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Items: 12

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.

EMBO Mol Med. 2018 Sep 17. pii: e9316. doi: 10.15252/emmm.201809316. [Epub ahead of print]

2.

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.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3.

PMID:
29764741
3.

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.

Mol Neurodegener. 2015 Sep 3;10:44. doi: 10.1186/s13024-015-0033-8.

4.

Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.

Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Jacobson LH, Staufenbiel M, Desrayaud S, Rondeau JM, Möbitz H, Neumann U.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5300-6. doi: 10.1016/j.bmcl.2013.07.071. Epub 2013 Aug 9.

PMID:
23981898
5.

Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides.

Rueeger H, Lueoend R, Rogel O, Rondeau JM, Möbitz H, Machauer R, Jacobson L, Staufenbiel M, Desrayaud S, Neumann U.

J Med Chem. 2012 Apr 12;55(7):3364-86. doi: 10.1021/jm300069y. Epub 2012 Mar 21.

PMID:
22380629
6.

Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.

Rueeger H, Rondeau JM, McCarthy C, Möbitz H, Tintelnot-Blomley M, Neumann U, Desrayaud S.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):1942-7. doi: 10.1016/j.bmcl.2011.02.038. Epub 2011 Feb 15.

PMID:
21388807
7.

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.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):603-7. doi: 10.1016/j.bmcl.2009.11.092. Epub 2009 Nov 22.

PMID:
19963375
8.

Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.

Abramowski D, Wiederhold KH, Furrer U, Jaton AL, Neuenschwander A, Runser MJ, Danner S, Reichwald J, Ammaturo D, Staab D, Stoeckli M, Rueeger H, Neumann U, Staufenbiel M.

J Pharmacol Exp Ther. 2008 Nov;327(2):411-24. doi: 10.1124/jpet.108.140327. Epub 2008 Aug 7.

9.

Signal peptide peptidase dependent cleavage of type II transmembrane substrates releases intracellular and extracellular signals.

Dev KK, Chatterjee S, Osinde M, Stauffer D, Morgan H, Kobialko M, Dengler U, Rueeger H, Martoglio B, Rovelli G.

Eur J Pharmacol. 2006 Jul 1;540(1-3):10-7. Epub 2006 Apr 15.

PMID:
16697367
10.

Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists.

Rueeger H, Gerspacher M, Buehlmayer P, Rigollier P, Yamaguchi Y, Schmidlin T, Whitebread S, Nuesslein-Hildesheim B, Nick H, Cricione L.

Bioorg Med Chem Lett. 2004 May 17;14(10):2451-7.

PMID:
15109631
11.

Targeting presenilin-type aspartic protease signal peptide peptidase with gamma-secretase inhibitors.

Weihofen A, Lemberg MK, Friedmann E, Rueeger H, Schmitz A, Paganetti P, Rovelli G, Martoglio B.

J Biol Chem. 2003 May 9;278(19):16528-33. Epub 2003 Mar 5.

12.

Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.

Rueeger H, Rigollier P, Yamaguchi Y, Schmidlin T, Schilling W, Criscione L, Whitebread S, Chiesi M, Walker MW, Dhanoa D, Islam I, Zhang J, Gluchowski C.

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1175-9.

PMID:
10866375

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