Platinum (iv) complex and pharmaceutical composition...

C - Chemistry – Metallurgy – 07 – F

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C07F 15/00 (2006.01) A61K 31/28 (2006.01)

Patent

CA 2225591

A diamine-platinum (IV) complex represented by the following formula (1): Image wherein R1 and R2 together represent R5O-CH(CH2NH2)2 (R5 represents hydrogen, acetyl, trifluoroacetyl, benzoyl, cycloalkylcarbonyl or methanesulfonyl) or a C5-8 1,2-cycloalkanediamine; R3 and R4 each represents hydrogen or R6CO- (R6 represents alkyl, halogenoalkyl, cycloalkyl, aryl or aralkyl); and two X's together represent a malonic acid residue or glycolic acid residue which may have a substituent capable of coordinating to the platinum in formula (1) by an O,O-coordination or an N-acylamino acid residue coordinating to the platinum in formula (1) by an O,N-coordination; and a pharmaceutical composition comprising as an active ingredient the above-described diamine-platinum (IV) complex.

Un complexe diamine-platine (IV) représenté par la formule suivante (1) : Image où R1 et R2 sont, ensemble, R5O-CH(CH2NH2)2 (R5 représente un atome d'hydrogène ou un groupe acétyle, trifluoroacétyle, benzoyle, cycloalkylcarbonyle ou méthanesulfonyle) ou une 1,2-cycloalcanediamine en C5-C8; R3 et R4 représentent l'un et l'autre un atome d'hydrogène ou R6CO- (R6 représente un groupe alkyle, haloalkyle, cycloalkyle, aryle ou aralkyle); et deux X, ensemble, représentent un résidu d'acide malonique ou un résidu d'acide glycolique qui peut porter un substituant capable de coordination avec le platine de la formule (1) par une coordination O,O, ou un résidu d'acide N-acylamino capable de coordination au platine de formule (1) par une coordination O,N; et une composition pharmaceutique comprenant comme actif ingrédient le complexe diamine-platine (IV) décrit ci-dessus.

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