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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: cumin f. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin.
Göschke R, Stutz S, Rasetti V, Cohen NC, Rahuel J, Rigollier P, Baum HP, Forgiarini P, Schnell CR, Wagner T, Gruetter MG, Fuhrer W, Schilling W, Cumin F, Wood JM, Maibaum J. Göschke R, et al. Among authors: cumin f. J Med Chem. 2007 Oct 4;50(20):4818-31. doi: 10.1021/jm070314y. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824679
Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.
Maibaum J, Stutz S, Göschke R, Rigollier P, Yamaguchi Y, Cumin F, Rahuel J, Baum HP, Cohen NC, Schnell CR, Fuhrer W, Gruetter MG, Schilling W, Wood JM. Maibaum J, et al. Among authors: cumin f. J Med Chem. 2007 Oct 4;50(20):4832-44. doi: 10.1021/jm070316i. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824680
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: cumin f. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Ehara T, Irie O, Kosaka T, Kanazawa T, Breitenstein W, Grosche P, Ostermann N, Suzuki M, Kawakami S, Konishi K, Hitomi Y, Toyao A, Gunji H, Cumin F, Schiering N, Wagner T, Rigel DF, Webb RL, Maibaum J, Yokokawa F. Ehara T, et al. Among authors: cumin f. ACS Med Chem Lett. 2014 Apr 21;5(7):787-92. doi: 10.1021/ml500137b. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050166 Free PMC article.
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J. Lorthiois E, et al. Among authors: cumin f. J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30. J Med Chem. 2017. PMID: 28621538
61 results