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1. 发明申请

US20100113425A1 PYRROLOBENZODIAZEPINES 有权
标题翻译： PYRROBOBENZODIAZEPINES
公开(公告)号：US20100113425A1
公开(公告)日：2010-05-06
申请号：US12610478
申请日：2009-11-02
申请人： Philip Wilson Howard , Zhizhi Chen , Stephen John Gregson
发明人： Philip Wilson Howard , Zhizhi Chen , Stephen John Gregson
IPC分类号： A61K31/551 , A61P35/02 , A61P35/00 , C07D487/04
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：式I化合物或其溶剂化物，其中：R2是任选取代的C5-20芳基; R 6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 7选自H，R，OH，OR，SH，SR，NH 2，NHR，NHRR'，硝基，Me 3 Sn和卤素; R“是C3-12亚烷基，该链可被一个或多个杂原子和/或芳环中断; X选自O，S或NH; z是2或3; M是一价药学上可接受的阳离子; R 2'，R 6'，R 7'，R 9'，X'和M'分别选自与R 2，R 6，R 7，R 9，X和M相同的基团，或M和M'可以一起表示二价药学上可接受的阳离子。

2. 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。

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. 发明授权

US07557099B2 Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂作为二聚细胞毒性吡咯并苯并二氮杂合成中的关键中间体
公开(公告)号：US07557099B2
公开(公告)日：2009-07-07
申请号：US10598482
申请日：2005-03-01
申请人： Philip Wilson Howard , Gyoung-Dong Kang
发明人： Philip Wilson Howard , Gyoung-Dong Kang
IPC分类号： C07D519/00 , C07D487/04 , A61K31/55
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; R2 and R3 are independently selected from —H, ═O, ═CH2, —CN, —R, OR, halo, ═CH—R, O—SO2—R, CO2R and COR; R10 is a carbamate-based nitrogen protecting group; and R11 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; R2和R3独立地选自-H，-O，-CH2，-CN，-R，OR，卤素，-CH-R，O-SO2-R，CO2R和COR; R10是氨基甲酸酯类氮保护基; R 11为氧保护基。

5. 发明授权

US07429658B2 Synthesis of protected pyrrolobenzodiazepines 有权
标题翻译：保护的吡咯并苯并二氮杂的合成
公开(公告)号：US07429658B2
公开(公告)日：2008-09-30
申请号：US10571274
申请日：2004-09-10
申请人： Philip Howard , Luke Masterson
发明人： Philip Howard , Luke Masterson
IPC分类号： C07D487/04 , C07D207/00 , C07C261/00
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：

6. 发明申请

US20070173497A1 11-Hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines 有权
标题翻译： 11-羟基-5H-吡咯并[2,1-c] [1,4]苯并二氮杂-5-酮衍生物作为制备c2取代的吡咯并苯并二氮杂的关键中间体
公开(公告)号：US20070173497A1
公开(公告)日：2007-07-26
申请号：US10598518
申请日：2005-03-01
申请人： Philip Howard , Stephen Gregson
发明人： Philip Howard , Stephen Gregson
IPC分类号： A61K31/54
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.
摘要翻译：本发明人已经开发了用于生产在C2位具有离去基团的C2取代的PBD的关键中间体，N10位的氨基甲酸酯保护基和C11位的被保护的羟基。在第一方面，本发明包括具有式（I）的化合物，其中：R 10是氨基甲酸酯基氮保护基; R 11是氧保护基; R 2是不稳定的离去基团。在另一方面，本发明包括由第一方面定义的式（I）化合物合成式（III）化合物或其溶剂化物的方法，其中R 16，是O-R 11，其中R 11如在第一方面中所定义，或OH或R 10和R 16一起形成 N10和C11之间的双键; 并且R 15是R.其它取代基在权利要求中限定。本发明的其它方面涉及式（III）的化合物（当R 10和R 16在N 10和C 11之间形成双键时，包括其溶剂合物，以及药物盐），包含它们的药物组合物及其在制备用于治疗增殖性疾病的药物中的用途。

7. 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。

8. 发明申请

US20110160192A1 BIARYL AMINO ACIDS AND THEIR USE IN DNA BINDING OLIGOMERS 审中-公开
标题翻译： BIARYL氨基酸及其在DNA结合寡聚体中的用途
公开(公告)号：US20110160192A1
公开(公告)日：2011-06-30
申请号：US13041849
申请日：2011-03-07
申请人： Philip Wilson Howard , Geoffrey Wells
发明人： Philip Wilson Howard , Geoffrey Wells
IPC分类号： A61K31/5517 , C07D417/12 , C07D405/14 , C07D403/12 , C07D407/12 , C07D417/14 , C07D401/14 , C07D409/14 , C07D487/04 , A61K31/427 , A61K31/4025 , A61K31/341 , A61K31/4439 , A61K31/4178 , A61P35/00
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 Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.
摘要翻译：式（I）化合物：Z'-CO-A-B-NH-Z（I）其中：Z为H或氨基保护基; Z'是OH，被保护或活化的羟基或Cl; A是任选取代的C 5-6亚芳基; B是任选取代的C 5-6亚芳基。

9. 发明授权

US07741319B2 11-hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines 有权
标题翻译： 11-羟基-5H-吡咯并[2,1-c] [1,4]苯并二氮杂-5-酮衍生物作为制备c2取代的吡咯并苯并二氮杂的关键中间体
公开(公告)号：US07741319B2
公开(公告)日：2010-06-22
申请号：US10598518
申请日：2005-03-01
申请人： Philip Wilson Howard , Stephen John Gregson
发明人： Philip Wilson Howard , Stephen John Gregson
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.
摘要翻译：本发明人已经开发了用于生产在C2位具有离去基团的C2取代的PBD的关键中间体，N10位的氨基甲酸酯保护基和C11位的被保护的羟基。在第一方面，本发明包括具有式（I）的化合物，其中：R 10是氨基甲酸酯基氮保护基; R11为氧保护基; R2是不稳定的离去组。在另一方面，本发明包括由第一方面定义的式（I）化合物合成式（III）化合物或其溶剂合物的方法，R 16为O-R 11，其中R 11 在第一方面中定义，或OH或R 10和R 16一起形成N10和C11之间的双键; R 15为R。其它取代基在权利要求中限定。本发明的其它方面涉及式（III）化合物（包括当R 10和R 16在N 10和C 11之间形成双键时的溶剂合物及其药用盐），包含它们的药物组合物及其在制备用于治疗增殖性疾病的药物。

10. 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。

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