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51. 发明公开

EP1720881A1 11-HYDROXY-5H-PYRROLO[2,1-C][1,4]BENZODIAZEPIN-5-ONE DERIVATIVES AS KEY INTERMEDIATES FOR THE PREPARATION OF C2 SUBSTITUTED PYRROLOBENZODIAZEPINS 有权转让
标题翻译： 11-羟基-5H-吡咯并[2,1-C] [1,4]苯并二氮杂-5-酮衍生物作为用于制备C 2取代PYRROLOBENZODIAZEPINE关键中间体
公开(公告)号：EP1720881A1
公开(公告)日：2006-11-15
申请号：EP05717846.9
申请日：2005-03-01
申请人： Spirogen Limited
发明人： HOWARD, Philip Wilson , GREGSON, Stephen John
IPC分类号： C07D487/04 , C07D519/00 , A61K31/5517 , A61P35/00
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 : R10 is a carbamate-based nitrogen protecting group; R11 is an oxygen protecting group; and R2 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, R16 is either O-R11, wherein R11 is as defined in the first aspect, or OH, or R10 and R16 together form a double bond between N10 and C11; and R15 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 R10 and R16 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.

52. 发明公开

EP1720880A1 C8, C8' LINKED 5-OXO-1,2,3,11A-TETRAHYDRO-5H-PYRROLO[2,1-C][1,4]BENZODIAZEPINE DIMERS WITH 1H-PYRROLE-DICARBOXYLIC ACID AMIDE LINKERS AND OLIGOMERIC ANALOGS THEREOF AS WELL AS RELATED COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译： C8，C8“相关-5-氧代基-1,2,3,11a-四氢-5H-吡咯并[2,1-C] [1,4] WITH 1H-PYRROLDICARBONSÄUREAMIDLINKERN以及它们的低聚的类似物，以及用于治疗增殖相关化合物BENZODIAZEPINDIMERE 疾病
公开(公告)号：EP1720880A1
公开(公告)日：2006-11-15
申请号：EP05717845.1
申请日：2005-03-01
申请人： Spirogen Limited
发明人： HOWARD, Philip Wilson , GREGSON, Stephen John , TIBERGHIEN, Arnaud Charles
IPC分类号： C07D487/04 , C07D519/00 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I): PBD-A-Y-X- (Het)na-L- (Het)nb-L- (Het)nc-T- (Het')nd-L- (Het')ne-L- (Het')nf-X' -Y' -A' -PBD' and salts, solvates and chemically protected forms thereof, are disclosed wherein the PBD units have the formulae (PBD) (PBD') with the bonds at the 8 position on each molecule bond to the A and A' groups respectively ; A is selected from O, S, NH or a single bond , and each Het and Het' is respectively an amino-heteroarylene-carbonyl group ; X and X' are both either NH or C (=O) -Q-C (=O) - wherein Q is a divalent group such that HY = R ; in a second aspectm the invention comprises compounds of the general formula (II) : PBD-A-Y-X-(Het)ng-[L-(Het)nh] nj-X' -Y' -A' -PBD'. Wherein : PBD and PBD' are as defined above, X and X' are either NH and C(=O) respectively or C(O) and NH respectively ; the other substituents are defined in the claims. Further aspects of the present invention relate to their use in the manufacture of a medicament for the treatment of a proliferative disease.

53. 发明公开

EP1675857A2 PYRROLOBENZODIAZEPINE DERIVATIVES, COMPOSITIONS COMPRISING THE SAME AND METHODS RELATED THERETO 有权
标题翻译： PYRROLOBENZODIAZEPINDERIVATE，组成含以及任何相关程序
公开(公告)号：EP1675857A2
公开(公告)日：2006-07-05
申请号：EP04817338.9
申请日：2004-10-22
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , Spirogen Limited , STARKS ASSOCIATES, INC. , Midwest Research Institute
发明人： VISHNUVAJJALA, B., Rao , LIU, Paul, S. , SNADER, Kenneth, M. , THURSTON, David , HOWARD, Philip, W. , TURNER, Gregory , Hsiao, Luke.Y
IPC分类号： C07D487/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I) wherein X, Y, R1-R7, T1, T2, Z, and p are as described herein; a pharmaceutical composition comprising a compound of Formula (I) and a carrier; a method of inhibiting growth of a cell, which method comprises administering in an amount effective to inhibit growth a compound of Formula (I); a method of treating cancer in a mammal, which method comprises administering in an amount effective to treat cancer a compound of Formula (I); a method of treating a viral, parasitic, or bacterial infection of a cell, which method comprises administering in an amount effective to treat a viral, parasitic, or bacterial infection a compound of Formula (I); and a method of preparing a compound of Formula (I) as described herein.

54. 发明公开

EP1109812A2 PYRROLOBENZODIAZEPINES 有权
公开(公告)号：EP1109812A2
公开(公告)日：2001-06-27
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.
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。

55. 发明公开

EP1107970A2 COLLECTIONS OF COMPOUNDS 审中-公开
标题翻译：化合物的集合
公开(公告)号：EP1107970A2
公开(公告)日：2001-06-20
申请号：EP99941767.8
申请日：1999-08-27
申请人： Spirogen Limited
发明人： THURSTON, David Edwin,Cancer Research Campaign , HOWARD, Philip Wilson,Cancer Research Campaign
IPC分类号： C07D487/04
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。

56. 发明公开

EP1107969A2 COLLECTIONS OF COMPOUNDS 有权
标题翻译：化合物的集合
公开(公告)号：EP1107969A2
公开(公告)日：2001-06-20
申请号：EP99941765.2
申请日：1999-08-27
申请人： Spirogen Limited
发明人： THURSTON, David, EdwinCancer Research Campaign , HOWARD, Philip, WilsonUniversity of Portsmouth
IPC分类号： C07D487/04
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。

57. 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.

58. 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。

59. 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。

60. 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.

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