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1. 发明申请

WO2019152911A1 NOVEL SMALL MOLECULE DRUG CONJUGATES OF GEMCITABINE DERIVATIVES 审中-公开
公开(公告)号：WO2019152911A1
公开(公告)日：2019-08-08
申请号：PCT/US2019/016477
申请日：2019-02-04
申请人： EVERETT, Steven Albert , COBURN, Craig Alan
发明人： EVERETT, Steven Albert , COBURN, Craig Alan
IPC分类号： A61K47/54 , C07H19/10 , A61K31/7068 , A61P35/00
摘要： Disclosed are compounds having formula (I) or a pharmaceutically acceptable salt, ester, amide, solvate, or stereoisomer thereof, wherein L, Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 , Z 6 , and Effector are each as defined in the specification; compositions thereof; uses thereof; and methods of use thereof.

2. 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。

3. 发明申请

WO2019152955A1 SMALL MOLECULE DRUG CONJUGATES OF GEMCITABINE MONOPHOSPHATE 审中-公开
公开(公告)号：WO2019152955A1
公开(公告)日：2019-08-08
申请号：PCT/US2019/016557
申请日：2019-02-04
申请人： EVERETT, Steven Albert , COBURN, Craig Alan
发明人： EVERETT, Steven Albert , COBURN, Craig Alan
IPC分类号： A61K47/54 , C07H19/10 , A61K31/7068 , A61P35/00
CPC分类号： A61K47/545 , A61K31/7068 , A61P35/00 , C07H19/10 , G01N33/57484 , G01N2333/90245
摘要： Disclosed are compounds having formula (I): or a pharmaceutically acceptable salt, ester, amide, solvate, or stereoisomer thereof, wherein L, Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 , Z 6 are each as defined in the specification; compositions thereof; uses thereof; and methods of use thereof.

4. 发明申请

WO2010125350A1 TREATMENT OR PROPHYLAXIS OF PROLIFERATIVE CONDITIONS 审中-公开
标题翻译：治疗或预防性增生症状
公开(公告)号：WO2010125350A1
公开(公告)日：2010-11-04
申请号：PCT/GB2010/000860
申请日：2010-04-30
申请人： UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE , EVERETT, Steven, Albert , ULHAQ, Saraj
发明人： EVERETT, Steven, Albert , ULHAQ, Saraj
IPC分类号： A61K31/343 , A61K31/352 , A61K31/4184 , A61K31/428 , A61K31/664 , C07D307/80 , C07D311/16 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D417/12 , A61P35/00 , A61P9/10
CPC分类号： A61K47/545 , A61K31/343 , A61K31/352 , A61K31/37 , A61K31/381 , A61K31/4184 , A61K31/428 , A61K31/513 , A61K31/52 , A61K31/664 , A61K31/665 , C07D307/80 , C07D311/16 , C07D311/18 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D417/12 , C07D487/04 , C07D491/22
摘要： The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
摘要翻译：本发明涉及用于治疗或预防癌症和其它增殖性病症的新化合物，其特征在于表达细胞色素P450 1B1（CYP1B1）和其等位基因变体的细胞。本发明还提供药物组合物，其包含用于医学治疗的一种或多种这样的化合物，例如用于治疗癌症或其它增殖性疾病的预防，以及用于治疗人或非人动物患者中的癌症或其它病症的方法。本发明还提供了用于鉴定用于治疗预防癌症和其它增殖性病症的新化合物的方法，其特征在于表达CYP1B1的细胞及其等位变体。本发明还提供了确定本发明化合物治疗癌症的功效的方法。

5. 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。

6. 发明申请

WO2019152955A9 SMALL MOLECULE DRUG CONJUGATES OF GEMCITABINE MONOPHOSPHATE 审中-公开
公开(公告)号：WO2019152955A9
公开(公告)日：2019-08-08
申请号：PCT/US2019/016557
申请日：2019-02-04
申请人： EVERETT, Steven Albert , COBURN, Craig Alan
发明人： EVERETT, Steven Albert , COBURN, Craig Alan
IPC分类号： A61K47/54 , C07H19/10 , A61K31/7068 , A61P35/00
摘要： Disclosed are compounds having formula (I): or a pharmaceutically acceptable salt, ester, amide, solvate, or stereoisomer thereof, wherein L, Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 , Z 6 are each as defined in the specification; compositions thereof; uses thereof; and methods of use thereof.

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。

9. 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。

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