C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
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.
Chen Roger Shen-Chu
Man Hon-Wah
Muller George W.
Stirling David I.
Celgene Corporation
Smart & Biggar
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