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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: sirockin f. 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 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: sirockin f. 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 and structure-based optimization of adenain inhibitors.
Mac Sweeney A, Grosche P, Ellis D, Combrink K, Erbel P, Hughes N, Sirockin F, Melkko S, Bernardi A, Ramage P, Jarousse N, Altmann E. Mac Sweeney A, et al. Among authors: sirockin f. ACS Med Chem Lett. 2014 Jun 20;5(8):937-41. doi: 10.1021/ml500224t. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147618 Free PMC article.
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Grosche P, Sirockin F, Mac Sweeney A, Ramage P, Erbel P, Melkko S, Bernardi A, Hughes N, Ellis D, Combrink KD, Jarousse N, Altmann E. Grosche P, et al. Among authors: sirockin f. Bioorg Med Chem Lett. 2015 Feb 1;25(3):438-43. doi: 10.1016/j.bmcl.2014.12.057. Epub 2014 Dec 24. Bioorg Med Chem Lett. 2015. PMID: 25571794
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: sirockin f. 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
Structural basis of species-selective antagonist binding to the succinate receptor.
Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP. Haffke M, et al. Among authors: sirockin f. Nature. 2019 Oct;574(7779):581-585. doi: 10.1038/s41586-019-1663-8. Epub 2019 Oct 23. Nature. 2019. PMID: 31645725
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: sirockin f. 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
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: sirockin f. 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
Building Compound Archives for the Future.
Lewis R, Deheuvels J, Ertl P, Pirard B, Sirockin F. Lewis R, et al. Among authors: sirockin f. Mol Inform. 2016 Dec;35(11-12):580-582. doi: 10.1002/minf.201600042. Epub 2016 Jun 1. Mol Inform. 2016. PMID: 27870238
22 results