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pyrrolobenzodiazepines and conjugates thereof
专利权人:
SPIROGEN SÀRL
发明人:
PHILIP WILSON HOWARD
申请号:
BR112015014669
公开号:
BR112015014669A2
申请日:
2013.12.20
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
summary "pyrrolobenzodiazepines and conjugates thereof" means a compound of formula I: and salts and solvates thereof, wherein: when there is a double bond present between c2 and c3, r2 is selected from the group consisting of: (ia) group C 5-10 aryl, 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 bis-oxyC 1-3 alkylene; (ib) saturated aliphatic C1-5 alkyl; (ic) saturated C 3-6 cycloalkyl; (id), wherein each of r11, r12 and r13 is independently selected from h, saturated C1-3 alkyl, c2-3 alkenyl, c2-3 alkynyl and cyclopropyl, where the total number of carbon atoms in group r2 is not larger than 5; (ie), wherein one of r15a and r15b is h and the other is selected from: phenyl, phenyl which is optionally substituted by a group selected from halo, methyl, methoxy, pyridyl; and thiophenyl; and (if), where r14 is selected from: h; saturated C1-3 alkyl; C 2-3 alkenyl; c2-3 alkynyl; cyclopropyl; phenyl, phenyl which is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; when there is a single bond present between c2 and c3, r2 e, where r16a and r16b are independently selected from h, f, saturated C1-4 alkyl, c2-3 alkenyl, these alkyl and alkenyl groups which are optionally substituted by a selected group from C 1-4 alkyl starch and C 1-4 alkyl ester; or, when one of r16a and r16b is h, the other is selected from nitrile and a C1-4 alkyl ester; when there is a double bond present between c2 'and c3', r12 is selected from the group consisting of: (ia) aryl group c5-10, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano carboxy, ester, C 1-7 alkyl, C 3-7 heterocyclyl and bis-oxyC 1-3 alkylene; (ib) saturated aliphatic C1-5 alkyl; (ic) saturated C 3-6 cycloalkyl; (id), wherein each of r21, r22 and r23 is independently selected from h, saturated C1-3 alkyl, c2-3 alkenyl, c2-3 alky
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