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Rozprawy doktorskie na temat "Chimie pharmaceutique – Innovation"
Berabez, Rayan. "Conception et validation préclinique de nouveaux inhibiteurs de LIMK pour le traitement de la Neurofibromatose de type 1". Electronic Thesis or Diss., Orléans, 2023. http://www.theses.fr/2023ORLE1070.
Pełny tekst źródłaNeurofibromatosis type 1 (NF1) is a genetic disease characterized by the development of cutaneous neurofibromas (cNF) (benign tumors) located at nerve endings. LIM kinases (LIMKs), enzymes responsible for cytoskeleton dynamics, have emerged in recent years as valid therapeutic targets for this disease. These enzymes are overactivated in several pathologies including NF1, glioblastoma or osteosarcoma. A medicinal chemistry project was therefore initiated with the aim of designing new selective inhibitors of LIMKs. Initially, structure-activity relationship (SAR) studies were conducted on the 3 main pharmacomodulation sites of the pyrrolopyrimidine-type compounds previously developed by our team. The development of various synthetic strategies was undertaken, allowing efficient access to a large number of final products (84). Optimization of the aniline portion of the compounds led to the synthesis of 49 LIMKs inhibitors, with inhibition constants lower than 5 nM for several derivatives. Subsequently, an optimized 15 steps synthetic route was developed to replace the previously unchanged central ring 3,6-dihydropyridine with a derivative of 1-aminocyclohex-3-ene-1-carboxylic acid. Finally, a new series of inhibitors was developed by replacing the heterocyclic pyrrolo[2,3-d]pyrimidine base by 7-azaindole derivatives. Improved LIMK vs. ROCK selectivity was observed among the 23 obtained products. Following extensive in vitro evaluation of our best inhibitors on several cell lines, two compounds were selected for in vivo trials on an original mouse model of NF1. In parallel, new modes of LIMKs inhibition were developed with the synthesis of an irreversible inhibitor targeting LIMK1, as well as 4 PROTACs that induced LIMKs degradation through the ubiquitin-proteasome system in several cell lines
Saulia, Emmrick André. "Cyanobactéries diazotrophes du Pacifique Sud : variabilité saisonnière, caractérisation morpho-génétique/chimique et potentiel de valorisation". Electronic Thesis or Diss., Nouvelle Calédonie, 2019. http://www.theses.fr/2019NCAL0003.
Pełny tekst źródłaThe southwest Pacific Ocean and the waters of New Caledonia are characterized by high abundances of cyanobacteria. Among these cyanobacteria, some have the ability to fix atmospheric nitrogen (N2), and are called diazotrophic cyanobacteria. These organisms are known to contain high added value metabolites and nutrients in varying proportions, which give them potential for economic development that may be of interest to New Caledonia. Several of these cyanobacteria have been isolated in culture from the coastal and offshore waters of the Southwest Pacific, but the precise characterization of their diversity and their potential for recovery are still unknown. With a view to a better knowledge of diversity and a possible economic valuation, the objectives of this doctoral work were (i) to study the seasonal variability of the diversity / activity of diazotrophic cyanobacteria in the lagoon of Noumea, (i) to carry out a morphogenetic and proteomic characterization of indigenous strains recently isolated in culture and (iii) to evaluate their potential for valorization
Książki na temat "Chimie pharmaceutique – Innovation"
1922-, Harms A. F., red. Innovative approaches in drug research: Proceedings of the third Noordwijkerhout Symposium on Medicinal Chemistry, held in the Netherlands, September 3-6, 1985. Amsterdam: Elsevier, 1986.
Znajdź pełny tekst źródła1950-, Malerba Franco, red. Sectoral systems of innovation: Concepts, issues and analyses of six major sectors in Europe. Cambridge, UK: Cambridge University Press, 2004.
Znajdź pełny tekst źródłaKansal, Ruchin, i Jeff Huth. Redefining Innovation: Embracing the 80-80 Rule to Ignite Growth in the Biopharmaceutical Industry. Productivity Press, 2018.
Znajdź pełny tekst źródłaKansal, Ruchin, i Jeff Huth. Redefining Innovation: Embracing the 80-80 Rule to Ignite Growth in the Biopharmaceutical Industry. Productivity Press, 2018.
Znajdź pełny tekst źródłaRedefining Innovation: Embracing the 80-80 Rule to Ignite Growth in the Biopharmaceutical Industry. Taylor & Francis Group, 2018.
Znajdź pełny tekst źródłaMahapatra, Debarshi Kar, i Sanjay Kumar Bharti. Handbook of Research on Medicinal Chemistry: Innovations and Methodologies. Apple Academic Press, Incorporated, 2017.
Znajdź pełny tekst źródłaMahapatra, Debarshi Kar, i Sanjay Kumar Bharti. Handbook of Research on Medicinal Chemistry: Innovations and Methodologies. Apple Academic Press, Incorporated, 2017.
Znajdź pełny tekst źródłaHandbook of Research on Medicinal Chemistry: Innovations and Methodologies. Taylor & Francis Group, 2017.
Znajdź pełny tekst źródłaHarms. Innovative Drug Research: (Materials Science Monographs). Elsevier Publishing Company, 1986.
Znajdź pełny tekst źródła