未登录Novel Macrocyclic NLRP3 Inhibitors
Mesch, Stefanie; Shannon, Jonathan; Miller, David; Macleod, Angus; Bouche, Lea; Johnston, Heather J.; Matthews, Kim; Paehler, Axel; Best, Stuart; Guba, Wolfgang; Alanine, Thomas; Halai, Reena; Charge, Lorna; Garside, Samantha; Thom, Stephen; Incerti-Pradillos, Celia; Mcpherson, Christopher; Carrillo, Jokin; St-Gallay, Steve; Rigo, Pierre; Schlicht, Sonja; Hendrick, Alan G.; Lerner, Christian; Piali, Luca; Blaising, Julie; Mracsko, Eva Z.; Jaeschke, Georg; Cooper, Matthew A. .png)
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收藏Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with OsimertinibObst-Sander, Ulrike; Ricci, Antonio; Kuhn, Bernd; Friess, Thomas; Koldewey, Philipp; Kuglstatter, Andreas; Hewings, David; Goergler, Annick; Steiner, Sandra; Rueher, Daniel; Imhoff, Marie-Paule; Raschetti, Noemi; Marty, Hans-Peter; Dietzig, Aline; Rynn, Caroline; Ehler, Andreas; Burger, Dominique; Kornacker, Martin; Schaffland, Jeannine Petrig; Herting, Frank; Pao, William; Bischoff, James R.; Martoglio, Bruno; Nagel, Yvonne Alice; Jaeschke, Georg 分享 收藏 Chemical, Analytical and Pharmacokinetic Characterisation of RO7304898, an API Consisting of Two Rapidly Interconverting DiastereoisomersHeinig, Katja; Sladojevich, Filippo; Schaffland, Jeannine Petrig; Jaeschke, Georg; Ross, Alfred; Koldewey, Philipp; Miladinovic, Sasa M.; Wang, Jin; Rynn, Caroline 分享 收藏 Results and evaluation of a first-in-human study of RG7342, an mGlu5 positive allosteric modulator, utilizing Bayesian adaptive methodsSturm, Stefan; Delporte, Marie-Laure; Hadi, Salah; Schobel, Scott; Lindemann, Lothar; Weikert, Robert; Jaeschke, Georg; Derks, Michael; Palermo, Giuseppe 分享 收藏 mGluR5 Modulation of Behavioral and Epileptic Phenotypes in a Mouse Model of Tuberous Sclerosis ComplexKelly, Elyza; Schaeffer, Samantha M.; Dhamne, Sameer C.; Lipton, Jonathan O.; Lindemann, Lothar; Honer, Michael; Jaeschke, Georg; Super, Chloe E.; Lammers, Stephen H. T.; Modi, Meera E.; Silverman, Jill L.; Dreier, John R.; Kwiatkowski, David J.; Rotenberg, Alexander; Sahin, Mustafa 分享 收藏 Blocking metabotropic glutamate receptor subtype 5 relieves maladaptive chronic stress consequencesPeterlik, Daniel; Stangl, Christina; Bauer, Amelie; Bludau, Anna; Keller, Jana; Grabski, Dominik; Killian, Tobias; Schmidt, Dominic; Zajicek, Franziska; Jaeschke, Georg; Lindemann, Lothar; Reber, Stefan O.; Flor, Peter J.; Uschold-Schmidt, Nicole 分享 收藏 Pharmacology of Basimglurant (RO4917523, RG7090), a Unique Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator in Clinical Development for DepressionLindemann, Lothar; Porter, Richard H.; Scharf, Sebastian H.; Kuennecke, Basil; Bruns, Andreas; von Kienlin, Markus; Harrison, Anthony C.; Paehler, Axel; Funk, Christoph; Gloge, Andreas; Schneider, Manfred; Parrott, Neil J.; Polonchuk, Liudmila; Niederhauser, Urs; Morairty, Stephen R.; Kilduff, Thomas S.; Vieira, Eric; Kolczewski, Sabine; Wichmann, Juergen; Hartung, Thomas; Honer, Michael; Borroni, Edilio; Moreau, Jean-Luc; Prinssen, Eric; Spooren, Will; Wettstein, Joseph G.; Jaeschke, Georg 分享 收藏 Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators: Discovery of 2-Chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyllpyridine (Basimglurant, R04917523), a Promising Novel Medicine for Psychiatric DiseasesJaeschke, Georg; Kolczewski, Sabine; Spooren, Will; Vieira, Eric; Bitter-Stoll, Nadia; Boissin, Patrick; Borroni, Edilio; Buettelmann, Bernd; Ceccarelli, Simona; Clemann, Nicole; David, Beatrice; Funk, Christoph; Guba, Wolfgang; Harrison, Anthony; Hartung, Thomas; Honer, Michael; Huwyler, Joerg; Kuratli, Martin; Niederhauser, Urs; Paehler, Axel; Peters, Jens-Uwe; Petersen, Ann; Prinssen, Eric; Ricci, Antonio; Rueher, Daniel; Rueher, Marianne; Schneider, Manfred; Spurr, Paul; Stoll, Theodor; Taennler, Daniel; Wichmann, Juergen; Porter, Richard H.; Wettstein, Joseph G.; Lindemann, Lothar 分享 收藏 分享 收藏 Chronic Metabotropic Glutamate Receptor 5 Inhibition Corrects Local Alterations of Brain Activity and Improves Cognitive Performance in Fragile X MiceMichalon, Aubin; Bruns, Andreas; Risterucci, Celine; Honer, Michael; Ballard, Theresa M.; Ozmen, Laurence; Jaeschke, Georg; Wettstein, Joseph G.; von Kienlin, Markus; Kuennecke, Basil; Lindemann, Lothar 分享 收藏 分享 收藏 CTEP: A Novel, Potent, Long-Acting, and Orally Bioavailable Metabotropic Glutamate Receptor 5 InhibitorLindemann, Lothar; Jaeschke, Georg; Michalon, Aubin; Vieira, Eric; Honer, Michael; Spooren, Will; Porter, Richard; Hartung, Thomas; Kolczewski, Sabine; Buettelmann, Bernd; Flament, Christophe; Diener, Catherine; Fischer, Christophe; Gatti, Silvia; Prinssen, Eric P.; Parrott, Neil; Hoffmann, Gerhard; Wettstein, Joseph G. 分享 收藏 分享 收藏 Metabolite identification via LC-SPE-NMR-MS of the in vitro biooxidation products of a lead mGIu5 allosteric antagonist and impact on the improvement of metabolic stability in the seriesCeccarelli, Simona M.; Schlotterbeck, Goetz; Boissin, Patrick; Binder, Martin; Buettelmann, Bernd; Hanlon, Steven; Jaeschke, Georg; Kolczewski, Sabine; Kupfer, Ernst; Peters, Jens-Uwe; Porter, Richard H. P.; Prinssen, Eric P.; Rueher, Marianne; Ruf, Iris; Spooren, Will; Staempfli, Andreas; Vieira, Eric 分享 收藏 Predicting properties and tuning physicochemical in lead optimization:: Amine basicitiesMorgenthaler, Martin; Schweizer, Eliane; Hoffmann-Roeder, Ania; Benini, Fausta; Martin, Rainer E.; Jaeschke, Georg; Wagner, Bjoern; Fischer, Holger; Bendels, Stefanie; Zimmerli, Daniel; Schneider, Josef; Diederich, Francois; Kansy, Manfred; Mueller, Klaus 分享 收藏 分享 收藏 Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors确定与3,3 ′-二氟苯并哒嗪对大鼠mGlu5受体的变构调节作用有关的关键氨基酸Mühlemann, A; Ward, NA; Kratochwil, N; Diener, C; Fischer, C; Stucki, A; Jaeschke, G; Malherbe, P; Porter, RHP 分享 收藏 Fenobam:: A clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activityPorter, RHP; Jaeschke, G; Spooren, W; Ballard, TM; Büttelmann, B; Kolczewski, S; Peters, JU; Prinssen, E; Wichmann, J; Vieira, E; Mühlemann, A; Gatti, S; Mutel, V; Malherbe, P 分享 收藏 分享 收藏 分享 收藏 
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