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1. 发明申请

WO2016166301A1 SITE-SPECIFIC ANTIBODY-DRUG CONJUGATES 审中-公开
标题翻译：站点特异性抗体药物联合
公开(公告)号：WO2016166301A1
公开(公告)日：2016-10-20
申请号：PCT/EP2016/058373
申请日：2016-04-15
申请人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson
发明人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson
IPC分类号： A61K47/48 , C07K16/00 , A61P35/00
CPC分类号： A61K47/6803 , A61K47/6867 , A61P35/00 , C07K16/2896 , Y02P20/55
摘要： Site-specific antibody-drug conjugates are described, in particular conjugates comprising pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker. The site of conjugation, along with modification of the antiobody moiety, allows for improved safety and efficacy of the ADC.
摘要翻译：描述了位点特异性抗体 - 药物偶联物，特别是包含具有接头形式的不稳定保护基的吡咯并苯并二氮杂（PBD）的缀合物。缀合位点以及抗体部分的修饰允许改善ADC的安全性和功效。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO2004068454A3 PIXEL STRUCTURE AND AN ASSOCIATED METHOD OF FABRICATING THE SAME 审中-公开
标题翻译：像素结构及其相关方法
公开(公告)号：WO2004068454A3
公开(公告)日：2005-03-24
申请号：PCT/US2004001067
申请日：2004-01-14
申请人： DRS SENSORS & TARGETING SYS , IONESCU ADRIAN C , HOWARD PHILIP EARL
发明人： IONESCU ADRIAN C , HOWARD PHILIP EARL
IPC分类号： G01J5/00 , G01J5/20 , G09G20060101 , G09G1/00 , H01L27/146 , H01L31/02
CPC分类号： H01L27/14669 , G01J5/20
摘要： A pixel structure (10), which forms one element of a focal plane array, includes a bolometer having a detector (20) and an insulator (14). The detector (20) is made from a material that absorbs incident thermal radiation and has an electrical resistance that varies in response to changes in the temperature of the material. The insulator (14) has a plurality of serpentine legs disposed completely underneath die detector (20) so that insulator (14) extends between the detector (20) and the substrate (12). And the insulator (14) supports the detector (20) in a spaced-apart relationship with respect to the substrate (12) to thermally isolate the detector (10) from the substrate (12). To further improve the performance of the bolometer, the bolometer includes a resonant layer (18) between the detector (10) and the insulator (14). The resonant layer is disposed such that areas defined between the detector (20) and the resonant layer (18), and between the resonant layer (18) and the insulator (14), form first and second resonant cavities, respectively.
摘要翻译：形成焦平面阵列的一个元件的像素结构（10）包括具有检测器（20）和绝缘体（14）的辐射热计。检测器（20）由吸收入射热辐射的材料制成，并具有响应材料温度变化而变化的电阻。绝缘体（14）具有完全设置在管芯检测器（20）下方的多个蛇形腿，使得绝缘体（14）在检测器（20）和衬底（12）之间延伸。并且绝缘体（14）相对于衬底（12）以间隔开的关系支撑检测器（20），以将检测器（10）与衬底（12）热隔离。为了进一步提高测辐射热谱仪的性能，测辐射热计包括在检测器（10）和绝缘体（14）之间的谐振层（18）。谐振层被设置成使得限定在检测器（20）和谐振层（18）之间以及谐振层（18）和绝缘体（14）之间的区域分别形成第一和第二谐振腔。

6. 发明申请

WO0012508B1 PYRROLBENZODIAZEPINES 审中-公开
公开(公告)号：WO0012508B1
公开(公告)日：2000-11-02
申请号：PCT/GB9902838
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , 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，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，每个单体相同或不同，并且具有式）或（Ib），其中所述单体的R8基团形成具有式-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; 不同之处在于当A为单键时，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。

7. 发明申请

WO0012508A3 PYRROLBENZODIAZEPINES 审中-公开
公开(公告)号：WO0012508A3
公开(公告)日：2000-09-21
申请号：PCT/GB9902838
申请日：1999-08-27
申请人： UNIV PORTSMOUTH , THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
发明人： THURSTON DAVID EDWIN , HOWARD PHILIP WILSON
IPC分类号： A61K31/5517 , A61P31/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , 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。

8. 发明申请

WO2016166304A1 SITE-SPECIFIC ANTIBODY-DRUG CONJUGATES 审中-公开
标题翻译：位点特异性抗体 - 药物偶联物
公开(公告)号：WO2016166304A1
公开(公告)日：2016-10-20
申请号：PCT/EP2016/058376
申请日：2016-04-15
申请人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson
发明人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson
IPC分类号： A61K47/48 , C07K16/00 , C07K16/28 , A61P35/00
CPC分类号： A61K47/6803 , A61K47/6867 , A61P35/00 , C07K16/2896 , Y02P20/55
摘要： Site-specific antibody-drug conjugates are described, in particular conjugates comprising pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker. The site of conjugation, along with modification of the antiobody moiety, allows for improved safety and efficacy of the ADC.
摘要翻译：描述了位点特异性抗体 - 药物缀合物，特别是包含具有接头形式的不稳定保护基的吡咯并苯并二氮杂（PBD）的缀合物。缀合位点，连同抗体部分的修饰，可以提高ADC的安全性和功效。

9. 发明申请

WO2016166302A1 HUMANIZED ANTI-AXL ANTIBODIES AND THEIR CONJUGATES 审中-公开
标题翻译：人类抗轴索抗体及其结合
公开(公告)号：WO2016166302A1
公开(公告)日：2016-10-20
申请号：PCT/EP2016/058374
申请日：2016-04-15
申请人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson , WILLIAMS, David G
发明人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson , WILLIAMS, David G
IPC分类号： A61K47/48 , A61P35/00 , C07K16/28
CPC分类号： C07K16/2863 , A61K47/6803 , A61K47/6851 , A61K47/6867 , A61P35/00 , C07K2317/24 , Y02P20/55
摘要： The present disclosure relates to humanized anti-Axl antibodies and conjugates thereof. Conjugates comprising pyrroiobenzodiazepines (PBDs) having a labile protecting group in the form of a linker to the antibody are described.
摘要翻译：本公开涉及人源化抗Ax1抗体及其缀合物。描述了包含具有与抗体接头形式的不稳定保护基的吡咯并苯并二氮杂（PBD）的缀合物。

10. 发明申请

WO2016166298A1 SITE-SPECIFIC ANTIBODY-DRUG CONJUGATES 审中-公开
标题翻译：站点特异性抗体药物联合
公开(公告)号：WO2016166298A1
公开(公告)日：2016-10-20
申请号：PCT/EP2016/058370
申请日：2016-04-15
申请人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson
发明人： VAN BERKEL, Patricius Hendrikus Cornelis , HOWARD, Philip Wilson
IPC分类号： A61K47/48 , A61P35/00 , C07K16/28
CPC分类号： A61K47/6803 , A61K47/6849 , A61P35/00 , C07K16/30 , Y02P20/55
摘要： Site-specific antibody-drug conjugates are described, in particular conjugates comprising an antibody that binds CD19 and which comprises an amino acid substitution of an interchain cysteine residue by an amino acid that is not cysteine, and pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker. The site of conjugation, along with modification of the antiobody moiety, allows for improved safety and efficacy of the ADC.
摘要翻译：本发明描述了特异性抗体 - 药物偶联物，特别是包含结合CD19的抗体的缀合物，其包含不是半胱氨酸的氨基酸的链间半胱氨酸残基的氨基酸取代和具有不稳定保护基的吡咯并苯并二氮杂（PBD）以接头的形式。缀合位点以及抗体部分的修饰允许改善ADC的安全性和功效。

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