Pharmaceutically active isoindoline derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 487/04 (2006.01) A61K 31/4035 (2006.01) A61K 31/4178 (2006.01) A61K 31/4188 (2006.01) A61K 31/4196 (2006.01) A61K 31/4245 (2006.01) A61K 31/437 (2006.01) A61K 31/4985 (2006.01) A61P 11/06 (2006.01) C07D 209/46 (2006.01) C07D 209/48 (2006.01) C07D 209/49 (2006.01) C07D 403/04 (2006.01) C07D 413/04 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2392081

Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an .alpha.-(3, 4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of dis-ease states mediated by, TNF.alpha. and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsul-fonylethyl]-4,5-diaminoisoindoline- 1,3-dione.

L'invention concerne l'isoindoline-1-one et l'isoindoline-1, 3-dione substituées dans la position 2 par un groupe alkyle alpha -(3,4-disubstitué phényle) et dans la position 4 et/ou 5 par un groupe renfermant un azote. Ces composés sont des inhibiteurs du TNF alpha et de la phosphodiestérase, et sont donc utiles dans le traitement des maladies y étant associées. Une forme d'exécution type est représentée par 2-[3-éthoxy-4-méthoxyphényl)-2-méthylsulfonyléthyl]-4, 5-diaminoisoindoline-1, 3-dione.

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