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Page 1
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. Among authors: metz dp. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.
Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD. Gonzalez-Lopez de Turiso F, et al. J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29. J Med Chem. 2012. PMID: 22876881
Synthesis and SAR study of potent and selective PI3Kδ inhibitors.
Bui M, Hao X, Shin Y, Cardozo M, He X, Henne K, Suchomel J, McCarter J, McGee LR, San Miguel T, Medina JC, Mohn D, Tran T, Wannberg S, Wong J, Wong S, Zalameda L, Metz D, Cushing TD. Bui M, et al. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17. Bioorg Med Chem Lett. 2015. PMID: 25666823
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Shin Y, Suchomel J, Cardozo M, Duquette J, He X, Henne K, Hu YL, Kelly RC, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wong S, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Shin Y, et al. J Med Chem. 2016 Jan 14;59(1):431-47. doi: 10.1021/acs.jmedchem.5b01651. Epub 2015 Dec 21. J Med Chem. 2016. PMID: 26652588
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Gonzalez-Lopez de Turiso F, et al. J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25. J Med Chem. 2016. PMID: 27411843
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Martin MW, Newcomb J, Nunes JJ, McGowan DC, Armistead DM, Boucher C, Buchanan JL, Buckner W, Chai L, Elbaum D, Epstein LF, Faust T, Flynn S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Lee JH, Metz D, Middleton S, Mohn D, Morgenstern K, Morrison MJ, Novak PM, Oliveira-dos-Santos A, Powers D, Rose P, Schneider S, Sell S, Tudor Y, Turci SM, Welcher AA, White RD, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Amouzegh P, Ermann M, Jenkins J, Johnston D, Napier S, Power E. Martin MW, et al. J Med Chem. 2006 Aug 10;49(16):4981-91. doi: 10.1021/jm060435i. J Med Chem. 2006. PMID: 16884310
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Buchanan JL, Buckner WH, Cee VJ, Chai L, Deak HL, Epstein LF, Faust T, Gallant P, Geuns-Meyer SD, Gore A, Gu Y, Henkle B, Hodous BL, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, Masse CE, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, White RD, Zhao H, Zhu L, Zhu X. DiMauro EF, et al. J Med Chem. 2006 Sep 21;49(19):5671-86. doi: 10.1021/jm0605482. J Med Chem. 2006. PMID: 16970394
Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Chai L, Chaffee SC, Deak HL, Epstein LF, Faust T, Gallant P, Gore A, Gu Y, Henkle B, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, Zhao H, Zhu L, Zhu X. DiMauro EF, et al. J Med Chem. 2008 Mar 27;51(6):1681-94. doi: 10.1021/jm7010996. Epub 2008 Mar 6. J Med Chem. 2008. PMID: 18321037
20 results