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21. 发明公开

EP1812004A1 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：EP1812004A1
公开(公告)日：2007-08-01
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.

22. 发明公开

EP1706385A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 有权
标题翻译：吡唑衍生物作为蛋白激酶的调节剂
公开(公告)号：EP1706385A1
公开(公告)日：2006-10-04
申请号：EP04806258.2
申请日：2004-12-23
申请人： Astex Therapeutics Limited , Cancer Research Technology Limited , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
发明人： BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
IPC分类号： C07D231/12 , C07D413/10 , C07D401/10 , A61K31/415 , A61P37/02
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds 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 Rl 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 inker 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 a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; Rl is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

24. 发明公开

EP2125805A1 SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY 审中-公开
标题翻译：蛋白激酶抑制效应取代的哌啶
公开(公告)号：EP2125805A1
公开(公告)日：2009-12-02
申请号：EP07848736.0
申请日：2007-12-20
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
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 CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N- C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, 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; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b 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 R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.

25. 发明公开

EP2037931A2 PHARMACEUTICAL COMBINATIONS OF PK INHIBITORS AND OTHER ACTIVE AGENTS 审中-公开
标题翻译： PK抑制剂和其他代理人的药物组合，
公开(公告)号：EP2037931A2
公开(公告)日：2009-03-25
申请号：EP07732540.5
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
发明人： THOMPSON, Neil, Thomas , LYONS, John, Francis , BOYLE, Robert, George , GRIMSHAW, Kyla, Merriom , GARRETT, Michelle, Dawn , COLLINS, Ian
IPC分类号： A61K31/52 , A61K45/06 , A61P35/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/52 , A61K31/5377 , A61K2300/00
摘要： The invention provides a combination for use as a protein kinase B inhibitor, the combination comprising (or consisting essentially of) an ancillary compound and: (I) a compound of the formula: or salts, solvates, tautomers or N-oxides thereof, wherein R1, Q1, Q2, E, G, T, R4, J1 and J2 are as defined in the claims; or (II) a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein R1, R2, R3, R4, E, A, T, J1 and J2 are as defined in the claims.

26. 发明公开

EP2013206A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP2013206A1
公开(公告)日：2009-01-14
申请号：EP07732554.6
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
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; Rla is an optionally substituted aryl or heteroaryl group; Rlb 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, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 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 CRZ; J1-J2 is selected from N=C(RZ), (RZ)C=N, (RZ)N-C(O), (RZ)2C-C(O), N=N and (RZ)C=C(R6); J4 -J3 is a group N=C(RZ) or a group (RZ)N-CO; and RZ 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，溶剂化物，互变异构体和N-氧化物; 其中TG选自组（1）和（2）：其中星号（*）表示基团E与基团X的连接点; R 1a是任选取代的芳基或杂芳基; R 1b是氢或基团R 1a; X是任选取代的具有8至12个环成员的双环杂环基团，其中至多5个是选自O，N和S的杂原子; 和A，E，R2，R3，R4，Q1和Q2如权利要求中所定义; 条件是当E是芳基或杂芳基时，则Q2不是键; 并进一步提供部分（a）不是基团（BG1）或（BG2）; 其中（BG1）和（BG2）各自任选被取代; T是N或CRZ; （RZ）C = N，（RZ）NC（O），（RZ）2C-C（O），N = N和（RZ）C = C（R 6））; J4-J3是基团N = C（RZ）或基团（RZ）N-CO; 并且RZ是氢或取代基。式（I）化合物具有PKA和PKB激酶抑制活性并可用于治疗癌症。

27. 发明公开

EP1812003A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：邻缩合吡啶和嘧啶衍生物（例如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：EP1812003A1
公开(公告)日：2007-08-01
申请号：EP05796842.2
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 , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , 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 , C07D473/00
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N=C(R6), (R7)C=N, (R8)N-C(O), (R8)2C-C(O), N=N or (R7)C=C(R6); A is an optionally substituted saturated C1-7 hydrocarbon 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, 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 CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4 alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents as defined in the claims.

28. 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。

29. 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。

30. 发明申请

WO2009103966A1 BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE 审中-公开
标题翻译：双氰胺 - 氨基化合物及其用途
公开(公告)号：WO2009103966A1
公开(公告)日：2009-08-27
申请号：PCT/GB2009/000438
申请日：2009-02-19
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , COLLINS, Ian , READER, John, Charles , WILLIAMS, David, Hugh , KLAIR, Sukhbinder, Singh , SCANLON, Jane, Elizabeth , PITON, Nelly , CHERRY, Michael
发明人： COLLINS, Ian , READER, John, Charles , WILLIAMS, David, Hugh , KLAIR, Sukhbinder, Singh , SCANLON, Jane, Elizabeth , PITON, Nelly , CHERRY, Michael
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D405/14 , C07D471/04 , A61K31/497
CPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA 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 II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation: (I).
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及下列通式的某些双环芳基 - 芳基胺化合物（本文称为BCAA化合物），其特别地抑制检测点激酶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的用途，以抑制CHK1激酶功能，以及治疗由CHK1介导的疾病和病症，即通过抑制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）电离辐射：（I）。

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