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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: valeur e. 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.
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: valeur e. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
Namoto K, Sirockin F, Sellner H, Wiesmann C, Villard F, Moreau RJ, Valeur E, Paulding SC, Schleeger S, Schipp K, Loup J, Andrews L, Swale R, Robinson M, Farady CJ. Namoto K, et al. Among authors: valeur e. Bioorg Med Chem Lett. 2018 Mar 1;28(5):906-909. doi: 10.1016/j.bmcl.2018.01.064. Epub 2018 Feb 1. Bioorg Med Chem Lett. 2018. PMID: 29433930
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
Hardcastle IR, Liu J, Valeur E, Watson A, Ahmed SU, Blackburn TJ, Bennaceur K, Clegg W, Drummond C, Endicott JA, Golding BT, Griffin RJ, Gruber J, Haggerty K, Harrington RW, Hutton C, Kemp S, Lu X, McDonnell JM, Newell DR, Noble ME, Payne SL, Revill CH, Riedinger C, Xu Q, Lunec J. Hardcastle IR, et al. Among authors: valeur e. J Med Chem. 2011 Mar 10;54(5):1233-43. doi: 10.1021/jm1011929. Epub 2011 Feb 11. J Med Chem. 2011. PMID: 21314128
Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Roche D, Carniato D, Leriche C, Lepifre F, Christmann-Franck S, Graedler U, Charon C, Bozec S, Doare L, Schmidlin F, Lecomte M, Valeur E. Roche D, et al. Among authors: valeur e. Bioorg Med Chem Lett. 2009 May 15;19(10):2674-8. doi: 10.1016/j.bmcl.2009.03.140. Epub 2009 Apr 1. Bioorg Med Chem Lett. 2009. PMID: 19395260
Late-Stage Functionalization of Histidine in Unprotected Peptides.
Noisier AFM, Johansson MJ, Knerr L, Hayes MA, Drury WJ 3rd, Valeur E, Malins LR, Gopalakrishnan R. Noisier AFM, et al. Among authors: valeur e. Angew Chem Int Ed Engl. 2019 Dec 19;58(52):19096-19102. doi: 10.1002/anie.201910888. Epub 2019 Nov 7. Angew Chem Int Ed Engl. 2019. PMID: 31609503
24 results