Howard, Philip Wilson,Masterson, Luke,Tiberghien, Arnaud,Jeffrey, Scott,Burke, Patrick,Senter, Peter
申请号：
ES14173641
公开号：
ES2623057T3
申请日:
2011.04.15
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A compound with the formula I: ** Formula ** in which: R2 is of the formula II: ** Formula ** in which A is a C5-7 aryl group, X is selected from the group consisting of: OH, SH, CO2H, COH, N>； = C>； = O, NHNH2, CONHNH2, ** Formula ** and NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl and: (i) Q1 is a single link and Q2 is selected from a single link and -Z- (CH2) n-, where Z is selected from a single link, O, S and NH and is 1 to 3； or (ii) Q1 is -CH>； = CH- and Q2 is a single link； R12 is selected from: (iia) saturated aliphatic C1-5 alkyl； (iib) saturated C3-6 cycloalkyl； (iic) ** Formula ** in which each of R21, R22 and R23 is independently selected from H, saturated C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl and cyclopropyl, where the total number of atoms of carbon in the R12 group is not greater than 5； (iid) ** Formula ** wherein one of R25a and R25b is H and the other is selected from: phenyl, phenyl which is optionally substituted with a group selected from halo, methyl, methoxy, pyridyl and thiophenyl； and (iie) ** Formula ** wherein R24 is selected from H, saturated C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl； cyclopropyl； phenyl, phenyl which is optionally substituted with a group selected from halo, methyl, methoxy, pyridyl and thiophenyl； R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR ', nitro, Me3Sn and halo； R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR ', nitro, Me3Sn and halo； where R and R 'are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups； either: (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl； (b) R10 and R11 form a double nitrogen-carbon bond between the nitrogen and carbon atoms to which they are attached； or (c) R10 is H and R11 is SOzM, where z is 2 or 3 and M is a pharmaceutically acceptable monovalent cation； R '' is a C3-12 alkylene group, whose chain may be interrupted by one or more heteroatoms and / or a
