Patrick Henry BEUSKER,Henri Johannes SPIJKER,Johannes Albertus Frederikus JOOSTEN,Tijl HUIJBREGTS,Franciscus Marinus Hendrikus DE GROOT
申请号:
US14174794
公开号:
US20150216844A1
申请日:
2014.02.06
申请国别(地区):
US
年份:
2015
代理人:
摘要:
This invention relates to novel agents that are analogs of the DNA-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.