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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

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.

3. 发明公开

EP1814552A2 COMPOUNDS FOR TREATING PROTEIN-KINASE MEDIATED DISORDERS 审中-公开
标题翻译：化合物用于治疗由蛋白激酶介导的疾病
公开(公告)号：EP1814552A2
公开(公告)日：2007-08-08
申请号：EP05801609.8
申请日：2005-11-09
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The 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 , WALKER, David Winter , CALDWELL, John , COLLINS, Ian
IPC分类号： A61K31/505 , A61P35/00 , C07D239/88 , C07D401/12 , C07D401/04 , C07D401/06 , C07D403/12
CPC分类号： C07D403/12 , A61K31/505 , C07D239/88 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J2-J1 is N=CR7 or R1aN-CO; G is OH or NR5R6; E is CONR7, NR7CO, C(R8)=C(R8) or (X)m(CR8R8a)n where X is O, S or NR7; provided that when J2-J1 is R1aN-CO, E is other than NR7CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R4 and R4a are absent, or A is a saturated optionally group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N.

4. 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.

5. 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。

6. 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。

7. 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。}

8. 发明申请

WO2007125321A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125321A2
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001518
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 , C07D473/34 , C07D487/04 , A61K31/4523 , A61K31/519 , A61K31/52
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
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.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中T为N或CR 5; J 1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 ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替，或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的部分; 并且其中连接基团Q 1的碳原子可以任选地具有一个或多个选自氟和羟基的取代基; Q 2是含有1至3个碳原子的键或饱和烃连接基团，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; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 3，R 4，R 6和R 8，如权利要求中所定义，其中所述化合物用于：（a）治疗或预防其中指示调节（例如抑制）ROCK激酶或蛋白激酶P70S6K的疾病或病症; 和/或（b）治疗其中指示调节（例如抑制）ROCK激酶或蛋白激酶P70S6K的受试者或患者群体。}

9. 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

10. 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。

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