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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.
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
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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
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Unexpected active-site flexibility in the structure of human neutrophil elastase in complex with a new dihydropyrimidone inhibitor.
Hansen G, Gielen-Haertwig H, Reinemer P, Schomburg D, Harrenga A, Niefind K.
Hansen G, et al. Among authors: gielen haertwig h.
J Mol Biol. 2011 Jun 24;409(5):681-91. doi: 10.1016/j.jmb.2011.04.047. Epub 2011 Apr 27.
J Mol Biol. 2011.
PMID: 21549129
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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.
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