Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 18, 2012, Pages 5903-5908

  Raheem, Izzat T ^a   Breslin, Michael J ^a   Fandozzi, Christine ^a   Fuerst, Joy ^a   Hill, Nicole ^a   Huszar, Sarah ^a   Kandebo, Monika ^a   Kim, Somang H ^a   Ma, Bennett ^a   McGaughey, Georgia ^a   Renger, John J ^a   Schreier, John D ^a   Sharma, Sujata ^a   Smith, Sean ^a   Uslaner, Jason ^a   Yan, Youwei ^a   Coleman, Paul J ^a   Cox, Christopher D ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Conditioned avoidance response assay; Hyperlocomotion assay; Phosphodiesterase 10A inhibitor; Schizophrenia; Tetrahydropyridopyrimidine

Indexed keywords

CYCLIC GMP; DONEPEZIL; HALOPERIDOL; NEUROLEPTIC AGENT; OLANZAPINE; PHOSPHODIESTERASE 10A INHIBITOR; PHOSPHODIESTERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CATALEPSY; CONTROLLED STUDY; CORPUS STRIATUM; DOG; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG POTENCY; DRUG TARGETING; HAPLORHINI; HIGH THROUGHPUT SCREENING; LOCOMOTION; NONHUMAN; PHARMACODYNAMICS; PREDICTION; PROLACTIN RELEASE; RAT; SCHIZOPHRENIA; STRUCTURE ACTIVITY RELATION; WEIGHT GAIN;

ADMINISTRATION, ORAL; ANIMALS; CYCLIC GMP; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; MOLECULAR STRUCTURE; PHOSPHODIESTERASE INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; PYRIDINES; PYRIMIDINES; RATS; SCHIZOPHRENIA; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84865451685     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.07.072     Document Type: Article

References (41)

1. J. van Os, and S. Kapur Lancet 374 2009 635
2. C. Tsutsumi, H. Uchida, T. Suzuki, K. Watanabe, H. Takeuchi, S. Nakajima, Y. Kimura, Y. Tsutsumi, K. Ishii, Y. Imasaka, and S. Kapur Schizophr. Res. 130 2011 40
3. W.A. Ray, C.P. Chung, K.T. Murray, K. Hall, and C.M.N. Stein Engl. J. Med. 360 2009 225
4. H. Uchida, D.C. Mamo, B.H. Mulsant, B.G. Pollock, and S. Kapur J. Clin. Psychiatry 70 2009 397
5. M.F. Green, K.H. Nuechterlein, J.M. Gold, D.M. Barch, J. Cohen, S. Essock, W.S. Fenton, F. Frese, T.E. Goldberg, R.K. Heaton, R.S. Keefe, R.S. Kern, H. Kraemer, E. Stover, D.R. Weinberger, S. Zalcman, and S.R. Marder Biol. Psychiatry 56 2004 301
6. R.S. Keefe, R.M. Bilder, S.M. Davis, P.D. Harvey, B.W. Palmer, J.M. Gold, H.Y. Meltzer, M.F. Green, G. Capuano, T.S. Stroup, J.P. McEvoy, M.S. Swartz, R.A. Rosenheck, D.O. Perkins, C.E. Davis, J.K. Hsiao, and J.A. Lieberman Arch. Gen. Psychiatry 64 2007 633
7. R.S. Kern, M.F. Green, K.H. Nuechterlein, and B.H. Deng Schizophr. Res. 72 2004 11
8. Y.H. Jeon, Y.S. Heo, C.M. Kim, Y.L. Hyun, T.G. Lee, S. Ro, and J.M. Cho Cell. Mol. Life Sci. 62 2005 1198
9. D.T. Manallack, R.A. Hughes, and P.E. Thompson J. Med. Chem. 48 2005 3449
10. D.C. Grootendorst, and R.F. Klaus Curr. Opin. Allergy Clin. Immunol. 2 2002 61
11. P.J. Barnes Nat. Rev. Drug Discov. 1 2002 437
12. J.N. Travadi, and S.K. Patole Pediatr. Pulmonol. 36 2003 457
13. D. Marko, G. Pahlke, K.-H. Merz, and G. Eisenbrand Chem. Res. Toxicol. 13 2000 944
14. H.A. Ghofrani, I.H. Osterloh, and F. Grimminger Nat. Rev. Drug Discov. 5 2006 689
15. D.A. Kass, H.C. Champion, and J.A. Beavo Circ. Res. 101 2007 1084
16. F.S. Menniti, W.S. Faraci, and C.J. Schmidt Nat. Rev. Drug Discov. 5 2006 660
17. D.P. Rotella Nat. Rev. Drug Discov. 1 2002 674
18. S.H. Soderling, S.J. Bayuga, and J.A. Beavo Proc. Natl. Acad. Sci. U.S.A. 96 1999 7071
19. K. Fujishige, J. Kotera, H. Michibata, K. Yuasa, S. Takebayashi, K. Okumura, and K. Omori J. Biol. Chem. 274 1999 18438
20. K. Loughney, P.B. Snyder, L. Uher, G.J. Rosman, K. Ferguson, and V.A. Florio Gene 234 1999 109
21. A.T. Bender, and J.A. Beavo Pharmacol. Rev. 58 2006 488
22. F.S. Menniti, T.A. Chappie, J.M. Humphrey, and C.J. Schmidt Curr. Opin. Investig. Drugs 8 2007 54
23. T.F. Seeger, B. Bartlett, T.M. Coskran, J.S. Culp, L.C. James, D.L. Krull, J. Lanfear, A.M. Ryan, C.J. Schmidt, C.A. Strick, A.H. Varghese, R.D. Williams, P.G. Wylie, and F.S. Menniti Brain Res. 985 2003 113
24. T.M. Coskran, D. Morton, F.S. Menniti, W.O. Adamowicz, R.J. Kleiman, A.M. Ryan, C.A. Strick, C.J. Schmidt, and D.T. Stephenson J. Histochem. Cytochem. 54 2006 1205
25. Z. Xie, W.O. Adamowicz, W.D. Eldred, A.B. Jakowski, R.J. Kleiman, D.G. Morton, D.T. Stephenson, C.A. Strick, R.D. Williams, and F.S. Menniti Neuroscience 139 2006 597
26. E. Perez-Costas, M. Melender-Rerro, and R.C. Roberts J. Neurochem. 113 2010 287
27. E.H. Simpson, C. Kellendonk, and E. Kandel Neuron 65 2010 585
28. A.A. Baumeister, and J.L. Francis J. Hist. Neurosci. 11 2002 265
29. J. Delay, P. Deniker, and J.M. Harl Ann. Med. Psychol. 110 1952 112
30. M.R. DeLong, and T. Wichmann Arch. Neurol. 64 2007 20
31. T.A. Chappie, J.M. Humphrey, M.P. Allen, K.G. Estep, C.B. Fox, L.A. Lebel, S. Liras, E.S. Marr, F.S. Menniti, J. Pandit, C.J. Schmidt, M. Tu, R.D. Williams, and F.V. Yang J. Med. Chem. 50 2007 182
32. P.R. Verhoest, D.S. Chapin, M. Corman, K. Fonseca, J.F. Harms, X. Hou, E.S. Marr, F.S. Menniti, F. Nelson, R. O'Connor, J. Pandit, C. Proulx-LaFrance, A.W. Schmidt, C.J. Schmidt, J.A. Suiciak, and S. Liras J. Med. Chem. 52 2009 5188
33. N. Hoefgen, H. Stange, R. Schindler, H.-J. Lankau, C. Grunwald, B. Langen, U. Egerland, P. Tremmel, M.N. Pangalos, K.L. Marquis, T. Hage, B.L. Harrison, M.S. Malamas, N.J. Brandon, and T. Kronbach J. Med. Chem. 53 2010 4399
34. M.L. Wanderberg, S. Kapur, A. Soliman, C. Jones, and F. Vaccarino Psychopharmacology 150 2000 422
35. M.L. Wadenberg, A. Soliman, S.C. VanderSpek, and S. Kapur Neuropsychopharmacology 25 2001 633
36. S.M. Grauer, V.L. Pulito, R.L. Navarra, M.P. Kelly, C. Kelley, R. Graf, B. Langen, S. Logue, J. Brennan, L. Jiang, E. Charych, U. Egerland, F. Liu, K.L. Marquis, M. Malamas, T. Hage, T.A. Comery, and N.J. Brandon J. Pharmacol. Exp. Ther. 331 2009 574
37. J.S. Rodefer, E.R. Murphy, and M.G. Baxter Eur. J. Neurosci. 21 2005 1070
38. i) were determined as described by: S.D. Mosser, S.L. Gaul, B. Bednar, K.S. Koblan, and R.A.J. Bednar Assoc. Laboratory Automation 8 2003 54
39. I.T. Raheem, J.D. Schreier, and M.J. Breslin Tetrahedron Lett. 52 2011 3849
40. Smith, S. M.; Uslaner, J. M.; Cox, C. D.; Huszar, S. L.; Cannon, C. E.; Vardigan, J. D.; Eddins, D.; Toolan, D. M.; Kandebo, M.; Yao, L.; Raheem, I. T.; Schreier, J. D.; Breslin, M. J.; Coleman, P. J.; Renger, J. J. Neuropharmacology 2012, [Epub ahead of print].
41. H. Wang, Y. Liu, J. Hou, M. Zheng, H. Robinson, and H. Ke Proc. Natl. Acad. Sci. U.S.A. 104 2007 5782