Target-Based Identification and Optimization of 5‑Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay
Knoepfel, Thomas, Nimsgern, Pierre, Jacquier, Sébastien, Bourrel, Marjorie, Vangrevelinghe, Eric, Glatthar, Ralf, Behnke, Dirk, Alper, Phil B, Michellys, Pierre-Yves, Deane, Jonathan, Junt, Tobias, Zipfel, Géraldine, Limonta, Sarah, Hawtin, Stuart, Andre, Cedric, Boulay, Thomas, Loetscher, Pius, Faller, Michael, Blank, Jutta, Feifel, Roland, Betschart, Claudia
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
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The mTOR kinase inhibitor Everolimus decreases S6 kinase phosphorylation but fails to reduce mutant huntingtin levels in brain and is not neuroprotective in the R6/2 mouse model of Huntington's disease
Fox, Jonathan H, Connor, Teal, Chopra, Vanita, Dorsey, Kate, Kama, Jibrin A, Bleckmann, Dorothee, Betschart, Claudia, Hoyer, Daniel, Frentzel, Stefan, Difiglia, Marian, Paganetti, Paolo, Hersch, Steven M
Published in Molecular neurodegeneration (22.06.2010)
Published in Molecular neurodegeneration (22.06.2010)
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Distinct effects of IPSU and suvorexant on mouse sleep architecture
Hoyer, Daniel, Dürst, Thomas, Fendt, Markus, Jacobson, Laura H, Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Laue, Grit, Ofner, Silvio, Legangneux, Eric, Gee, Christine E
Published in Frontiers in neuroscience (01.01.2013)
Published in Frontiers in neuroscience (01.01.2013)
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Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors
Callander, Gabrielle E, Olorunda, Morenike, Monna, Dominique, Schuepbach, Edi, Langenegger, Daniel, Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Fendt, Markus, Laue, Grit, Ofner, Silvio, Briard, Emmanuelle, Gee, Christine E, Jacobson, Laura H, Hoyer, Daniel
Published in Frontiers in neuroscience (01.01.2013)
Published in Frontiers in neuroscience (01.01.2013)
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Huntingtin cleavage product A forms in neurons and is reduced by gamma-secretase inhibitors
Kegel, Kimberly B, Sapp, Ellen, Alexander, Jonathan, Reeves, Patrick, Bleckmann, Dorothee, Sobin, Linsday, Masso, Nicholas, Valencia, Antonio, Jeong, Hyunkyung, Krainc, Dimitri, Palacino, James, Curtis, Daniel, Kuhn, Rainer, Betschart, Claudia, Sena-Esteves, Miguel, Aronin, Neil, Paganetti, Paolo, Difiglia, Marian
Published in Molecular neurodegeneration (14.12.2010)
Published in Molecular neurodegeneration (14.12.2010)
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Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture for the Treatment of Insomnia
Betschart, Claudia, Hintermann, Samuel, Behnke, Dirk, Cotesta, Simona, Fendt, Markus, Gee, Christine E, Jacobson, Laura H, Laue, Grit, Ofner, Silvio, Chaudhari, Vinod, Badiger, Sangamesh, Pandit, Chetan, Wagner, Juergen, Hoyer, Daniel
Published in Journal of medicinal chemistry (10.10.2013)
Published in Journal of medicinal chemistry (10.10.2013)
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Structure-Based and Property-Driven Optimization of N‑Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors
Hoegenauer, Klemens, Kallen, Joerg, Jiménez-Núñez, Eloísa, Strang, Ross, Ertl, Peter, Cooke, Nigel G, Hintermann, Samuel, Voegtle, Markus, Betschart, Claudia, McKay, Daniel J. J, Wagner, Juergen, Ottl, Johannes, Beerli, Christian, Billich, Andreas, Dawson, Janet, Kaupmann, Klemens, Streiff, Markus, Gobeau, Nathalie, Harlfinger, Stephanie, Stringer, Rowan, Guntermann, Christine
Published in Journal of medicinal chemistry (12.12.2019)
Published in Journal of medicinal chemistry (12.12.2019)
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Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway
Alper, Phil B., Deane, Jonathan, Betschart, Claudia, Buffet, David, Collignon Zipfel, Géraldine, Gordon, Perry, Hampton, Janice, Hawtin, Stuart, Ibanez, Maureen, Jiang, Tao, Junt, Tobias, Knoepfel, Thomas, Liu, Bo, Maginnis, Jillian, McKeever, Una, Michellys, Pierre-Yves, Mutnick, Daniel, Nayak, Bishnu, Niwa, Satoru, Richmond, Wendy, Rush, James S., Syka, Peter, Zhang, Yi, Zhu, Xuefeng
Published in Bioorganic & medicinal chemistry letters (01.09.2020)
Published in Bioorganic & medicinal chemistry letters (01.09.2020)
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Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases
Alper, Phil, Betschart, Claudia, André, Cédric, Boulay, Thomas, Cheng, Dai, Deane, Jonathan, Faller, Michael, Feifel, Roland, Glatthar, Ralf, Han, Dong, Hemmig, Rene, Jiang, Tao, Knoepfel, Thomas, Maginnis, Jillian, Mutnick, Daniel, Pei, Wei, Ruzzante, Giulia, Syka, Peter, Zhang, Guobao, Zhang, Yi, Zink, Florence, Zipfel, Géraldine, Hawtin, Stuart, Junt, Tobias, Michellys, Pierre-Yves
Published in ACS medicinal chemistry letters (10.08.2023)
Published in ACS medicinal chemistry letters (10.08.2023)
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Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist
Betschart, Claudia, Faller, Michael, Zink, Florence, Hemmig, René, Blank, Jutta, Vangrevelinghe, Eric, Bourrel, Marjorie, Glatthar, Ralf, Behnke, Dirk, Barker, Kerstin, Heizmann, Andreas, Angst, Daniela, Nimsgern, Pierre, Jacquier, Sébastien, Junt, Tobias, Zipfel, Géraldine, Ruzzante, Giulia, Loetscher, Pius, Limonta, Sarah, Hawtin, Stuart, Andre, Cedric Bernard, Boulay, Thomas, Feifel, Roland, Knoepfel, Thomas
Published in ACS medicinal chemistry letters (14.04.2022)
Published in ACS medicinal chemistry letters (14.04.2022)
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Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs)
Behnke, Dirk, Cotesta, Simona, Hintermann, Samuel, Fendt, Markus, Gee, Christine E., Jacobson, Laura H., Laue, Grit, Meyer, Arndt, Wagner, Trixie, Badiger, Sangamesh, Chaudhari, Vinod, Chebrolu, Murali, Pandit, Chetan, Hoyer, Daniel, Betschart, Claudia
Published in Bioorganic & medicinal chemistry letters (01.12.2015)
Published in Bioorganic & medicinal chemistry letters (01.12.2015)
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Preclinical characterization of the Toll-like receptor 7/8 antagonist MHV370 for lupus therapy
Hawtin, Stuart, André, Cédric, Collignon-Zipfel, Géraldine, Appenzeller, Simone, Bannert, Bettina, Baumgartner, Lea, Beck, Damian, Betschart, Claudia, Boulay, Thomas, Brunner, Hermine I., Ceci, Melanie, Deane, Jonathan, Feifel, Roland, Ferrero, Enrico, Kyburz, Diego, Lafossas, Frederique, Loetscher, Pius, Merz-Stoeckle, Christina, Michellys, Pierre, Nuesslein-Hildesheim, Barbara, Raulf, Friedrich, Rush, James S., Ruzzante, Giulia, Stein, Thomas, Zaharevitz, Samantha, Wieczorek, Grazyna, Siegel, Richard, Gergely, Peter, Shisha, Tamas, Junt, Tobias
Published in Cell reports. Medicine (16.05.2023)
Published in Cell reports. Medicine (16.05.2023)
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Structure-Based Design and Synthesis of Macroheterocyclic Peptidomimetic Inhibitors of the Aspartic Protease β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE)
Hanessian, Stephen, Yang, Gaoqiang, Rondeau, Jean-Michel, Neumann, Ulf, Betschart, Claudia, Tintelnot-Blomley, Marina
Published in Journal of medicinal chemistry (27.07.2006)
Published in Journal of medicinal chemistry (27.07.2006)
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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
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic β-secretase (BACE-1) inhibitors
Hanessian, Stephen, Shao, Zhihui, Betschart, Claudia, Rondeau, Jean-Michel, Neumann, Ulf, Tintelnot-Blomley, Marina
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
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Corrigendum to “Structure-based design and synthesis of novel P2/P3 modified, non-peptidic β-secretase (BACE-1) inhibitors” [Bioorg. Med. Chem. Lett. 20 (2010) 1924–1927]
Hanessian, Stephen, Shao, Zhihui, Betschart, Claudia, Rondeau, Jean-Michel, Neumann, Ulf, Tintelnot-Blomley, Marina
Published in Bioorganic & medicinal chemistry letters (15.04.2013)
Published in Bioorganic & medicinal chemistry letters (15.04.2013)
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Journal Article
Structure-based design and synthesis of macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors
Machauer, Rainer, Veenstra, Siem, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Betschart, Claudia, Neumann, Ulf, Paganetti, Paolo
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
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Journal Article
Discovery of 1 H -pyrazolo[3,4- b ]pyridines as potent dual orexin receptor antagonists (DORAs)
Behnke, Dirk, Cotesta, Simona, Hintermann, Samuel, Fendt, Markus, Gee, Christine E., Jacobson, Laura H., Laue, Grit, Meyer, Arndt, Wagner, Trixie, Badiger, Sangamesh, Chaudhari, Vinod, Chebrolu, Murali, Pandit, Chetan, Hoyer, Daniel, Betschart, Claudia
Published in Bioorganic & medicinal chemistry letters (01.12.2015)
Published in Bioorganic & medicinal chemistry letters (01.12.2015)
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Journal Article
Macrocyclic peptidomimetic β-secretase (BACE-1) inhibitors with activity in vivo
Machauer, Rainer, Laumen, Kurt, Veenstra, Siem, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Betschart, Claudia, Jaton, Anne-Lise, Desrayaud, Sandrine, Staufenbiel, Matthias, Rabe, Sabine, Paganetti, Paolo, Neumann, Ulf
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
Published in Bioorganic & medicinal chemistry letters (01.03.2009)
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Journal Article
2-Cyano-pyrimidines: A New Chemotype for Inhibitors of the Cysteine Protease Cathepsin K
Altmann, Eva, Aichholz, Reiner, Betschart, Claudia, Buhl, Thomas, Green, Jonathan, Irie, Osamu, Teno, Naoki, Lattmann, René, Tintelnot-Blomley, Marina, Missbach, Martin
Published in Journal of medicinal chemistry (22.02.2007)
Published in Journal of medicinal chemistry (22.02.2007)
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