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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. Among authors: ingram r. J Med Chem. 2007 May 17;50(10):2310-8. doi: 10.1021/jm060173k. Epub 2007 Apr 20. J Med Chem. 2007. PMID: 17444623
IK682, a tight binding inhibitor of TACE.
Niu X, Umland S, Ingram R, Beyer BM, Liu YH, Sun J, Lundell D, Orth P. Niu X, et al. Among authors: ingram r. Arch Biochem Biophys. 2006 Jul 1;451(1):43-50. doi: 10.1016/j.abb.2006.03.034. Epub 2006 May 5. Arch Biochem Biophys. 2006. PMID: 16762314
Crystal structure of the catalytic domain of human ADAM33.
Orth P, Reichert P, Wang W, Prosise WW, Yarosh-Tomaine T, Hammond G, Ingram RN, Xiao L, Mirza UA, Zou J, Strickland C, Taremi SS, Le HV, Madison V. Orth P, et al. J Mol Biol. 2004 Jan 2;335(1):129-37. doi: 10.1016/j.jmb.2003.10.037. J Mol Biol. 2004. PMID: 14659745
Key steps in the structure-based optimization of the hepatitis C virus NS3/4A protease inhibitor SCH503034.
Madison V, 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, et al. Among authors: ingram r. J Synchrotron Radiat. 2008 May;15(Pt 3):204-7. doi: 10.1107/S0909049507064229. Epub 2008 Apr 18. J Synchrotron Radiat. 2008. PMID: 18421139 Free PMC article.
Discovery of hydroxy pyrimidine Factor IXa inhibitors.
Jayne CL, Andreani T, Chan TY, Chelliah MV, Clasby MC, Dwyer M, Eagen KA, Fried S, Greenlee WJ, Guo Z, Hawes B, Hruza A, Ingram R, Keertikar KM, Neelamkavil S, Reichert P, Xia Y, Chackalamannil S. Jayne CL, et al. Among authors: ingram r. Bioorg Med Chem Lett. 2020 Aug 1;30(15):127279. doi: 10.1016/j.bmcl.2020.127279. Epub 2020 May 23. Bioorg Med Chem Lett. 2020. PMID: 32527459
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.
Arasappan A, Njoroge FG, Chan TY, Bennett F, Bogen SL, Chen K, Gu H, Hong L, Jao E, Liu YT, Lovey RG, Parekh T, Pike RE, Pinto P, Santhanam B, Venkatraman S, Vaccaro H, Wang H, Yang X, Zhu Z, Mckittrick B, Saksena AK, Girijavallabhan V, Pichardo J, Butkiewicz N, Ingram R, Malcolm B, Prongay A, Yao N, Marten B, Madison V, Kemp S, Levy O, Lim-Wilby M, Tamura S, Ganguly AK. Arasappan A, et al. Among authors: ingram r. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4180-4. doi: 10.1016/j.bmcl.2005.06.091. Bioorg Med Chem Lett. 2005. PMID: 16087332
587 results