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11. 发明申请

WO2006136837A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006136837A2
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002297
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , THOMPSON, Neil, Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle, Dawn , LYONS, John, Francis , THOMPSON, Kyla, Merriom
发明人： THOMPSON, Neil, Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle, Dawn , LYONS, John, Francis , THOMPSON, Kyla, Merriom
CPC分类号： A61K45/06 , A61K31/415 , A61K31/454 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R 1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R 1 is an aryl or heteroaryl group; and R 2 , R 3 , R 4 and R 5 are as defined in the claims. Also provided are patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.
摘要翻译：本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团，在R 1和R 2之间延伸的最大链长为5个原子的连接基团和4个原子的最大链长度在E和NR 2 R 3之间延伸，其中连接基团中的一个碳原子可以任选被氧或氮原子取代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3 O 3的碳原子a时，组; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; R 2，R 3，R 4和R 5如权利要求中所定义。还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

12. 发明申请

WO2007125315A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125315A2
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001510
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , DAVIES, Thomas, Glanmor , GARRETT, Michelle, Dawn , BOYLE, Robert, George , COLLINS, Ian
发明人： DAVIES, Thomas, Glanmor , GARRETT, Michelle, Dawn , BOYLE, Robert, George , COLLINS, Ian
IPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , A61K31/407 , A61K31/4188
CPC分类号： C07D473/34 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The invention provides a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or 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 ); A is an optionally substituted saturated C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R 1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH 2 , O, S or NH and G is a C 1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R 1 is hydrogen or an aryl or heteroaryl group; R 2 and R 3 are each hydrogen, optionally substituted C 1-4 hydrocarbyl or optionally substituted C 1-4 acyl; or NR 2 R 3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR 2 R 3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C 1-4 alkyl; or NR 2 R 3 and the adjacent carbon atom of linker group A together form a cyano group; or R 1 , A and NR 2 R 3 together form a cyano group; and R 4 , R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen and various substituents as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated.
摘要翻译：本发明提供了具有式（I）的化合物：或其盐，溶剂化物，互变异构体或N-氧化物，其中T是N或CR 5; J 1 -J 2是N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7 ）C = C（R ^{6 ）; A是任选取代的饱和C 1-7烃连接基团，其具有5个原子的最大链长在R 1和NR 2 R之间延伸并且在E和NR 2 R 3 3之间延伸的最大链长度为4个原子，连接基团中的一个碳原子任选地被氧或氮取代; E为单环或双环碳环或杂环基团或无环基团XG，其中X为CH 2，O，S或NH且G为C 1-4亚烷基链其中一个碳原子任选被O，S或NH替代; R 1是氢或芳基或杂芳基; R 2和R 3分别为氢，任选取代的C 1-4烃基或任选取代的C 1-4烃基 >酰基; 或NR 2 R 3形成咪唑基或具有4-7个环成员的饱和单环杂环基; 或NR 2 R 3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4取代，烷基; 或NR 2 R 3和接头基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 和R 4，R 5，R 6，R 7和R 8各自独立地选自氢，各自独立地选自氢和权利要求中定义的各种取代基，其中所述化合物用于：（a）治疗或预防其中调节（例如抑制）ROCK激酶或蛋白激酶p70S6K 被指示; 和/或（b）治疗其中指示ROCK激酶或蛋白激酶p70S6K的调节（例如抑制）的受试者或患者群体。}

13. 发明申请

WO2006136821A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006136821A1
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002276
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , DAVIES, Thomas, Glanmor , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle, Dawn
发明人： DAVIES, Thomas, Glanmor , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle, Dawn
IPC分类号： C07D231/12 , C07D401/10 , C07D403/10 , C07D403/12 , C07D401/04 , C07D413/10 , A61K31/415 , A61K31/4155 , A61P35/00 , A61P9/00 , A61P3/00 , A61P29/00
CPC分类号： C07D401/14 , C07D231/12 , C07D401/04 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10
摘要： The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R 1 is an aryl or heteroaryl group; and R 2, R 3 , R 4 and R 5 are as defined in the claims.
摘要翻译：本发明提供具有ROCK激酶和/或蛋白激酶p70S6K抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团的最大链长度为5个原子延伸在R 1和NR 2 R 3之间，在E和NR 2 R 3之间延伸的4个原子的最大链长度其中连接基团中的一个碳原子可以任选被氧或氮原子取代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3 O 3的碳原子a时，组; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; 和R 2，R 3，R 4和R 5如权利要求中所定义。

14. 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。

15. 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。

16. 发明申请

WO2009053694A1 THERAPEUTIC OXY-PHENYL-ARYL COMPOUNDS AND THEIR USE 审中-公开
标题翻译：治疗性氧苯丙氨酸化合物及其用途
公开(公告)号：WO2009053694A1
公开(公告)日：2009-04-30
申请号：PCT/GB2008/003586
申请日：2008-10-23
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , COLLINS, Ian , CALDWELL, John, Jamieson , OLIVER, Antony, William , RAYNHAM, Tony, Michael , WELSH, Emma, Jane , MATIJSSEN, Cornelius, Albertus, Johannes
发明人： COLLINS, Ian , CALDWELL, John, Jamieson , OLIVER, Antony, William , RAYNHAM, Tony, Michael , WELSH, Emma, Jane , MATIJSSEN, Cornelius, Albertus, Johannes
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , A61K31/505 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia , inhibit Checkpoint Kinase 2 (CHK2) 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 CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II 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的领域，更具体地涉及本文所述的某些氧苯基芳基化合物（本文称为OPA化合物），其特别地抑制了检测点激酶2（CHK2）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的用途，以抑制CHK2激酶功能，以及用于治疗由CHK2介导的疾病和病症，即通过抑制CHK2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）电离辐射。

17. 发明公开

EP2029592A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP2029592A1
公开(公告)日：2009-03-04
申请号：EP07732559.5
申请日：2007-04-25
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Technology Limited , AstraZeneca AB
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 J1-J2 is CH=CH, N=CH, CH=N, HN-C(O) or CH2CO; 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.

18. 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） - 。}~~

19. 发明公开

EP1933832A2 PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：与吡衍生物作为蛋白激酶调节剂的药物组合
公开(公告)号：EP1933832A2
公开(公告)日：2008-06-25
申请号：EP06755597.9
申请日：2006-06-21
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Technology Limited
发明人： THOMPSON, Neil Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle Dawn , LYONS, John Francis , THOMPSON, Kyla Merriom
IPC分类号： A61K31/415 , A61K31/454 , A61P35/00 , A61P37/00
CPC分类号： A61K45/06 , A61K31/415 , A61K31/454 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.

20. 发明授权

EP1812004B1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 有权
标题翻译： ORTHO CONDENSED吡啶和PYRIDIMIDIN衍生物（例如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：EP1812004B1
公开(公告)日：2011-06-22
申请号：EP05797685.4
申请日：2005-10-25
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： BERDINI, Valerio , BOYLE, Robert George , SAXTY, Gordon , WALKER, David Winter , WOODHEAD, Steven John , WYATT, Paul Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana Faria , DONALD, Alastair
IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; Jl-J2 is N=C(R6), (R7)C=N, (R8)N-C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.

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