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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: schafer s, schafer m. 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: schafer s, schafer m. ChemMedChem. 2016 Jan 19;11(2):199-206. doi: 10.1002/cmdc.201500269. Epub 2015 Sep 3. ChemMedChem. 2016. PMID: 26333652
Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer.
Lücking U, Scholz A, Lienau P, Siemeister G, Kosemund D, Bohlmann R, Briem H, Terebesi I, Meyer K, Prelle K, Denner K, Bömer U, Schäfer M, Eis K, Valencia R, Ince S, von Nussbaum F, Mumberg D, Ziegelbauer K, Klebl B, Choidas A, Nussbaumer P, Baumann M, Schultz-Fademrecht C, Rühter G, Eickhoff J, Brands M. Lücking U, et al. Among authors: schafer m. ChemMedChem. 2017 Nov 8;12(21):1776-1793. doi: 10.1002/cmdc.201700447. Epub 2017 Oct 16. ChemMedChem. 2017. PMID: 28961375 Free PMC article.
The lab oddity prevails: discovery of pan-CDK inhibitor (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the treatment of cancer.
Lücking U, Jautelat R, Krüger M, Brumby T, Lienau P, Schäfer M, Briem H, Schulze J, Hillisch A, Reichel A, Wengner AM, Siemeister G. Lücking U, et al. Among authors: schafer m. ChemMedChem. 2013 Jul;8(7):1067-85. doi: 10.1002/cmdc.201300096. Epub 2013 May 13. ChemMedChem. 2013. PMID: 23671017
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.
Lücking U, Wortmann L, Wengner AM, Lefranc J, Lienau P, Briem H, Siemeister G, Bömer U, Denner K, Schäfer M, Koppitz M, Eis K, Bartels F, Bader B, Bone W, Moosmayer D, Holton SJ, Eberspächer U, Grudzinska-Goebel J, Schatz C, Deeg G, Mumberg D, von Nussbaum F. Lücking U, et al. Among authors: schafer m. J Med Chem. 2020 Jul 9;63(13):7293-7325. doi: 10.1021/acs.jmedchem.0c00369. Epub 2020 Jun 28. J Med Chem. 2020. PMID: 32502336
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer.
Lücking U, Kosemund D, Böhnke N, Lienau P, Siemeister G, Denner K, Bohlmann R, Briem H, Terebesi I, Bömer U, Schäfer M, Ince S, Mumberg D, Scholz A, Izumi R, Hwang S, von Nussbaum F. Lücking U, et al. Among authors: schafer m. J Med Chem. 2021 Aug 12;64(15):11651-11674. doi: 10.1021/acs.jmedchem.1c01000. Epub 2021 Jul 15. J Med Chem. 2021. PMID: 34264057
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Panknin O, Wagenfeld A, Bone W, Bender E, Nowak-Reppel K, Fernández-Montalván AE, Nubbemeyer R, Bäurle S, Ring S, Schmees N, Prien O, Schäfer M, Friedrich C, Zollner TM, Steinmeyer A, Mueller T, Langer G. Panknin O, et al. Among authors: schafer m. J Med Chem. 2020 Oct 22;63(20):11854-11881. doi: 10.1021/acs.jmedchem.0c01076. Epub 2020 Oct 6. J Med Chem. 2020. PMID: 32960053
Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo.
Wortmann L, Lindenthal B, Muhn P, Walter A, Nubbemeyer R, Heldmann D, Sobek L, Morandi F, Schrey AK, Moosmayer D, Günther J, Kuhnke J, Koppitz M, Lücking U, Röhn U, Schäfer M, Nowak-Reppel K, Kühne R, Weinmann H, Langer G. Wortmann L, et al. Among authors: schafer m. J Med Chem. 2019 Nov 27;62(22):10321-10341. doi: 10.1021/acs.jmedchem.9b01382. Epub 2019 Nov 13. J Med Chem. 2019. PMID: 31670515
2,062 results