公开(公告)号：EP2173739B1

公开(公告)日：2013-07-31

申请号：EP07808517.2

申请日：2007-08-01

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  SPIJKER, Henri Johannes ,  JOOSTEN, Johannes Albertus Frederikus ,  HUIJBREGTS, Tijl ,  DE GROOT, Franciscus Marinus Hendrikus

IPC分类号： C07D403/06 ,  C07D403/14 ,  A61K31/403 ,  A61P35/00

CPC分类号： C07D403/06 ,  C07D403/14

公开(公告)号：EP2173739A1

公开(公告)日：2010-04-14

申请号：EP07808517.2

申请日：2007-08-01

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  SPIJKER, Henri Johannes ,  JOOSTEN, Johannes Albertus Frederikus ,  HUIJBREGTS, Tijl ,  DE GROOT, Franciscus Marinus Hendrikus

IPC分类号： C07D403/06 ,  C07D403/14 ,  A61K31/403 ,  A61P35/00

CPC分类号： C07D403/06 ,  C07D403/14

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.