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1. 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。

2. 发明申请

WO2005085260A1 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2005085260A1
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000915
申请日：2005-03-09
申请人： SPIROGEN LIMITED , HOWARD, Philip Wilson , GREGSON, Stephen, John , TAYLOR, Peter William , THURSTON, David Edwin , HADJIVASSILEVA, Tsveta Stepanova
发明人： HOWARD, Philip Wilson , GREGSON, Stephen, John , TAYLOR, Peter William , THURSTON, David Edwin , HADJIVASSILEVA, Tsveta Stepanova
IPC分类号： C07D519/00
CPC分类号： C07D519/00 , Y02P20/55
摘要： A compound of formula (I) and salts and solvates thereof, wherein: R 10 is a nitrogen protecting group and R 11 is either OH or O-R 12 , wherein R 12 is an oxygen protecting group, or R 10 and R 11 together form a double bond between N10 and C11; and R 10 ' and R 11 ' are selected from the same options as R 10 and R 11 respectively.
摘要翻译：式（I）化合物及其盐和溶剂化物，其中：R 10是氮保护基，R 11是OH或OR 12，其中R 12是氧保护基，或 R 10和R 11一起形成N10和C11之间的双键; 和R 10'和R 11'分别选自与R 10和R 11相同的选择。

3. 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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