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Page 1
The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.
Neumann U, Ufer M, Jacobson LH, Rouzade-Dominguez ML, Huledal G, Kolly C, Lüönd RM, Machauer R, Veenstra SJ, Hurth K, Rueeger H, Tintelnot-Blomley M, Staufenbiel M, Shimshek DR, Perrot L, Frieauff W, Dubost V, Schiller H, Vogg B, Beltz K, Avrameas A, Kretz S, Pezous N, Rondeau JM, Beckmann N, Hartmann A, Vormfelde S, David OJ, Galli B, Ramos R, Graf A, Lopez Lopez C. Neumann U, et al. Among authors: tintelnot blomley m. EMBO Mol Med. 2018 Nov;10(11):e9316. doi: 10.15252/emmm.201809316. EMBO Mol Med. 2018. PMID: 30224383 Free PMC article. Clinical Trial.
A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice.
Neumann U, Rueeger H, Machauer R, Veenstra SJ, Lueoend RM, Tintelnot-Blomley M, Laue G, Beltz K, Vogg B, Schmid P, Frieauff W, Shimshek DR, Staufenbiel M, Jacobson LH. Neumann U, et al. Among authors: tintelnot blomley m. Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8. Mol Neurodegener. 2015. PMID: 26336937 Free PMC article.
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.
Veenstra SJ, Rueeger H, Voegtle M, Lueoend R, Holzer P, Hurth K, Tintelnot-Blomley M, Frederiksen M, Rondeau JM, Jacobson L, Staufenbiel M, Neumann U, Machauer R. Veenstra SJ, et al. Among authors: tintelnot blomley m. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3. Bioorg Med Chem Lett. 2018. PMID: 29764741
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.
Machauer R, Lueoend R, Hurth K, Veenstra SJ, Rueeger H, Voegtle M, Tintelnot-Blomley M, Rondeau JM, Jacobson LH, Laue G, Beltz K, Neumann U. Machauer R, et al. Among authors: tintelnot blomley m. J Med Chem. 2021 Oct 28;64(20):15262-15279. doi: 10.1021/acs.jmedchem.1c01300. Epub 2021 Oct 14. J Med Chem. 2021. PMID: 34648711
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.
Machauer R, Laumen K, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Jaton AL, Desrayaud S, Staufenbiel M, Rabe S, Paganetti P, Neumann U. Machauer R, et al. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1366-70. doi: 10.1016/j.bmcl.2009.01.055. Epub 2009 Jan 22. Bioorg Med Chem Lett. 2009. PMID: 19195887
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.
Lerchner A, Machauer R, Betschart C, Veenstra S, Rueeger H, McCarthy C, Tintelnot-Blomley M, Jaton AL, Rabe S, Desrayaud S, Enz A, Staufenbiel M, Paganetti P, Rondeau JM, Neumann U. Lerchner A, et al. Among authors: tintelnot blomley m. Bioorg Med Chem Lett. 2010 Jan 15;20(2):603-7. doi: 10.1016/j.bmcl.2009.11.092. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 19963375
Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360.
Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Holzer P, Hurth K, Voegtle M, Frederiksen M, Rondeau JM, Tintelnot-Blomley M, Jacobson LH, Staufenbiel M, Laue G, Neumann U. Rueeger H, et al. Among authors: tintelnot blomley m. J Med Chem. 2021 Apr 22;64(8):4677-4696. doi: 10.1021/acs.jmedchem.0c02143. Epub 2021 Apr 12. J Med Chem. 2021. PMID: 33844524
25 results