申请人:——
公开号:US20030069428A1
公开(公告)日:2003-04-10
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&agr;. A typical embodiment is 2-(2,6-dioxo-3-hydroxy-5-fluoro-piperidin-5-yl)-4-aminoisoindolin-1-one.
2-取代2,6-二氧杂环己-3-羟基哌啶-5-基基的异吲哚啉-1-酮和异吲哚啉-1,3-二酮,可以在5-位进一步取代烷基或卤素,在4-位取代烷基或含氮基团,是TNF&agr;介导的疾病状态的抑制剂,因此在治疗这些疾病方面非常有用。一个典型的实施例是2-(2,6-二氧杂环己-3-羟基-5-氟哌啶-5-基)-4-氨基异吲哚啉-1-酮。