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1. 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.

2. 发明公开

EP1902032A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP1902032A1
公开(公告)日：2008-03-26
申请号：EP06755582.1
申请日：2006-06-21
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Campaign Technology Limited
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 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.
摘要翻译：本发明提供了具有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，连接基团具有5个原子的最大链长在R1和NR2R3之间以及在E和NR2R3之间延伸的4个原子的最大链长，其中接头基团中的一个碳原子可以任选地被氧或氮原子替代; 并且其中连接基团A的碳原子可以任选地带有一个或多个选自氧代，氟和羟基的取代基，条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α处，并且条件是当存在时，氧代基团相对于NR 2 R 3基团位于碳原子α处; E是单环或双环碳环或杂环基团; R1是芳基或杂芳基; R2，R3，R4和R5如权利要求中所定义。

3. 发明申请

WO2013171470A1 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-(TRIFLUOROMETHYL)-2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译： 5 - [[4 - [[MORPHOLIN-2-YL]甲基氨基] -5-（三氟甲基）-2-吡啶基]氨基]吡嗪-2-羰基酮及其治疗方法
公开(公告)号：WO2013171470A1
公开(公告)日：2013-11-21
申请号：PCT/GB2013/051233
申请日：2013-05-14
申请人： CANCER RESEARCH TECHNOLOGY LIMITED
发明人： COLLINS, Ian , MATTHEWS, Thomas Peter , FARIA DA FONSECA MCHARDY, Tatiana , OSBORNE, James , LAINCHBURY, Michael , WALTON, Michael Ian , GARRETT, Michelle Dawn
IPC分类号： C07D401/12 , A61K31/506 , A61P35/00
CPC分类号： C07D413/14 , A61K9/0053 , A61K31/4745 , A61K31/5377 , A61K31/7068 , A61K45/06 , C07D401/12
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5- (trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as "TFM 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 a thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; (e) ionising radiation; (f) an inhibitor of a mitosis regulator or a mitotic checkpoint regulator; (g) an inhibitor of a DNA damage signal transducer; or (h) an inhibitor of a DNA damage repair enzyme.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地，本发明涉及5 - [[4 - [[吗啉-2-基]甲基氨基] -5-（三氟甲基）-2-吡啶基]氨基]吡嗪-2-甲腈化合物（本文称为“TFM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）抗代谢物或胸苷酸合酶（TS）抑制剂; （d）微管靶向剂; （e）电离辐射; （f）有丝分裂调节剂或有丝分裂检查点调节剂的抑制剂; （g）DNA损伤信号传感器的抑制剂; 或（h）DNA损伤修复酶的抑制剂。

4. 发明公开

EP2016077A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP2016077A2
公开(公告)日：2009-01-21
申请号：EP07732548.8
申请日：2007-04-25
申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Campaign Technology Limited
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 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, 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; （R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C（R6）。 A是任选取代的饱和C1-7烃连接基团，其具有在R1和NR2R3之间延伸的5个原子的最大链长和在E和NR2R3之间延伸的4个原子的最大链长，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X-G，其中X为CH2，O，S或NH，G为C1-4亚烷基链，其中一个碳原子任选被O，S或NH替代; R1是氢或芳基或杂芳基; R2和R3各自为氢，任选取代的C1-4烃基或任选取代的C1-4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烷基取代; 或NR 2 R 3和接头基团A的相邻碳原子一起形成氰基; 或R1，A和NR2R3一起形成氰基; 和R4，R5，R6，R7和R8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）治疗或预防疾病或病症，其中调节指出了ROCK激酶或蛋白激酶p70S6K的抑制作用; 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。

5. 发明公开

EP3210980A1 PROCESS FOR MANUFACTURING 5-[[4-[[MORPHOLIN-2-YL]METHYLAMINO]-5-(TRIFLUOROMETHYL)- 2-PYRIDYL]AMINO]PYRAZINE-2-CARBONITRILE 有权转让
标题翻译：制备5 - [[4 - [[吗啉] -2-基]甲基氨基] -5-（三氟甲基）-2-吡啶基]氨基]吡嗪-2-碳腈
公开(公告)号：EP3210980A1
公开(公告)日：2017-08-30
申请号：EP17152400.2
申请日：2013-05-14
申请人： CANCER RESEARCH TECHNOLOGY LIMITED
发明人： COLLINS, Ian , MATTHEWS, Thomas Peter , FARIA DA FONSECA MCHARDY, Tatiana , OSBORNE, James , LAINCHBURY, Michael , WALTON, Michael Ian , GARRETT, Michelle Dawn
IPC分类号： C07D401/12 , A61K31/506 , A61P35/00 , C07D213/74
CPC分类号： C07D413/14 , A61K9/0053 , A61K31/4745 , A61K31/5377 , A61K31/7068 , A61K45/06 , C07D401/12
摘要： The present invention pertains generally to the field of therapeutic compounds.
More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as "TFM 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 a thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; (e) ionising radiation; (f) an inhibitor of a mitosis regulator or a mitotic checkpoint regulator; (g) an inhibitor of a DNA damage signal transducer; or (h) an inhibitor of a DNA damage repair enzyme.
摘要翻译：本发明一般涉及治疗性化合物领域。更具体地说，本发明涉及5 - [[4 - [[吗啉-2-基]甲氨基] -5-（三氟甲基）-2-吡啶基]氨基]吡嗪-2-甲腈化合物（本文称为“TFM化合物 “），其中尤其抑制关卡激酶1（CHK1）激酶功能。本发明还涉及包含此类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用于抑制CHK1激酶功能以及用于治疗由CHK1介导的疾病和病症的用途，所述疾病和病症是通过抑制CHK1激酶功能等（包括增殖性病症如癌症等），任选地与另一种药剂组合，例如（a）DNA拓扑异构酶I或II抑制剂; （b）DNA损伤剂; （c）抗代谢物或胸苷酸合酶（TS）抑制剂; （d）微管靶向剂; （e）电离辐射; （f）有丝分裂调节剂或有丝分裂检查点调节剂的抑制剂; （g）DNA损伤信号传感器的抑制剂; 或（h）DNA损伤修复酶的抑制剂。

6. 发明公开

EP3719018A1 PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 审中-实审
公开(公告)号：EP3719018A1
公开(公告)日：2020-10-07
申请号：EP19216213.9
申请日：2007-04-25
申请人： Astex Therapeutics Ltd , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited
发明人： DAVIES, Thomas Glanmor , GARRETT, Michelle Dawn , BOYLE, Robert George , COLLINS, Ian
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , A61K31/4523 , A61K31/519 , A61K31/52 , A61K31/522 , A61P35/00
摘要： The invention provides a compound of 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 ); 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; Q 1 is a bond or a saturated C 1-3 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 CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 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 α with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen;
R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are 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.

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