Thiadiazolidinones as gsk-3 inhibitors

C - Chemistry – Metallurgy – 07 – D

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C07D 285/08 (2006.01) A61K 31/433 (2006.01) A61P 3/10 (2006.01) A61P 25/28 (2006.01) C07D 417/10 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2559740

Provided are thiadiazolidine compounds of Formula (I) wherein R1 is an organic group having at least 8 atoms selected from C or O, which is not linked directly to the N through a -C(O)- and comprising at least an aromatic ring, and their pharmaceutical compositions. These compounds are selective GSK-3 inhibitors and have improved bioavailability. They are useful for the treatment of GSK-3 mediated diseases, among others Alzheimer's disease, type II diabetes, depression and brain injury.

La présente invention a trait à des composés de formule (I), dans laquelle : R¿1? est un groupe organique ayant au moins 8 atomes choisis parmi C et O, qui n'est pas en liaison directe avec l'atome d'azote via un -C(O)- et comportant au moins un noyau aromatique, et leurs compositions pharmaceutiques. Ces composés sont des inhibiteurs sélectifs de la GSK-3 et présentent une biodisponibilité améliorée. Ils sont utiles pour le traitement de maladies liées à la GSK-3, comprenant entre autres la maladie d'Alzheimer, le diabète de type II, la dépression et la lésion cérébrale.

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