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1. 发明申请

WO2004085421A3 BIOREDUCTIVELY-ACTIVATED PRODRUGS 审中-公开
标题翻译：生物活性物质
公开(公告)号：WO2004085421A3
公开(公告)日：2005-03-24
申请号：PCT/GB2004001330
申请日：2004-03-26
申请人： ANGIOGENE PHARM LTD , GRAY LAB CANCER RES TRUST , DAVIS PETER DAVID , NAYLOR MATTHEW ALEXANDER , THOMSON PETER , EVERETT STEVEN ALBERT , STRATFORD MICHAEL RICHARD LACE , WARDMAN PETER
发明人： DAVIS PETER DAVID , NAYLOR MATTHEW ALEXANDER , THOMSON PETER , EVERETT STEVEN ALBERT , STRATFORD MICHAEL RICHARD LACE , WARDMAN PETER
IPC分类号： A61K31/445 , C07D233/54 , C07D233/91 , C07D333/42 , C07D409/04 , C07D473/38 , C07D519/00 , C07D333/36 , C07D417/04
CPC分类号： C07D409/04 , A61K31/445 , C07D233/91 , C07D333/42 , C07D473/38
摘要： The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: Ar is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3) wherein R1, and R2, which may be the same or different are independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, aryl, COR3 or, together with the intervening carbon atom, form an optionally substituted heterocycloalkyl or carbocyclic ring ; L is -OC(O)- or -OP(O)(OR6)-; n is0or1;X is 0, S, NR7 or a single covalent bond; R3 is OR4 or NR4R5; R4, R5, R6 and R7 are each independently hydrogen or optionally substituted alkyl or, where Rr is NR4R5, R4 and R5 can be joined to form, together with the intervening nitrogen atom, a heterocycloalkyl ring; R8 is hydrogen, alkoxy or diatkylaminoalkyl; R9 is optionally substituted alkyl; R10 is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; R11 and R12 are independently hydrogen, alkyl, alkoxy, thioatkoxy, amino, alkylamino, dialkylamino, morpholino, piperidino,piperazino or l-aziridinyl; A is an optionally substituted aryl or heteroaryl ring; and Dr is a moiety such that DrXH represents a cytotoxic or cytostatic compound.
摘要翻译：本发明涉及式（1）化合物或其药学上可接受的盐，其中：Ar是具有至少一个硝基或叠氮基的取代的芳基或杂芳基，或者是式（2）或（3）的基团）其中可以相同或不同的R 1和R 2独立地是任选取代的烷基，任选取代的烯基，任选取代的炔基，芳基，COR 3或与中间碳原子一起形成任选取代的杂环烷基或碳环; L是-OC（O） - 或-OP（O）（OR 6） - ; n为0或1; X为0，S，NR 7或单个共价键; R3是OR4或NR4R5; R 4，R 5，R 6和R 7各自独立地为氢或任选取代的烷基，或其中R r为NR 4 R 5，可以连接R 4和R 5与杂环氮原子一起形成杂环烷基环; R8是氢，烷氧基或二烷基氨基烷基; R9是任选取代的烷基; R 10是氢，烷基，烷氧基或二烷基氨基烷基; R 11和R 12独立地是氢，烷基，烷氧基，硫代烷氧基，氨基，烷基氨基，二烷基氨基，吗啉代，哌啶子基，哌嗪基或1-氮杂环丁烷基; A是任选取代的芳基或杂芳基环; Dr是一个部分，使得DrXH代表细胞毒性或细胞抑制性化合物。

2. 发明申请

WO1997023456A1 INDOLOQUINONE DERIVATIVES AS BIOREDUCTIVE AGENTS 审中-公开
标题翻译：吲哚喹啉衍生物作为生物降解剂
公开(公告)号：WO1997023456A1
公开(公告)日：1997-07-03
申请号：PCT/GB1996003176
申请日：1996-12-20
申请人： BRITISH TECHNOLOGY GROUP LTD. , STRATFORD, Ian, James , NAYLOR, Matthew, Alexander , JAFFAR, Mohammed , ADAMS, Gerald, Edward
发明人： BRITISH TECHNOLOGY GROUP LTD.
IPC分类号： C07D209/42
CPC分类号： C07D209/12 , A61K31/404
摘要： Use of a compound of general formula (I) or salt thereof wherein R and R are independently selected from hydrogen, halogen and C1-6 alkyl or haloalkyl, C2-6 alkenyl or haloalkenyl, C1-6 alkoxy, phenoxy, C1-6 alkylthio, phenylthio, primary and secondary amino or hydroxy groups and R is hydrogen, hydroxy, a C1-6 alkyl or haloalkyl, C2-6 alkenyl or haloalkenyl or C1-6 alkoxy or haloalkoxy group is provided for the manufacture of a medicament for the treatment of neoplasms, particularly solid cancerous tumours characterised in that R is selected from a C1-6 alkyl or haloalkyl group, -CO2R where R is hydrogen or a C1-6 alkyl or haloalkyl group, or a group -CH2-X where X is selected from groups of formula -S-R , -O-R , and (a) where R is a hydrogen or a leaving group, the acid HR6 of which has a pKa of 10 or less and R and R are the same or different and are selected from C1-6 alkyl or haloalkyl or together with the interjacent nitrogen form a heterocyclic ring of 5 to 7 atoms optionally substituted by C1-4 alkyl or haloalkyl and R is selected from hydrogen, C1-4 alkyl and haloalkyl or groups-(CH2)nCHR R of more than four carbon atoms where n is an integer of 0 to 2 and R and R are independently selected from a C1-4 alkyl or haloalkyl group, or R and R together with the interjacent carbon atom form a C3-7 cycloalkyl or cycloalkenyl ring optionally substituted with one or more C1-4 alkyl or haloalkyl, or C2-4 alkenyl or haloalkenyl groups.
摘要翻译：使用通式（I）的化合物或其盐，其中R和R 4独立地选自氢，卤素和C 1-6烷基或卤代烷基，C 2-6烯基或卤代烯基，C 1-6烷氧基，苯氧基，C 1 -6烷硫基，苯硫基，伯和仲氨基或羟基，R 3为氢，羟基，C 1-6烷基或卤代烷基，C 2-6烯基或卤代链烯基或C 1-6烷氧基或卤代烷氧基，用于制备用于治疗肿瘤，特别是固体癌性肿瘤的药物，其特征在于R 1选自C 1-6烷基或卤代烷基，-CO 2 R 5，其中R 5是氢或C 1-6烷基或卤代烷基，或基团-CH 2 -X（其中X选自式-SR 6，-OR 6）和（a）其中R 6为氢或离去基团的基团，该酸 HR6的pKa为10以下，R 7和R 8相同或不同，选自C 1-6烷基或卤代烷基，或与中间的氮一起形成杂环任选被C 1-4烷基或卤代烷基取代的5至7个原子，R 2选自氢，C 1-4烷基和卤代烷基或多于四个碳原子的基团 - （CH 2）n CHR 9 R 10，其中 n为0〜2的整数，R 9和R 10独立地选自C 1-4烷基或卤代烷基，或R 9和R 10与中间碳原子一起形成C 3 -7环烷基或环烯基，任选被一个或多个C 1-4烷基或卤代烷基取代，或C 2-4链烯基或卤代烯基。

3. 发明申请

WO1993000900A1 1,2-DIHYDRO-8-PIPERAZINYL-4-PHENYLIMIDAZOPYRIDOPYRAZINE OXIDES AND 1,2-DIHYDRO-8-PIPERAZINYL-4 PHENYLIMIDAZOQUINOXALINE OXIDES USEFUL FOR TREATING TUMORS 审中-公开
标题翻译： 1,2-二羟基-8-哌嗪基-4-苯甲酰氨基吡啶氧化物和1,2-二羟基-8-哌嗪-4-基苯基氧杂环己烷氧化物有助于治疗肿瘤
公开(公告)号：WO1993000900A1
公开(公告)日：1993-01-21
申请号：PCT/GB1992001203
申请日：1992-07-03
申请人： BRITISH TECHNOLOGY GROUP LIMITED , ADAMS, Gerald, Edward , FIELDEN, Edward, Martin , NAYLOR, Matthew, Alexander , STRATFORD, Ian, James
发明人： BRITISH TECHNOLOGY GROUP LIMITED
IPC分类号： A61K31/495
CPC分类号： A61K31/495
摘要： 1,2-Dihydro-8-piperazinyl-4-phenylimidazopyridopyrazine oxides and 1,2-dihydro-8-piperazinyl-4-phenylimidazo quinoxaline oxides are useful in the treatment of cancer and in particular in the treatment of hypoxic tumours.

4. 发明申请

WO2004085361A1 BIOREDUCTIVELY ACTIVATED STILBENE PRODRUGS 审中-公开
标题翻译：生物活化的STILBENE PRODRUGS
公开(公告)号：WO2004085361A1
公开(公告)日：2004-10-07
申请号：PCT/GB2004/001341
申请日：2004-03-26
申请人： ANGIOGENE PHARMACEUTICALS LIMITED , GRAY LABORATORY CANCER RESEARCH TRUST , DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
发明人： DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
IPC分类号： C07C43/23
CPC分类号： C07D333/44 , C07D209/12
摘要： A compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein Ar is a substituted heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3); R1 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; R 2 is alkyl, alkoxy, thialkoxy or halo; R 3 , R 4 and R 5 are each independently alkyl, alkoxy, thialkoxy or halo with the proviso that at least two of R 3 , R 4 or R 5 are alkoxy; L is -OC(O)- or -OP(O)(OR 6 )-; n is 0 or 1; X is O, S or NR 7 ; Y is hydrogen, alkyl, alkoxy, thialkoxy, halo, hydroxy or dihydrogenphosphate; R 6 is hydrogen or alkyl; R 7 is hydrogen or alkyl; R 8 is hydrogen, alkoxy or dialkylaminoalkyl; R 9 is optionally substituted alkyl; R 10 is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; R 11 and R 12 are independently hydrogen, alkyl, alkoxy, thialkoxy, amono alkylamino, dialkylamino, morpholino, alkylmorpholino, piperidino, alkylpiperidiono, piperazino, alkylpiperazino or 1-aziridinyl; and A, together with the carbon atoms to which it is fused, is an optionally substituted aryl or heteroaryl ring.
摘要翻译：式（1）化合物或其药学上可接受的盐，其中Ar是带有至少一个硝基或叠氮基的取代杂芳基，或者是式（2）或（3）的基团。 R 1是氢，任选取代的烷基，任选取代的芳基或任选取代的杂芳基; R2是烷基，烷氧基，硫烷氧基或卤素; R3，R4和R5各自独立地是烷基，烷氧基，硫烷氧基或卤素，条件是R3，R4或R5中的至少两个是烷氧基; L是-OC（O） - 或-OP（O）（OR 6） - ; n为0或1; X是O，S或NR7; Y是氢，烷基，烷氧基，硫烷氧基，卤素，羟基或磷酸二氢酯; R6是氢或烷基; R7是氢或烷基; R8是氢，烷氧基或二烷基氨基烷基; R9是任选取代的烷基; R 10是氢，烷基，烷氧基或二烷基氨基烷基; R 11和R 12独立地是氢，烷基，烷氧基，硫烷氧基，氨基烷基氨基，二烷基氨基，吗啉代，烷基吗啉代，哌啶子基，烷基哌啶子基，哌嗪基，烷基哌嗪基或1-氮杂环丙烷基。和A与其稠合的碳原子一起是任选取代的芳基或杂芳基环。

5. 发明申请

WO2006032908A1 BIOREDUCTIVELY-ACTIVATED PRODRUGS 审中-公开
标题翻译：生物活化剂PRODRUGS
公开(公告)号：WO2006032908A1
公开(公告)日：2006-03-30
申请号：PCT/GB2005/003676
申请日：2005-09-26
申请人： ANGIOGENE PHARMACEUTICALS LIMITED , THE GRAY LABORATORY CANCER RESEARCH TRUST , DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
发明人： DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
IPC分类号： C07D493/04 , A61K31/381 , A61P35/00
CPC分类号： C07D493/04 , A61K31/381 , A61K45/06 , A61K2300/00
摘要： A compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: - Ar is a substituted heteroaryl group bearing at least one nitro or azido group or is a benzoquinone, naphthoquinone or fused heterocyloquinone; - R1 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; - R2 is a glycoside, OH, optionally substituted alkyl, optionally substituted alkoxy, C 2 -C 8 alkenyl, C 1 -C 8 hydroxyalkyl, optionally substituted arylamino, optionally substituted aryl C 1 -C 4 alkylamino or hydroxyalkylamino; and - R3 and R4 are each independently H or halo.
摘要翻译：式（1）化合物或其药学上可接受的盐，其中：-Ar是带有至少一个硝基或叠氮基的取代杂芳基，或者是苯醌，萘醌或稠合异链烷醌; R 1是氢，任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的环烷基，任选取代的杂环烷基，任选取代的芳基或任选取代的杂芳基; -R 2是糖苷，OH，任选取代的烷基，任选取代的烷氧基，C 2 -C 8烯基，C 1 -C 3 任选取代的芳基氨基，任选取代的芳基C 1 -C 4烷基氨基或羟烷基氨基; 且R 3和R 4各自独立地为H或卤素。

6. 发明申请

WO1993000904A1 DIHYDROPYRIMIDO-QUINOXALINES AND DIHYDROPYRIMIDO-PYRIDOPYRAZINES USEFUL FOR TREATING TUMOURS 审中-公开
标题翻译：用于治疗肿瘤的二羟基二咪喹啉和二羟基吡啶二吡咯烷酮
公开(公告)号：WO1993000904A1
公开(公告)日：1993-01-21
申请号：PCT/GB1992001204
申请日：1992-07-03
申请人： BRITISH TECHNOLOGY GROUP LIMITED , ADAMS, Gerald, Edward , FIELDEN, Edward, Martin , NAYLOR, Matthew, Alexander , STRATFORD, Ian, James
发明人： BRITISH TECHNOLOGY GROUP LIMITED
IPC分类号： A61K31/505
CPC分类号： A61K31/505
摘要： Dihydropyrimido-quinoxalines and dihydropyrimido-pyridopyrazines are useful in the treatment of cancer and in particular the treatment of hypoxic tumours.

7. 发明申请

WO2006032921A1 BIOREDUCTIVELY-ACTIVATED PRODRUGS 审中-公开
标题翻译：生物活性物质
公开(公告)号：WO2006032921A1
公开(公告)日：2006-03-30
申请号：PCT/GB2005/003697
申请日：2005-09-26
申请人： ANGIOGENE PHARMACEUTICALS LIMITED , THE GRAY LABORATORY CANCER RESEARCH TRUST , DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
发明人： DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , A61K31/7052 , A61P35/00
CPC分类号： C07H19/20 , C07H19/06 , C07H19/10 , C07H19/16
摘要： The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, Formula: (1); wherein: R1 is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is an optionally substituted benzoquinone, optionally substituted naphthoquinone or optionally substituted fused heterocycloquinone; R2 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, aryl or heteroaryl; and R3 is selected such that R3NH2 represents a cytotoxic nucleoside analogue or an ester or phosphate ester prodrug of a cytotoxic nucleoside analogue, with the proviso that if R1 is an aryl group then R2 is not H.
摘要翻译：本发明涉及式（1）化合物或其药学上可接受的盐，式（1）; 其中：R1是带有至少一个硝基或叠氮基的取代的芳基或杂芳基，或是任选取代的苯醌，任选取代的萘醌或任选取代的稠合杂环醌; R 2为H，任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的环烷基，任选取代的杂环烷基，芳基或杂芳基; 并且选择R3，使得R3NH2表示细胞毒性核苷类似物或细胞毒性核苷类似物的酯或磷酸酯前药，条件是如果R 1是芳基，则R 2不是H.

8. 发明申请

WO2004085421A2 BIOREDUCTIVELY-ACTIVATED PRODRUGS 审中-公开
标题翻译：生物活化剂PRODRUGS
公开(公告)号：WO2004085421A2
公开(公告)日：2004-10-07
申请号：PCT/GB2004/001330
申请日：2004-03-26
申请人： ANGIOGENE PHARMACEUTICALS LIMITED , GRAY LABORATORY CANCER RESEARCH TRUST , DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
发明人： DAVIS, Peter, David , NAYLOR, Matthew, Alexander , THOMSON, Peter , EVERETT, Steven, Albert , STRATFORD, Michael, Richard, Lacey , WARDMAN, Peter
IPC分类号： C07D333/36
CPC分类号： C07D409/04 , A61K31/445 , C07D233/91 , C07D333/42 , C07D473/38
摘要： The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: Ar is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is a group of formula (2) or (3) wherein R 1 , and R2, which may be the same or different are independently optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, aryl, COR 3 or, together with the intervening carbon atom, form an optionally substituted heterocycloalkyl or carbocyclic ring ; L is -OC(O)- or -OP(O)(OR 6 )-; n is0or1;X is 0, S, NR 7 or a single covalent bond; R 3 is OR 4 or NR 4 R 5 ; R 4 , R 5 , R 6 and R 7 are each independently hydrogen or optionally substituted alkyl or, where R r is NR 4 R 5, R 4 and R 5 can be joined to form, together with the intervening nitrogen atom, a heterocycloalkyl ring; R 8 is hydrogen, alkoxy or diatkylaminoalkyl; R 9 is optionally substituted alkyl; Rio is hydrogen, alkyl, alkoxy or dialkylaminoalkyl; R 11 and R12 are independently hydrogen, alkyl, alkoxy, thioatkoxy, amino, alkylamino, dialkylamino, morpholino, piperidino,piperazino or l=aziridinyl; A is an optionally substituted aryl or heteroaryl ring; and Dr is a moiety such that DrXH represents a cytotoxic or cytostatic compound.
摘要翻译：本发明涉及式（1）化合物或其药学上可接受的盐，其中：Ar是具有至少一个硝基或叠氮基的取代的芳基或杂芳基，或者是式（2）或（3）的基团）其中可以相同或不同的R 1和R 2独立地是任选取代的烷基，任选取代的烯基，任选取代的炔基，芳基，COR 3或与中间碳原子一起形成任选取代的杂环烷基或碳环; L是-OC（O） - 或-OP（O）（OR 6） - ; n为0或1; X为0，S，NR 7或单个共价键; R3是OR4或NR4R5; R 4，R 5，R 6和R 7各自独立地为氢或任选取代的烷基，或其中R r为NR 4 R 5，R 4和R 5可以与杂环氮原子一起形成杂环烷基环; R8是氢，烷氧基或二烷基氨基烷基; R9为任选取代的烷基; R 3为氢，烷基，烷氧基或二烷基氨基烷基; R 11和R 12独立地是氢，烷基，烷氧基，硫代烷氧基，氨基，烷基氨基，二烷基氨基，吗啉代，哌啶子基，哌嗪基或l =氮丙啶基; A是任选取代的芳基或杂芳基环; Dr是一个部分，使得DrXH代表细胞毒性或细胞抑制性化合物。

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