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Targeted pyrrolobenzodiazapine conjugates
专利权人:
SEATTLE GENETICS INC.;SPIROGEN SARL
发明人:
JEFFREY SCOTT,HOWARD PHILIP WILSON,BURKE PATRICK,SENTER PETER
申请号:
NZ60293211
公开号:
NZ602932A
申请日:
2011.04.15
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed herein is a conjugate of formula I, L – (LU-D)p, wherein L is a cell binding agent that specifically binds to a target molecule on the surface of a target cell, LU is a Linker unit, p is 1 to 20; and D is a Drug unit comprising a PBD dimer of formula II, wherein the variable are defined herein. Additionally disclosed is the use of the conjugate in the treatment of a proliferative or autoimmune disease. Specific embodiments of the conjugate include (E)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N’-(4-((S)-7-methoxy-8-((5-(((S)-7-methoxy-2-(4-methoxyphenyl)-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl)oxy)pentyl)oxy)-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepin-2-yl)benzylidene)hexanehydrazide.
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