Pharmaceutically active isoindoline derivatives

Details Pharmaceutically active isoindoline derivatives Pharmaceutically active isoindoline derivatives

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/445 (2006.01) C07D 401/00 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2427619

Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with a 2,6-dioxo-3-hydroxypiperidin-5-yl group, which may be further substituted in the 5-position with alkyl or halogeno, and in the 4-position with alkyl or a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF.alpha.. A typical embodiment is 2-(2,6- dioxo-3-hydroxy-5-fluoro-piperidin-5-yl)-4-aminoisoindolin-1-one.

Isoindolin-1-one et isoindolin-1,3-dione substitués en position 2 par un groupe 2,6-dioxo-3-hydroxypipéridin-5-yle, qui peut être ultérieurement substitué en position 5 avec un alkyle ou un halogéno-, et en position 5 avec un alkyle ou un groupe contenant l'azote; en tant qu'inhibiteurs de TNF.alpha., ils sont utiles dans le traitement des états pathologiques à médiation par TNF.alpha.. Un mode de réalisation type est le 2-(2,6-dioxo-3-hydroxy-5-fluoro-pipéridin-5-yl)-4-amino-isoindolin-1-one.

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