HOWARD, PHILIP WILSON,GREGSON, STEPHEN JOHN,MASTERSON, LUKE
申请号：
CA2735477
公开号：
CA2735477C
申请日:
2009.10.16
申请国别(地区):
CA
年份:
2016
代理人:
摘要：
Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula(I), that are unsymmetricaldue at least to the values that the variables R12 and R2 represent. Formula(I), wherein: R2 is of formula (II), where A is a C5-7 arylgroup, X is selected from the group comprising: OH, SH, CO2H, COH, N=C=O, NHRN, wherein R N is selected from the groupcomprising H and C1-4 alkyl, and (OC2H4)m OCH3, where m is 1 to 3, and either:(i) Q1 is a single bond, and Q2 is selected from asingle bond and -Z-(CH2)n-, where Z is selected from a single bond, O, S andNH and n is from 1 to 3； or (ii) Q1 is -CH=CH-, andQ2 is a single bond； R12 is a C5-10 aryl group, optionally substituted by oneor more substituents selected from the group comprising:halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3alkylene. The other variables are as defined in theclaims. The compounds are useful for the treatment of proliferative diseases.
