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1. 发明申请

WO2008075110A1 SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY 审中-公开
标题翻译：含有异烟酰胺或邻苯二酚的取代的哌啶
公开(公告)号：WO2008075110A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050777
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
IPC分类号： C07D487/04 , C07D473/34 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D473/34 , C07D487/04
摘要： The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R )x N * (GP1) (2) GP is a group GP2: 10 (R )r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims
摘要翻译：本发明提供具有式（I）的PKA和PKB激酶抑制化合物的式（I）化合物：GP 1 JT 2 JN 4 RNH（I）或其盐，溶剂合物，互变异构体或N-氧化物，其中（1） GP是组GP1：HET 2a a QG（HNCO）f 7（R）x N *（GP1）（2）GP是组GP2：10（R）r O 2a a QG（CH 2）w NVHN * ）其中HET是含有至多4个杂原子环成员的单环或双环杂环基; 环V是5至10个环成员的单环或双环杂芳基; 并且J1，J2，R4，R7，R10，Q2a，Ga，x，w和f如权利要求中所定义

2. 发明申请

WO2007125325A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125325A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001522
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00 , C07D473/34
摘要： The invention provides compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein J 1 -J 2 is CH=CH, N=CH, CH=N, HN-C(O) or CH 2 CO; T is N or CH and GP is as defined in the claims. The compounds have activity as inhibitors of PKA and PKB kinases and are useful in the treatment of cancers.
摘要翻译：本发明提供了式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中J 1是H，CH = CH，N = CH，CH = N，HN-C（O）或CH 2 CO; T是N或CH，GP如权利要求中所定义。该化合物具有作为PKA和PKB激酶抑制剂的活性，可用于治疗癌症。

3. 发明申请

WO2009044162A1 PYRAZIN-2-YL-PYRIDIN-2-YL-AMINE AND PYRAZIN-2-YL-PYRIMIDIN-4-YL-AMINE COMPOUNDS AND THEIR USE 审中-公开
标题翻译：吡嗪-2-基-L-吡啶-2-基胺和吡嗪-2-基-L-吡啶基-4-甲酰胺化合物及其用途
公开(公告)号：WO2009044162A1
公开(公告)日：2009-04-09
申请号：PCT/GB2008/003362
申请日：2008-10-06
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , COLLINS, Ian , READER, John, Charles , MATTHEWS, Thomas, Peter , CHEUNG, Kwai Ming , PROISY, Nicolas , WILLIAMS, David, Hugh , KLAIR, Sukhbinder, Singh , SCANLON, Jane, Elizabeth , PITON, Nelly , ADDISON, Glynn, Jonathan , CHERRY, Michael
发明人： COLLINS, Ian , READER, John, Charles , MATTHEWS, Thomas, Peter , CHEUNG, Kwai Ming , PROISY, Nicolas , WILLIAMS, David, Hugh , KLAIR, Sukhbinder, Singh , SCANLON, Jane, Elizabeth , PITON, Nelly , ADDISON, Glynn, Jonathan , CHERRY, Michael
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/497 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin- 2 - yl -pyridin- 2 -yl -amine and pyrazine - 2 - yl -pyrimidin- 4 - yl -amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1 ) kinase function The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1. that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or Il inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisiπq radiation. wherein: -X= is independently -CR A5 = or -N=; and the rest of the substituents are as specified in the claims.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及某些联芳基胺化合物（本文称为BAA化合物），特别是某些吡嗪-2-基 - 吡啶-2-基胺和吡嗪-2-基（I）的嘧啶-4-基 - 胺化合物，其特别是抑制检测点激酶1（CHK1）激酶功能。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物的用途，在体外和体内都抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症。通过抑制CHK1激酶功能等改善，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）ionisipq辐射。其中：-X =独立地是-CRA5 =或-N =; 并且其余的取代基如权利要求中所述。

4. 发明申请

WO2008075007A1 MORPHOLINO-SUBSTITUTED BICYCLOHETEROARYL COMPOUNDS AND THEIR USE AS ANTI CANCER AGENTS 审中-公开
标题翻译：吗啡取代的双环蛋白化合物及其作为抗癌剂的用途
公开(公告)号：WO2008075007A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004819
申请日：2007-12-14
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , COLLINS, Ian , READER, John, Charles , CHEUNG, Kwai, Ming , MATTHEWS, Thomas, Peter , PROISY, Nicolas , KLAIR, Sukhbinder, Singh
发明人： COLLINS, Ian , READER, John, Charles , CHEUNG, Kwai, Ming , MATTHEWS, Thomas, Peter , PROISY, Nicolas , KLAIR, Sukhbinder, Singh
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , A61K31/52 , A61K31/519 , A61K31/437 , A61P35/00 , A61P29/00
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： The present invention pertains generally to the field of therapeutic compounds, and mor specifically to certain morpholino-substituted bicydoheteroaryl compounds (referred to herein as MBHA compounds), of the following formula: and especially certain morpholino-substituted 7H- pyrrolo[2,3-dlpyrimidine and moφholino-substituted 1H-pyrazolo[3.4-b]pyridine compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or Il inhibitor, (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
摘要翻译：本发明一般涉及治疗化合物领域，具体涉及下列通式的某些吗啉代取代的双环杂芳基化合物（本文称为MBHA化合物），特别是某些吗啉代取代的7H-吡咯并[2,3- dl嘧啶和吗啉代取代的1H-吡唑并[3,4-b]吡啶化合物，其特别是抑制检测点激酶1（CHK1）激酶功能。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制CHK1激酶功能以及治疗由CHK1介导的疾病和病症的用途，其被改善通过抑制CHK1激酶功能等，包括增殖条件如癌症等，任选地与另一种试剂组合，例如（a）DNA拓扑异构酶I或II抑制剂，（b）DNA损伤剂; （c）抗代谢物或TS抑制剂; （d）微管靶向剂; 和（e）电离辐射。

5. 发明申请

WO2007125320A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125320A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001517
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESERARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , SAXTY, Gordon , VERDONK, Marinus, Leendert , CALDWELL, John , COLLINS, Ian , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
发明人： SAXTY, Gordon , VERDONK, Marinus, Leendert , CALDWELL, John , COLLINS, Ian , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
IPC分类号： C07D471/04 , C07D495/04 , C07D498/04 , A61K31/506 , A61P35/00
CPC分类号： C07D471/04 , C07D495/04
摘要： Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof; wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R la is an optionally substituted aryl or heteroaryl group; R lb is hydrogen or a group Rla; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R 2 , R 3 , R 4 , Q 1 and Q 2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BGl) and (BG2) are each optionally substituted; T is N or CR Z ; J 1 -J 2 is selected from N=C(R Z ), (R Z )C=N, (R Z )N-C(O), (R Z ) 2 C-C(O), N=N and (R Z )C=C(R 6 ); J 4 - J 3 is a group N=C(R Z ) or a group (R Z )N-CO; and R Z is hydrogen or a substituent. The compounds of the formula (I) have PKA and PKB kinase inhibiting activity and are useful in the treatment of cancers.
摘要翻译：式（I）化合物及其盐，溶剂合物，互变异构体和N-氧化物; 其中TG选自基团（1）和（2）：其中星号（*）表示基团E与基团X的连接点; R 1是任选取代的芳基或杂芳基; R 1b是氢或基团R 1a; X是具有8至12个环成员的任选取代的双环杂环基，其中多达5个是选自O，N和S的杂原子; 和A，E，R 2，R 3，R 4，Q 1和Q 2 如权利要求中所定义; 条件是当E是芳基或杂芳基时，则Q 2不是键; 并且进一步规定部分（a）不是基团（BG1）或（BG2）; 其中（BG1）和（BG2）各自任选被取代; T是N或CR Z; J <1> 1 2 选自N = C（R Z），（R Z）Z = NC（O），（R）Z CC（O），N = N和（R O） >ž）C = C（R ^{6 ）; J 3 - N 3是基团N = C（R Z）或基团（R Z），的N- CO; 并且R Z是氢或取代基。式（I）化合物具有PKA和PKB激酶抑制活性，可用于治疗癌症。}

6. 发明申请

WO2004072051A1 ISOXAZOLE COMPOUNDS AS INHIBITORS OF HEAT SHOCK PROTEINS 审中-公开
标题翻译：作为热休克蛋白的抑制剂的异噻唑化合物
公开(公告)号：WO2004072051A1
公开(公告)日：2004-08-26
申请号：PCT/GB2004/000506
申请日：2004-02-09
申请人： VERNALIS (CAMBRIDGE) LIMITED , CANCER RESEARCH TECHNOLOGY LTD , THE INSTITUTE OF CANCER RESEARCH , DRYSDALE, Martin, James , DYMOCK, Brian, William , FINCH, Harry , WEBB, Paul , MCDONALD, Edward , JAMES, Karen, Elizabeth , CHEUNG, Kwai, Ming , MATHEWS, Thomas, Peter
发明人： DRYSDALE, Martin, James , DYMOCK, Brian, William , FINCH, Harry , WEBB, Paul , MCDONALD, Edward , JAMES, Karen, Elizabeth , CHEUNG, Kwai, Ming , MATHEWS, Thomas, Peter
IPC分类号： C07D261/08
CPC分类号： A61K31/541 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D261/08 , C07D261/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D495/04
摘要： Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: (A), (B) wherein R 1 , is a group of formula (IA): -Ar 1 -(Alk 1 )p-(Z) r -(Alk 2 ) S -Q, wherein in any compatible combination Ar 1 is an optionally substituted aryl or heteroaryl radical, Alk 1 and Alk 2 are optionally substituted divalent C l -C 6 alkylene or C 2 -C 6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -(C=S)-, -SO 2 -, -C(=O)O-, -C(=O)NR A -, -C(=S)NR A -, - SO 2 NR A -, -NR A C(=O)-, -NR A SO 2 - or -NR A - wherein R A is hydrogen or C l -C 6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is (i) a group of formula (IA) above or (ii) a carboxamide radical; or (iii) a non aromatic carbocyclic or heterocyclic ring wherein a ring carbon is optionally substituted, and/or a ring nitrogen is optionally substituted by a group of formula -(Alk 1 )p-(Z) r -(Alk 2 ) s -Q wherein Q, Alk 1 , Alk 2 , Z, p, r and s are as defined above in relation to group (IA); and R 3 is hydrogen, optionally substituted cycloalkyl, cycloalkenyl, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, or C 1 -C 6 alkynyl; or a carboxyl, carboxamide, or carboxyl ester group.
摘要翻译：式（A）或（B）的异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症：（A），（B）其中R1是式（IA）的基团：-Ar 1 - （Alk 1）对 - （Z）r-（Alk 2）SQ，其中在任何相容的组合中，Ar 1是任选取代的芳基或杂芳基，Alk 1和Alk 2是任选取代的二价C 1 -C 6亚烷基或C 2 -C 6亚烯基，p，r和s独立地为0或1，Z为-O-，-S-， - （C = O） - ， - （C = S），-SO 2 - ， - C（= O）O-，-C（= O）NR A - ， - C（= S）NR A A - ， - SO 2 NR C（= O） - ， - NR A 2 - 或-NR A A - 其中R A A是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; R2是（i）上述式（IA）的基团或（ii）甲酰胺基团; 或（iii）非芳族碳环或杂环，其中环碳任选被取代，和/或环氮任选地被式 - （Alk 1）对 - （Z）r - （Alk < 其中Q，Alk 1，Alk 2，Z，p，r和s如上文关于组（IA）所定义; 并且R 3是氢，任选取代的环烷基，环烯基，C 1 -C 6烷基，C 1 -C 6烯基或C 1 -C 6炔基; 或羧基，羧酰胺或羧基酯基团。

7. 发明申请

WO2008075109A1 SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有蛋白激酶抑制活性的替代哌啶
公开(公告)号：WO2008075109A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050776
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
发明人： WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/52 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/34 , C07D519/00
摘要： The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N- C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); Q 3 is a bond or a saturated C 1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR 2 R 3 , CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R 1a and R 1b are the same or different and each is hydrogen or a substituent R 10 ; or R 1a and R 1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R 10 ; and R 2 , R 3 , R 4 , R 5 , R 7 , R 6 , R 8 , and R 10 are as defined in the claims.
摘要翻译：本发明提供了式（I）的PKA和PKB激酶抑制化合物; 或其盐，溶剂合物，互变异构体或N-氧化物，其中E是含有1,2,3或4个选自O，N和S的杂原子的五元杂芳基环，条件是不超过1个杂原子可以不是N; q和r各自为0或1; q + r为1或2; T是N或CR 5; J 1是N = C（R 6），（R 7）C = N，（R 8）N C（O），（R 8）2 CC（O），N = N或（R 0 > 7 ）C = C（R ^{6 ）; Q 3是任选被氟和羟基取代的键或饱和C 1-3烃连接基团; G是NR 2 R 3，CN或OH; m和n各自为0或1，条件是m + n为1或2，并且当环E的相邻环构件为S或O时，m或n各自为0; R 1a和R 1b相同或不同，各自为氢或取代基R 10; 或R 1a和R 1b与它们所连接的碳原子或杂原子一起形成5或6元芳基或杂芳基环，其中芳基或杂芳基环任选地被一个或多个取代基R 10取代; R 2，R 3，R 4，R 5，R 7， R 6，R 8和R 10如权利要求中所定义。}

8. 发明申请

WO2006079789A1 PYRIMIDOTHIOPHENE COMPOUNDS HAVING HSP90 INHIBITORY ACTIVITY 审中-公开
标题翻译：具有HSP90抑制活性的吡咯烷酮化合物
公开(公告)号：WO2006079789A1
公开(公告)日：2006-08-03
申请号：PCT/GB2006/000219
申请日：2006-01-23
申请人： VERNALIS R & D LTD , CANCER RESEARCH TECHNOLOGY LTD , THE INSTITUTE OF CANCER RESEARCH , MATTHEWS, Thomas, Peter , CHEUNG, Kwai, Ming , COLLINS, Ian , MCDONALD, Edward , BROUGH, Paul, Andrew , DRYSDALE, Martin, James
发明人： MATTHEWS, Thomas, Peter , CHEUNG, Kwai, Ming , COLLINS, Ian , MCDONALD, Edward , BROUGH, Paul, Andrew , DRYSDALE, Martin, James
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04
摘要： Compounds of formula (I) are HSP90 inhibitors, of utility in the treatment of, for example, cancers: wherein R 1 is -(Alk 1 ) p -(Z)r(Alk 2 ) s -Q wherein AIk 1 and AIk 2 are optionally substituted divalent C 1 C 3 alkylene or C 2 -C 3 alkenylene radicals, p, r and s are independently 0 or 1 , Z is -O-, -S-, -(C=O)-, -(C=S)-, -SO 2 -, -C(=O)O-, -C(=O)NR A , -C(=S)NRA-, -SO 2 NR A -NR A C(=O)-, -NR A SO 2 - or -NR A - wherein R A is hydrogen or C 1 -C 6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is optionally substituted aryl or heteroaryl; R 3 is hydrogen, an optional substituent, or an optionally substituted (C 1 -C- 6 )alkyl, aryl or heteroaryl radical; and R 4 is (i) a carboxylic ester, carboxamide or sulfonamide group, or (ii) a -CN group, or (iii) an optionally substituted C 1 -C 6 alkyl, aryl, heteroaryl, aryl(C 1 -C 6 alkyl)-, or heteroaryl(C 1 -C 6 alkyl)- group, or (iv) a group of formula -C(=O)R 5 wherein R 5 is hydroxyl, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C 1 -C 6 alkyl)-, aryl(C 1 -C 6 alkoxy)-, heteroaryl(C 1 -C 6 alkyl)-, or heteroaryl(C 1 -C- 6 alkoxy)-, or (v) a group of formula -C(=O)NHR 6 wherein R 6 is primary, secondary, tertiary or cyclic amino, or hydroxyl, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkyoxy, aryl, aryloxy, heteroaryl, heteroaryloxy, aryl(C 1 -C 6 alkyl)-, aryl(C 1 -C 6 alkoxy)-, heteroaryl(C 1 -C 6 alkyl)-, or heteroaryKC 1 -C 6 aikoxy)-.
摘要翻译：式（I）化合物是HSP90抑制剂，其可用于治疗例如癌症：其中R 1是 - （Alk 1）p < /（Z）r（Alk 2）其中Alk 1和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烷基，p，r和s 独立地是0或1，Z是-O - ， - S - ， - （C = O） - ， - （C = S） - ， - SO 2 - ， - C（= O） O-，-C（= O）NR A，-C（= S）NRA，-SO 2 NR A， C（= O） - ， - NR S - SO 2 - 或-NR A - 其中R 0 A是氢或C 1 -C 6烷基，Q是氢或任选取代的碳环或杂环基; R 2是任选取代的芳基或杂芳基; R 3是氢，任选的取代基或任选取代的（C 1 -C 6 -C 6 - ）烷基，芳基或杂芳基; 和R 4是（i）羧酸酯，羧酰胺或磺酰胺基，或（ii）-CN基，或（iii）任选取代的C 1 -C 烷基，芳基，杂芳基，芳基（C 1 -C 6 -C 6烷基） - 或杂芳基（C 1 -C 12 - -C（= O）R 5，其中R 5是（C 1 -C 6）烷基） - ，或（iv）式-C 羟基，任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基，芳基，芳氧基，杂芳基，杂芳氧基，芳基（C 1 -C 6烷基） - ，芳基（C 1 -C 6 - 烷氧基） - ，杂芳基（C 1 -C 6烷基） - 或杂芳基（C 1 -C 6 - 其中R 6为伯，仲，叔或环状氨基，或（v）式-C（= O）NHR 6基团，其中R 6为伯，仲，叔或环状氨基，或羟基，任选取代的C 1 -C 6烷基，C 1 -C 6烷氧基，芳基，芳氧基，杂芳基，杂芳氧基，芳基（C 1 -C 6烷基） - ，芳基（C ~~1 -C 6烷氧基） - ，杂芳基（C 1 -C 6烷基） - 或杂芳基K > 1 -C _{6 烷氧基） - 。}~~

9. 发明申请

WO2005000300A1 SUBSTITUTED 5-MEMBERED RING COMPOUNDS AND THEIR USE 审中-公开
标题翻译：取代的5元环化合物及其用途
公开(公告)号：WO2005000300A1
公开(公告)日：2005-01-06
申请号：PCT/GB2004/002755
申请日：2004-06-24
申请人： VERNALIS (CAMBRIDGE) LIMITED , CANCER RESEARCH TECHNOLOGY LTD. , THE INSTITUTE OF CANCER RESEARCH , CHEUNG, Kwai, Ming , DYMOCK, Brian, William , MACDONALD, Edward , DRYSDALE, Martin, James
发明人： CHEUNG, Kwai, Ming , DYMOCK, Brian, William , MACDONALD, Edward , DRYSDALE, Martin, James
IPC分类号： A61K31/427
CPC分类号： A61K31/4196 , A61K31/4192 , A61K31/427 , A61K31/433
摘要： Compound of a compound of formula (I) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R 1 R 2 R 3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor; or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie /CJD, Huntingdon's and Alzheimer's disease.
摘要翻译：式（I）化合物或其盐，N-氧化物，水合物或溶剂化物的化合物在制备抑制HSP90活性的组合物中的用途：其中环A是具有5个或更多个碳原子的芳族或非芳族碳环或杂环环原子，例如1,2,3-三唑基或1,2,4-三唑基或四唑基环; 和R1 R2 R3如本说明书中所定义的是HSP90的抑制剂，因此用于治疗例如癌症，病毒性疾病，炎性疾病如类风湿性关节炎，哮喘，多发性硬化，I型糖尿病，狼疮，牛皮癣和炎症性肠病; 囊性纤维化血管生成相关疾病如糖尿病性视网膜病变，血管瘤和子宫内膜异位症; 或用于保护正常细胞免受化疗诱导的毒性; 或未能进行凋亡的疾病是潜在的因素; 或由于心脏和脑中Hsp70的升高而保护缺氧缺血性损伤; 瘙痒病/ CJD，亨廷顿氏症和阿尔茨海默病。

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