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Page 1
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
Anselm L, Banner DW, Benz J, Zbinden KG, Himber J, Hilpert H, Huber W, Kuhn B, Mary JL, Otteneder MB, Panday N, Ricklin F, Stahl M, Thomi S, Haap W. Anselm L, et al. Among authors: hilpert h. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5313-9. doi: 10.1016/j.bmcl.2010.06.126. Epub 2010 Jul 1. Bioorg Med Chem Lett. 2010. PMID: 20650636
BACE1 inhibitors: a head group scan on a series of amides.
Woltering TJ, Wostl W, Hilpert H, Rogers-Evans M, Pinard E, Mayweg A, Göbel M, Banner DW, Benz J, Travagli M, Pollastrini M, Marconi G, Gabellieri E, Guba W, Mauser H, Andreini M, Jacobsen H, Power E, Narquizian R. Woltering TJ, et al. Among authors: hilpert h. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4239-43. doi: 10.1016/j.bmcl.2013.05.003. Epub 2013 May 18. Bioorg Med Chem Lett. 2013. PMID: 23735744
β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
Hilpert H, Guba W, Woltering TJ, Wostl W, Pinard E, Mauser H, Mayweg AV, Rogers-Evans M, Humm R, Krummenacher D, Muser T, Schnider C, Jacobsen H, Ozmen L, Bergadano A, Banner DW, Hochstrasser R, Kuglstatter A, David-Pierson P, Fischer H, Polara A, Narquizian R. Hilpert H, et al. J Med Chem. 2013 May 23;56(10):3980-95. doi: 10.1021/jm400225m. Epub 2013 May 2. J Med Chem. 2013. PMID: 23590342
Mapping the conformational space accessible to BACE2 using surface mutants and cocrystals with Fab fragments, Fynomers and Xaperones.
Banner DW, Gsell B, Benz J, Bertschinger J, Burger D, Brack S, Cuppuleri S, Debulpaep M, Gast A, Grabulovski D, Hennig M, Hilpert H, Huber W, Kuglstatter A, Kusznir E, Laeremans T, Matile H, Miscenic C, Rufer AC, Schlatter D, Steyaert J, Stihle M, Thoma R, Weber M, Ruf A. Banner DW, et al. Among authors: hilpert h. Acta Crystallogr D Biol Crystallogr. 2013 Jun;69(Pt 6):1124-37. doi: 10.1107/S0907444913006574. Epub 2013 May 15. Acta Crystallogr D Biol Crystallogr. 2013. PMID: 23695257
32 results