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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: meibom d. ChemMedChem. 2015 Jul;10(7):1163-73. doi: 10.1002/cmdc.201500131. Epub 2015 Jun 17. ChemMedChem. 2015. PMID: 26083237 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: meibom d. ChemMedChem. 2016 Jan 19;11(2):199-206. doi: 10.1002/cmdc.201500269. Epub 2015 Sep 3. ChemMedChem. 2016. PMID: 26333652
Potent and Selective Human Prostaglandin F (FP) Receptor Antagonist (BAY-6672) for the Treatment of Idiopathic Pulmonary Fibrosis (IPF).
Beck H, Thaler T, Meibom D, Meininghaus M, Jörißen H, Dietz L, Terjung C, Bairlein M, von Bühler CJ, Anlauf S, Fürstner C, Stellfeld T, Schneider D, Gericke KM, Buyck T, Lovis K, Münster U, Anlahr J, Kersten E, Levilain G, Marossek V, Kast R. Beck H, et al. Among authors: meibom d. J Med Chem. 2020 Oct 22;63(20):11639-11662. doi: 10.1021/acs.jmedchem.0c00834. Epub 2020 Oct 8. J Med Chem. 2020. PMID: 32969660
BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.
Meibom D, Micus S, Andreevski AL, Anlauf S, Bogner P, von Buehler CJ, Dieskau AP, Dreher J, Eitner F, Fliegner D, Follmann M, Gericke KM, Maassen S, Meyer J, Schlemmer KH, Steuber H, Tersteegen A, Wunder F. Meibom D, et al. J Med Chem. 2022 Dec 22;65(24):16420-16431. doi: 10.1021/acs.jmedchem.2c01267. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475653 Free PMC article.
BAY-6096: A Potent, Selective, and Highly Water-Soluble Adrenergic α2B Antagonist.
Meibom D, Meyer J, von Buehler CJ, Collins KD, Maassen S, Gericke KM, Hüser J, Mittendorf J, Ortega Hernandez N, Schamberger J, Stampfuss J, Straub A, Torge A, Witowski N, Wunder F. Meibom D, et al. J Med Chem. 2023 Apr 13;66(7):4659-4670. doi: 10.1021/acs.jmedchem.2c01690. Epub 2023 Mar 18. J Med Chem. 2023. PMID: 36932954 Free PMC article.
Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders.
Roehrig S, Ackerstaff J, Jiménez Núñez E, Teller H, Ellerbrock P, Meier K, Heitmeier S, Tersteegen A, Stampfuss J, Lang D, Schlemmer KH, Schaefer M, Gericke KM, Kinzel T, Meibom D, Schmidt M, Gerdes C, Follmann M, Hillisch A. Roehrig S, et al. Among authors: meibom d. J Med Chem. 2023 Sep 14;66(17):12203-12224. doi: 10.1021/acs.jmedchem.3c00795. Epub 2023 Sep 5. J Med Chem. 2023. PMID: 37669040 Free PMC article.
Linker-Dependent Folding Rationalizes PROTAC Cell Permeability.
Poongavanam V, Atilaw Y, Siegel S, Giese A, Lehmann L, Meibom D, Erdelyi M, Kihlberg J. Poongavanam V, et al. Among authors: meibom d. J Med Chem. 2022 Oct 13;65(19):13029-13040. doi: 10.1021/acs.jmedchem.2c00877. Epub 2022 Sep 28. J Med Chem. 2022. PMID: 36170570 Free PMC article.
Solution Conformations Shed Light on PROTAC Cell Permeability.
Atilaw Y, Poongavanam V, Svensson Nilsson C, Nguyen D, Giese A, Meibom D, Erdelyi M, Kihlberg J. Atilaw Y, et al. Among authors: meibom d. ACS Med Chem Lett. 2020 Dec 25;12(1):107-114. doi: 10.1021/acsmedchemlett.0c00556. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488971 Free PMC article.
12 results