Novel cc-1065 analogs and their conjugates

Details Novel cc-1065 analogs and their conjugates Novel cc-1065 analogs and their conjugates

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01)

Patent

CA 2742568

This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

La présente invention concerne de nouveaux analogues de lagent dalkylation dADN CC-1065 et leurs conjugués. De plus, cette invention concerne des intermédiaires pour la préparation desdits agents et conjugués. Les conjugués sont conçus pour libérer leur charge utile (multiple) après une ou plusieurs étapes dactivation et/ou à un taux et en une durée contrôlés par le conjugué afin de délivrer sélectivement et/ou libérer de manière contrôlable un ou plusieurs desdits agents dalkylation dADN. Les agents, conjugués, et intermédiaires peuvent être utilisés pour traiter une maladie qui est caractérisée par une prolifération (cellulaire) indésirable. À titre dexemple, les agents et les conjugués de cette invention peuvent être utilisés pour traiter une tumeur.

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