The BACE‐1 inhibitor CNP520 for prevention trials in Alzheimer's disease
Neumann, Ulf, Ufer, Mike, Jacobson, Laura H, Rouzade‐Dominguez, Marie‐Laure, Huledal, Gunilla, Kolly, Carine, Lüönd, Rainer M, Machauer, Rainer, Veenstra, Siem J, Hurth, Konstanze, Rueeger, Heinrich, Tintelnot‐Blomley, Marina, Staufenbiel, Matthias, Shimshek, Derya R, Perrot, Ludovic, Frieauff, Wilfried, Dubost, Valerie, Schiller, Hilmar, Vogg, Barbara, Beltz, Karen, Avrameas, Alexandre, Kretz, Sandrine, Pezous, Nicole, Rondeau, Jean‐Michel, Beckmann, Nicolau, Hartmann, Andreas, Vormfelde, Stefan, David, Olivier J, Galli, Bruno, Ramos, Rita, Graf, Ana, Lopez Lopez, Cristina
Published in EMBO molecular medicine (01.11.2018)
Published in EMBO molecular medicine (01.11.2018)
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Journal Article
Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors
Rueeger, Heinrich, Rondeau, Jean-Michel, McCarthy, Clive, Möbitz, Henrik, Tintelnot-Blomley, Marina, Neumann, Ulf, Desrayaud, Sandrine
Published in Bioorganic & medicinal chemistry letters (01.04.2011)
Published in Bioorganic & medicinal chemistry letters (01.04.2011)
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Journal Article
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious beta-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease
Machauer, Rainer, Lueoend, Rainer, Hurth, Konstanze, Veenstra, Siem J., Rueeger, Heinrich, Voegtle, Markus, Tintelnot-Blomley, Marina, Rondeau, Jean-Michel, Jacobson, Laura H., Laue, Grit, Beltz, Karen, Neumann, Ulf
Published in Journal of medicinal chemistry (28.10.2021)
Published in Journal of medicinal chemistry (28.10.2021)
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Journal Article
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, Heinrich, Lueoend, Rainer, Rogel, Olivier, Rondeau, Jean-Michel, Möbitz, Henrik, Machauer, Rainer, Jacobson, Laura, Staufenbiel, Matthias, Desrayaud, Sandrine, Neumann, Ulf
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Journal Article
Synthesis of the Potent, Selective, and Efficacious β‑Secretase (BACE1) Inhibitor NB-360
Rueeger, Heinrich, Lueoend, Rainer, Machauer, Rainer, Veenstra, Siem J, Holzer, Philipp, Hurth, Konstanze, Voegtle, Markus, Frederiksen, Mathias, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Jacobson, Laura H, Staufenbiel, Matthias, Laue, Grit, Neumann, Ulf
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
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Journal Article
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor
Fairhurst, Robin A., Furet, Pascal, Imbach-Weese, Patricia, Stauffer, Frédéric, Rueeger, Heinrich, McCarthy, Clive, Ripoche, Sebastien, Oswald, Susanne, Arnaud, Bertrand, Jary, Aline, Maira, Michel, Schnell, Christian, Guthy, Daniel A., Wartmann, Markus, Kiffe, Michael, Desrayaud, Sandrine, Blasco, Francesca, Widmer, Toni, Seiler, Frank, Gutmann, Sascha, Knapp, Mark, Caravatti, Giorgio
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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Journal Article
A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice
Neumann, Ulf, Rueeger, Heinrich, Machauer, Rainer, Veenstra, Siem Jacob, Lueoend, Rainer M, Tintelnot-Blomley, Marina, Laue, Grit, Beltz, Karen, Vogg, Barbara, Schmid, Peter, Frieauff, Wilfried, Shimshek, Derya R, Staufenbiel, Matthias, Jacobson, Laura H
Published in Molecular neurodegeneration (03.09.2015)
Published in Molecular neurodegeneration (03.09.2015)
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Journal Article
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors
Veenstra, Siem Jakob, Rueeger, Heinrich, Voegtle, Markus, Lueoend, Rainer, Holzer, Philipp, Hurth, Konstanze, Tintelnot-Blomley, Marina, Frederiksen, Mathias, Rondeau, Jean-Michel, Jacobson, Laura, Staufenbiel, Matthias, Neumann, Ulf, Machauer, Rainer
Published in Bioorganic & medicinal chemistry letters (01.07.2018)
Published in Bioorganic & medicinal chemistry letters (01.07.2018)
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Journal Article
BET bromodomain inhibitors regulate keratinocyte plasticity
Schutzius, Gabi, Kolter, Christian, Bergling, Sebastian, Tortelli, Federico, Fuchs, Florian, Renner, Steffen, Guagnano, Vito, Cotesta, Simona, Rueeger, Heinrich, Faller, Michael, Bouchez, Laure, Salathe, Adrian, Nigsch, Florian, Richards, Shola M., Louis, Malvina, Gruber, Viktoria, Aebi, Alexandra, Turner, Jonathan, Grandjean, Frederic, Li, Jun, Dimitri, Chris, Thomas, Jason R., Schirle, Markus, Blank, Jutta, Drueckes, Peter, Vaupel, Andrea, Tiedt, Ralph, Manley, Paul W., Klopp, Julia, Hemmig, Rene, Zink, Florence, Leroy, Nelly, Carbone, Walter, Roma, Guglielmo, Keller, Caroline Gubser, Dales, Natalie, Beyerbach, Armin, Zimmerlin, Alfred, Bonenfant, Debora, Terranova, Remi, Berwick, Amy, Sahambi, Sukhdeep, Reynolds, Aimee, Jennings, Lori L., Ruffner, Heinz, Tarsa, Peter, Bouwmeester, Tewis, Driver, Vickie, Frederiksen, Mathias, Lohmann, Felix, Kirkland, Susan
Published in Nature chemical biology (01.03.2021)
Published in Nature chemical biology (01.03.2021)
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Journal Article
Dynamics of Aβ Turnover and Deposition in Different β-Amyloid Precursor Protein Transgenic Mouse Models Following γ-Secretase Inhibition
Abramowski, Dorothee, Wiederhold, Karl-Heinz, Furrer, Ulrich, Jaton, Anne-Lise, Neuenschwander, Anton, Runser, Marie-Josephine, Danner, Simone, Reichwald, Julia, Ammaturo, Domenico, Staab, Dieter, Stoeckli, Markus, Rueeger, Heinrich, Neumann, Ulf, Staufenbiel, Matthias
Published in The Journal of pharmacology and experimental therapeutics (01.11.2008)
Published in The Journal of pharmacology and experimental therapeutics (01.11.2008)
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Journal Article
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, Heinrich, Lueoend, Rainer, Machauer, Rainer, Veenstra, Siem Jacob, Jacobson, Laura Helen, Staufenbiel, Matthias, Desrayaud, Sandrine, Rondeau, Jean-Michel, Möbitz, Henrik, Neumann, Ulf
Published in Bioorganic & medicinal chemistry letters (01.10.2013)
Published in Bioorganic & medicinal chemistry letters (01.10.2013)
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Journal Article
Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application
Lerchner, Andreas, Machauer, Rainer, Betschart, Claudia, Veenstra, Siem, Rueeger, Heinrich, McCarthy, Clive, Tintelnot-Blomley, Marina, Jaton, Anne-Lise, Rabe, Sabine, Desrayaud, Sandrine, Enz, Albert, Staufenbiel, Matthias, Paganetti, Paolo, Rondeau, Jean-Michel, Neumann, Ulf
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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Journal Article
The BACE ‐1 inhibitor CNP 520 for prevention trials in Alzheimer's disease
Neumann, Ulf, Ufer, Mike, Jacobson, Laura H, Rouzade‐Dominguez, Marie‐Laure, Huledal, Gunilla, Kolly, Carine, Lüönd, Rainer M, Machauer, Rainer, Veenstra, Siem J, Hurth, Konstanze, Rueeger, Heinrich, Tintelnot‐Blomley, Marina, Staufenbiel, Matthias, Shimshek, Derya R, Perrot, Ludovic, Frieauff, Wilfried, Dubost, Valerie, Schiller, Hilmar, Vogg, Barbara, Beltz, Karen, Avrameas, Alexandre, Kretz, Sandrine, Pezous, Nicole, Rondeau, Jean‐Michel, Beckmann, Nicolau, Hartmann, Andreas, Vormfelde, Stefan, David, Olivier J, Galli, Bruno, Ramos, Rita, Graf, Ana, Lopez Lopez, Cristina
Published in EMBO molecular medicine (01.11.2018)
Published in EMBO molecular medicine (01.11.2018)
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Journal Article
Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective I2-site APP-cleaving enzyme 1 (BACE1) inhibitors: Structure based design and in vivo reduction of amyloid I2-peptides
Rueeger, Heinrich, Lueoend, Rainer, Machauer, Rainer, Veenstra, Siem, Jacobson, Laura, Staufenbiel, Matthias, Desrayaud, Sandrine, Rondeau, Jean-Michel, Mobitz, Henrik, Neumann, Ulf
Published in Bioorganic & medicinal chemistry letters (01.10.2013)
Published in Bioorganic & medicinal chemistry letters (01.10.2013)
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Journal Article
PYRAZOLO-PYRROLIDIN-4-ONE DERIVATIVES AS BET INHIBITORS AND THEIR USE IN THE TREATMENT OF DISEASE
BLANK JUTTA, RUEEGER HEINRICH, COTESTA SIMONA, BOLD GUIDO, GUAGNANO VITO
Year of Publication 02.02.2016
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Year of Publication 02.02.2016
Patent
Targeting Presenilin-type Aspartic Protease Signal Peptide Peptidase with γ-Secretase Inhibitors
Weihofen, Andreas, Lemberg, Marius K., Friedmann, Elena, Rueeger, Heinrich, Schmitz, Albert, Paganetti, Paolo, Rovelli, Giorgio, Martoglio, Bruno
Published in The Journal of biological chemistry (09.05.2003)
Published in The Journal of biological chemistry (09.05.2003)
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Journal Article
A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-[beta] and neuroinflammation in APP transgenic mice
Neumann, Ulf, Rueeger, Heinrich, Machauer, Rainer, Veenstra, Siem Jacob, Lueoend, Rainer M, Tintelnot-Blomley, Marina, Laue, Grit, Beltz, Karen, Vogg, Barbara, Schmid, Peter, Frieauff, Wilfried, Shimshek, Derya R, Staufenbiel, Matthias, Jacobson, Laura H
Published in Molecular neurodegeneration (03.09.2015)
Published in Molecular neurodegeneration (03.09.2015)
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Journal Article
P4‐363: THE BACE INHIBITOR NB‐360 HAS EXCELLENT BRAIN PENETRATION AND EFFICACY ON AMYLOID‐B LOAD IN ANIMAL MODELS
Neumann, Ulf, Rueeger, Heinrich, Machauer, Rainer, Veenstra, Siem, Lueoend, Rainer, Tintelnot‐Blomley, Marina, Laue, Grit, Beltz, Karen, Vogg, Barbara, Shimshek, Derya, Frieauff, Wilfried, Schmid, Peter, Staufenbiel, Matthias, Jacobson, Laura H.
Published in Alzheimer's & dementia (01.07.2014)
Published in Alzheimer's & dementia (01.07.2014)
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Journal Article