Výsledky vyhledávání - "Francesco Tinazzi"

Route Selection and Process Development for a 5-Piperazinylquinaldine Derivative for the Treatment of Depression and Anxiety

Autor: Sara Rossi, Paolo Stabile, Jason W. B. Cooke, Gilles Laval, Paola Russo, Roberta Pachera, Ramona Moretti, Pieter Westerduin, Zadeo Cimarosti, Nicola Giubellina, Francesco Tinazzi, William Maton

Publikováno v: Organic Process Research & Development. 15:1287-1296

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 anxiety. Herein is described the work carried out to select the manufacturing route and the pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f192f5af1e4d746b5fb7e9edfa63ad2c
https://doi.org/10.1021/op200140v

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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

Autor: Fernando Bravo, Stefano Provera, Pieter Westerduin, Zadeo Cimarosti, Damiano Castoldi, Gillian E. Smith, Francesco Tinazzi

Publikováno v: Organic Process Research & Development. 14:1162-1168

Process development towards the improvement of the manufacturing process of casopitant mesylate (a drug developed by GlaxoSmithKline with activity on the central nervous system) identified a dynamic kinetic resolution opportunity for the improvement

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1e653e972bcf2bba4eb02a88d12466d1
https://doi.org/10.1021/op100121s

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Development of a Control Strategy for a Defluorinated Analogue in the Manufacturing Process of Casopitant Mesylate

Autor: Francesco Tinazzi, Pieter Westerduin, Damiano Castoldi, Fernando Bravo, Annalisa Galgano, Zadeo Cimarosti, Paul Stonestreet

Publikováno v: Organic Process Research & Development. 14:832-839

Casopitant mesylate was identified as part of the search for drugs with activity on the Central Nervous System (CNS) by GlaxoSmithKline. During late-phase development studies to develop the manufacturing process, a new impurity was found. This synthe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9ba9fb6c670a0198b4e4c8ba1c706ef3
https://doi.org/10.1021/op1000836

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The Synthesis of GV143253A: A Case Study for the Use of Analytical and Statistical Tools to Elucidate the Reaction Mechanism and to Optimize the Process

Autor: Francesco Tinazzi, Alcide Perboni, Luca Rovatti, Stefano Provera, Giuseppe Guercio

Publikováno v: Organic Process Research & Development. 14:840-848

GV143253A 1 is a broad-spectrum injectable β-lactam belonging to the class of trinem antibiotics. This article describes the work which enabled a detailed process understanding via several analytical techniques and the subsequent optimization of a k

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::550956663d2dccfed589e253f7c68396
https://doi.org/10.1021/op100097c

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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

Autor: Stefano Provera, Fernando Bravo, Damiano Papini, Pieter Westerduin, Damiano Castoldi, Zadeo Cimarosti, Alcide Perboni, Francesco Tinazzi

Publikováno v: Organic Process Research & Development. 14:805-814

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 potential activities on a number of therapeutic targets such as inflammatory bowel disease, o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4ed70aa22b18fd22e67ee1d2ab6d5c67
https://doi.org/10.1021/op1000622

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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

Autor: Orsola Vecchi, Fernando Bravo, Francesco Tinazzi, Paul Stonestreet, Giulio Camurri, Zadeo Cimarosti

Publikováno v: Organic Process Research & Development. 14:993-998

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 manufacturing process was developed and optimised by following a quality by design approach wher

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https://doi.org/10.1021/op900242x

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Synthesis of the NK1 Receptor Antagonist GW597599. Part 3: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine Urea, A Happy End

Autor: Corinne Leroi, Zadeo Cimarosti, Stefano Provera, Michael David Goodyear, Giuseppe Guercio, Marie Hourdin, Francesco Tinazzi, Ilaria Bientinesi, Alcide Perboni, Sergio Bacchi, Stefano Curti

Publikováno v: Organic Process Research & Development. 13:1100-1110

GW597599 1 is a novel NK-1 antagonist currently under investigation for the treatment of central nervous system disorders and emesis. The initial chemical development synthetic route, derived from the one used by medicinal chemistry, involved several

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::158b1f3c2b768396431325a7047235d2
https://doi.org/10.1021/op9002032

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