C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/70 (2006.01) C07C 45/00 (2006.01) C07C 45/41 (2006.01) C07C 45/51 (2006.01) C07C 45/75 (2006.01) C07C 47/232 (2006.01) C07C 47/277 (2006.01) C07C 49/245 (2006.01) C07C 69/76 (2006.01) C07C 259/06 (2006.01) C07C 261/00 (2006.01) C07C 327/22 (2006.01) C07D 209/02 (2006.01) C07D 307/02 (2006.01) C07D 333/22 (2006.01)
Patent
CA 2486402
Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha- chalcogenmethylcarbonyl group, such as an alpha-ketothio 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, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington~s disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.
L'histone désacétylase est une métallo-enzyme comportant du zinc au niveau de son site actif. Les composés possédant un groupe caractéristique de liaison au zinc, par exemple un groupe alpha-chalcogenméthylcarbonyle, tel qu'un groupe alpha-cétothio, peuvent inhiber l'histone désacetylase. L'inhibition de l'histone désacétylase peut réprimer l'expression de gènes, notamment l'expression de gènes associés à la suppression des tumeurs. En conséquence, l'inhibition de l'histone désacétylase peut constituer une voie détournée de traitement du cancer, des troubles hématologiques, par exemple des hémoglobinopathies, des affections autosomiques dominantes, telles que la maladie d'Aran-Duchenne et la maladie de Huntington, des troubles métaboliques d'origine génétique, tels que la mucoviscidose et la leucodystrophie avec insuffisance surrénale, ou un moyen de stimulation <i>ex vivo</i> des cellules hématopoïétiques.
Kaufman Robert J.
Lan-Hargest Hsuan-Yin
Errant Gene Therapeutics Llc
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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