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1. 发明申请

WO0012507A8 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO0012507A8
公开(公告)日：2000-10-19
申请号：PCT/GB9902837
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61P31/10 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07D207/08 , C07D487/04 , C07D519/00 , C07D207/20
CPC分类号： C07D487/04 , Y02P20/55
摘要： A compound with formula (I) where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, =O, =CH-R, =CH2, CH2-CO2R, CH2-CO2H, CH2-SO2R, O-SO2-R, CO2R, COR and CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, nitro, Me3Sn; X is S, O or NH; R11 is either H or R; and where there is optionally a double bond between C1 and C2 or C2 and C3; and R8 is selected from H, R, OH, OR, halo, amino, nitro, Me3Sn, or R7 and R8 together form a group -O-(CH2)p-O-, where p is 1 or 2. Such compounds may be used in methods of ADEPT, GDEPT, NPEPT or PDT.
摘要翻译：具有式（I）的化合物，其中R 10是治疗性除去的氮保护基; R2和R3独立地选自：H，R，OH，OR，= O，= CH-R，= CH2，CH2-CO2R，CH2-CO2H，CH2-SO2R，O-SO2-R，CO2R，COR和CN ; R 6，R 7和R 9独立地选自H，R，OH，OR，卤素，氨基，硝基，Me 3 Sn; X是S，O或NH; R11是H或R; 并且其中C1和C2或C2和C3之间任选具有双键; 并且R 8选自H，R，OH，OR，卤素，氨基，硝基，Me 3 Sn或R 7和R 8一起形成基团-O-（CH 2）p O-，其中p为1或2。在ADEPT，GDEPT，NPEPT或PDT的方法中。

2. 发明申请

WO0012506A3 COLLECTIONS OF COMPOUNDS 审中-公开
标题翻译：化合物的集合
公开(公告)号：WO0012506A3
公开(公告)日：2000-06-29
申请号：PCT/GB9902836
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61K38/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , C07D487/04 , C07K1/06 , C07K1/10 , C07K5/083 , C07K5/087 , C40B40/02 , C40B40/04 , C40B50/06 , C07B61/00 , C07D519/00 , G01N33/50
CPC分类号： C07D487/04 , Y02P20/55
摘要： A compound of formula (IV): O is a solid support; L is a linking group or a single bond; X' is selected from CO, NH, S, or O; A is O, S, NH, or a single bond; R2 and R3 are independently selected from: H, R, OH, OR, =O, =CH-R, =CH2, CH2-CO2R, CH2-CO2H, CH2-SO2R, O-SO2R, CO2R, COR, CN and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, and R9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn; R11 is either H or R; Q is S, O or NH; R10 is a nitrogen protecting group; and Y is a divalent group such that HY = R, and other related compounds and collections of compounds.
摘要翻译：式（IV）的化合物：O是固体载体; L是连接基团或单键; X'选自CO，NH，S或O; A是O，S，NH或单键; R2和R3独立地选自：H，R，OH，OR，= O，= CH-R，= CH2，CH2-CO2R，CH2-CO2H，CH2-SO2R，O-SO2R，CO2R，任选地是C1和C2或C2和C3之间的双键; R6，R7和R9独立地选自H，R，OH，OR，卤素，硝基，氨基，Me3Sn; R11是H或R; Q是S，O或NH; R10是氮保护基团; Y是二价基团，使得HY = R，以及其他相关化合物和化合物的集合。

3. 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。

4. 发明申请

WO0012509B1 COLLECTIONS OF COMPOUNDS 审中-公开
标题翻译：化合物的集合
公开(公告)号：WO0012509B1
公开(公告)日：2000-08-10
申请号：PCT/GB9902839
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61P31/00 , A61P43/00 , C07D487/04 , C07B61/00 , G01N33/50
CPC分类号： C07D487/04
摘要： A compound of formula (I), wherein: R2 and R3 are independently selected from H, R, OH, OR, =0, =CH-R, =CH2, CH2-CO2R, CH2-CO2H, CH2-SO2R, O-SO2R, CO2R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3; R6, R7, R8 and R9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn; R11 is either H or R; Q is S, O or NH; L is a linking group, or a single bond; O is a solid support; or where one or more of R2, R3, R6, R7 and R8 are independently: H-(T)n-X-Y-A- where: X is CO, NH, S or O; T is a combinatorial unit; Y is a divalent group such that HY = R; A is O, S, NH, or a single bond and n is a positive integer.
摘要翻译：其中：R 2和R 3独立地选自H，R，OH，OR 1 = CH 2 R 2 = CH 2，CH 2 -CO 2 R，CH 2 -CO 2 H，CH 2 -SO 2 R，O- SO2R，CO2R，COR和CN，并且在C1和C2或C2和C3之间任选地具有双键; R6，R7，R8和R9独立地选自H，R，OH，OR，卤素，硝基，氨基，Me3Sn; R11是H或R; Q是S，O或NH; L是连接基团或单键; O是坚实的支持; 或其中R 2，R 3，R 6，R 7和R 8中的一个或多个独立地为：其中：X是CO，NH，S或O; T是一个组合单位; Y是二价基团，使得HY = R; A是O，S，NH或单键，n是正整数。

5. 发明申请

WO2007039752A1 ALKYL 4- [4- (5-OXO-2, 3, 5, 11A-TETRAHYD0-5H-PYRR0L0 [2, 1-C] [1, 4] BENZODIAZEPINE-8-YLOXY) -BUTYRYLAMINO]-1H-PYRROLE-2-CARBOXYLATE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF A PROLIFERATIVE DISEASE 审中-公开
标题翻译：亚苄基4- [4-（5-氧代-2,3,5,11-四氢-2H-吲哚-5-基）[2,1-C] [1,4]苯并嗪-5-基） - 丁基]氨基] -1H-吡咯并[ 2-羧酸酯衍生物及相关化合物治疗增殖性疾病
公开(公告)号：WO2007039752A1
公开(公告)日：2007-04-12
申请号：PCT/GB2006/003718
申请日：2006-10-05
申请人： SPIROGEN LIMITED , HOWARD, Philip Wilson , THURSTON, David Edwin , WELLS, Geoffrey
发明人： HOWARD, Philip Wilson , THURSTON, David Edwin , WELLS, Geoffrey
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04
摘要： A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R 2 is selected from -H, -OH, =0, =CH 2 , -CN, -R, OR, halo, =CH-R, O-SO 2 -R, CO 2 R and COR; R 7 is 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 1-7 alkyl, C 3-20 heterocyclyl and C 5-20 aryl groups; R 10 and R 11 either together form a double bond, or are selected from H and YR Y , where Y is selected from O, S and NH and R Y is H or C 1-7 alkyl or H and SO x M, where x is 2 or 3, and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and R E is C 1-4 alkyl. The compound is useful for the treatment of proliferative diseases.
摘要翻译：式（I）化合物; 或其盐或溶剂合物，其中：虚线表示在C2和C3之间任选存在双键; R 2选自-H，-OH，= O，= CH 2，-CN，-R，OR，卤素，= CH-R，O-SO R 2和R 2，R 2和R C; R 7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 1-7 - 烷基，C 3-20 - 杂环基和C 5-20 - SUB>芳基; R 10和R 11一起形成双键，或选自H和YR Y，其中Y选自O，S 和NH和R Y是H或C 1-7烷基或H和SO x M，其中x是2或3，M 是一价药学上可接受的阳离子; 每个X独立地是亚杂芳基; n为1至6; 并且R E是C 1-4烷基。该化合物可用于治疗增殖性疾病。

6. 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。

7. 发明申请

WO0012508B1 PYRROLBENZODIAZEPINES 审中-公开
公开(公告)号：WO0012508B1
公开(公告)日：2000-11-02
申请号：PCT/GB9902838
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , C07D487/04 , C07D519/00 , A61K31/551
CPC分类号： C07D487/04
摘要： Compounds of formula (Ia) and (Ib) wherein A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn; and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula (Ia) or (Ib), where the R8 groups of the monomers form together a bridge having the formula -X-R'-X- linking the monomers, where R' is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon-carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula (Ia) when A is a single bond, then R2 is not CH=CH(CONH2) or CH=CH(CONMe2). Other related compounds are also disclosed.
摘要翻译：式（Ia）和（Ib）的化合物，其中A是CH 2或单键; R2选自：R，OH，OR，CO 2 H，CO 2 R，COH，COR，SO 2 R，CN; R 6，R 7和R 9独立地选自H，R，OH，OR，卤素，氨基，NHR，硝基，Me 3 Sn; 并且R 8选自H，R，OH，OR，卤素，氨基，NHR，硝基，Me 3 Sn，其中R如上所定义，或该化合物是二聚体，每个单体相同或不同，并且具有式）或（Ib），其中所述单体的R8基团形成具有式-X-R'-X连接单体的桥，其中R'是含有3至12个碳原子的亚烷基链，该链可以被一个或多个杂原子和/或芳环中断，并且可以含有一个或多个碳 - 碳双键或三键，并且每个X独立地选自O，S或N; 不同之处在于当A为单键时，式（Ia）化合物中，R 2不是CH = CH（CONH 2）或CH = CH（CONMe 2）。还公开了其它相关化合物。

8. 发明申请

WO0012508A3 PYRROLBENZODIAZEPINES 审中-公开
公开(公告)号：WO0012508A3
公开(公告)日：2000-09-21
申请号：PCT/GB9902838
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , C07D487/04 , C07D519/00 , A61K31/551
CPC分类号： C07D487/04
摘要： Compounds of formula (Ia) and (Ib) wherein A is CH2, or a single bond; R2 is selected from: R, OH, OR, CO2H, CO2R, COH, COR, SO2R, CN; R6, R7 and R9 are independently selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn; and R8 is selected from H, R, OH, OR, halo, amino, NHR, nitro, Me3Sn, where R is as defined above, or the compound is a dimer with each monomer being the same or different and being of formula (Ia) or (Ib), where the R8 groups of the monomers form together a bridge having the formula -X-R'-X- linking the monomers, where R' is an alkylene chain containing from 3 to 12 carbon atoms, which chain may be interrupted by one or more hetero-atoms and/or aromatic rings and may contain one or more carbon-carbon double or triple bonds, and each X is independently selected from O, S, or N; except that in a compound of formula (Ia) when A is a single bond, then R2 is not CH=CH(CONH2) or CH=CH(CONMe2). Other related compounds are also disclosed.
摘要翻译：式（Ia）和（Ib）的化合物，其中A是CH 2或单键; R2选自：R，OH，OR，CO2H，CO2R，COH，COR，SO2R，CN; R6，R7和R9独立地选自H，R，OH，OR，卤素，氨基，NHR，硝基，Me3Sn; 和R 8选自H，R，OH，OR，卤素，氨基，NHR，硝基，Me 3 Sn，其中R如上定义，或者该化合物是二聚体，每种单体相同或不同并且具有式）或（Ib），其中单体的R 8基团一起形成连接单体的具有式-X-R 1 -X-的桥，其中R'是含有3-12个碳原子的亚烷基链，该链可以被一个或多个杂原子和/或芳环中断，并且可以含有一个或多个碳 - 碳双键或三键，并且每个X独立地选自O，S或N; 除了在式（Ia）的化合物中当A是单键时，则R 2不是CH = CH（CONH 2）或CH = CH（CONMe 2）。其他相关化合物也被公开。

9. 发明申请

WO1993018045A1 ANTI-CANCER PYRROLOBENZODIAZEPINE DERIVATIVES 审中-公开
标题翻译：抗癌青霉烯酮衍生物
公开(公告)号：WO1993018045A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000483
申请日：1993-03-08
申请人： CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED , THURSTON, David, Edwin , BOSE, Deverakonda, Subhas
发明人： CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： There are disclosed, as novel compounds, pyrrolo [2,1-c][1,4] benzodiazepine (PBD) dimers of formula (I) where the PBD tricyclic structures may contain additional substituents in one or more of the 1, 2, 3, 6, 7, 9 and 11-positions and the C rings may optionally contain at least one further hetero ring atom, X is -O-, -S- or -NH-, and R is an alkylene chain containing from 3 to 12 carbon atoms, which chain may, if desired, be interrupted by one or more hetero-atoms and which chain may, if desired, contain one or more carbon-carbon double or triple bonds. These compounds are cytotoxic and have shown in vitro activity against a range of carcinoma cell lines.
摘要翻译：作为新化合物，公开了式（I）的吡咯并[2,1-c] [1,4]苯并二氮杂（PBD）二聚体，其中PBD三环结构可以在1，2， 3个，6个，7个，9个和11个位置，C环可以任选地含有至少一个另外的杂环原子，X是-O - ， - S-或-NH-，R 1是含有如果需要，该链可以被一个或多个杂原子中断，并且如果需要，该链可以包含一个或多个碳 - 碳双键或三键。这些化合物是细胞毒性的并且已经显示针对一系列癌细胞系的体外活性。

10. 发明申请

WO2005110423A2 PYRROLOBENZODIAZEPINE THERAPEUTIC AGENTS 审中-公开
标题翻译：吡罗昔康唑治疗药物
公开(公告)号：WO2005110423A2
公开(公告)日：2005-11-24
申请号：PCT/GB2005/001881
申请日：2005-05-13
申请人： SPIROGEN LIMITED , PEPPER, Christopher John , THURSTON, David Edwin
发明人： PEPPER, Christopher John , THURSTON, David Edwin
IPC分类号： A61K31/551
CPC分类号： A61K31/551 , A61K31/5517
摘要： A pyrrolobenzodiazepine dimer compound of Formula (I): or pharmaceutically acceptable salt or solvate thereof is useful as a therapeutic agent for the treatment of leukaemias, especially B-cell leukaemias, that exhibit resistance to other chemotherapeutic drugs, wherein: the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R 2 and R 3 are independently selected from -H, =O, =CH 2 , -CN, -R, OR, halo, =CH-R, O-SO 2 -R, CO 2 R and COR; R 6 , R 7 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 10 is a carbamate-based nitrogen protecting group and R 15 is either O-R 11 , wherein R 11 is an oxygen protecting group, or OH, or R 10 and R 15 together form a double bond between N10 and C11; R" is a C 3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings, and each X is independently selected from O, S, or NH; R 2' , R 3' , R 6' , R 7' , R 9' , R 10' and R 15' are all independently selected from the same lists as previously defined for R 2 , R 3 , R 6 , R 7 , R 9 , R 10 and R 15 respectively.
摘要翻译：式（I）的吡咯并苯并二氮杂二聚体化合物或其药学上可接受的盐或溶剂合物可用作治疗其他化疗药物抗白血病，特别是B细胞白血病的治疗剂，其中：虚线表示在C1和C2或C2和C3之间任选存在双键; R 2和R 3独立地选自-H，= O，= CH 2，-CN，-R，OR，卤素，= CH-R，O-SO 2 -R，CO 2 R和COR; R 6，R 7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 10是氨基甲酸酯基氮保护基，R 15是OR 11，其中R 11是氧保护基，或OH或R 10和R 15一起形成 N10和C11之间的双键; R“是C3-12亚烷基，该链可以被一个或多个杂原子和/或芳环中断，并且每个X独立地选自O，S或NH; R 2'，R 3' R 6，R 7，R 9'，R 10'和R 15'均独立地选自与R 2所定义的相同的列表， 3，R 6，R 7，R 9，R 10和R 15。

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