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Page 1
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.
Sutton JM, Clark DE, Dunsdon SJ, Fenton G, Fillmore A, Harris NV, Higgs C, Hurley CA, Krintel SL, MacKenzie RE, Duttaroy A, Gangl E, Maniara W, Sedrani R, Namoto K, Ostermann N, Gerhartz B, Sirockin F, Trappe J, Hassiepen U, Baeschlin DK. Sutton JM, et al. Among authors: ostermann n. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1464-8. doi: 10.1016/j.bmcl.2011.11.054. Epub 2011 Nov 20. Bioorg Med Chem Lett. 2012. PMID: 22177783
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK. Ostermann N, et al. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Lorthiois E, Breitenstein W, Cumin F, Ehrhardt C, Francotte E, Jacoby E, Ostermann N, Sellner H, Kosaka T, Webb RL, Rigel DF, Hassiepen U, Richert P, Wagner T, Maibaum J. Lorthiois E, et al. Among authors: ostermann n. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV.
Namoto K, Sirockin F, Ostermann N, Gessier F, Flohr S, Sedrani R, Gerhartz B, Trappe J, Hassiepen U, Duttaroy A, Ferreira S, Sutton JM, Clark DE, Fenton G, Beswick M, Baeschlin DK. Namoto K, et al. Among authors: ostermann n. Bioorg Med Chem Lett. 2014 Feb 1;24(3):731-6. doi: 10.1016/j.bmcl.2013.12.118. Epub 2014 Jan 6. Bioorg Med Chem Lett. 2014. PMID: 24439847
Small-molecule factor D inhibitors targeting the alternative complement pathway.
Maibaum J, Liao SM, Vulpetti A, Ostermann N, Randl S, Rüdisser S, Lorthiois E, Erbel P, Kinzel B, Kolb FA, Barbieri S, Wagner J, Durand C, Fettis K, Dussauge S, Hughes N, Delgado O, Hommel U, Gould T, Mac Sweeney A, Gerhartz B, Cumin F, Flohr S, Schubart A, Jaffee B, Harrison R, Risitano AM, Eder J, Anderson K. Maibaum J, et al. Among authors: ostermann n. Nat Chem Biol. 2016 Dec;12(12):1105-1110. doi: 10.1038/nchembio.2208. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775713
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
Vulpetti A, Randl S, Rüdisser S, Ostermann N, Erbel P, Mac Sweeney A, Zoller T, Salem B, Gerhartz B, Cumin F, Hommel U, Dalvit C, Lorthiois E, Maibaum J. Vulpetti A, et al. Among authors: ostermann n. J Med Chem. 2017 Mar 9;60(5):1946-1958. doi: 10.1021/acs.jmedchem.6b01684. Epub 2017 Feb 20. J Med Chem. 2017. PMID: 28157311
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: ostermann n. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
26 results