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88 results

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Page 1
Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression.
Degnan AP, Tora GO, Huang H, Conlon DA, Davis CD, Hanumegowda UM, Hou X, Hsiao Y, Hu J, Krause R, Li YW, Newton AE, Pieschl RL, Raybon J, Rosner T, Sun JH, Taber MT, Taylor SJ, Wong MK, Zhang H, Lodge NJ, Bronson JJ, Macor JE, Gillman KW. Degnan AP, et al. Among authors: bronson jj. ACS Chem Neurosci. 2016 Dec 21;7(12):1635-1640. doi: 10.1021/acschemneuro.6b00337. Epub 2016 Oct 18. ACS Chem Neurosci. 2016. PMID: 27744678
The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH. Burton CR, et al. Among authors: bronson jj. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE. Hartz RA, et al. Among authors: bronson jj. J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. J Med Chem. 2009. PMID: 19552436
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE. Hartz RA, et al. Among authors: bronson jj. J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y. J Med Chem. 2009. PMID: 19552437
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ. Hartz RA, et al. Among authors: bronson jj. J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v. J Med Chem. 2009. PMID: 19954247
5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
Schmitz WD, Brenner AB, Bronson JJ, Ditta JL, Griffin CR, Li YW, Lodge NJ, Molski TF, Olson RE, Zhuo X, Macor JE. Schmitz WD, et al. Among authors: bronson jj. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3579-83. doi: 10.1016/j.bmcl.2010.04.121. Epub 2010 May 17. Bioorg Med Chem Lett. 2010. PMID: 20483614
Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.
Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA. Marcin LR, et al. Among authors: bronson jj. Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079. Bioorg Med Chem Lett. 2011. PMID: 21078556
Potential CRF1R PET imaging agents: N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines.
Zuev D, Mattson RJ, Huang H, Mattson GK, Zueva L, Nielsen JM, Kozlowski ES, Huang XS, Wu D, Gao Q, Lodge NJ, Bronson JJ, Macor JE. Zuev D, et al. Among authors: bronson jj. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2484-8. doi: 10.1016/j.bmcl.2011.02.050. Epub 2011 Feb 17. Bioorg Med Chem Lett. 2011. PMID: 21411322
88 results