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105 results

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Page 1
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. Among authors: trappe j. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
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: trappe j. 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
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P. Fairhurst RA, et al. Among authors: trappe j. J Med Chem. 2020 Nov 12;63(21):12542-12573. doi: 10.1021/acs.jmedchem.0c01019. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32930584
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: trappe j. 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
Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region.
Fairhurst RA, Knoepfel T, Leblanc C, Buschmann N, Gaul C, Blank J, Galuba I, Trappe J, Zou C, Voshol J, Genick C, Brunet-Lefeuvre P, Bitsch F, Graus-Porta D, Furet P. Fairhurst RA, et al. Among authors: trappe j. Medchemcomm. 2017 Jun 8;8(8):1604-1613. doi: 10.1039/c7md00213k. eCollection 2017 Aug 1. Medchemcomm. 2017. PMID: 30108871 Free PMC article.
Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277.
Liniger M, Neuhaus C, Hofmann T, Fransioli-Ignazio L, Jordi M, Drueckes P, Trappe J, Fabbro D, Altmann KH. Liniger M, et al. Among authors: trappe j. ACS Med Chem Lett. 2010 Oct 20;2(1):22-7. doi: 10.1021/ml1001807. eCollection 2011 Jan 13. ACS Med Chem Lett. 2010. PMID: 24900250 Free PMC article.
Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Fedorov O, Huber K, Eisenreich A, Filippakopoulos P, King O, Bullock AN, Szklarczyk D, Jensen LJ, Fabbro D, Trappe J, Rauch U, Bracher F, Knapp S. Fedorov O, et al. Among authors: trappe j. Chem Biol. 2011 Jan 28;18(1):67-76. doi: 10.1016/j.chembiol.2010.11.009. Chem Biol. 2011. PMID: 21276940 Free PMC article.
Extended kinase profile and properties of the protein kinase inhibitor nilotinib.
Manley PW, Drueckes P, Fendrich G, Furet P, Liebetanz J, Martiny-Baron G, Mestan J, Trappe J, Wartmann M, Fabbro D. Manley PW, et al. Among authors: trappe j. Biochim Biophys Acta. 2010 Mar;1804(3):445-53. doi: 10.1016/j.bbapap.2009.11.008. Epub 2009 Nov 14. Biochim Biophys Acta. 2010. PMID: 19922818
105 results