Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7259-7264

  Tellew, John E ^a   Lanier, Marion ^a   Moorjani, Manisha ^a   Lin, Emily ^a   Luo, Zhiyong ^a   Slee, Deborah H ^a   Zhang, Xiaohu ^a   Hoare, Sam R J ^a   Grigoriadis, Dimitri E ^a   Denis, Yves St ^b   Fabio, Romano Di ^b   Modugno, Enza Di ^b   Saunders, John ^a   Williams, John P ^a  

^a Neurocrine Biosciences ^*  (United States)

^b GSK   (Italy)

Author keywords

Corticotropin releasing factor; CRF1 antagonist; GSK561679

Indexed keywords

CORTICOTROPIN RELEASING FACTOR ANTAGONIST; GSK 561679; NBI 77860; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG STRUCTURE; DRUG TISSUE LEVEL; HUMAN; IN VITRO STUDY; NONHUMAN; RAT;

AZABICYCLO COMPOUNDS; HUMANS; MICROSOMES, LIVER; OXADIAZOLES; PROTEIN BINDING; PYRAZOLES; PYRIDINES; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; RECOMBINANT PROTEINS;

EID: 78449271015     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.095     Document Type: Article

References (19)

1. L. Arborelius, M.J. Owens, P.M. Plotsky, and C.B. Nemeroff J. Endocrinol. 160 1999 1
2. D.E. Grigoriadis Expert Opin. Ther. Targets 9 2005 651
3. P.J. Gilligan, and Y.-W. Li Curr. Opin. Drug Discov. Devel. 7 2004 487
4. J.E. Tellew, and Z. Luo Curr. Top. Med. Chem. 7 2008 506
5. C.D. Dzierba, R.A. Hartz, and J.J. Bronson Annu. Rep. Med. Chem. 43 2008 3
6. F. Holsboer, and M. Ising Eur. J. Pharmacol. 583 2008 350
7. C. Chen, and D.E. Grigoriadis Drug Dev. Res. 65 2005 216
8. M. Ising, U.S. Zimmermann, H.E. Künzel, M. Uhr, A.C. Foster, S.M. Learned-Coughlin, F. Holsboer, and D.E. Grigoriadis Neuropsychopharmacology 32 2007 1941
9. B. Binneman, D. Feltner, S. Kolluri, Y. Shi, R. Qiu, and T. Stiger Am. J. Psychiatry 165 2008 617
10. V. Coric, H.H. Feldman, D.A. Oren, A. Shekhar, J. Pultz, R.C. Dockens, X. Wu, K.A. Gentile, S.-P. Huang, E. Emison, T. Delmonte, B.B. D'Souza, D.L. Zimbroff, J.A. Grebb, A.W. Goddard, and E.G. Stock Depress. Anxiety 27 2010 417
11. C. Chen Curr. Med. Chem. 13 2006 1261
12. C. Chen, K.M. Wilcoxen, C.Q. Huang, Y.-F. Xie, J.R. McCarthy, T.R. Webb, Y.F. Zhu, J. Saunders, X.-J. Liu, T.-K. Chen, H. Bozigian, and D.E. Grigoriadis J. Med. Chem. 47 2004 4787
13. Calculator Plugins were used for Structure Property Prediction and Calculation, Marvin 5.1.2 2008ChemAxon (http://www.chemaxon.com ).
14. P.J. Gilligan, C. Baldauf, A. Cocuzza, D. Chidester, R. Zaczek, L.W. Fitzgerald, J. McElroy, M.A. Smith, H.-S.L. Shen, J. Saye, D. Christ, G. Trainor, D.W. Robertson, and P. Hartig Bioorg. Med. Chem. 8 2000 181
15. R.S. Gross, Z. Guo, B. Dyck, T. Coon, C.Q. Huang, R.F. Lowe, D. Marinkovic, M. Moorjani, J. Nelson, S. Zamani-Kord, D.E. Grigoriadis, S.R.J. Hoare, P.D. Crowe, J.H. Bu, M. Haddach, J. McCarthy, J. Saunders, R. Sullivan, T. Chen, and J.P. Williams J. Med. Chem. 48 2005 5780
16. C.W. Liaw, D.E. Grigoriadis, M.T. Lorang, E.B. De Souza, and R.A. Maki Mol. Endocrinol. 11 1997 2048
17. C.N. Hodge, P.E. Aldrich, Z.R. Wasserman, C.H. Fernandez, G.A. Nemeth, A. Arvanitis, R.S. Cheeseman, R.J. Chorvat, E. Ciganek, T.E. Christos, P.J. Gilligan, P. Krenitsky, E. Scholfield, and P. Strucely J. Med. Chem. 42 1999 819
18. A. Hamzé, J.-F. Hernandez, P. Fulcrand, and J. Martinez J. Org. Chem. 68 2003 7316
19. Enantiomeric excess was determined by normal-phase chiral HPLC using Chiralcel OD columns with hexane/ethanol or hexane/isopropanol as eluant (in the presence of diethylamine as an additive in some cases).