Anti-cancer drug aldehyde conjugate drugs with enhanced...

C - Chemistry – Metallurgy – 07 – D

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C07D 413/14 (2006.01) A61K 31/395 (2006.01) C07D 413/02 (2006.01) C07H 15/244 (2006.01)

Patent

CA 2286181

This invention provides anti-cancer drug aldehyde conjugates. More particularly provided are anthracycline formaldehyde conjugates. The dimeric formaldehyde conjugate of epidoxorubicin is more hydrolytically stable than the dimeric formaldehyde conjugate of doxorubicin and the dimeric formaldehyde conjugate of daunorubicin. Pro-drugs which are more stable to hydrolysis are also provided.

L'invention concerne des médicaments anticancéreux à base de conjugués d'aldéhyde. L'invention concerne plus particulièrement des conjugués d'anthracycline-formaldéhyde. Le conjugué dimère de formaldéhyde d'épidoxorubicine est plus stable à l'hydrolyse que le conjugué dimère de formaldéhyde de doxorubicine et que le conjugué dimère de formaldéhyde de daunorubicine. Font aussi l'objet de cette invention des promédicaments qui sont plus stables à l'hydrolyse.

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