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41. 发明授权

EP1879901B1 PYRROLOBENZODIAZEPINES 有权
公开(公告)号：EP1879901B1
公开(公告)日：2009-12-23
申请号：EP06726846.6
申请日：2006-04-21
申请人： Spirogen Limited
发明人： GREGSON, Stephen J., University of London , CHEN, Zhizhi, University of London , HOWARD, Philip Wilson, University of London
IPC分类号： C07D519/00 , A61P35/00 , A61K31/5517
CPC分类号： C07D519/00

42. 发明授权

EP1727808B1 BIARYL AMINO ACIDS AND THEIR USE IN DNA BINDING OLIGOMERS 有权
标题翻译： BIARYLAMINOSÄUREN及其USE IN DNA结合的低聚物
公开(公告)号：EP1727808B1
公开(公告)日：2008-11-12
申请号：EP05717831.1
申请日：2005-03-01
申请人： Spirogen Limited
发明人： HOWARD, Philip, Wilson , WELLS, Geoffrey
IPC分类号： C07D277/56 , C07D307/68 , C07D213/73 , C07D333/38 , C07D207/34 , C07D233/90 , C07D487/04 , C07D417/12 , C07D417/14 , C07D405/14 , C07D409/14 , C07D403/14 , A61K31/427 , A61K31/4025
CPC分类号： C07D277/56 , C07D207/34 , C07D213/73 , C07D233/90 , C07D307/68 , C07D333/38 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D487/04 , Y02P20/55
摘要： Compounds of formula (I): Z’ -CO-A-B-NH-Z (I) wherein: Z is H or an amino protecting group; Z’ is OH, a protected or activated hydroxyl group or C1; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.

43. 发明公开

EP1755612A2 PYRROLOBENZODIAZEPINE THERAPEUTIC AGENTS USEFUL IN THE TREATMENT OF LEUKAEMIAS 有权
标题翻译：治疗Pyrrolobenzodiazepine治疗白血病
公开(公告)号：EP1755612A2
公开(公告)日：2007-02-28
申请号：EP05744802.9
申请日：2005-05-13
申请人： Spirogen Limited
发明人： PEPPER, Christopher John , THURSTON, David Edwin The School of Pharmacy
IPC分类号： A61K31/551 , A61K31/5517 , A61P35/02
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; R2 and R3 are independently selected from -H, =O, =CH2, -CN, -R, OR, halo, =CH-R, O-SO2-R, CO2R and COR; R6, R7 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', nitro, Me3Sn and halo; where R and R' are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 is a carbamate-based nitrogen protecting group and R15 is either O-R11, wherein R11 is an oxygen protecting group, or OH, or R10 and R15 together form a double bond between N10 and C11; R' is a C3-12 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; R2', R3', R6', R7', R9', R10' and R15' are all independently selected from the same lists as previously defined for R2, R3, R6, R7, R9, R10 and R15 respectively.

44. 发明公开

EP1727808A2 BIARYL AMINO ACIDS AND THEIR USE IN DNA BINDING OLIGOMERS 有权
标题翻译： BIARYLAMINOSÄUREN及其USE IN DNA结合的低聚物
公开(公告)号：EP1727808A2
公开(公告)日：2006-12-06
申请号：EP05717831.1
申请日：2005-03-01
申请人： Spirogen Limited
发明人： HOWARD, Philip, Wilson , WELLS, Geoffrey
IPC分类号： C07D277/56 , C07D307/68 , C07D213/73 , C07D333/38 , C07D207/34 , C07D233/90 , C07D487/04 , C07D417/12 , C07D417/14 , C07D405/14 , C07D409/14 , C07D403/14 , A61K31/427 , A61K31/4025
CPC分类号： C07D277/56 , C07D207/34 , C07D213/73 , C07D233/90 , C07D307/68 , C07D333/38 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D487/04 , Y02P20/55
摘要： Compounds of formula (I): Z’ -CO-A-B-NH-Z (I) wherein: Z is H or an amino protecting group; Z’ is OH, a protected or activated hydroxyl group or C1; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.

45. 发明公开

EP1193270A3 Pyrrolobenzodiazepines 有权
标题翻译： Pyrrolobenzodiazepine
公开(公告)号：EP1193270A3
公开(公告)日：2002-04-17
申请号：EP01129700.9
申请日：1999-08-27
申请人： Spirogen Limited
发明人： Thurston, David Edwin, School of Pharmacy , Howard, Philip Wilson, School of Pharmacy
IPC分类号： C07D487/04 , A61K31/551 , A61P31/00 , C07D519/00
CPC分类号： C07D487/04
摘要： Compounds of the formulae 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 R 2 is not CH=CH(CONH 2 ) or CH=CH(CONMe 2 ). 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具有式Ia或 Ib，其中R8基团单体形成具有式-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，该链可以被一个或更多的杂原子和/或芳环，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; 除了当A是单键时，在式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。

46. 发明公开

EP1931671A1 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 有权
标题翻译： 4- [4-（5-氧代2,3,5,11A四氢-5H-吡咯并[2,1-C] [1,4]苯并二氮杂-8-基氧基） - 丁酰基] -1H-吡咯-2- -CARBONSÄUREALKYLESTERDERIVATE及其复合增殖性疾病的治疗
公开(公告)号：EP1931671A1
公开(公告)日：2008-06-18
申请号：EP06794669.9
申请日：2006-10-05
申请人： Spirogen Limited
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; R2 is selected from -H, -OH, =0, =CH2, -CN, -R, OR, halo, =CH-R, O-SO2-R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', nitro, Me3Sn and halo, where R and R' are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and YRY, where Y is selected from O, S and NH and RY is H or C1-7 alkyl or H and SOxM, 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 RE is C1-4 alkyl. The compound is useful for the treatment of proliferative diseases.

47. 发明公开

EP1879901A1 PYRROLOBENZODIAZEPINES 有权
公开(公告)号：EP1879901A1
公开(公告)日：2008-01-23
申请号：EP06726846.6
申请日：2006-04-21
申请人： Spirogen Limited
发明人： GREGSON, Stephen J., University of London , CHEN, Zhizhi, University of London , HOWARD, Philip Wilson, University of London
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: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', nitro, Me3Sn and halo; where R and R' are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR', nitro, Me3Sn and halo; R' is a C3-12 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; R2', R6', R7', R9', X' and M' are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M' may together represent a divalent pharmaceutically acceptable cation.
摘要翻译：下式化合物或其溶剂化物：其中：R 2是任选取代的C 5-20芳基; R6和R9独立地选自H，R，OH，OR，SH，SR，NH2，NHR，NRR'，硝基，Me3Sn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; R7选自H，R，OH，OR，SH，SR，NH2，NHR，NHRR'，硝基，Me3Sn和卤素; R'为C3-12亚烷基，该链可以被一个或多个杂原子和/或芳环间隔; X选自O，S或NH; z是2或3; M是单价药学上可接受的阳离子; R2'，R6'，R7'，R9'，X'和M'分别选自与R2，R6，R7，R9，X和M相同的基团，或者M和M'可以一起表示二价药学上可接受的阳离子。

48. 发明公开

EP1723152A1 PYRROLOBENZODIAZEPINES 有权
公开(公告)号：EP1723152A1
公开(公告)日：2006-11-22
申请号：EP05717979.8
申请日：2005-03-09
申请人： Spirogen Limited
发明人： HOWARD, Philip Wilson , GREGSON, Stephen, John , TAYLOR, Peter William, School of Pharmacy , THURSTON, David Edwin , HADJIVASSILEVA, Tsveta Stepanova
IPC分类号： C07D519/00 , A61K31/5517 , A61P35/00 , A61P31/04 , C07D487/00
CPC分类号： C07D519/00 , Y02P20/55
摘要： A compound of formula (I) and salts and solvates thereof, wherein: R10 is a nitrogen protecting group and R11 is either OH or O-R12, wherein R12 is an oxygen protecting group, or R10 and R11 together form a double bond between N10 and C11; and R10' and R11' are selected from the same options as R10 and R11 respectively.
摘要翻译：式（I）化合物及其盐和溶剂合物，其中：R10为氮保护基，R11为OH或O-R12，其中R12为氧保护基，或R10和R11一起在N10之间形成双键和C11; 和R10'和R11'分别从与R10和R11相同的选项中选择。

49. 发明公开

EP1575955A1 PYRROLOBENZODIAZEPINES 有权
标题翻译： PYRROLOBENZODIAZEPINE用于治疗增生性疾病
公开(公告)号：EP1575955A1
公开(公告)日：2005-09-21
申请号：EP03773870.5
申请日：2003-11-14
申请人： Spirogen Limited
发明人： THURSTON, David EdwinSchool of Pharmacy , HOWARD, Philip WilsonSchool of Pharmacy
IPC分类号： C07D487/04 , A61K31/551 , A61P35/00
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 R2 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.

50. 发明授权

EP1109812B1 PYRROLOBENZODIAZEPINES 有权
标题翻译： PYRROLOBENZODIAZEPINE
公开(公告)号：EP1109812B1
公开(公告)日：2005-05-04
申请号：EP99943066.3
申请日：1999-08-27
申请人： Spirogen Limited
发明人： THURSTON, David Edwin, Cancer Res. Campaign , HOWARD, Philip Wilson
IPC分类号： 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.

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