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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: tersteegen a. ChemMedChem. 2015 Jul;10(7):1163-73. doi: 10.1002/cmdc.201500131. Epub 2015 Jun 17. ChemMedChem. 2015. PMID: 26083237 Free PMC article.
The novel selective PDE9 inhibitor BAY 73-6691 improves learning and memory in rodents.
van der Staay FJ, Rutten K, Bärfacker L, Devry J, Erb C, Heckroth H, Karthaus D, Tersteegen A, van Kampen M, Blokland A, Prickaerts J, Reymann KG, Schröder UH, Hendrix M. van der Staay FJ, et al. Among authors: tersteegen a. Neuropharmacology. 2008 Oct;55(5):908-18. doi: 10.1016/j.neuropharm.2008.07.005. Epub 2008 Jul 12. Neuropharmacology. 2008. PMID: 18674549
Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
Hillisch A, Gericke KM, Allerheiligen S, Roehrig S, Schaefer M, Tersteegen A, Schulz S, Lienau P, Gnoth M, Puetter V, Hillig RC, Heitmeier S. Hillisch A, et al. Among authors: tersteegen a. J Med Chem. 2020 Nov 12;63(21):12574-12594. doi: 10.1021/acs.jmedchem.0c01035. Epub 2020 Oct 27. J Med Chem. 2020. PMID: 33108181 Free article.
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. Among authors: tersteegen a. 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.
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: tersteegen a. 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.
PDE-10A inhibitors as insulin secretagogues.
Cantin LD, Magnuson S, Gunn D, Barucci N, Breuhaus M, Bullock WH, Burke J, Claus TH, Daly M, Decarr L, Gore-Willse A, Hoover-Litty H, Kumarasinghe ES, Li Y, Liang SX, Livingston JN, Lowinger T, Macdougall M, Ogutu HO, Olague A, Ott-Morgan R, Schoenleber RW, Tersteegen A, Wickens P, Zhang Z, Zhu J, Zhu L, Sweet LJ. Cantin LD, et al. Among authors: tersteegen a. Bioorg Med Chem Lett. 2007 May 15;17(10):2869-73. doi: 10.1016/j.bmcl.2007.02.061. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17400452
Targeting the heme-oxidized nitric oxide receptor for selective vasodilatation of diseased blood vessels.
Stasch JP, Schmidt PM, Nedvetsky PI, Nedvetskaya TY, H S AK, Meurer S, Deile M, Taye A, Knorr A, Lapp H, Müller H, Turgay Y, Rothkegel C, Tersteegen A, Kemp-Harper B, Müller-Esterl W, Schmidt HH. Stasch JP, et al. Among authors: tersteegen a. J Clin Invest. 2006 Sep;116(9):2552-61. doi: 10.1172/JCI28371. J Clin Invest. 2006. PMID: 16955146 Free PMC article.
27 results