Polymeric thiol-linked prodrugs employing benzyl elimination...

C - Chemistry – Metallurgy – 08 – G

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C08G 65/329 (2006.01) A61K 47/30 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2465090

Thiol-linked polymeric prodrugs, methods of making and using the same are disclosed. The use of a sulfhydryl bond in combination with a benzyl elimination system results in the formation of prodrugs which can take advantage of plasma enzymes in vivo for regeneration of the parent molecule. A preferred prodrug in accordance with the invention is formula (I) where S-MP is 6-mercaptopurine.

L'invention concerne des promédicaments polymères à liaison thiol et des procédés permettant de les fabriquer et de les utiliser. L'utilisation d'une liaison sulphydryle en combinaison avec un système d'élimination de benzyle donne lieu à la formation de promédicaments pouvant tirer parti d'enzymes plasmatiques in vivo pour régénérer la molécule parente. Un promédicament préféré selon l'invention est de formule (I), dans laquelle S-MP est 6-mercaptopurine.

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