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Page 1
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J. Schubart A, et al. Among authors: maibaum j. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29. Proc Natl Acad Sci U S A. 2019. PMID: 30926668 Free PMC article.
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: maibaum j. 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. J Med Chem. 2007 Oct 4;50(20):4832-44. doi: 10.1021/jm070316i. Epub 2007 Sep 8. J Med Chem. 2007. PMID: 17824680
Direct renin inhibitors as a new therapy for hypertension.
Webb RL, Schiering N, Sedrani R, Maibaum J. Webb RL, et al. Among authors: maibaum j. J Med Chem. 2010 Nov 11;53(21):7490-520. doi: 10.1021/jm901885s. J Med Chem. 2010. PMID: 20731374 Review. No abstract available.
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: maibaum 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
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: maibaum j. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
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: maibaum j. 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.
26 results