Search Results - "Norcross, Roger D."

selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system by Bradaia, Amyaouch, Trube, Gerhard, Stalder, Henri, Norcross, Roger D, Ozmen, Laurence, Wettstein, Joseph G, Pinard, Audrée, Buchy, Danièle, Gassmann, Martin, Hoener, Marius C, Bettler, Bernhard

“…Trace amine-associated receptor 1 (TAAR1) is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids…”
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Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a Promising Novel Medicine To Treat Schizophrenia by Pinard, Emmanuel, Alanine, Alexander, Alberati, Daniela, Bender, Markus, Borroni, Edilio, Bourdeaux, Patrick, Brom, Virginie, Burner, Serge, Fischer, Holger, Hainzl, Dominik, Halm, Remy, Hauser, Nicole, Jolidon, Synese, Lengyel, Judith, Marty, Hans-Peter, Meyer, Thierry, Moreau, Jean-Luc, Mory, Roland, Narquizian, Robert, Nettekoven, Mathias, Norcross, Roger D, Puellmann, Bernd, Schmid, Philipp, Schmitt, Sebastien, Stalder, Henri, Wermuth, Roger, Wettstein, Joseph G, Zimmerli, Daniel

“…The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the…”
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Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): Discovery of EPPTB ( RO5212773) by Stalder, Henri, Hoener, Marius C., Norcross, Roger D.

“…High throughput screening of the Roche compound library identified benzanilides such as 1 and 2 as antagonists of TAAR1. Optimisation of this hit series led to…”
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Incretin-like effects of small molecule trace amine-associated receptor 1 agonists by Raab, Susanne, Wang, Haiyan, Uhles, Sabine, Cole, Nadine, Alvarez-Sanchez, Ruben, Künnecke, Basil, Ullmer, Christoph, Matile, Hugues, Bedoucha, Marc, Norcross, Roger D, Ottaway-Parker, Nickki, Perez-Tilve, Diego, Conde Knape, Karin, Tschöp, Matthias H, Hoener, Marius C, Sewing, Sabine

“…Abstract Objective Type 2 diabetes and obesity are emerging pandemics in the 21st century creating worldwide urgency for the development of novel and safe…”
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Total Synthesis of Bioactive Marine Macrolides by Norcross, Roger D, Paterson, Ian

“…Chemical efforts directed toward the synthesis of a specific subset of biologically active marine natural products, namely those compounds that possess a…”
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Bis(oxazoline) and Bis(oxazolinyl)pyridine Copper Complexes as Enantioselective Diels−Alder Catalysts:  Reaction Scope and Synthetic Applications by Evans, David A, Barnes, David M, Johnson, Jeffrey S, Lectka, Thomas, von Matt, Peter, Miller, Scott J, Murry, Jerry A, Norcross, Roger D, Shaughnessy, Eileen A, Campos, Kevin R

“…The scope of the Diels−Alder reaction catalyzed by bis(oxazoline) copper complexes has been investigated. In particular, [Cu((S,S)-t-Bu-box)](SbF6)2 (1b) has…”
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A UGT2B10 splicing polymorphism common in african populations may greatly increase drug exposure by Fowler, Stephen, Kletzl, Heidemarie, Finel, Moshe, Manevski, Nenad, Schmid, Paul, Tuerck, Dietrich, Norcross, Roger D, Hoener, Marius C, Spleiss, Olivia, Iglesias, Victor A

“…RO5263397 [(S)-4-(3-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine], a new compound that showed promising results in animal models of schizophrenia, is…”
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Studies in Macrolide Synthesis: A Stereocontrolled Synthesis of Oleandolide Employing Reagent- and Substrate-Controlled Aldol Reactions of (S)-1-(Benzyloxy)-2-methylpentan-3-one by Paterson, Ian, Norcross, Roger D, Ward, Richard A, Romea, Pedro, Lister, M. Anne

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Trace Amine-Associated Receptor 1 Partial Agonism Reveals Novel Paradigm for Neuropsychiatric Therapeutics by Revel, Florent G, Moreau, Jean-Luc, Gainetdinov, Raul R, Ferragud, Antonio, Velázquez-Sánchez, Clara, Sotnikova, Tatyana D, Morairty, Stephen R, Harmeier, Anja, Groebke Zbinden, Katrin, Norcross, Roger D, Bradaia, Amyaouch, Kilduff, Thomas S, Biemans, Barbara, Pouzet, Bruno, Caron, Marc G, Canales, Juan J, Wallace, Tanya L, Wettstein, Joseph G, Hoener, Marius C

“…Background Trace amines, compounds structurally related to classical biogenic amines, represent endogenous ligands of the trace amine-associated receptor 1…”
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Optimisation of imidazole compounds as selective TAAR1 agonists: Discovery of RO5073012 by Galley, Guido, Stalder, Henri, Goergler, Annick, Hoener, Marius C., Norcross, Roger D.

“…A series of imidazole compounds has been identified which affords potent and selective partial and full agonists of the TAAR1 receptor. Starting from…”
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Brain-Specific Overexpression of Trace Amine-Associated Receptor I Alters Monoaminergic Neurotransmission and Decreases Sensitivity to Amphetamine by REVEL, Florent G, MEYER, Claas A, INVERNIZZI, Roberto W, WETTSTEIN, Joseph G, MOREAU, Jean-Luc, HOENER, Marius C, BRADAIA, Amyaouch, JEANNEAU, Karine, CALCAGNO, Eleonora, ANDRE, Cédric B, HAENGGI, Markus, MISS, Marie-Thérèse, GALLEY, Guido, NORCROSS, Roger D

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4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: Drug-like and non-xanthine based A2B adenosine receptor antagonists by Cheung, Adrian Wai-Hing, Brinkman, John, Firooznia, Fariborz, Flohr, Alexander, Grimsby, Joseph, Gubler, Mary Lou, Guertin, Kevin, Hamid, Rachid, Marcopulos, Nicholas, Norcross, Roger D., Qi, Lida, Ramsey, Gwendolyn, Tan, Jenny, Wen, Yang, Sarabu, Ramakanth

“…7-N-Acetamide-4-methoxy-2-aminobenzothiazole 4-fluorobenzamide (compound 1) was chosen as a drug-like and non-xanthine based starting point for the discovery…”
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Brain-specific overexpression of trace amine-associated receptor 1 alters monoaminergic neurotransmission and decreases sensitivity to amphetamine by Revel, Florent G, Meyer, Claas A, Bradaia, Amyaouch, Jeanneau, Karine, Calcagno, Eleonora, André, Cédric B, Haenggi, Markus, Miss, Marie-Thérèse, Galley, Guido, Norcross, Roger D, Invernizzi, Roberto W, Wettstein, Joseph G, Moreau, Jean-Luc, Hoener, Marius C

“…Trace amines (TAs) such as β-phenylethylamine, p-tyramine, or tryptamine are biogenic amines found in the brain at low concentrations that have been implicated…”
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Discovery and Characterization of 2‑Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists by Galley, Guido, Beurier, Angélica, Décoret, Guillaume, Goergler, Annick, Hutter, Roman, Mohr, Susanne, Pähler, Axel, Schmid, Philipp, Türck, Dietrich, Unger, Robert, Zbinden, Katrin Groebke, Hoener, Marius C, Norcross, Roger D

“…2-Aminooxazolines were discovered as a novel structural class of TAAR1 ligands. Starting from a known adrenergic compound 1, structural modifications were made…”
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Synthesis of enantiomerically pure [14C]-labelled morpholine derivatives for a class of trace amine-associate receptor 1 agonists by Edelmann, Martin R., Hartung, Thomas, Trussardi, René, Iding, Hans, Galley, Guido, Pflieger, Philippe, Norcross, Roger D.

“…Various agonists of the trace amine‐associate receptor 1, under consideration as potential clinical development candidates, were labelled with carbon‐14 for…”
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Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors by Pinard, Emmanuel, Alberati, Daniela, Borroni, Edilio, Fischer, Holger, Hainzl, Dominik, Jolidon, Synèse, Moreau, Jean-Luc, Narquizian, Robert, Nettekoven, Matthias, Norcross, Roger D., Stalder, Henri, Thomas, Andrew W.

“…Screening of the Roche compound library led to the identification of the benzoylpiperazine 7 as a structurally novel GlyT1 inhibitor. The SAR which was…”
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Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors by Pinard, Emmanuel, Alberati, Daniela, Bender, Markus, Borroni, Edilio, Brom, Virginie, Burner, Serge, Fischer, Holger, Hainzl, Dominik, Halm, Remy, Hauser, Nicole, Jolidon, Synèse, Lengyel, Judith, Marty, Hans-Peter, Meyer, Thierry, Moreau, Jean-Luc, Mory, Roland, Narquizian, Robert, Norcross, Roger D., Schmid, Philipp, Wermuth, Roger, Zimmerli, Daniel

“…Benzoylisoindolines were discovered as a novel structural class of GlyT1 inhibitors. The SAR studies followed by the lead optimization effort focused primarily…”
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Stereocontrolled Total Synthesis of (+)-Altohyrtin A/Spongistatin 1 by Paterson, Ian, Chen, David Y.-K., Coster, Mark J., Aceña, Jose L., Bach, Jordi, Gibson, Karl R., Keown, Linda E., Oballa, Renata M., Trieselmann, Thomas, Wallace, Debra J., Hodgson, Andrew P., Norcross, Roger D.

“…As an exceptionally potent antimitotic macrolide, altohyrtin A/spongistatin 1 shows great promise in cancer chemotherapy but its extreme scarcity in the…”
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The stereocontrolled total synthesis of altohyrtin A/spongistatin 1: the AB-spiroacetal segment by Paterson, Ian, Coster, Mark J, Chen, David Y-K, Oballa, Renata M, Wallace, Debra J, Norcross, Roger D

“…The convergent synthesis of the C1-C15 AB-spiroacetal subunit of altohyrtin A/spongistatin 1 is described. This highly stereocontrolled synthesis relies on…”
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Radiosynthesis of [5-[11C]methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-[5-(tetrahydro-pyran-4-yl)-1,3-dihydro-isoindol-2-yl]-methanone ([11C]RO5013853), a novel PET tracer for the glycine transporter type I (GlyT1) by Pinard, Emmanuel, Burner, Serge, Cueni, Philipp, Hartung, Thomas, Norcross, Roger D., Schmid, Philipp, Waldmeier, Pius, Zielinski, Guy, Ravert, Hayden T., Holt, Daniel P., Dannals, Robert F.

“…The glycine transporter type 1 (GlyT1) has emerged as a key novel target for the treatment of schizophrenia. We have recently discovered and developed…”
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