N,o-amidomalonate platinum complexes

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 15/00 (2006.01) A61K 31/28 (2006.01) A61K 47/48 (2006.01) A61P 35/04 (2006.01)

Patent

CA 2396702

The present invention relates purified platinum complexes in which platinum is coordinated to form a single N,O- or O,O-chelate of an amidomalonate. The chelates, and pharmaceutically acceptable formulations thereof, are useful for the treatment of cancer. The platinum chelates may additionally be linked to one or more functional groups which increases water solubility and/or assists in tumor targeting of the chelate. Examples of tumor targeting moieties include polymers, in which one or more platinum chelates are attached to the polymer backbone via linkers capable of being cleaved in the body, and molecules with a high affinity for receptors which are concentrated or upregulated in tumor tissue and/or the tumor vasculature.

L'invention concerne des complexes de platine purifiés dans lesquels le platine forme un chélate unique N,O- ou O,O- avec un amidomalonate. Les chélates, ainsi que leurs formulations acceptables sur le plan pharmaceutique, sont utiles pour le traitement de cancer. Ces chélates de platine peuvent, en outre, être liés à un ou à plusieurs groupes fonctionnels qui leur confèrent une meilleure solubilité dans l'eau et/ou qui permettent un meilleur ciblage de tumeur par le chélate. Des exemples de groupes permettant un ciblage de tumeur comprennent des polymères, au squelette desquels sont attachés un ou plusieurs chélates de platine via des lieurs pouvant subir une coupure dans le corps, ainsi que des molécules à degré d'affinité élevé pour des récepteurs qui sont concentrés ou régulés positivement dans le tissu et/ou dans le système vasculaire d'une tumeur.

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