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Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: fischmann to. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.
Prongay AJ, Guo Z, Yao N, Pichardo J, Fischmann T, Strickland C, Myers J Jr, Weber PC, Beyer BM, Ingram R, Hong Z, Prosise WW, Ramanathan L, Taremi SS, Yarosh-Tomaine T, Zhang R, Senior M, Yang RS, Malcolm B, Arasappan A, Bennett F, Bogen SL, Chen K, Jao E, Liu YT, Lovey RG, Saksena AK, Venkatraman S, Girijavallabhan V, Njoroge FG, Madison V. Prongay AJ, et al. J Med Chem. 2007 May 17;50(10):2310-8. doi: 10.1021/jm060173k. Epub 2007 Apr 20. J Med Chem. 2007. PMID: 17444623
Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.
Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ. Dwyer MP, et al. Among authors: fischmann to. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. doi: 10.1016/j.bmcl.2007.09.018. Epub 2007 Sep 8. Bioorg Med Chem Lett. 2007. PMID: 17904366
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.
Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ. Paruch K, et al. Among authors: fischmann to. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. doi: 10.1016/j.bmcl.2007.09.017. Epub 2007 Sep 8. Bioorg Med Chem Lett. 2007. PMID: 17904841
Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.
Hegde VR, Borges S, Pu H, Patel M, Gullo VP, Wu B, Kirschmeier P, Williams MJ, Madison V, Fischmann T, Chan TM. Hegde VR, et al. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1384-7. doi: 10.1016/j.bmcl.2010.01.007. Epub 2010 Jan 7. Bioorg Med Chem Lett. 2010. PMID: 20097066
51 results