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Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.
Wagner J, von Matt P, Sedrani R, Albert R, Cooke N, Ehrhardt C, Geiser M, Rummel G, Stark W, Strauss A, Cowan-Jacob SW, Beerli C, Weckbecker G, Evenou JP, Zenke G, Cottens S. Wagner J, et al. Among authors: weckbecker g. J Med Chem. 2009 Oct 22;52(20):6193-6. doi: 10.1021/jm901108b. J Med Chem. 2009. PMID: 19827831
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Wagner J, von Matt P, Faller B, Cooke NG, Albert R, Sedrani R, Wiegand H, Jean C, Beerli C, Weckbecker G, Evenou JP, Zenke G, Cottens S. Wagner J, et al. Among authors: weckbecker g. J Med Chem. 2011 Sep 8;54(17):6028-39. doi: 10.1021/jm200469u. Epub 2011 Aug 8. J Med Chem. 2011. PMID: 21797275
Orally bioavailable competitive CCR5 antagonists.
Thoma G, Nuninger F, Schaefer M, Akyel KG, Albert R, Beerli C, Bruns C, Francotte E, Luyten M, MacKenzie D, Oberer L, Streiff MB, Wagner T, Walter H, Weckbecker G, Zerwes HG. Thoma G, et al. Among authors: weckbecker g. J Med Chem. 2004 Apr 8;47(8):1939-55. doi: 10.1021/jm031046g. J Med Chem. 2004. PMID: 15055994
Effects of the novel protein kinase C inhibitor AEB071 (Sotrastaurin) on rat cardiac allograft survival using single agent treatment or combination therapy with cyclosporine, everolimus or FTY720.
Weckbecker G, Pally C, Beerli C, Burkhart C, Wieczorek G, Metzler B, Morris RE, Wagner J, Bruns C. Weckbecker G, et al. Transpl Int. 2010 May 1;23(5):543-52. doi: 10.1111/j.1432-2277.2009.01015.x. Epub 2009 Dec 9. Transpl Int. 2010. PMID: 20003043 Free article.
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Gommermann N, Buehlmayer P, von Matt A, Breitenstein W, Masuya K, Pirard B, Furet P, Cowan-Jacob SW, Weckbecker G. Gommermann N, et al. Among authors: weckbecker g. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3628-31. doi: 10.1016/j.bmcl.2010.04.112. Epub 2010 Apr 29. Bioorg Med Chem Lett. 2010. PMID: 20483608
1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.
Wattanasin S, Kallen J, Myers S, Guo Q, Sabio M, Ehrhardt C, Albert R, Hommel U, Weckbecker G, Welzenbach K, Weitz-Schmidt G. Wattanasin S, et al. Among authors: weckbecker g. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1217-20. doi: 10.1016/j.bmcl.2004.11.072. Bioorg Med Chem Lett. 2005. PMID: 15686945
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