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    PYRROLOBENZODIAZEPINES
    1.
    发明申请
    PYRROLOBENZODIAZEPINES 有权
    PYRROBOBENZODIAZEPINES

    公开(公告)号：US20100113425A1

    公开(公告)日：2010-05-06

    申请号：US12610478

    申请日：2009-11-02

    申请人： Philip Wilson Howard ,  Zhizhi Chen ,  Stephen John Gregson

    发明人： Philip Wilson Howard ,  Zhizhi Chen ,  Stephen John Gregson

    IPC分类号： A61K31/551 ,  A61P35/02 ,  A61P35/00 ,  C07D487/04

    CPC分类号： C07D519/00

    摘要： Compounds of the formula I: or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; 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; R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2′, R6′, R7′, R9′, X′ and M′ are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M′ may together represent a divalent pharmaceutically acceptable cation.

    摘要翻译： 式I化合物或其溶剂化物，其中：R2是任选取代的C5-20芳基; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，硝基，Me 3 Sn和卤素; 其中R和R'独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基; R 7选自H，R，OH，OR，SH，SR，NH 2，NHR，NHRR'，硝基，Me 3 Sn和卤素; R“是C3-12亚烷基，该链可被一个或多个杂原子和/或芳环中断; X选自O，S或NH; z是2或3; M是一价药学上可接受的阳离子; R 2'，R 6'，R 7'，R 9'，X'和M'分别选自与R 2，R 6，R 7，R 9，X和M相同的基团，或M和M'可以一起表示二价药学上可接受的阳离子 。

    Pyrrolobenzodiazepines
    2.
    发明授权
    Pyrrolobenzodiazepines 有权
    吡咯并苯并二氮杂卓

    公开(公告)号：US08633185B2

    公开(公告)日：2014-01-21

    申请号：US12610478

    申请日：2009-11-02

    申请人： Philip Wilson Howard ,  Zhizhi Chen ,  Stephen John Gregson

    发明人： Philip Wilson Howard ,  Zhizhi Chen ,  Stephen John Gregson

    IPC分类号： C07D519/00 ,  A61K31/5517 ,  A61P35/00

    CPC分类号： C07D519/00

    摘要： Compounds of the formula I: or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; 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; R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2′, R6′, R7′, R9′, X′ and M′ are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M′ may together represent a divalent pharmaceutically acceptable cation.

    摘要翻译： 式I化合物或其溶剂化物，其中：R2是任选取代的C5-20芳基; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，硝基，Me 3 Sn和卤素; 其中R和R'独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基; R 7选自H，R，OH，OR，SH，SR，NH 2，NHR，NHRR'，硝基，Me 3 Sn和卤素; R“是C3-12亚烷基，该链可被一个或多个杂原子和/或芳环中断; X选自O，S或NH; z为2或3; M是一价药学上可接受的阳离子; R 2'，R 6'，R 7'，R 9'，X'和M'分别选自与R 2，R 6，R 7，R 9，X和M相同的基团，或M和M'可以一起表示二价药学上可接受的阳离子 。

    Pyrrolobenzodiazepines
    5.
    发明授权
    Pyrrolobenzodiazepines 有权
    吡咯并苯并二氮杂卓

    公开(公告)号：US08487092B2

    公开(公告)日：2013-07-16

    申请号：US13124232

    申请日：2009-10-16

    申请人： Philip Wilson Howard ,  Stephen John Gregson ,  ZhiZhi Chen ,  Arnaud Charles Tiberghien ,  Luke Masterson

    发明人： Philip Wilson Howard ,  Stephen John Gregson ,  ZhiZhi Chen ,  Arnaud Charles Tiberghien ,  Luke Masterson

    IPC分类号： C07D519/00

    CPC分类号： C07D519/00

    摘要： The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, R, CO2R, COR, CHO, CO2H, and halo; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R″—X— linking the monomers; wherein R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g. benzene or pyridine; and each X is independently selected from O, S, or N(H); or any pair of adjacent groups from R6 to R9 together form a group —O—(CH2)p—O—, where p is 1 or 2, and salts and solvates thereof, and their use as intermediates for the preparation of other PBD compounds.

    摘要翻译： 本发明涉及某些吡咯并苯并二氮杂（PBD），特别是含有C2取代的吡咯并苯并二氮杂二聚体，包括式（T）化合物：其中：R2为CHR2A，R2A独立地选自H，R，CO2R，COR，CHO，CO2H ，和卤素; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 8独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基; 或者化合物是每个单体具有式（M）的二聚体，其中每个单体的R 7基团或R 8基团一起形成具有式-X-R“-X-连接单体的二聚体桥; 其中R“是C 3-12亚烷基，该链可被一个或多个杂原子间隔，例如， O，S，N（H）和/或芳环，例如。 苯或吡啶; 并且每个X独立地选自O，S或N（H）; 或R6至R9的任何一对相邻基团一起形成-O-（CH 2）p -O-基团，其中p为1或2，以及其盐和溶剂化物，以及它们作为制备其它PBD化合物的中间体的用途。

    PYRROLOBENZODIAZEPINES
    6.
    发明申请
    PYRROLOBENZODIAZEPINES 有权
    PYRROBOBENZODIAZEPINES

    公开(公告)号：US20110201803A1

    公开(公告)日：2011-08-18

    申请号：US13124232

    申请日：2009-10-16

    申请人： Philip Wilson Howard ,  Stephen John Gregson ,  Zhizhi Chen ,  Arnaud Charles Tiberghien ,  Luke Masterson

    发明人： Philip Wilson Howard ,  Stephen John Gregson ,  Zhizhi Chen ,  Arnaud Charles Tiberghien ,  Luke Masterson

    IPC分类号： C07D487/04

    CPC分类号： C07D519/00

    摘要： The invention relates to certain pyrrolobenzodiazepines (PBDs), and in particular pyrrolobenzodiazepine dimers bearing C2 substitutions, including compounds of formula (T): wherein: R2 is CHR2A, and R2A is independently selected from H, R, CO2R, COR, CHO, CO2H, and halo; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R8 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR′, NO2, Me3Sn and halo; R is independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R7 groups or R8 groups of each monomer form together a dimer bridge having the formula —X—R″—X— linking the monomers; wherein R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms, e.g. O, S, N(H), and/or aromatic rings, e.g. benzene or pyridine; and each X is independently selected from O, S, or N(H); or any pair of adjacent groups from R6 to R9 together form a group —O—(CH2)p—O—, where p is 1 or 2, and salts and solvates thereof, and their use as intermediates for the preparation of other PBD compounds.

    摘要翻译： 本发明涉及某些吡咯并苯并二氮杂（PBD），特别是含有C2取代的吡咯并苯并二氮杂二聚体，包括式（T）化合物：其中：R2为CHR2A，R2A独立地选自H，R，CO2R，COR，CHO，CO2H ，和卤素; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 8独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基; 或者化合物是每个单体具有式（M）的二聚体，其中每个单体的R 7基团或R 8基团一起形成具有式-X-R“-X-连接单体的二聚体桥; 其中R“是C 3-12亚烷基，该链可被一个或多个杂原子间隔，例如。 O，S，N（H）和/或芳环，例如。 苯或吡啶; 并且每个X独立地选自O，S或N（H）; 或从R6至R9的任何一对相邻基团一起形成-O-（CH 2）p -O-基团，其中p为1或2，以及其盐和溶剂化物，以及它们作为制备其它PBD化合物的中间体的用途 。

    Pyrrolobenzodiazepines
    7.
    发明授权
    Pyrrolobenzodiazepines 有权
    吡咯并苯并二氮杂卓

    公开(公告)号：US07612062B2

    公开(公告)日：2009-11-03

    申请号：US11911890

    申请日：2006-04-21

    申请人： Stephen John Gregson ,  Philip Wilson Howard ,  Zhizhi Chen

    发明人： Stephen John Gregson ,  Philip Wilson Howard ,  Zhizhi Chen

    IPC分类号： C07D519/00 ,  A61K31/5517 ,  A61P35/00

    CPC分类号： C07D519/00

    摘要： Compounds of the formula: (I) or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; 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; R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2′, R6′, R7′, R9′, X′ and M′ are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M′ may together represent a divalent pharmaceutically acceptable cation.

    摘要翻译： 式（I）或其溶剂化物的化合物，其中：R 2是任选取代的C 5-20芳基; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，硝基，Me 3 Sn和卤素; 其中R和R'独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基; R 7选自H，R，OH，OR，SH，SR，NH 2，NHR，NHRR'，硝基，Me 3 Sn和卤素; R“是C3-12亚烷基，该链可被一个或多个杂原子和/或芳环中断; X选自O，S或NH; z为2或3; M是一价药学上可接受的阳离子; R 2'，R 6'，R 7'，R 9'，X'和M'分别选自与R 2，R 6，R 7，R 9，X和M相同的基团，或M和M'可以一起表示二价药学上可接受的阳离子 。

    Pyrrolobenzodiazepines
    8.
    发明申请
    Pyrrolobenzodiazepines 有权
    吡咯并苯并二氮杂卓

    公开(公告)号：US20080167293A1

    公开(公告)日：2008-07-10

    申请号：US11911890

    申请日：2006-04-21

    申请人： Philip Wilson Howard ,  Zhizhi Chen ,  Stephen John Gregson

    发明人： Philip Wilson Howard ,  Zhizhi Chen ,  Stephen John Gregson

    IPC分类号： A61K31/5513 ,  C07D487/00 ,  A61P35/00

    CPC分类号： C07D519/00

    摘要： Compounds of the formula: (I) or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; 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; R″ is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2′, R6′, R7′, R9′, X′ and M′ are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M′ may together represent a divalent pharmaceutically acceptable cation.

    摘要翻译： 式（I）或其溶剂合物的化合物，其中：R 2是任选取代的C 5-20芳基; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'， 硝基，Me 3 Sn和卤素; 其中R和R'独立地选自任选取代的C 1-12烷基，C 3-20 - 杂环基和C 5-20芳基 ; R 7选自H，R，OH，OR，SH，SR，NH 2，NHR，NHRR'，硝基，Me 3 Sn和卤素; R“是C 3-12亚烷基，该链可以被一个或多个杂原子和/或芳环中断; X选自O，S或NH; z为2或3; M是一价药学上可接受的阳离子; R 2，R 6，R 7，R 9，X'和M'分别为 分别选自与R 2，R 6，R 7，R 9，X和M分别相同的基团 ，或M和M'可以一起表示二价药学上可接受的阳离子。