Platinum complexes with mononitrile-containing ligands

C - Chemistry – Metallurgy – 07 – F

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

Patent

CA 2612721

Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L1 and L2 )which can be hydrolyzed in vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.

Cette invention concerne des nouveaux complexes à base de platine présentant un substituant (mononitrile) lié par covalence au platine, un ou plusieurs ligands donneurs d'azote capables de former des liaisons hydrogène avec les bases dans l'ADN et ARN et des groupes partants (c'est-à-dire L1 et L2 ) qui peuvent être hydrolysés in vivo à des espèces actives qui peuvent, ensuite, former des produits d'addition coordonnés avec l'ADN ou l'ARN sur les bases Guanine ou Adénine. En outre, cette invention concerne des schémas de réactions permettant la synthèse de ces complexes de platine, ainsi que des méthodes permettant de traiter divers types de cancer par administration d'une dose pharmaceutiquement efficace de ces complexes de platine.

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