Syntarga Bv

Byondis B.v.

Wiro Michael Petrus Bernardus Menge

Rudy Gerardus Elisabeth Coumans

Patrick Henry Beusker

Franciscus Marinus Hendrikus De Groot

Henri Johannes Spijker

Johannes Albertus Frederikus Joosten

Ronald Christiaan Elgersma

Franciscus Marinus Hendrikus Groot De

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.

Conjugates of CC-1065 analogs and bifunctional linkers

The present invention relates to a process for the synthesis of mono-protected &#x3b1;,&#x3c9;-diamino alkanes, the use of said process in a process for the synthesis of a linker drug comprising an &#x3b1;,&#x3c9;-diamino alkane moiety and the use of the process of the present invention in a process for preparing an antibody-drug conjugate comprising an &#x3b1;,&#x3c9;-diamino alkane moiety.

Process for the preparation of mono-protected &#x3b1;,&#x3c9;-diamino alkanes

CC-1065 analogs and their conjugates

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Nijmegen, Netherlands

Wiro Michael Petrus Bernardus Menge