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1. 发明申请

US20040198722A1 Collections of compounds 审中-公开
标题翻译：化合物的集合
公开(公告)号：US20040198722A1
公开(公告)日：2004-10-07
申请号：US10824743
申请日：2004-04-15
申请人： Spirogen Limited
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： G01N033/53 , A61K031/551
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, nullO, nullCHnullR, nullCH2, CH2nullCO2R, CH2nullCO2H, CH2nullSO2R, OnullSO2R, 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: Hnull(T)nnullXnullYnullAnull where: X is CO, NH, S or O; T is a combinatorial unit; Y is a divalent group such that HYnullR; A is O, S, NH, or a single bond and n is a positive integer. 1
摘要翻译：式（I）化合物，其中：R2和R3独立地选自H，R，OH，OR，= O，= CH-R，= CH2，CH2-CO2R，CH2-CO2H，CH2-SO2R， SO2R，CO2R，COR和CN，C1和C2或C2和C3之间可以有双键; R 6，R 7，R 8和R 9独立地选自H，R，OH，OR，卤素，硝基，氨基，Me 3 Sn; 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：H-（T）n -X-Y-A-其中：X为CO，NH，S或O; T是组合单元; Y是二价基团，使得HY = R; A是O，S，NH或单键，n是正整数。

2. 发明申请

US20030195196A1 Pyrrolobenzodiazepines 审中-公开
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US20030195196A1
公开(公告)日：2003-10-16
申请号：US10379049
申请日：2003-03-04
申请人： Spirogen Limited
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： A61K031/551 , C07D487/04 , C07F007/22
CPC分类号： C07D487/04 , Y02P20/55
摘要： A compound with formula (I) 1 where R10 is a therapeutically removable nitrogen protecting group; R2 and R3 are independently selected from: H, R, OH, OR, nullO, nullCHnullR, nullCH2, CH2nullCO2R, CH2nullCO2H, CH2nullSO2R, OnullSO2nullR, 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 nullOnull(CH2)pnullOnull, 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 <下标10>是可治疗去除的氮保护基; R <下标> 2 和R <下标3 独立地选自：H，R，OH，OR，= O，= CH-R，= CH <下标2 ，CH <下标> 2 -CO <下标> 2 R，CH <下标> 2 -CO <下标> 2 H，CH < R，COR和CN;突出显示> -SO <下标> 2 R，O-SO <下标> 2 -R，CO < R <下标> 7 和R <下标> 9 独立地选自H，R，OH，OR，卤素，氨基，硝基，Me <下标 > 3 Sn; X是S，O或NH; R <下标> 11 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 <下标8 选自H，R，OH，OR，卤素，氨基，硝基，Me <下标3 Sn或R <下标7 和R 一起形成基团-O-（CH <下标> 2 ）<下标> p -O-，其中p是1或2.可以使用这样的化合物在ADEPT，GDEPT，NPEPT或PDT的方法中。

3. 发明申请

US20030120069A1 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US20030120069A1
公开(公告)日：2003-06-26
申请号：US10021213
申请日：2001-12-12
申请人： Spirogen Limited
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： A61K031/551 , C07D487/12
CPC分类号： C07D487/04
摘要： Compounds of the formulae Ia and Ib: 1 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 nullXnullRnullnullXnull linking the monomers, where Rnull 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 CHnullCH(CONH2) or CHnullCH(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，其各单体相同或不同并且具有式Ia或 Ib，其中R8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，该链可被一个或多个杂原子和/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。

4. 发明申请

US20040092736A1 Collections of compounds 有权
标题翻译：化合物的集合
公开(公告)号：US20040092736A1
公开(公告)日：2004-05-13
申请号：US10602521
申请日：2003-06-24
申请人： Spirogen Limited
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： C07D243/14 , G01N033/53
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; Xnull 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, nullO, nullCHnullR, nullCH2, CH2nullCO2R, CH2nullCO2H, CH2nullSO2R, OnullSO2R, 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 HYnullR, and other related compounds and collections of compounds. 1
摘要翻译：式（Ⅳ）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，COR，可选地是C1和C2或C2和C3之间的双键; R 6，R 7和R 9独立地选自H，R，OH，OR，卤素，硝基，氨基，Me 3 Sn; R11是H或R; Q为S，O或NH; R10为氮保护基; 并且Y是二价基团，使得HY = R，以及其它相关化合物和化合物的集合。

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

WO2005085259A2 PYRROLOBENZODIAZEPINES 审中-公开
公开(公告)号：WO2005085259A2
公开(公告)日：2005-09-15
申请号：PCT/GB2005/000770
申请日：2005-03-01
申请人： SPIROGEN LIMITED , HOWARD, Philip Wilson , KANG, Gyoung-Dong
发明人： HOWARD, Philip Wilson , KANG, Gyoung-Dong
IPC分类号： C07D519/00
CPC分类号： C07D487/04 , Y02P20/55
摘要： Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, 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 10 is a carbamate-based nitrogen protecting group; and R 11 is an oxygen protecting group.
摘要翻译：化合物和式（Ia）或（Ib）化合物的合成方法及其盐，溶剂合物和化学保护形式，其中虚线表示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 10是氨基甲酸酯基氮保护基; R 11为氧保护基。

7. 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。

8. 发明申请

WO2009060215A1 POLYAMIDES 审中-公开
标题翻译：聚酰胺的
公开(公告)号：WO2009060215A1
公开(公告)日：2009-05-14
申请号：PCT/GB2008/003767
申请日：2008-11-07
申请人： SPIROGEN LIMITED , HOWARD, Philip , MASTERSON, Luke
发明人： HOWARD, Philip , MASTERSON, Luke
IPC分类号： C07D417/12 , C07D233/90 , C07D403/12 , A61K31/4164 , A61P35/00
CPC分类号： C07D233/90 , C07D403/12 , C07D417/12
摘要： A polyamide moiety comprising at least one unit of formula I: -β 1 -X 1 -Y 1 -X 3 -X 4 -β 3 - (I) wherein: Y 1 is either X 2 -β 2 or β 2 -X 2 ; β 1 is -R β -CH 2 -NH- β a -, wherein β a is a β-alanine residue and R β is chosen from optionally substituted C 1-7 alkylene, C 1-7 alkenylene and C 1-7 alkynylene groups; β 2 and β 3 are β-alanine residues; and X 1 , X 2 , X 3 and X 4 are independently fragments of formula (II): wherein E is an optionally substituted C 5-6 heteroarylene group.
摘要翻译：包含至少一个式I的单元的聚酰胺部分：-β1-X1-Y1-X3-X4-β3-（Ⅰ）其中：Y1是X2-β2或β2-X2; ß1是-Rß-CH2-NH-ßa-，其中ßa是β-丙氨酸残基，Rβ选自任选取代的C 1-7亚烷基，C 1-7亚烯基和C 1-7亚炔基; ß2和ß3是β-丙氨酸残基; 并且X 1，X 2，X 3和X 4独立地是式（II）的片段：其中E是任选取代的C 5-6亚杂芳基。

9. 发明申请

WO2005023814A1 SYNTHESIS OF PROTECTED PYRROLOBENZODIAZEPINES 审中-公开
标题翻译：保护的吡咯烷酮的合成
公开(公告)号：WO2005023814A1
公开(公告)日：2005-03-17
申请号：PCT/GB2004/003873
申请日：2004-09-10
申请人： SPIROGEN LIMITED , HOWARD, Philip , MASTERSON, Luke
发明人： HOWARD, Philip , MASTERSON, Luke
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A method of synthesis of a N-10 protected PBD compound of formula (I) via an intermediate of formula (II) or formula (V).
摘要翻译：通过式（II）或式（V）的中间体合成式（I）的N-10保护的PBD化合物的方法。

10. 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。

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