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1. 发明授权

US07704924B2 Library of compounds comprising pyrrolobenzodiazepine moieties 有权
标题翻译：包含吡咯并苯并二氮杂部分的化合物文库
公开(公告)号：US07704924B2
公开(公告)日：2010-04-27
申请号：US10602521
申请日：2003-06-24
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： C40B40/10
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）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; R 2和R 3独立地选自：H，R，OH，OR，= O，= CH-R，= CH 2，CH 2 -CO 2 R，CH 2 -CO 2 H，CH 2 -SO 2 R，O-SO 2 R，CO 2 R，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是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。

2. 发明申请

US20080214525A1 Alkyl 4- [4- (5-Oxo-2,3,5, 11A-Tetrahydo-5H-Pyrrolo [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） - 丁酰氨基] -1H-吡咯 - 2-羧酸酯衍生物和相关化合物用于治疗增殖性疾病
公开(公告)号：US20080214525A1
公开(公告)日：2008-09-04
申请号：US12089459
申请日：2006-10-05
申请人： Philip Wilson Howard , David Edwin Thurston , Geoffrey Wells
发明人： Philip Wilson Howard , David Edwin Thurston , Geoffrey Wells
IPC分类号： A61K31/55 , C07D223/10 , A61P43/00
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 R 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.
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。

3. 发明授权

US07067511B2 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US07067511B2
公开(公告)日：2006-06-27
申请号：US10021213
申请日：2001-12-12
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： A61K31/55 , C07D487/00 , A61P35/00
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 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; R 2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; 和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，或化合物是每个单体相同或不同并且具有式Ia或Ib的二聚体，其中单体的R 8 C基团一起形成具有式-X-R'-X-连接的桥单体，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，以及每个X独立地选自O，S或N; 但是当A为单键时，在式Ia化合物中，R 2不为CH-CH（CONH 2 H）或CH-CH（CONH 2） 2 ）。还公开了其它相关化合物。

4. 发明授权

US06747144B1 Collections of compounds 失效
标题翻译：化合物的集合
公开(公告)号：US06747144B1
公开(公告)日：2004-06-08
申请号：US09763813
申请日：2001-02-26
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： C07D48704
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, ═O, ═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：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 ，O-SO 2 R，CO 2 R，COR和CN，并且任选地在C1和C2或C2和C3之间具有双键; 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

5. 发明授权

US08637664B2 Alkyl 4- [4- (5-oxo-2,3,5, 11a-tetrahydo-5H-pyrrolo [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） - 丁酰基氨基] -1H-吡咯 - 2-羧酸酯衍生物和相关化合物，用于治疗增殖性疾病
公开(公告)号：US08637664B2
公开(公告)日：2014-01-28
申请号：US12089459
申请日：2006-10-05
申请人： Philip Wilson Howard , David Edwin Thurston , Geoffrey Wells
发明人： Philip Wilson Howard , David Edwin Thurston , Geoffrey Wells
IPC分类号： C07D223/10 , A01N43/62 , A61K31/55
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 R 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.
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 2 -R，CO 2 R和COR; 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 C5-20芳基; R 10和R 11一起形成双键，或选自H和YRY，其中Y选自O，S和NH，R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; 和RE是C 1-4烷基。该化合物可用于治疗增殖性疾病。

6. 发明授权

US07407951B2 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US07407951B2
公开(公告)日：2008-08-05
申请号：US10534825
申请日：2003-11-14
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
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.
摘要翻译：公开了式（I）化合物：式（I）及其盐，溶剂合物，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。

7. 发明授权

US06909006B1 Cyclopropylindole derivatives 失效
标题翻译：环丙基吲哚衍生物
公开(公告)号：US06909006B1
公开(公告)日：2005-06-21
申请号：US10069202
申请日：2000-02-22
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： A61P43/00 , C07B61/00 , C07D209/60 , C07D209/96 , C07K1/04
CPC分类号： C07D209/96 , C07D209/60 , C07K1/047 , C40B40/00 , Y02P20/55
摘要： Compounds of formula (III) or (V), wherein is a solid support; L is a linking group or a single bond; T is a combinatorial unit; n is a positive integer, where if n is greater than 1, each T may be different: X is an electrophilic leaving group; Y is selected from NH-Prot, O-Prot, S-Prot, NO2, —NHOH. N3, NHR, NRR, N═NR, N(O)RR, NHSO2R, N═N═PhR, SR or SSR, where Prot represents a protecting group; A and B collectively represent a fused benzene or pyrrole ring (in either orientation), which is optionally substituted by up to respectively 4 or 2 groups independently selected from R, OH, OR, halo, nitro, amino, Me3Sn, CO2H, CO2R, R1 is a nitrogen protecting group, where if Y includes a protecting group, these protecting groups are orthogonal and R2 and R7 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn, and other related compounds and collections of compounds.
摘要翻译：式（III）或（V）的化合物，其中为固体载体; L是连接基团或单键; T是组合单元; n是正整数，其中如果n大于1，则每个T可以不同：X是亲电离去基团; Y选自NH-Prot，O-Prot，S-Prot，NO 2，-NHOH。 N，N，N，N，N，R，N-N-PhR，SR或SSR，其中Prot代表保护基; A和B共同表示稠合的苯或吡咯环（任一方向），其任选被至多独立地选自R，OH，OR，卤素，硝基，氨基，Me 3，其中如果Y包括保护基团，则其中R 1，R 2，R 2，R 2，R 1，R 2，这些保护基是正交的，R 2和R 7独立地选自H，R，OH，OR，卤素，硝基，氨基，Me 3， SUB> Sn和其他相关化合物和化合物的集合。

8. 发明授权

US06562806B1 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US06562806B1
公开(公告)日：2003-05-13
申请号：US09763814
申请日：2001-02-26
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： A61K31555
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。

9. 发明授权

US07528126B2 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US07528126B2
公开(公告)日：2009-05-05
申请号：US10598691
申请日：2005-03-09
申请人： Philip Wilson Howard , Stephen John Gregson , Peter William Taylor , David Edwin Thurston , Tsveta Stefanova Hadjivassileva
发明人： Philip Wilson Howard , Stephen John Gregson , Peter William Taylor , David Edwin Thurston , Tsveta Stefanova Hadjivassileva
IPC分类号： C07D519/00 , A61K31/5517
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）的化合物及其盐和溶剂合物，其中：R 10是氮保护基，R 11是OH或O-R 12，其中R 12是氧保护基，或R 10和R 11在N 10之间一起形成双键和C11; R10'和R11'分别选自与R10和R11相同的选项。

10. 发明授权

US07265105B2 Pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂卓
公开(公告)号：US07265105B2
公开(公告)日：2007-09-04
申请号：US11367241
申请日：2006-03-02
申请人： David Edwin Thurston , Philip Wilson Howard
发明人： David Edwin Thurston , Philip Wilson Howard
IPC分类号： A61P35/00 , A61K31/55 , C07D487/00
CPC分类号： C07D487/04
摘要： A compound of the formula II: wherein: R′2 is CHR″2, where R″2 is H. R6 and R9 are H and R7 is OMe and the compound is a dimer with each monomer being the same and being of formula II, where the R8 groups of the monomers form together a bridge having the formula —O—(CH2)p—O—, where p is 5, linking the monomers.
摘要翻译：式II的化合物：其中：R'2是CHR“2，其中R”2是H.R _{6和R 9是H，R 7是OMe，并且化合物是每个单体相同并且是式II的二聚体，其中单体的R 8基团一起形成具有式-O-（CH 2 CH 2）p -O-的桥，其中p为5 ，连接单体。}

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