Water-soluble cc-1065 analogs and their conjugates

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 209/60 (2006.01) A61K 31/404 (2006.01) A61K 31/454 (2006.01) A61K 31/5377 (2006.01) A61P 35/00 (2006.01) C07D 401/14 (2006.01) C07H 17/02 (2006.01)

Patent

CA 2641899

This invention relates to novel analogs of the DNA-binding alkylating agent CC- 1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their 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.

L'invention concerne de nouveaux analogues du CC-1065, agent alkylant de liaison à l'ADN, et leur conjugués. En outre, l'invention concerne des intermédiaires pour la préparation desdits agents et de leurs conjugués. Lesdits conjugués sont conçus pour libérer leur (multiple) charge utile après une ou plusieurs étapes d'activation et/ou à un taux et dans un laps de temps contrôlés par le conjugué de manière à administrer sélectivement et/ou à libérer de manière contrôlée un ou plusieurs desdits agents alkylants de l'ADN. Lesdits agents, conjugués et intermédiaires peuvent être utilisés pour traiter une affection caractérisée par une prolifération (cellulaire) indésirée. Par exemple, les agents et les conjugués de l'invention peuvent être utilisés pour traiter une tumeur.

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