Targeted bisplatinum polyamines as pro-drugs: selective...

C - Chemistry – Metallurgy – 07 – F

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C07F 15/00 (2006.01)

Patent

CA 2457118

Pro-drug forms of linear polyamine-bridged platinum compounds and methods for their production and use are provided. The polyamine-bridge portion of the compounds is based on spermine or spermidine, and the central amines of the polyamine-bridge are chemically bonded to labile blocking groups. The presence of the blocking groups serves to minimize the toxicity of the Pt compounds upon administration. Selective removal of the blocking groups and release of the active, unblocked species occurs upon exposure to suitable environmental conditions.

L'invention concerne des formes de promédicaments de composés du platine ponté de polyamine linéaire et des méthodes de leur production. La partie de polyamide pontée desdits composés est à base de spermine et de spermidine, et les aminés centraux de la polyamine pontée sont liés chimiquement à des groupes de blocage labiles. La présence desdits groupes de blocage sert à minimiser la toxicité des composés de Pt jusqu'à l'administration. Le piégeage sélectif desdits groupes de blocage et l'élimination d'espèces actives non-bloquées s'effectue lors d'une exposition à des conditions environnementales favorables.

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