Structure-Activity Relationship, Biological, and Pharmacological Characterization of the Proline Sulfonamide ACT-462206: a Potent, Brain-Penetrant Dual Orexin 1/Orexin 2 Receptor A... von Boss, Christoph, Roch-Brisbare, Catherine, Steiner, Michel A., Treiber, Alexander, Dietrich, Hendrik, Jenck, Francois, von Raumer, Markus, Sifferlen, Thierry, Brotschi, Christine, Heidmann, Bibia, Williams, Jodi T., Aissaoui, Hamed, Siegrist, Romain, Gatfield, John

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Structure–activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Par... von Sifferlen, Thierry, Koberstein, Ralf, Cottreel, Emmanuelle, Boller, Amandine, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph

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Synthesis, structure–activity relationship studies, and identification of novel 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 1 von Sifferlen, Thierry, Koberstein, Ralf, Cottreel, Emmanuelle, Boller, Amandine, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph

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Design and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors von Bezençon, Olivier, Bur, Daniel, Weller, Thomas, Richard-Bildstein, Sylvia, Remeň, Luboš, Sifferlen, Thierry, Corminboeuf, Olivier, Grisostomi, Corinna, Boss, Christoph, Prade, Lars, Delahaye, Stéphane, Treiber, Alexander, Strickner, Panja, Binkert, Christoph, Hess, Patrick, Steiner, Beat, Fischli, Walter

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Scalable Preparation of 1‐Aminoethyl Substituted Chromanes von Diethelm, Stefan, Schmidt, Gunther, Sifferlen, Thierry, Boller, Amandine, Cornu, Laurent, Schmitt, Christine

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Discovery of Nivasorexant (ACT-539313): The First Selective Orexin‑1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials von Williams, Jodi T., Bolli, Martin H., Brotschi, Christine, Sifferlen, Thierry, Steiner, Michel A., Treiber, Alexander, Gatfield, John, Boss, Christoph

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Orexin Receptor Antagonism: A New Principle in Neuroscience von Boss, Christoph, Brisbare-Roch, Catherine, Jenck, Francois, Aissaoui, Hamed, Koberstein, Ralf, Sifferlen, Thierry, Weller, Thomas

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The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders von Boss, Christoph, Gatfield, John, Brotschi, Christine, Heidmann, Bibia, Sifferlen, Thierry, Raumer, Markus, Schmidt, Gunther, Williams, Jodi T., Treiber, Alexander, Roch, Catherine

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Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats von Brotschi, Christine, Bolli, Martin H, Gatfield, John, Roch, Catherine, Sifferlen, Thierry, Treiber, Alexander, Williams, Jodi T, Boss, Christoph

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Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep‐Promoting Properties in Rats von Brotschi, Christine, Roch, Catherine, Gatfield, John, Treiber, Alexander, Williams, Jodi T., Sifferlen, Thierry, Heidmann, Bibia, Jenck, Francois, Bolli, Martin H., Boss, Christoph

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From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs von Brotschi, Christine, Bolli, Martin H., Gatfield, John, Heidmann, Bibia, Jenck, Francois, Roch, Catherine, Sifferlen, Thierry, Treiber, Alexander, Williams, Jodi T., Boss, Christoph

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Front Cover: The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders (ChemMedChem 23/2020) von Boss, Christoph, Gatfield, John, Brotschi, Christine, Heidmann, Bibia, Sifferlen, Thierry, Raumer, Markus, Schmidt, Gunther, Williams, Jodi T., Treiber, Alexander, Roch, Catherine

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Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2 von Sifferlen, Thierry, Boller, Amandine, Chardonneau, Audrey, Cottreel, Emmanuelle, Gatfield, John, Treiber, Alexander, Roch, Catherine, Jenck, Francois, Aissaoui, Hamed, Williams, Jodi T, Brotschi, Christine, Heidmann, Bibia, Siegrist, Romain, Boss, Christoph

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Tetrahydroisoquinolines as Orexin Receptor Antagonists: Strategies for Lead Optimization by Solution-Phase Chemistry von Koberstein, Ralf, Treiber, Alexander, Sifferlen, Thierry, Nayler, Oliver, Mueller, Celia, Jenck, François, Fischli, Walter, Clozel, Martine, Bur, Daniel, Aissaoui, Hamed, Weller, Thomas

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Abstract 1809: ACT-1002-4391 - A novel potent antagonist of the prostaglandin E2 receptors EP2 and EP4 with excellent duality von Jeay, Sébastien, Diethelm, Stefan, Knopf, Agnes, Goxe, Marie, Daugan, Marie, Erupathil, Julie, Pothier, Julien, Pozzi, Davide, Sifferlen, Thierry, Wyder, Lorenza, Lyothier, Isabelle, Corminboeuf, Olivier, Lehembre, Francois, Renz, Imke, Meyer, Dominique

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Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach von Heidmann, Bibia, Gatfield, John, Roch, Catherine, Treiber, Alexander, Tortoioli, Simone, Brotschi, Christine, Williams, Jodi T., Bolli, Martin H., Abele, Stefan, Sifferlen, Thierry, Jenck, François, Boss, Christoph

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Discovery of substituted lactams as novel dual orexin receptor antagonists. Synthesis, preliminary structure-activity relationship studies and efforts towards improved metabolic st... von Sifferlen, Thierry, Boller, Amandine, Chardonneau, Audrey, Cottreel, Emmanuelle, Hoecker, Johannes, Aissaoui, Hamed, Williams, Jodi T, Brotschi, Christine, Heidmann, Bibia, Siegrist, Romain, Gatfield, John, Treiber, Alexander, Brisbare-Roch, Catherine, Jenck, Francois, Boss, Christoph

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Cover Picture: Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach (ChemMedChem 19/2016) von Heidmann, Bibia, Gatfield, John, Roch, Catherine, Treiber, Alexander, Tortoioli, Simone, Brotschi, Christine, Williams, Jodi T., Bolli, Martin H., Abele, Stefan, Sifferlen, Thierry, Jenck, François, Boss, Christoph

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Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists von Sifferlen, Thierry, Boss, Christoph, Cottreel, Emmanuelle, Koberstein, Ralf, Gude, Markus, Aissaoui, Hamed, Weller, Thomas, Gatfield, John, Brisbare-Roch, Catherine, Jenck, Francois

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Discovery and optimisation of 1-acyl-2-benzylpyrrolidines as potent dual orexin receptor antagonists von Williams, Jodi T., Gatfield, John, Roch, Catherine, Treiber, Alexander, Jenck, Francois, Bolli, Martin H., Brotschi, Christine, Sifferlen, Thierry, Heidmann, Bibia, Boss, Christoph

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