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1. 发明申请

US20130028917A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：US20130028917A1
公开(公告)日：2013-01-31
申请号：US13641198
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
IPC分类号： A61K39/395 , A61P35/00 , C07D519/00 , C07K16/00 , C07K16/30
CPC分类号： C07D487/04 , A61K47/6849 , A61K47/6855 , A61K47/6869 , C07D519/00
摘要： Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
摘要翻译：公开了用于制备作为通过N10位置连接的PBD分子的缀合物的缀合物和化合物，以及缀合物用于治疗包括癌症在内的增殖性疾病的用途。

2. 发明申请

US20110256157A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：US20110256157A1
公开(公告)日：2011-10-20
申请号：US13087575
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , John A. Flygare , Janet L. Gunzner , Paul Polakis , Andrew Polson , Helga E. Raab , Susan D. Spencer
IPC分类号： A61K39/395 , B65D85/84 , C07K5/062 , C07K17/02 , C07D487/04
CPC分类号： C07D487/04 , A61K47/6849 , A61K47/6855 , A61K47/6869 , C07D519/00
摘要： Conjugates and compounds for making conjugates which are PBD molecules linked via the N10 position are disclosed, along with the use of the conjugates for treating proliferative diseases, including cancer.
摘要翻译：公开了用于制备作为通过N10位置连接的PBD分子的缀合物的缀合物和化合物，以及缀合物用于治疗包括癌症在内的增殖性疾病的用途。

3. 发明授权

US08829184B2 Intermediates useful for the synthesis of pyrrolobenzodiazepines 有权
标题翻译：可用于合成吡咯并苯并二氮杂卓的中间体
公开(公告)号：US08829184B2
公开(公告)日：2014-09-09
申请号：US13641237
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien
IPC分类号： C07D207/20 , C07D207/22 , C07D207/24 , C07D487/04
CPC分类号： C07D207/24 , C07D207/20 , C07D207/22 , C07D487/04
摘要： A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
摘要翻译：式（I）化合物：其基本上不含任何相应的式（IB）化合物：制备此类化合物的方法以及该化合物的进一步转化。

4. 发明申请

US20130035484A1 INTERMEDIATES USEFUL FOR THE SYNTHESIS OF PYRROLOBENZODIAZEPINES 有权
标题翻译：中间体用于合成紫杉酚的中间体
公开(公告)号：US20130035484A1
公开(公告)日：2013-02-07
申请号：US13641237
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien
IPC分类号： C07D207/16 , C07D487/04 , C07D519/00 , C07F7/18 , C07D403/12 , C07D207/08 , C07D207/12
CPC分类号： C07D207/24 , C07D207/20 , C07D207/22 , C07D487/04
摘要： A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
摘要翻译：式（I）化合物：其基本上不含任何相应的式（IB）化合物：制备此类化合物的方法以及该化合物的进一步转化。

5. 发明授权

US08697688B2 Pyrrolobenzodiazepines used to treat proliferative diseases 有权
标题翻译：用于治疗增殖性疾病的吡咯并苯并二氮杂卓
公开(公告)号：US08697688B2
公开(公告)日：2014-04-15
申请号：US13641180
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , Scott Jeffrey , Patrick Burke , Peter Senter
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , Scott Jeffrey , Patrick Burke , Peter Senter
IPC分类号： A01N43/62 , A61K31/55
CPC分类号： C07D487/04 , A61K47/6803 , A61K47/6849 , A61K47/6851 , C07D519/00
摘要： Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
摘要翻译：吡咯并苯并二氮杂二聚体I在一个单体单元上具有C2-C3双键和C2位上的芳基，C2-C3双键和C2位上的共轭双键或三键或C2位烷基在其他单体单元上，以及这些化合物的共轭物。

6. 发明申请

US20130059800A1 PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES 有权
标题翻译：用于治疗增殖性疾病的吡罗昔康唑
公开(公告)号：US20130059800A1
公开(公告)日：2013-03-07
申请号：US13641180
申请日：2011-04-15
申请人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , Scott Jeffrey , Patrick Burke , Peter Senter
发明人： Philip Wilson Howard , Luke Masterson , Arnaud Tiberghien , Scott Jeffrey , Patrick Burke , Peter Senter
IPC分类号： C07D487/04 , A61K38/05 , A61P35/00 , A61P21/04 , A61P17/06 , A61P19/08 , A61P9/10 , A61P19/02 , C07F7/10 , A61P35/02
CPC分类号： C07D487/04 , A61K47/6803 , A61K47/6849 , A61K47/6851 , C07D519/00
摘要： Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
摘要翻译：吡咯并苯并二氮杂二聚体I在一个单体单元上具有C2-C3双键和C2位上的芳基，C2-C3双键和C2位上的共轭双键或三键或C2位烷基在其他单体单元上，以及这些化合物的共轭物。

7. 发明授权

US08592576B2 Unsymmetrical pyrrolobenzodiazepine-dimers for treatment of proliferative diseases 有权
标题翻译：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。

8. 发明授权

US08487092B2 Pyrrolobenzodiazepines 有权
标题翻译：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。

9. 发明申请

US20110201803A1 PYRROLOBENZODIAZEPINES 有权
标题翻译： 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。

10. 发明申请

US20110196148A1 UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES 有权
标题翻译：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。

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