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PYRROLOBENZODIAZEPINES
专利权人:
SPIROGEN SÀRL
发明人:
PHILIP WILSON HOWARD
申请号:
BR112014008981
公开号:
BR112014008981A2
申请日:
2012.10.12
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
summary "pyrrolobenzodiazepines" a compound of formula i: wherein: r2 is of formula ii: where a is an aryl group c5-7, x is selected from the group comprising: nhnh2, conhnh2,,, and: 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, if nh and n is from 1 to 3; or q1 is -ch = ch-, and q2 is a single bond; R 12 is a C 5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C 1-7 alkyl, C 3-7 heterocyclyl and C 1-3 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 c 1-12 alkyl, c 3-20 heterocyclyl and c 5-20 aryl groups; r7 is selected from h, r, oh, or, sh, sr, nh2, nhr, nhrr ', nitro, me3sn and halo; or: r10 is h, and r11 is oh, now where r is C1-4 alkyl; R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are attached; or r10 is h and r11 is alone, where z is 2 or 3 and m is a pharmaceutically acceptable monovalent cation; R 'is a C 3-12 alkylene group whose 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, where if r11 and r11' are alone, m can represent a divalent cation pharmaceutically acceptable.resumo “pirrolobenzodiazepinas” um composto com a fórmula i: em que: r2 é da fórmula ii: onde a é um grupo arila c5-7, x é selecionado a partir do grupo compreendendo: nhnh2, conhnh2, , , e: q1 é uma ligação única, e q2 é selecionado a partir de uma ligação única e -z-(ch2)n-, onde z é selecionado a partir de uma ligação única, o, s e nh e n é a partir de 1 a 3; ou q1 é -ch=ch-, e q2 é uma ligação única; r12 é um grupo arila c5-10, opcionalmente substituído po
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