Search Results - "Cimarosti, Zadeo"

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 by Di Fabio, Romano, Griffante, Cristiana, Alvaro, Giuseppe, Pentassuglia, Giorgio, Pizzi, Domenica A, Donati, Daniele, Rossi, Tino, Guercio, Giuseppe, Mattioli, Mario, Cimarosti, Zadeo, Marchioro, Carla, Provera, Stefano, Zonzini, Laura, Montanari, Dino, Melotto, Sergio, Gerrard, Philip A, Trist, David G, Ratti, Emiliangelo, Corsi, Mauro

“…In an effort to discover novel druglike NK1 receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an…”
Get full text

Synthesis of the NK1 Receptor Antagonist GW597599. Part 3: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine Urea, A Happy End by Guercio, Giuseppe, Bacchi, Sergio, Perboni, Alcide, Leroi, Corinne, Tinazzi, Francesco, Bientinesi, Ilaria, Hourdin, Marie, Goodyear, Michael, Curti, Stefano, Provera, Stefano, Cimarosti, Zadeo

“…GW597599 1 is a novel NK-1 antagonist currently under investigation for the treatment of central nervous system disorders and emesis. The initial chemical…”
Get full text

Correction to “Development of a Control Strategy for a Defluorinated Analogue in the Manufacturing Process of Casopitant Mesylate” by Bravo, Fernando, Cimarosti, Zadeo, Tinazzi, Francesco, Castoldi, Damiano, Stonestreet, Paul, Galgano, Annalisa, Westerduin, Pieter

Get full text

Application of Quality by Design Principles to Support Development of a Control Strategy for the Control of Genotoxic Impurities in the Manufacturing Process of a Drug Substance by Cimarosti, Zadeo, Bravo, Fernando, Stonestreet, Paul, Tinazzi, Francesco, Vecchi, Orsola, Camurri, Giulio

“…As part of the search for drugs with activity on the central nervous system (CNS) a fluoroaryl-amine was identified and developed by GlaxoSmithKline. The…”
Get full text

Application of Quality by Design Principles for the Definition of a Robust Crystallization Process for Casopitant Mesylate by Castagnoli, Carlo, Yahyah, Mohammed, Cimarosti, Zadeo, Peterson, John J

“…GlaxoSmithKline (GSK) has identified casopitant as a potent NK1 antagonist. It was selected for its potential activities on a number of therapeutic targets…”
Get full text

Application of the QbD Principles in the Development of the Casopitant Mesylate Manufacturing Process. Process Research Studies for the Definition of the Control Strategy of some Drug Substance-CQAs for Stages 2a, 2b, and 2c by Cimarosti, Zadeo, Bravo, Fernando, Castoldi, Damiano, Tinazzi, Francesco, Provera, Stefano, Perboni, Alcide, Papini, Damiano, Westerduin, Pieter

“…Casopitant was identified as a potent NK1 antagonist by GlaxoSmithKline (GSK). It was selected as part of a wide drug discovery programme within GSK for its…”
Get full text

Development of Drug Substances as Mixture of Polymorphs: Studies to Control Form 3 in Casopitant Mesylate by Cimarosti, Zadeo, Castagnoli, Carlo, Rossetti, Marco, Scarati, Mirka, Day, Caroline, Johnson, Brendan, Westerduin, Pieter

“…Polymorphism is characterized as the ability of a drug substance to exist as two or more crystalline phases that have different arrangements and/or…”
Get full text

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 by 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

“…A large body of compelling preclinical evidence supports the clinical use of neurokinin (NK) receptor antagonists in a plethora of CNS and non-CNS therapeutic…”
Get full text

Development of an Efficient Large-Scale Synthesis for a 4 H -imidazo[5,1- c ][1,4]benzoxazine-3-carboxamide Derivative for Depression and Anxiety by Giubellina, Nicola, Stabile, Paolo, Laval, Gilles, Perboni, Alcide D., Cimarosti, Zadeo, Westerduin, Pieter, Cooke, Jason W. B.

Get full text

NMR spectroscopy and surface tension measurements applied to the study of self-association of casopitant mesylate, a novel NK1 antagonist by Provera, Stefano, Beato, Stefania, Cimarosti, Zadeo, Turco, Lucilla, Casazza, Andrea, Caivano, Grazia, Marchioro, Carla

“…The aggregation behaviour of casopitant mesylate, a new NK1 antagonist drug, was investigated by means of NMR spectroscopy and surface tension measurements…”
Get full text

Development of a Control Strategy for a Defluorinated Analogue in the Manufacturing Process of Casopitant Mesylate by Bravo, Fernando, Cimarosti, Zadeo, Tinazzi, Francesco, Castoldi, Damiano, Stonestreet, Paul, Galgano, Annalisa, Westerduin, Pieter

“…Casopitant mesylate was identified as part of the search for drugs with activity on the Central Nervous System (CNS) by GlaxoSmithKline. During late-phase…”
Get full text

Application of the Quality by Design Principles for the Development of the Crystallization Process for a Piperazinyl-Quinoline and Definition of the Control Strategy for Form 1 by Cimarosti, Zadeo, Rossi, Sara, Tramarin, Davide, Laval, Gilles, Stabile, Paolo, Giubellina, Nicola, Maton, William, Allieri, Brigida, Campi, Francesca, Cooke, Jason, Westerduin, Pieter

“…The studies carried out to develop a robust crystallization method for the substituted piperazinyl-quinoline (1) a compound potentially active in the treatment…”
Get full text

Development of a Dynamic Kinetic Resolution for the Isolation of an Intermediate in the Synthesis of Casopitant Mesylate: Application of QbD Principles in the Definition of the Parameter Ranges, Issues in the Scale-Up and Mitigation Strategies by Bravo, Fernando, Cimarosti, Zadeo, Tinazzi, Francesco, Smith, Gillian E, Castoldi, Damiano, Provera, Stefano, Westerduin, Pieter

“…Process development towards the improvement of the manufacturing process of casopitant mesylate (a drug developed by GlaxoSmithKline with activity on the…”
Get full text

Development of an Efficient Large-Scale Synthesis for a 4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide Derivative for Depression and Anxiety by Giubellina, Nicola, Stabile, Paolo, Laval, Gilles, Perboni, Alcide D, Cimarosti, Zadeo, Westerduin, Pieter, Cooke, Jason W. B

“…The development and scale-up of an optimized synthesis for a novel drug candidate for depression and anxiety is presented. The updated synthesis represents a…”
Get full text

Detection, identification and quantification of a new de-fluorinated impurity in casopitant mesylate drug substance during late phase development: An analytical challenge involving a multidisciplinary approach by Turco, Lucilla, Provera, Stefano, Curcuruto, Ornella, Bernabè, Elena, Nicoletti, Anna, Martini, Luca, Castoldi, Damiano, Cimarosti, Zadeo, Papini, Damiano, Marchioro, Carla, Dams, Riet

“…During late phase development of the selective NK1 receptor antagonist casopitant mesylate, a de-fluorinated impurity was discovered and quantified by an…”
Get full text

Route Selection and Process Development for a 5-Piperazinylquinaldine Derivative for the Treatment of Depression and Anxiety by Cimarosti, Zadeo, Giubellina, Nicola, Stabile, Paolo, Laval, Gilles, Tinazzi, Francesco, Maton, William, Pachera, Roberta, Russo, Paola, Moretti, Ramona, Rossi, Sara, Cooke, Jason W. B., Westerduin, Pieter

“…1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone, 1, was identified as a potential drug for the treatment of depression and…”
Get full text

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 NK 1 Receptor Antagonist by Di Fabio, Romano, Griffante, Cristiana, Alvaro, Giuseppe, Pentassuglia, Giorgio, Pizzi, Domenica A., Donati, Daniele, Rossi, Tino, Guercio, Giuseppe, Mattioli, Mario, Cimarosti, Zadeo, Marchioro, Carla, Provera, Stefano, Zonzini, Laura, Montanari, Dino, Melotto, Sergio, Gerrard, Philip A., Trist, David G., Ratti, Emiliangelo, Corsi, Mauro

Get full text