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Page 1
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: mattson rj. J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v. J Med Chem. 2009. PMID: 19954247
Aminotriazine 5-HT7 antagonists.
Mattson RJ, Denhart DJ, Catt JD, Dee MF, Deskus JA, Ditta JL, Epperson J, Dalton King H, Gao A, Poss MA, Purandare A, Tortolani D, Zhao Y, Yang H, Yeola S, Palmer J, Torrente J, Stark A, Johnson G. Mattson RJ, et al. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4245-8. doi: 10.1016/j.bmcl.2004.06.008. Bioorg Med Chem Lett. 2004. PMID: 15261279
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: mattson rj. 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: mattson rj. J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y. J Med Chem. 2009. PMID: 19552437
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: mattson rj. 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
[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: mattson rj. 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
Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.
Lodge NJ, Li YW, Chin FT, Dischino DD, Zoghbi SS, Deskus JA, Mattson RJ, Imaizumi M, Pieschl R, Molski TF, Fujita M, Dulac H, Zaczek R, Bronson JJ, Macor JE, Innis RB, Pike VW. Lodge NJ, et al. Among authors: mattson rj. Nucl Med Biol. 2014 Jul;41(6):524-35. doi: 10.1016/j.nucmedbio.2014.03.005. Epub 2014 Mar 29. Nucl Med Biol. 2014. PMID: 24793011 Free PMC article.
32 results