Histone deacetylase inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 235/04 (2006.01) A61K 31/16 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) C07C 57/42 (2006.01) C07C 57/60 (2006.01) C07C 69/52 (2006.01) C07C 259/06 (2006.01) C07D 307/54 (2006.01)

Patent

CA 2442366

Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

L'invention porte sur une histone déacétylase qui est une métalloenzyme avec zinc au niveau du site actif. Des composés ayant une fraction se liant au zinc telle qu'un groupe acide hydroxamique ou un groupe acide carboxylique peuvent inhiber l'histone déacétylase. L'inhibition de l'histone déacétylase peut réprimer l'expression génique, y compris l'expression des gènes relatifs à la suppression tumorale. Selon cette invention, l'inhibition de l'histone déacétylase peut être une alternative dans le traitement du cancer, des troubles hématologiques tels que les hémoglobinopathies et des troubles métaboliques liés aux gènes tels que la mucoviscidose et l'adrénoleucodystrophie.

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