Delivery and activation through liposome incorporation of...

A - Human Necessities – 61 – K

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167/119, 167/163

A61K 9/127 (2006.01) A61K 31/282 (2006.01)

Patent

CA 2273497

Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having formula (I) where R1 is diaminocycloalkyl, and R2 and R3 each have formula (a) where R4, R5, and R6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having formula (II): R1-Pt-X2 where X is halogen.

La présente invention concerne des compositions antitumorales, ainsi que des procédés de préparation et d'utilisation de ces compositions permettant de combattre la croissance tumorale chez les mammifères. L'invention permet de tirer parti de la conversion intraliposomique d'un complexe de platine. Ce complexe est représenté par la formule générale (I) dans laquelle R¿1? est diaminocycloalkyl, R¿2? et R¿3? étant représentés chacun par la formule spécifique (a). Dans cette formule spécifique (a), R¿4?, R¿5? et R¿6? sont chacun indépendamment des groupes fonctionnels C¿1?-C¿5? hydrocarbures. La conversion aboutit à la formation d'un complexe représenté par la formule générale (II) R¿1?-Pt-X¿2? dans laquelle X est halogène.

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