Azetidine and cyclobutane derivatives as jak inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/437 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2718271

The method includes the steps of performing in-vitro liver, intestinal and/or expressed enzyme assays with selected ethnobotanical substances, for both humans and a variety of animal species, to produce an array of resulting chemical entities, such as metabolites, for the human and the animals. Comparisons are then made between the chemical entities from the human in-vitro studies and the animal in-vitro studies to determine the closest match. The animal with the closest match is then used for an in-vivo study. If a match is present between the animal in-vivo results and the human in-vitro results, the matched chemical entity is isolated or synthesized and then further tested to determine the suitability of the matched chemical entity as a treatment drug.

L'invention concerne un procédé qui comprend les étapes consistant à effectuer des analyses, in vitro, d'enzymes de foie, intestinales et/ou exprimées avec des substances ethnobotaniques sélectionnées, à la fois pour des êtres humains et diverses espèces animales, afin de produire un réseau d'entités chimiques résultantes, telles que des métabolites, pour l'homme et les animaux. Des comparaisons sont ensuite faites entre les entités chimiques provenant des études in vitro humaines et des études in vitro animales pour déterminer la correspondance la plus proche. L'animal ayant la correspondance la plus proche est ensuite utilisé pour une étude in vivo. Si une correspondance existe entre les résultats animaux in vivo et les résultats humains in vitro, l'entité chimique appariée est isolée ou synthétisée pour être ensuite davantage analysée afin de déterminer lapplicabilité de l'entité chimique appariée en tant que médicament de traitement.

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