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Page 1
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: li vm. ChemMedChem. 2015 Jul;10(7):1163-73. doi: 10.1002/cmdc.201500131. Epub 2015 Jun 17. ChemMedChem. 2015. PMID: 26083237 Free PMC article.
Novel tetrahydrochinoline derived CETP inhibitors.
Schmeck C, Gielen-Haertwig H, Vakalopoulos A, Bischoff H, Li V, Wirtz G, Weber O. Schmeck C, et al. 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
Chromanol derivatives--a novel class of CETP inhibitors.
Vakalopoulos A, Schmeck C, Thutewohl M, Li V, Bischoff H, Lustig K, Weber O, Paulsen H, Elias H. Vakalopoulos A, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):488-91. doi: 10.1016/j.bmcl.2010.10.110. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2011. PMID: 21084191
Prediction of a potentially effective dose in humans for BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically-based pharmacokinetic modelling.
Weber O, Willmann S, Bischoff H, Li V, Vakalopoulos A, Lustig K, Hafner FT, Heinig R, Schmeck C, Buehner K. Weber O, et al. Br J Clin Pharmacol. 2012 Feb;73(2):219-31. doi: 10.1111/j.1365-2125.2011.04064.x. Br J Clin Pharmacol. 2012. PMID: 21762205 Free PMC article.
Potent and Selective Human Neutrophil Elastase Inhibitors with Novel Equatorial Ring Topology: in vivo Efficacy of the Polar Pyrimidopyridazine BAY-8040 in a Pulmonary Arterial Hypertension Rat Model.
von Nussbaum F, Li VM, Meibom D, Anlauf S, Bechem M, Delbeck M, Gerisch M, Harrenga A, Karthaus D, Lang D, Lustig K, Mittendorf J, Schäfer M, Schäfer S, Schamberger J. von Nussbaum F, et al. Among authors: li vm. ChemMedChem. 2016 Jan 19;11(2):199-206. doi: 10.1002/cmdc.201500269. Epub 2015 Sep 3. ChemMedChem. 2016. PMID: 26333652
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.
Follmann M, Ackerstaff J, Redlich G, Wunder F, Lang D, Kern A, Fey P, Griebenow N, Kroh W, Becker-Pelster EM, Kretschmer A, Geiss V, Li V, Straub A, Mittendorf J, Jautelat R, Schirok H, Schlemmer KH, Lustig K, Gerisch M, Knorr A, Tinel H, Mondritzki T, Trübel H, Sandner P, Stasch JP. Follmann M, et al. J Med Chem. 2017 Jun 22;60(12):5146-5161. doi: 10.1021/acs.jmedchem.7b00449. Epub 2017 Jun 12. J Med Chem. 2017. PMID: 28557445 Free article.
New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension.
Vakalopoulos A, Wunder F, Hartung IV, Redlich G, Jautelat R, Buchgraber P, Hassfeld J, Gromov AV, Lindner N, Bierer D, Gries J, Kroh W, Paulsen H, Mittendorf J, Lang D, Becker-Pelster E, Brockschnieder D, Geiss V, Li V, Straub A, Knorr A, Mondritzki T, Trübel H, Raschke M, Schaefer M, Thomas D, Sandner P, Stasch JP, Follmann M. Vakalopoulos A, et al. J Med Chem. 2023 Jun 8;66(11):7280-7303. doi: 10.1021/acs.jmedchem.2c02082. Epub 2023 Apr 11. J Med Chem. 2023. PMID: 37040336
Dibenzodioxocinones--a new class of CETP inhibitors.
Brückner D, Hafner FT, Li V, Schmeck C, Telser J, Vakalopoulos A, Wirtz G. Brückner D, et al. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3611-4. doi: 10.1016/j.bmcl.2005.05.073. Bioorg Med Chem Lett. 2005. PMID: 15975789
Donated chemical probes for open science.
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A. Müller S, et al. Among authors: li vm. Elife. 2018 Apr 20;7:e34311. doi: 10.7554/eLife.34311. Elife. 2018. PMID: 29676732 Free PMC article.
25 results