Platinum complex, its preparation and therapeutic application

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 15/00 (2006.01) A61K 31/282 (2006.01)

Patent

CA 2331464

Disclosed is a platinum complex of the general formula (I) wherein X represents a halogen atom and A represents a group -NH2-R wherein R is a tricyclic hydrocarbon moiety containing 10 to 14 carbon atoms which may be optionally substituted on the tricyclic ring by one or two alkyl group(s) containing 1 to 4 carbon atoms, and, furthermore, an inclusion complex of the above platinum complex with beta- or gamma cyclodextrin which may be optionally substituted by a hydroxyalkyl group of 1 to 6 carbon atoms. There are also disclosed a method for the preparation of the complex of the fomula (I) based on bringing into reaction a solution of an alkaline metal salt of ammin-trihalogenplatinate(II) in a polar organic solvent or in water with a primary amine of formula R-NH2, wherein R is a tricyclic hydrogen moiety containing to 14 carbon atoms, which may be optionally substituted on the tricyclic ring by one or two alkyl group(s) each containing 1 to 4 carbon atoms, at the temperature in the range of 0 to 100°C, as well as a method for manufacture of the above inclusion complex. The both disclosed complexes may be used as such or as a part of a pharmaceutical composition in a therapy of oncologic diseases.

L'invention concerne un complexe de platine représenté par la formule (I) dans laquelle X représente un atome d'halogène et A représente une amine primaire tricyclique contenant 10 à 14 atomes de carbone et pouvant être éventuellement substituée sur le noyau tricylique par un ou deux groupes alkyle contenant 1 à 4 atomes de carbone et, de plus, complexe d'inclusion dudit complexe de platine avec bêta- ou gamma-cyclodextrine pouvant être éventuellement substituée par un groupe hydroxyalkyle de 1 à 6 atomes de carbone. Elle concerne également un procédé servant à préparer ce complexe représenté par la formule (I) et consistant à provoquer la réaction d'une solution d'un sel de métal alcalin d'ammine-trihalogénoplatinate (II) dans un solvant organique polaire ou dans de l'eau avec l'amine tricyclique correspondante à une température située entre 0 et 100 DEG C, ainsi qu'un procédé servant à préparer ledit complexe d'inclusion. On peut mettre en application ces deux complexes seuls ou en tant que partie d'une composition pharmaceutique dans une thérapie de maladies cancéreuses.

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