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    Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases
    6.
    发明授权
    Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases 有权
    用于治疗增殖性疾病的不对称吡咯并苯并二氮杂二聚体

    公开(公告)号：US08592576B2

    公开(公告)日：2013-11-26

    申请号：US13123327

    申请日：2009-10-16

    申请人： Philip Wilson Howard ,  Stephen John Gregson ,  Luke Masterson

    发明人： Philip Wilson Howard ,  Stephen John Gregson ,  Luke Masterson

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N═C═O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, 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. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.

    摘要翻译： 声称是式（I）的不对称吡咯并苯并二氮杂二聚体（PBD-二聚体），其至少与变量R12和R2表示的值不对称。 式（I）其中：R2为式（Ⅱ），其中A为C5-7芳基，X选自OH，SH，CO2H，COH，N = C = O，NHRN，其中 RN选自H和C 1-4烷基，和（OC 2 H 4）m OCH 3，其中m为1至3，以及：（i）Q1为单键，Q2选自单键和-Z - （CH 2）n - ，其中Z选自单键，O，S和NH，n为1至3; 或（ii）Q1为-CH = CH-，Q2为单键; R 12是任选被一个或多个选自以下的取代基取代的C 5-10芳基：卤素，硝基，氰基，醚，C 1-7烷基，C 3-7杂环基和双 - 氧C 1-3亚烷基。 其他变量如权利要求中所定义。 该化合物可用于治疗增殖性疾病。

    Pyrrolobenzodiazepines
    7.
    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
    9.
    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 。

    UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES
    10.
    发明申请
    UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES 有权
    用于治疗增殖性疾病的非对称吡嗪二酮

    公开(公告)号：US20110196148A1

    公开(公告)日：2011-08-11

    申请号：US13123327

    申请日：2009-10-16

    申请人： Philip Wilson Howard ,  Stephen John Gregson ,  Luke Masterson

    发明人： Philip Wilson Howard ,  Stephen John Gregson ,  Luke Masterson

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： Claimed are unsymmetrical Pyrrolobenzodiazepine-dimers (PBD-dimers) of formula (I), that are unsymmetrical due at least to the values that the variables R12 and R2 represent. Formula (I), wherein: R2 is of formula (II), where A is a C5-7 aryl group, X is selected from the group comprising: OH, SH, CO2H, COH, N═C═O, NHRN, wherein RN is selected from the group comprising H and C1-4 alkyl, and (OC2H4)mOCH3, where m is 1 to 3, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)m—, 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. The other variables are as defined in the claims. The compounds are useful for the treatment of proliferative diseases.

    摘要翻译： 声称是式（I）的不对称吡咯并苯并二氮杂二聚体（PBD-二聚体），其至少与变量R12和R2表示的值不对称。 式（I）其中：R2为式（II），其中A为C5-7芳基，X选自OH，SH，CO2H，COH，N = C = O，NHRN，其中 RN选自H和C 1-4烷基，和（OC 2 H 4）m OCH 3，其中m为1至3，以及：（i）Q1为单键，Q2选自单键和-Z - （CH 2）m - ，其中Z选自单键，O，S和NH，n为1至3; 或（ii）Q1是-CH = CH-，Q2是单键; R 12是任选被一个或多个选自以下的取代基取代的C 5-10芳基：卤素，硝基，氰基，醚，C 1-7烷基，C 3-7杂环基和双 - 氧C 1-3亚烷基。 其他变量如权利要求中所定义。 该化合物可用于治疗增殖性疾病。