Substituted...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 401/04 (2006.01) A61K 31/445 (2006.01)

Patent

CA 2317834

A chiral compound is described, in racemic, (R)- or (S)- form, which is a 2-(2,6-dioxo-3-fluoropiperidin-3-yl)- isoindoline of the formula: (see formula I) in which Y is oxygen or H2 and each of R1, R2, R3, and R4, independently of the others, is hydrogen, halo, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or amino, or the acid addition salts of said 2-(2,6-dioxo-3- fluoropiperidin-3-yl)-isoindolines which contain a nitrogen atom capable of being protonated. 1-Oxo-2-(2,6-dioxo-3- fluoropiperidin-3-yl)-isoindolines and 1,3-dioxo-2-(2,6- dioxo-3-fluoropiperidin-3-yl)-isoindolines reduce the levels of inflammatory cytokines such as TNF.alpha. in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxo-3--fluoropiperidin-3-yl)- isoindoline.

L'invention concerne des 1-oxo-2-(2,6-dioxo-3-fluoropipéridine-3-yl)isoindolines et des 1,3-dioxo-2-(2,6-dioxo-3-fluoropipéridine-3-yl)isoindolines pour réduire les taux de cytokines inflammatoires tels que les taux de TNF - alpha chez le mammifère. Un mode de réalisation classique est le 1,3-dioxo-2-(2,6-dioxo-3-fluoropipéridine-3-yl)-isoindoline.

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