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    Pyrrolobenzodiazepines
    1.
    发明授权
    Pyrrolobenzodiazepines 有权

    公开(公告)号：US09399073B2

    公开(公告)日：2016-07-26

    申请号：US14351173

    申请日：2012-10-12

    申请人： MEDIMMUNE LIMITED ,  SEATTLE GENETICS, INC.

    发明人： Philip Wilson Howard ,  Arnaud Tiberghien ,  Scott Jeffrey ,  Patrick Burke

    IPC分类号： C07D487/04 ,  A61K47/48 ,  C07D519/00 ,  C07H15/22

    CPC分类号： A61K47/48338 ,  A61K47/48092 ,  A61K47/549 ,  A61K47/65 ,  C07D487/04 ,  C07D519/00 ,  C07H15/22

    摘要： A compound with the formula (I), wherein: R2 is of formula (II), where X is selected from the group comprising: OH, SH, CO2H, COH, N═C═O, NHNH2, CONHNH2, formula (A), formula (B), NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl; RC1, RC2 and RC3 are independently selected from H and unsubstituted C1-2 alkyl; and either: R12 is selected from the group consisting of: (ia) 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; (ib) C1-5 saturated aliphatic alkyl; (ic) C3-6 saturated cycloalkyl; (id) formula (C), wherein each of R21, R22 and R23 are independently selected from H, C1-3 saturated alkyl, C2-3 alkenyl, C2-3 alkynyl and cyclopropyl, where the total number of carbon atoms in the R12 group is no more than 5; (ie) formula (D), wherein one of R25a and R25b is H and the other is selected from: phenyl, which phenyl is optionally substituted by a group selected from halo, methyl, methoxy; pyridyl; and thiophenyl; and (if) formula (E), where R24 is selected from: H; C1-3 saturated alkyl; C2-3 alkenyl; C2-3 alkynyl; cyclopropyl; phenyl, which phenyl is optionally substituted by 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; 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.

    PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES
    10.
    发明申请
    PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES 有权
    。。IA IA。。。。。。。。。。

    公开(公告)号：US20160289239A1

    公开(公告)日：2016-10-06

    申请号：US15181900

    申请日：2016-06-14

    申请人： SEATTLE GENETICS, INC. ,  MEDIMMUNE LIMITED

    发明人： Scott Jeffrey ,  Patrick Burke ,  Philip Wilson Howard

    IPC分类号： C07D487/04 ,  A61K31/5517 ,  A61K47/48

    CPC分类号： A61K31/5517 ,  A61K47/55 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6889 ,  A61P35/00 ,  C07D487/04

    摘要： A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of: wherein: (a) R10 is H, and R11 is OH, ORA, where RA is saturated 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, or both M together are a divalent pharmaceutically acceptable cation.

    摘要翻译： 选自下式的化合物或其药学上可接受的盐或溶剂合物或其结合物其中：（a）R 10是H，R 11是OH，ORA，其中RA是饱和C 1-4烷基; （b）R 10和R 11在它们所结合的氮原子和碳原子之间形成氮 - 碳双键; 或（c）R 10为H且R 11为SO 2 M，其中z为2或3，M为一价药学上可接受的阳离子，或两者均为二价药学上可接受的阳离子。