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1. 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。

2. 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。

3. 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。

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