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Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.
von Nussbaum F, Li VM, Allerheiligen S, Anlauf S, Bärfacker L, Bechem M, Delbeck M, Fitzgerald MF, Gerisch M, Gielen-Haertwig H, Haning H, Karthaus D, Lang D, Lustig K, Meibom D, Mittendorf J, Rosentreter U, Schäfer M, Schäfer S, Schamberger J, Telan LA, Tersteegen A. von Nussbaum F, et al. Among authors: gielen haertwig h. ChemMedChem. 2015 Jul;10(7):1163-73. doi: 10.1002/cmdc.201500131. Epub 2015 Jun 17. ChemMedChem. 2015. PMID: 26083237 Free PMC article.
Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases.
Bärfacker L, Kuhl A, Hillisch A, Grosser R, Figueroa-Pérez S, Heckroth H, Nitsche A, Ergüden JK, Gielen-Haertwig H, Schlemmer KH, Mittendorf J, Paulsen H, Platzek J, Kolkhof P. Bärfacker L, et al. Among authors: gielen haertwig h. ChemMedChem. 2012 Aug;7(8):1385-403. doi: 10.1002/cmdc.201200081. Epub 2012 Jul 12. ChemMedChem. 2012. PMID: 22791416
Novel tetrahydrochinoline derived CETP inhibitors.
Schmeck C, Gielen-Haertwig H, Vakalopoulos A, Bischoff H, Li V, Wirtz G, Weber O. Schmeck C, et al. Among authors: gielen haertwig h. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1740-3. doi: 10.1016/j.bmcl.2010.01.071. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137927
Future unmet medical need as a guiding principle for pharmaceutical R&D.
Vennemann M, Ruland V, Kruse JP, Harloff C, Trübel H, Gielen-Haertwig H. Vennemann M, et al. Among authors: gielen haertwig h. Drug Discov Today. 2019 Sep;24(9):1924-1929. doi: 10.1016/j.drudis.2019.06.004. Epub 2019 Jun 21. Drug Discov Today. 2019. PMID: 31233729 Review.