Discovery Process and Pharmacological Characterization of 2-(S)-(4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide (Vestipitant) as a Potent, Selective, and Orally Active NK1 Receptor Antagonist
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Published in Journal of medicinal chemistry (28.05.2009)
Published in Journal of medicinal chemistry (28.05.2009)
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Synthesis and structure–activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists
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Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists
Micheli, Fabrizio, Cremonesi, Susanna, Semeraro, Teresa, Tarsi, Luca, Tomelleri, Silvia, Cavanni, Paolo, Oliosi, Beatrice, Perdonà, Elisabetta, Sava, Anna, Zonzini, Laura, Feriani, Aldo, Braggio, Simone, Heidbreder, Christian
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
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1,2,4-Triazolyl 5‑Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists
Micheli, Fabrizio, Bacchi, Alessia, Braggio, Simone, Castelletti, Laura, Cavallini, Palmina, Cavanni, Paolo, Cremonesi, Susanna, Dal Cin, Michele, Feriani, Aldo, Gehanne, Sylvie, Kajbaf, Mahmud, Marchió, Luciano, Nola, Selena, Oliosi, Beatrice, Pellacani, Annalisa, Perdonà, Elisabetta, Sava, Anna, Semeraro, Teresa, Tarsi, Luca, Tomelleri, Silvia, Wong, Andrea, Visentini, Filippo, Zonzini, Laura, Heidbreder, Christian
Published in Journal of medicinal chemistry (22.09.2016)
Published in Journal of medicinal chemistry (22.09.2016)
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1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists
Micheli, Fabrizio, Bernardelli, Andrea, Bianchi, Federica, Braggio, Simone, Castelletti, Laura, Cavallini, Palmina, Cavanni, Paolo, Cremonesi, Susanna, Cin, Michele Dal, Feriani, Aldo, Oliosi, Beatrice, Semeraro, Teresa, Tarsi, Luca, Tomelleri, Silvia, Wong, Andrea, Visentini, Filippo, Zonzini, Laura, Heidbreder, Christian
Published in Bioorganic & medicinal chemistry (15.04.2016)
Published in Bioorganic & medicinal chemistry (15.04.2016)
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The NK 1 receptor antagonist aprepitant attenuates NK 1 agonist‐induced scratching behaviour in the gerbil after intra‐dermal, topical or oral administration
Costantini, Vivian J. A., Corsi, Mauro, Dünstl, Georg, Bettelini, Letizia, Zonzini, Laura, Gerrard, Philip
Published in Experimental dermatology (01.04.2015)
Published in Experimental dermatology (01.04.2015)
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The NK1 receptor antagonist aprepitant attenuates NK1 agonist-induced scratching behaviour in the gerbil after intra-dermal, topical or oral administration
Costantini, Vivian J. A., Corsi, Mauro, Dünstl, Georg, Bettelini, Letizia, Zonzini, Laura, Gerrard, Philip
Published in Experimental dermatology (01.04.2015)
Published in Experimental dermatology (01.04.2015)
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1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: A New Series of Potent and Selective Triple Reuptake Inhibitors
Micheli, Fabrizio, Cavanni, Paolo, Arban, Roberto, Benedetti, Roberto, Bertani, Barbara, Bettati, Michela, Bettelini, Letizia, Bonanomi, Giorgio, Braggio, Simone, Checchia, Anna, Davalli, Silvia, Di Fabio, Romano, Fazzolari, Elettra, Fontana, Stefano, Marchioro, Carla, Minick, Doug, Negri, Michele, Oliosi, Beatrice, Read, Kevin D, Sartori, Ilaria, Tedesco, Giovanna, Tarsi, Luca, Terreni, Silvia, Visentini, Filippo, Zocchi, Alessandro, Zonzini, Laura
Published in Journal of medicinal chemistry (25.03.2010)
Published in Journal of medicinal chemistry (25.03.2010)
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Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045)
Bromidge, Steven M, Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J, Granci, Enrica, Leslie, Colin P, Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M, Worby, Angela, Zonzini, Laura, Zucchelli, Valeria
Published in Journal of medicinal chemistry (12.08.2010)
Published in Journal of medicinal chemistry (12.08.2010)
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In vitro and in vivo characterization of the novel GABA B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)
Perdona’, Elisabetta, Costantini, Vivian J.A., Tessari, Michela, Martinelli, Prisca, Carignani, Corrado, Valerio, Enzo, Mok, M.H. Selina, Zonzini, Laura, Visentini, Filippo, Gianotti, Massimo, Gordon, Laurie, Rocheville, Magalie, Corsi, Mauro, Capelli, Anna Maria
Published in Neuropharmacology (01.10.2011)
Published in Neuropharmacology (01.10.2011)
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Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT 1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4 H -imidazo[5,1- c ][1,4]benzoxazine-3-carboxamide (GSK588045)
Bromidge, Steven M., Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J., Granci, Enrica, Leslie, Colin P., Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M., Worby, Angela, Zonzini, Laura, Zucchelli, Valeria
Published in Journal of medicinal chemistry (12.08.2010)
Published in Journal of medicinal chemistry (12.08.2010)
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Discovery and Biological Characterization of (2R,4S)-1′-Acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4′-bipiperidine-1-carboxamide as a New Potent and Selective Neurokinin 1 (NK1) Receptor Antagonist Clinical Candidate
Di Fabio, Romano, Alvaro, Giuseppe, Griffante, Cristiana, Pizzi, Domenica A, Donati, Daniele, Mattioli, Mario, Cimarosti, Zadeo, Guercio, Giuseppe, Marchioro, Carla, Provera, Stefano, Zonzini, Laura, Montanari, Dino, Melotto, Sergio, Gerrard, Philip A, Trist, David G, Ratti, Emiliangelo, Corsi, Mauro
Published in Journal of medicinal chemistry (24.02.2011)
Published in Journal of medicinal chemistry (24.02.2011)
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In vivo rat PK profiling in drug discovery: new challenges
Zonzini, Laura, Bianchi, Federica, Cesari, Nicola, Sartori, Matteo
Published in Expert opinion on drug discovery (01.11.2010)
Published in Expert opinion on drug discovery (01.11.2010)
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1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: Further insights into a class of triple re-uptake inhibitors
Micheli, Fabrizio, Cavanni, Paolo, Bettati, Michela, Bonanomi, Giorgio, Di Fabio, Romano, Fazzolari, Elettra, Marchioro, Carla, Roscic, Maja, Tarsi, Luca, Visentini, Filippo, Zonzini, Laura, Worby, Angela
Published in Bioorganic & medicinal chemistry (01.06.2011)
Published in Bioorganic & medicinal chemistry (01.06.2011)
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Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: A new class of Neuropeptide S antagonists
MICHELI, Fabrizio, DI FABIO, Romano, ZARANTONELLO, Paola, ZONZINI, Laura, CAPELLI, Anna Maria, GIACOMETTI, Angelo, ROTH, Adelheid, MORO, Elisa, MERLO, Giancarlo, PAIO, Alfredo, MERLO-PICH, Emilio, TOMELLERI, Silvia, TONELLI, Federica
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
Published in Bioorganic & medicinal chemistry letters (15.12.2010)
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Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists
Pizzi, Domenica Antonia, Leslie, Colin Philip, Mazzali, Angelica, Seri, Catia, Biagetti, Matteo, Bentley, Jonathan, Genski, Thorsten, Di Fabio, Romano, Contini, Stefania, Sabbatini, Fabio Maria, Zonzini, Laura, Caberlotto, Laura
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
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Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT 1A/B/D Receptor Antagonist
Leslie, Colin P., Biagetti, Matteo, Bison, Silvia, Bromidge, Steven M., Di Fabio, Romano, Donati, Daniele, Falchi, Alessandro, Garnier, Martine J., Jaxa-Chamiec, Albert, Manchee, Gary, Merlo, Giancarlo, Pizzi, Domenica A., Stasi, Luigi P., Tibasco, Jessica, Vong, Antonio, Ward, Simon E., Zonzini, Laura
Published in Journal of medicinal chemistry (09.12.2010)
Published in Journal of medicinal chemistry (09.12.2010)
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Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D Receptor Antagonist
Leslie, Colin P, Biagetti, Matteo, Bison, Silvia, Bromidge, Steven M, Di Fabio, Romano, Donati, Daniele, Falchi, Alessandro, Garnier, Martine J, Jaxa-Chamiec, Albert, Manchee, Gary, Merlo, Giancarlo, Pizzi, Domenica A, Stasi, Luigi P, Tibasco, Jessica, Vong, Antonio, Ward, Simon E, Zonzini, Laura
Published in Journal of medicinal chemistry (09.12.2010)
Published in Journal of medicinal chemistry (09.12.2010)
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8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II
Bromidge, Steven M, Bertani, Barbara, Borriello, Manuela, Bozzoli, Andrea, Faedo, Stefania, Gianotti, Massimo, Gordon, Laurie J, Hill, Matthew, Zucchelli, Valeria, Watson, Jeannette M, Zonzini, Laura
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
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In vitro and in vivo characterization of the novel GABA sub(B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2- p iperidinyl}ethanol (CMPPE))
Perdona', Elisabetta, Costantini, Vivian JA, Tessari, Michela, Martinelli, Prisca, Carignani, Corrado, Valerio, Enzo, Mok, MHSelina, Zonzini, Laura, Visentini, Filippo, Gianotti, Massimo, Gordon, Laurie, Rocheville, Magalie, Corsi, Mauro, Capelli, Anna Maria
Published in Neuropharmacology (01.11.2011)
Published in Neuropharmacology (01.11.2011)
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