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1. 发明申请

WO2005042535A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2005042535A1
公开(公告)日：2005-05-12
申请号：PCT/GB2004/004497
申请日：2004-10-22
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , THURSTON, David, Edwin , GREGSON, Stephen, John
发明人： HOWARD, Philip, Wilson , THURSTON, David, Edwin , GREGSON, Stephen, John
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound of formula (I): or solvate thereof, wherein n is 1 to 10, and M and M' are independently selected from monovalent pharmaceutically acceptable cations, or together represent a divalent pharmaceutically acceptable cation.
摘要翻译：式（I）的化合物或其溶剂合物，其中n为1-10，M和M'独立地选自一价药学上可接受的阳离子，或一起代表二价药学上可接受的阳离子。

2. 发明申请

WO2004043963A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2004043963A1
公开(公告)日：2004-05-27
申请号：PCT/GB2003/004963
申请日：2003-11-14
申请人： SPIROGEN LIMITED , THURSTON, David, Edwin , HOWARD, Philip, Wilson
发明人： THURSTON, David, Edwin , HOWARD, Philip, Wilson
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/551
摘要： Compounds of formula (I) : formula (I) and salts, solvates, chemically protected forms, and prodrugs thereof, are disclosed wherein R 2 is selected from: an optionally substituted napthyl group; an optionally substituted thiophenyl or furanyl group; and a phenyl group substituted by: one or more chloro or fluoro groups; an ethyl or propyl group; a 4-t-butyl group; a 2-methyl group; or two methyl groups in the 2- and 6- positions.
摘要翻译：公开了式（I）化合物：式（I）及其盐，溶剂化物，化学保护形式及其前药，其中R 2选自：任选取代的萘基; 任选取代的噻吩基或呋喃基; 和被一个或多个氯或氟基取代的苯基; 乙基或丙基; 4-叔丁基; 2-甲基; 或2-和6-位的两个甲基。

3. 发明申请

WO2010010347A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2010010347A1
公开(公告)日：2010-01-28
申请号：PCT/GB2009/001819
申请日：2009-07-22
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , GREGSON, Stephen, John , CHEN, Zhizhi , TIBERGHIEN, Arnaud, Charles , MASTERSON, Luke
发明人： HOWARD, Philip, Wilson , GREGSON, Stephen, John , CHEN, Zhizhi , TIBERGHIEN, Arnaud, Charles , MASTERSON, Luke
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04
摘要： Methods of preparing ZC-423 (I) which result in varying enantiomeric ratios.
摘要翻译：制备ZC-423（I）的方法，其导致不同的对映异构体比例。

4. 发明申请

WO2010043880A1 UNSYMMETRICAL PYRROLOBENZODIAZEPINE-DIMERS FOR TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
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：WO2010043880A1
公开(公告)日：2010-04-22
申请号：PCT/GB2009/002498
申请日：2009-10-16
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , GREGSON, Stephen, John , MASTERSON, Luke
发明人： HOWARD, Philip, Wilson , GREGSON, Stephen, John , MASTERSON, Luke
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
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 R 12 and R 2 represent. Formula (I), wherein: R 2 is of formula (II), where A is a C 5-7 aryl group, X is selected from the group comprising: OH, SH, CO 2 H, COH, N=C=O, NHR N , wherein R N is selected from the group comprising H and C 1-4 alkyl, and (OC 2 H 4 ) m OCH 3 , where m is 1 to 3, and either: (i) Q 1 is a single bond, and Q 2 is selected from a single bond and -Z-(CH 2 ) n -, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q 1 is -CH=CH-, and Q 2 is a single bond; R 12 is a C 5-10 aryl group, 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-oxy-C 1-3 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。

5. 发明申请

WO2005085251A1 11-HYDROXY-5H-PYRROLO[2,1-C][1,4]BENZODIAZEPIN-5-ONE DERIVATIVES AS KEY INTERMEDIATES FOR THE PREPARATION OF C2 SUBSTITUTED PYRROLOBENZODIAZEPINES 审中-公开
标题翻译： 11-羟基-5H-吡咯并[2,1-C] [1,4]苯并咪唑-5-酮衍生物作为制备C2取代的吡咯烷酮的主要中间体
公开(公告)号：WO2005085251A1
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000768
申请日：2005-03-01
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , GREGSON, Stephen, John
发明人： HOWARD, Philip, Wilson , GREGSON, Stephen, John
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： The present inventors have developed a key intermediate for the production of C2 substituted PBDs, which has a leaving group at the C2 position, a carbamate protecting group at the N10 position and a protected hydroxy group at the C11 position. In a first aspect, the present invention comprises a compound with a the formula (I), wherein : R 10 is a carbamate-based nitrogen protecting group; R 11 is an oxygen protecting group; and R 2 is a labile leaving group. In a further aspect, the present invention comprises a method of synthesising a compound of formula (III), or a solvate thereof, from a compound of formula (I) as defined in the first aspect, R 16 is either O-R11, wherein R 11 is as defined in the first aspect, or OH, or R 10 and R 16 together form a double bond between N10 and C11; and R 15 is R. The other substituents are defined in the claims. Further aspects of the present invention relate to compounds of formula (III) (including solvates thereof when R 10 and R 16 form a double bond between N10 and C11, and pharmaceutical salts thereof), pharmaceutical compositions comprising these, and their use in the manufacture of a medicament for the treatment of a proliferative disease.
摘要翻译：本发明人已经开发了用于生产在C2位具有离去基团的C2取代的PBD的关键中间体，N10位的氨基甲酸酯保护基和C11位的被保护的羟基。在第一方面，本发明包括具有式（I）的化合物，其中：R 10是氨基甲酸酯基氮保护基; R 11是氧保护基; 而R 2是不稳定的离去基团。在另一方面，本发明包括由第一方面定义的式（I）化合物合成式（III）化合物或其溶剂合物的方法，R 16为O-R 11 其中R 11如在第一方面中所定义，或OH或R 10和R 16一起在N10和C11之间形成双键; R 15为R.其它取代基在权利要求书中定义。本发明的其它方面涉及式（III）的化合物（当R 10和R 16在N 10和C 11之间形成双键时，包括其溶剂合物及其药用盐），包含它们的药物组合物及其用于制备用于治疗增殖性疾病的药物。

6. 发明申请

WO2010043877A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2010043877A1
公开(公告)日：2010-04-22
申请号：PCT/GB2009/002495
申请日：2009-10-16
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , GREGSON, Stephen, John , CHEN, ZhiZhi , TIBERGHIEN, Arnaud, Charles , MASTERSON, Luke
发明人： HOWARD, Philip, Wilson , GREGSON, Stephen, John , CHEN, ZhiZhi , TIBERGHIEN, Arnaud, Charles , MASTERSON, Luke
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: R 2 is CHR 2A , and R 2A is independently selected from H, R, CO 2 R, COR, CHO, CO 2 H, and halo; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', NO 2 , Me 3 Sn and halo; R 7 is independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', NO 2 , Me 3 Sn and halo; R 8 is independently selected from H, R, OH, OR, SH, SR, NH 2, NHR, NRR', NO 2 , Me 3 Sn and halo; R is independently selected from optionally substituted C 1-12 alkyl, C 3-20 heterocyclyl and C 5-20 aryl groups; or the compound is a dimer with each monomer being of formula (M), where the R 7 groups or R 8 groups of each monomer form together a dimer bridge having the formula -X-R"-X- linking the monomers; wherein R" is a C 3-I2 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 R 6 to R 9 together form a group -O-(CH 2 ) 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是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基团形成具有式-XR“-X-连接单体的二聚体桥，其中R”是C 3 -I2亚烷基，该链可以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，以及其盐和溶剂合物，以及它们作为制备其它PBD化合物的中间体的用途。

7. 发明申请

WO2006111759A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2006111759A1
公开(公告)日：2006-10-26
申请号：PCT/GB2006/001456
申请日：2006-04-21
申请人： SPIROGEN LIMITED , GREGSON, Stephen, John , HOWARD, Philip, Wilson , CHEN, Zhizhi
发明人： GREGSON, Stephen, John , HOWARD, Philip, Wilson , CHEN, Zhizhi
IPC分类号： C07D519/00 , A61P35/00 , A61K31/5517
CPC分类号： C07D519/00
摘要： Compounds of the formula: (I) or solvate thereof, wherein: R 2 is an optionally substituted C 5-20 aryl group; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', nitro, Me 3 Sn and halo; where R and R' are independently selected from optionally substituted C 1-12 alkyl, C 3-20 heterocyclyl and C 5-20 aryl groups; R 7 is selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NHRR', nitro, Me 3 Sn and halo; R" is a C 3-12 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; R 2 ', R 6 ', R 7 ', R 9 ', X' and M' are selected from the same groups as R 2 , R 6 , R 7 , R 9 , 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'选自与R 2，R 6，R 7，R 9相同的基团分别为X和M，或M和M'可以一起表示二价药学上可接受的阳离子。

8. 发明申请

WO2011130616A1 PYRROLOBENZODIAZEPINES USED TO TREAT PROLIFERATIVE DISEASES 审中-公开
标题翻译：用于治疗增殖性疾病的吡罗昔康唑
公开(公告)号：WO2011130616A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032668
申请日：2011-04-15
申请人： SPIROGEN LIMITED , SEATTLE GENETICS, INC. , HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
IPC分类号： C07D519/00 , A61K31/5517 , A61P35/00
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。

9. 发明申请

WO2011130598A1 PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
标题翻译：。。。。。。。。。。。。
公开(公告)号：WO2011130598A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032632
申请日：2011-04-15
申请人： SPIROGEN LIMITED , HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , FLYGARE, John, A. , GUNZNER, Janet, L. , POLAKIS, Paul , POLSON, Andrew , RAAB, Helga, E. , SPENCER, Susan, D.
发明人： HOWARD, Philip, Wilson , MASTERSON, Luke , TIBERGHIEN, Arnaud , FLYGARE, John, A. , GUNZNER, Janet, L. , POLAKIS, Paul , POLSON, Andrew , RAAB, Helga, E. , SPENCER, Susan, D.
IPC分类号： A61K47/48 , C07D487/04 , A61P35/00
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。

10. 发明申请

WO2011130613A1 TARGETED PYRROLOBENZODIAZAPINE CONJUGATES 审中-公开
标题翻译：目标吡咯并唑酸联用
公开(公告)号：WO2011130613A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/032664
申请日：2011-04-15
申请人： SEATTLE GENETICS, INC. , SPIROGEN LIMITED , HOWARD, Philip, Wilson , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
发明人： HOWARD, Philip, Wilson , JEFFREY, Scott , BURKE, Patrick , SENTER, Peter
IPC分类号： A61K47/48 , A61P35/00 , A61P37/00
CPC分类号： C07K16/3038 , A61K31/5517 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6861 , A61K47/6867 , A61K47/6889 , A61K2039/505 , C07K16/2812 , C07K16/2875 , C07K16/2878 , C07K16/30 , C07K16/3061 , C07K2317/21 , C07K2317/24 , Y02A50/385 , Y02A50/414 , Y02A50/423
摘要： Provided are Conjugate comprising PBDs conjugated to a targeting agent and methods of using such PBDs.
摘要翻译：提供了包含与靶向剂缀合的PBD的缀合物和使用这种PBD的方法。

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