Neuroprotective iron chelators and pharmaceutical...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/70 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 38/08 (2006.01) A61K 38/09 (2006.01) A61K 38/22 (2006.01) A61K 45/06 (2006.01) A61P 39/04 (2006.01) C07D 213/69 (2006.01) C07D 215/12 (2006.01) C07K 5/09 (2006.01) C07K 7/06 (2006.01) C07K 7/23 (2006.01) C07K 14/575 (2006.01)

Patent

CA 2505476

Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.

Cette invention concerne des chélateurs du fer dotés de propriétés neuroprotectrices et d'une bonne capacité au transport qui sont utiles dans la thérapie par chélation du fer pour le traitement de pathologies, troubles ou états associés à une surcharge en fer et à un stress oxydatif tels que : maladie ou trouble neurodégénératif ou cérébrovasculaire, maladie néoplasique, hémochromatose, thalassémie, maladie cardiovasculaire, diabète, troubles inflammatoires, cardiotoxicité des anthracyclines, infection virale, infection causée par des protozoaires, infection causée par des levures, ralentissement du vieillissement et prévention et/ou traitement du vieillissement de la peau et protection de la peau contre le rayonnement solaire et/ou le rayonnement ultraviolet. La fonction de chelation du fer est assurée par une 8-hydroquinoline, un hydropyridinone et une fraction hydroxamate, la fonction neuroprotectrice du composé par un peptide neuroprotecteur, et la fonction antiapoptotique et neuroprotective combinée par un groupe propargyle.

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