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PYRROLOBENZODIAZÉPINES
专利权人:
Spirogen Sàrl
发明人:
申请号:
EP12772780.8
公开号:
EP2751110A1
申请日:
2012.10.12
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
A compound with the formula I: wherein: R2 is of formula II: where A is a C5-7 aryl group, X is selected from the group comprising: NHNH2, CONHNH2, formula III, formula IV, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH═CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, 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; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR′, nitro, Me3Sn and halo; either: (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is SOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, and/or aromatic rings; Y and Y′ are selected from O, S, or NH; R6′, R7′, R9′ are selected from the same groups as R6, R7 and R9 respectively and R10′ and R11′ are the same as R10 and R11, wherein if R11 and R11′ are SOzM, M may represent a divalent pharmaceutically acceptable cation.Composé de formule I. Dans la formule I, R2 est de formule II : où A est un groupe aryle C5-7, X est choisi dans le groupe comprenant : NHNH2, CONHNH2, formule III, formule IV, et soit : (i) Q1 est une liaison simple, et Q2 est choisi parmi une liaison simple et -Z-(CH2)n-, où Z est choisi parmi une liaison simple, O, S et NH et n vaut de
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