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1. 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。

2. 发明申请

WO0100854A2 CHIMERIC PROTEINS MEDIATING TARGETED APOPTOSIS 审中-公开
标题翻译：嵌合蛋白介导靶向性凋亡
公开(公告)号：WO0100854A2
公开(公告)日：2001-01-04
申请号：PCT/GB0002449
申请日：2000-06-26
申请人： ANGIOGENE PHARM LTD , DAVIS PETER DAVID
发明人： DAVIS PETER DAVID
IPC分类号： A61K38/00 , C07K14/705 , C07K14/71 , C12N15/62 , A61K38/17 , C07K19/00
CPC分类号： C07K14/70585 , A61K38/00 , C07K14/70525 , C07K14/70578 , C07K14/71 , C07K2319/00
摘要： Chimeric cell-surface proteins are described which may be used in the selective induction of apoptosis in particular target cell types such as cancer cells in vivo or in vitro . Nucleic acid sequences encoding such proteins and methods of use relating to cancer and other therapies are provided.
摘要翻译：描述了嵌合细胞表面蛋白，其可用于在特定靶细胞类型如体内或体外的癌细胞中选择性诱导细胞凋亡。提供了编码这些蛋白质的核酸序列以及涉及癌症和其他疗法的使用方法。

3. 发明申请

WO1998018782A1 2-PYRIMIDINEAMINE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译： 2-吡啶胺胺衍生物及其制备方法
公开(公告)号：WO1998018782A1
公开(公告)日：1998-05-07
申请号：PCT/GB1997002949
申请日：1997-10-27
申请人： CELLTECH THERAPEUTICS LIMITED , DAVIS, Peter, David , MOFFAT, David, Festus, Charles , BATCHELOR, Mark, James , HUTCHINGS, Martin, Clive , PARRY, David, Mark
发明人： CELLTECH THERAPEUTICS LIMITED
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R is a hydrogen or halogen atom or a group -X -R where X is a direct bond or a linker atom or group, and R is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.
摘要翻译：描述通式（1）的化合物，其中：Ar是任选取代的芳基; R 2是氢或卤原子或基团-X 1 -R 2a，其中X 1是直接键或连接原子或基团，R 2a是任选取代的直链或支链烷基，烯基或炔基; R 3是任选取代的杂环烷基; 及其盐，溶剂合物，水合物和N-氧化物。化合物是选择性蛋白酪氨酸激酶抑制剂，特别是激酶ZAP-70和syk，并且可用于预防和治疗涉及不适当血小板活化的免疫或过敏性疾病和疾病。

4. 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.

5. 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。

6. 发明申请

WO0112579A3 NEW STILBENES WITH VASCULAR DAMAGING ACTIVITY 审中-公开
标题翻译：具有血管损伤活性的新型血栓
公开(公告)号：WO0112579A3
公开(公告)日：2001-10-11
申请号：PCT/GB0003067
申请日：2000-08-09
申请人： ANGIOGENE PHARM LTD , DAVIS PETER DAVID
发明人： DAVIS PETER DAVID
IPC分类号： A61K31/661 , A61K31/09 , A61K47/48 , A61P35/00 , C07C43/23 , C07F9/09 , C07F9/12
CPC分类号： C07C43/23 , A61K47/52 , C07F9/12
摘要： A group of novel cis-stilbenes as disclosed of formula (1) wherein: R , R and R are each independently alkyl, R is alkyl, haloalkyl, alkenyl, alkynyl, alkylthio, alkylsulphinyl, alkylsulphonyl or halo, R is hydrogen, alkoxy, alkyl, alkylthio, hydroxy or halo, or a pharmaceutically acceptable salt thereof or a prodrug such as a phosphate ester. These compounds have vascular damaging activity and are therefore potentially of value in treatment of diseases where reversal of neovascularisation may have therapeutic benefit.
摘要翻译：如式（1）所公开的一组新颖的顺式 - 均二苯乙烯，其中：R 1，R 2和R 3各自独立地为烷基，R 4为烷基，卤代烷基，烯基，炔基，烷硫基，烷基亚磺酰基，烷基磺酰基或卤素，R 5是氢，烷氧基，烷基，烷硫基，羟基或卤素，或其药学上可接受的盐或前体药物如磷酸酯。这些化合物具有血管损伤活性，因此可能在治疗新血管形成逆转可能具有治疗益处的疾病中具有价值。

7. 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。

8. 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。

9. 发明申请

WO2002087587A2 FUSED BICYCLIC AMINES 审中-公开
标题翻译：熔融双酚A
公开(公告)号：WO2002087587A2
公开(公告)日：2002-11-07
申请号：PCT/GB2002/002011
申请日：2002-05-02
申请人： CELLTECH R & D LIMITED , MOFFAT, David, Festus, Charles , BATCHELLOR, Mark, James , BROOKINGS, Daniel, Christopher , DAVIS, Peter, David
发明人： MOFFAT, David, Festus, Charles , BATCHELLOR, Mark, James , BROOKINGS, Daniel, Christopher , DAVIS, Peter, David
IPC分类号： A61K31/517
CPC分类号： C07D401/12 , C07D239/93 , C07D239/94 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： Compounds of formula (1) are described wherein Ar is an optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or alkyl group, X is a nitrogen atom or a C(R 1a ) group, n is zero or the integer 1 or 2 and R, R 1 , R 2 , R 3 and R 4 are substituents defined in the specification. The compounds are able to inhibit the activity of Class 1 receptor tyrosine kinases and are of use in the treatment of hyperproliferative disorders such as psoriasis.
摘要翻译：描述式（1）化合物，其中Ar是任选取代的芳基，杂芳基，芳烷基，杂芳烷基或烷基，X是氮原子或C（R 1a）基团，n是0或整数1或2 R 1，R 2，R 2，R 3和R 4是说明书中定义的取代基。该化合物能够抑制1类受体酪氨酸激酶的活性，并且可用于治疗过度增殖性疾病如牛皮癣。

10. 发明申请

WO1998028281A1 FUSED POLYCYCLIC 2-AMINOPYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：融合的多环式2-氨基吡啶衍生物，其制备及其作为蛋白酪氨酸激酶抑制剂的用途
公开(公告)号：WO1998028281A1
公开(公告)日：1998-07-02
申请号：PCT/GB1997003509
申请日：1997-12-22
申请人： CELLTECH THERAPEUTICS LIMITED , DAVIS, Jeremy, Martin , DAVIS, Peter, David , MOFFAT, David, Festus, Charles , BATCHELOR, Mark, James
发明人： CELLTECH THERAPEUTICS LIMITED
IPC分类号： C07D239/84
CPC分类号： C07D401/12 , C07D239/70 , C07D471/04 , C07D495/04
摘要： Fused polycyclic 2-aminopyrimidines of formula (1) wherein Ar is an optionally substituted aromatic or heteroaromatic group; X is a carbon or nitrogen atom; Y is a carbon or nitrogen atom; Z is a linker group; A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56 and p59 and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56 and/or p59 activity is believed to have a role.
摘要翻译：式（1）的稠合多环2-氨基嘧啶，其中Ar是任选取代的芳族或杂芳族基团; X是碳原子或氮原子; Y是碳或氮原子; Z是连接基团; A与X和Y一起形成任选取代的单环或双环芳族或杂芳基; 并描述了其盐，溶剂合物，水合物和N-氧化物。该化合物是蛋白酪氨酸激酶p56和p59 的有效和选择性抑制剂，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中不适当的p56 和/或p59 活动被认为有一个角色。

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