Patrick Henry BEUSKER,Rudy Gerardus Elisabeth COUMANS,Ronald Christiaan ELGERSMA,Wiro Michael Petrus Bernardus MENGE,Johannes Albertus Frederikus JOOSTEN,Henri Johannes SPIJKER,Franciscus Marinus Hend
申请号:
US15461560
公开号:
US20170274090A1
申请日:
2017.03.17
申请国别(地区):
US
年份:
2017
代理人:
摘要:
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.