LERCHEN, HANS-GEORG,REBSTOCK, ANNE-SOPHIE,MARX, LEO,JOHANNES, SARAH ANNA LIESA,STELTE-LUDWIG, BEATRIX,DIETZ, LISA,JOERISSEN, HANNAH,MAHLERT, CHRISTOPH,GREVEN, SIMONE,SOMMER, ANETTE
申请号：
CA3047491
公开号：
CA3047491A1
申请日:
2017.12.18
申请国别(地区):
CA
年份:
2018
代理人:
摘要：
The invention relates to prodrugs or conjugates of a new type, of general formula (Ia), in which formula La, n, R, and D have the meanings indicated in the description, said prodrugs or conjugates having a structural pattern reduced to an asparagine derivative as a cleaving site for tumor-associated proteases such as legumain, wherein cytotoxic active agents such as kinesin spindle protein inhibitors are released by legumain cleavage. The invention further relates to the use of said prodrugs or conjugates to treat and/or prevent diseases and to the use of said prodrugs or conjugates to produce drugs for treating and/or preventing diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer diseases. By means of the reduction of the legumain-cleavable substrate peptide sequence to an asparagine derivative as a structural pattern, an increase in stability in the lysosomes of healthy organs is achieved together with high anti-tumor activity.
