scopus 로고
    • Clinical relevance of P-glycoprotein in drug therapy
    • (b) Lin, J. H.; Yamakazi, M. Clinical relevance of P-glycoprotein in drug therapy. Drug Metab. Rev. 2003, 35, 417-454
    • (2003) Drug Metab. Rev , vol.35 , pp. 417-454
    • Lin, J.H.1    Yamakazi, M.2
  • 40
    • 0344927037 scopus 로고    scopus 로고
    • Hirose, M.; Egashira, S.; Goto, Y. Takashi, H.; Ohtake, N.; Iwaasa, H.; Hata, M.; Fukami, T.; Kanatani, A,; Yamada, K. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist. Bioorg. Med. Chem. Lett. 2003, 13, 4497-4499.
    • Hirose, M.; Egashira, S.; Goto, Y. Takashi, H.; Ohtake, N.; Iwaasa, H.; Hata, M.; Fukami, T.; Kanatani, A,; Yamada, K. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist. Bioorg. Med. Chem. Lett. 2003, 13, 4497-4499.
  • 41
    • 48249084668 scopus 로고    scopus 로고
    • Aranyi, P.; Balogh, M.; Batori, S.; Bence, J.; Finet, M.; Kapui, Z.; Philippo, C.; Szabo, T.; Szlavik, Z.; Tomoskozi, Z.; Urban-Szabo, K.; Venier, O. (Sanofi-Aventis) Pyrimidine derivatives as orexin receptor antagonists. WO2005075458 (2005).
    • Aranyi, P.; Balogh, M.; Batori, S.; Bence, J.; Finet, M.; Kapui, Z.; Philippo, C.; Szabo, T.; Szlavik, Z.; Tomoskozi, Z.; Urban-Szabo, K.; Venier, O. (Sanofi-Aventis) Pyrimidine derivatives as orexin receptor antagonists. WO2005075458 (2005).
  • 42
    • 48249156305 scopus 로고    scopus 로고
    • Aletru, M.; Aranyi, P.; Balogh, M.; Batori, S.; Bence, J.; Bovy, P.; Kapui, Z.; Mikus, E.; Namane, C,; Philippo, C.; Szabo, T.; Tomoskozi, Z.; Urban-Szabo, K. (Sanofi-Aventis) Pyrazole derivatives and use thereof as orexin receptor antagonists. WO2005060959 (2005).
    • Aletru, M.; Aranyi, P.; Balogh, M.; Batori, S.; Bence, J.; Bovy, P.; Kapui, Z.; Mikus, E.; Namane, C,; Philippo, C.; Szabo, T.; Tomoskozi, Z.; Urban-Szabo, K. (Sanofi-Aventis) Pyrazole derivatives and use thereof as orexin receptor antagonists. WO2005060959 (2005).
  • 43
    • 48249141526 scopus 로고    scopus 로고
    • Courte-Manche, G.; Despeyroux, P.; Fontaine, E.; Rochard, P.; Serradeil Le Gal, C. (Sanofi-Aventis) Sulfonamide derivatives, their preparation and their therapeutic application, WO2006024779 (2006);
    • (a) Courte-Manche, G.; Despeyroux, P.; Fontaine, E.; Rochard, P.; Serradeil Le Gal, C. (Sanofi-Aventis) Sulfonamide derivatives, their preparation and their therapeutic application, WO2006024779 (2006);
  • 44
    • 48249150060 scopus 로고    scopus 로고
    • Despeyroux, P.; Fontaine, E.; Courte-Manche, G.; Rochard, P.; Serradeil-Le Gal, C. (Sanofi-Aventis) Sulfonamide derivatives, preparation thereof and therapeutic application, WO2007085718 (2007).
    • (b) Despeyroux, P.; Fontaine, E.; Courte-Manche, G.; Rochard, P.; Serradeil-Le Gal, C. (Sanofi-Aventis) Sulfonamide derivatives, preparation thereof and therapeutic application, WO2007085718 (2007).


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