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Page 1
Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.
Toyn JH, Boy KM, Raybon J, Meredith JE Jr, Robertson AS, Guss V, Hoque N, Sweeney F, Zhuo X, Clarke W, Snow K, Denton RR, Zuev D, Thompson LA, Morrison J, Grace J, Berisha F, Furlong M, Wang JS, Lentz KA, Padmanabha R, Cook L, Wei C, Drexler DM, Macor JE, Albright CF, Gasior M, Olson RE, Hong Q, Soares HD, AbuTarif M, Ahlijanian MK. Toyn JH, et al. Among authors: grace j. J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. doi: 10.1124/jpet.116.232249. Epub 2016 Apr 20. J Pharmacol Exp Ther. 2016. PMID: 27189974 Free PMC article.
Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.
Gillman KW, Higgins MA, Poindexter GS, Browning M, Clarke WJ, Flowers S, Grace JE Jr, Hogan JB, McGovern RT, Iben LG, Mattson GK, Ortiz A, Rassnick S, Russell JW, Antal-Zimanyi I. Gillman KW, et al. Among authors: grace je jr. Bioorg Med Chem. 2006 Aug 15;14(16):5517-26. doi: 10.1016/j.bmc.2006.04.042. Epub 2006 May 11. Bioorg Med Chem. 2006. PMID: 16697206
P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.
Meredith JE Jr, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF. Meredith JE Jr, et al. Among authors: grace je jr. J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499745
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: grace je. 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: grace je. 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: grace je. J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v. J Med Chem. 2009. PMID: 19954247
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: grace je. 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
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE. Thompson LA, et al. Among authors: grace je. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21974952
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA, Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE. Deskus JA, et al. Among authors: grace je jr. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23010264
710 results