Drug delivery agents incorporating mitomycin

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/48 (2006.01) C07D 487/14 (2006.01) C07K 5/083 (2006.01) C07K 5/103 (2006.01)

Patent

CA 2168007

A conjugate of a carrier polymer and aziridine ring containing mitomycin (MMC) drug molecules is prepared by coupling the MMC molecules via their aziridine imino groups to spacer groups that terminate in protected amino groups, deprotecting said amino groups, recovering and purifying the spacer-MMC derivatives, and then coupling these derivatives via said deprotected terminal amino groups to the carrier polymer. Alternatively, the MMC may first be treated with an activating agent, e.g. carbodiimidazole, to form on activated MMC derivative which is then coupled directly to spacer groups linked to the carrier polymer.

On prépare un conjugué d'un polymère excipient et d'un cycle d'aziridine contenant des molécules médicamenteuses de mytomycine (MMC) en couplant les molécules MMC par l'intermédiaire de leurs groupes imino aziridine à des groupes espaceurs qui se terminent en groupes amino protégés, déprotégeant ces groupes amino, en récupérant et purifiant les dérivés des groupes espaceurs-MMC, et enfin en couplant ces dérivés par l'intermédiaire de ces groupes amino terminaux déprotégés au polymère excipient. Dans une autre variante, les molécules MMC peuvent d'abord être traitées avec un agent d'activation, par exemple le carbodiimidazole, afin de se former sur le dérivé activé de MMC qui est ensuite couplé directement aux groupes espaceurs liés au polymère excipient.

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