Výsledky vyhledávání - "Zadeo Cimarosti"

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

Autor: Sara Rossi, Davide Tramarin, William Maton, Brigida Allieri, Francesca Campi, Pieter Westerduin, Gilles Laval, Jason W. B. Cooke, Zadeo Cimarosti, Paolo Stabile, Nicola Giubellina

Publikováno v: Organic Process Research & Development. 16:1598-1606

The studies carried out to develop a robust crystallization method for the substituted piperazinyl-quinoline (1) a compound potentially active in the treatment of depression, are described in this contribution. These studies include the control of a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7047d1fcd161eb000d8b634507416017
https://doi.org/10.1021/op300126e

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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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Application of Quality by Design Principles for the Definition of a Robust Crystallization Process for Casopitant Mesylate

Autor: Zadeo Cimarosti, Mohammed Yahyah, John J. Peterson, Carlo Castagnoli

Publikováno v: Organic Process Research & Development. 14:1407-1419

GlaxoSmithKline (GSK) has identified casopitant as a potent NK1 antagonist. It was selected for its potential activities on a number of therapeutic targets such as inflammatory bowel disease, overactive bladder, CNS disorders and others. The mesylate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::875cde9fd6b0eb77276736b13d4b3322
https://doi.org/10.1021/op100209c

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Development of Drug Substances as Mixture of Polymorphs: Studies to Control Form 3 in Casopitant Mesylate

Autor: Caroline J. Day, Pieter Westerduin, Carlo Castagnoli, Zadeo Cimarosti, Brendan M. Johnson, Marco Rossetti, Mirka Scarati

Publikováno v: Organic Process Research & Development. 14:1337-1346

Polymorphism is characterized as the ability of a drug substance to exist as two or more crystalline phases that have different arrangements and/or conformations of the molecules in the crystal lat...

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https://doi.org/10.1021/op100150b

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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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Development of an Efficient Large-Scale Synthesis for a 4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide Derivative for Depression and Anxiety

Autor: Pieter Westerduin, Alcide Perboni, Zadeo Cimarosti, Gilles Laval, Paolo Stabile, Jason W. B. Cooke, Nicola Giubellina

Publikováno v: Organic Process Research & Development. 14:859-867

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 convergent and efficient four-stage app...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a849e4d9e4ea3d5c744984d16434a0ec
https://doi.org/10.1021/op100103v

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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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