Histamine-3 receptor inverse agonists for the treatment of obesity: Validation of the target and identification of novel series

Chimia

Volumn 63, Issue 5, 2009, Pages 275-278

  Plancher, Jean Marc ^a   Pierson, Pascale David ^b   Freichel, Christian ^b   Arthur, Silvia Gatti Mac ^b   Hertel, Cornelia ^b   Huwyler, Jörg ^b   Mohr, Peter ^b   Nakagawa, Toshito ^b   Nettekoven, Matthias ^b   Raab, Susanne ^b   Richter, Hans ^b   Roche, Olivier ^b   Sarmiento, Rosa Maria Rodríguez ^b   Schmitt, Monique ^b   Schuler, Franz ^b   Takahashi, Tadakatsu ^b   Taylor, Sven ^b   Ullmer, Christoph ^b   Wiegand, Ruby ^b  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b NONE

Author keywords

HERG; Histamine 3 receptor; Inverse agonist; Obesity; Pharmacophore model

Indexed keywords

EID: 67649828099     PISSN: 00094293     EISSN: None     Source Type: Journal    
DOI: 10.2533/chimia.2009.275     Document Type: Article

References (29)

1. M. E. Parsons, C. R. Ganellin, Br. J. Pharmacol. 2006, 147, S127.
2. a) S. J. Hill, C. R. Ganellin, H. Timmerman, J.C. Schwartz, N. P. Shankley, J. M. Young, W. Schunack, R. Levi, H. L. Haas, Pharmacol. Rev. 1997, 49, 253
3. b) S. J. Offord, Clin. Pharmacol. Ther. 2002, 71, Abst WPIII-27 P83;
4. c) M. Harada, M. Terai, H. Maeno, Biochem.Pharmacol 1983, 32, 1635.
5. a) J.-M. Arrang, M. Garbarg, J.-C. Schwartz, Nature 1983, 302, 832
6. b) R. Leurs, P. Blandina, C. Tedford, H. Timmerman, Trends Pharmacol.Sci. 1998, 19, 177
7. c) R. Leurs, H. Timmerman, in 'The Histamine H3-Receptor: A Target for New Drugs', Ed. Elsevier, Amsterdam, 1998
8. d) H. Stark, J.-M. Arrang, X. Ligneau, M. Garbarg, C. R. Ganellin, J. C. Schwartz, W. Schunack, in 'The Histamine H3-receptor and its Ligands in Progress in Medicinal Chemistry', Ed. Elsevier, Amsterdam, 2001.
9. a) T. A. Esbenshade, G. B. Fox, M. D. Cowart, Mol. Interventions 2006, 6, 77
10. b) T. A. Esbenshade, K. E. Browman, R. S. Bitner, M. Strakhova, M. D. Cowart, J. D. Brioni, Brit. J.Pharmacol. 2008, 1.
11. A. A. Hancock, Bio. Pharm. 2006, 71, 1103.
12. O. Roche, R. M. Rodriguez Sarmiento, Bio. Med. Chem. Lett. 2007, 17, 3670.
13. O. Roche, M. Nettekoven, W. Vifian, R. M. Rodriguez Sarmiento, Bio. Med. Chem. Lett.2008, 18, 4377.
14. M. Nettekoven, J.-M. Plancher, H. Richter, O. Roche, R. M Rodriguez Sarmiento, S. Taylor, Bio. Med. Chem. Lett, in press.
15. a) G. B. Fox, J. B. Pan, T. A. Esbenshade, R. S. Bitner, A. L. Nikkei, T. Miller, C. H. Kang, Y. L. Bennani, L. A. Black, R. Faghih, A. A. Hancock, M. W. Decker, Pharm. Bio. & Behav. 2002, 72, 741.
16. (b) X. Ligneau, J.-S. Lin, G. Vanni-Mercier, M. Jouvet, J. L. Muir, C. R. Ganellin, H. Stark, S. Elz, W. Schunack, J.-C. Schwartz, J. Pharm. Exp. Ther. 1998, 287, 658.
17. a) L. Jia, H. Sun, Bio. Med. Chem. 2008, 16, 6252
18. b) E. Raschi, V. Vasina, E. Poluzzi, F. De Ponti, Pharmacol. Res. 2008, 57, 181
19. c) M. J. Waring, C. Johnstone, Bio. Med. Chem. Lett. 2007, 17, 1759
20. d) A. M. Aronov, J. Med. Chem. 2006, 49, 6917.
21. H. Fischer, M. Kansy, PCT Int. Appl. US 2007027632 Al, 2007.
22. LYophilisation Solubility Assay (LYSA): solubility was measured from lyophilized DMSO stock solutions spectrophotometrically at pH = 6.5 in a 0.05M phosphate buffer.
23. M. Kansy, F. Senner, K. Gubemator, J. Med. Chem. 1998, 41, 1007.
24. a) M. Nettekoven, J.-M. Plancher, H. Richter, O. Roche, S. Taylor, PCT Int. Appl. WO 2007115938A1, 2007
25. b) M. Nettekoven, J.-M. Plancher, O. Roche, T. Takahashi, S. Taylor, PCT Int. Appl. WO2007080140, 2007
26. c) M. Nettekoven, J.-M. Plancher, H. Richter, O. Roche, S. Taylor, U.S. Pat. Appl. Publ. US 2007123525 Al, 2007
27. d) M. Nettekoven, J.-M. Plancher, H. Richter, O. Roche, R. M. Rodriguez Sarmiento, S. Taylor, U.S. Pat. Appl. Publ. US 2007123526 Al, 2007
28. e) M. Nettekoven, J.-M. Plancher, H. Richter, O. Roche, V. Runtz-Schmitt, S. Taylor, U.S. Pat. Appl. Publ. US 2007123515 Al, 2007
29. f) M. H. Nettekoven, J.-M. Plancher, O. Roche, R. M. Rodriguez-Sarmiento, U.S. Pat. Appl. Publ. US 2006160855 Al, 2006.