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1. 发明申请

WO2006051290A3 COMPOUNDS FOR TREATING PROTEIN-KINASE MEDIATED DISORDERS 审中-公开
标题翻译：用于治疗蛋白激酶介导性疾病的化合物
公开(公告)号：WO2006051290A3
公开(公告)日：2006-09-14
申请号：PCT/GB2005004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , 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
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 , C07D401/04 , C07D401/06 , C07D401/12 , 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; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a 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.
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，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是在E和G之间延伸的最大链长为5个原子的饱和任选基团，一个碳连接基团A中的原子任选被O或N取代。

2. 发明申请

WO2007125310A2 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2007125310A2
公开(公告)日：2007-11-08
申请号：PCT/GB2007001502
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , THOMPSON NEIL THOMAS , LYONS JOHN FRANCIS , BOYLE ROBERT GEORGE , GRIMSHAW KYLA MERRIOM , GARRETT MICHELLE DAWN , COLLINS IAN
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 R 1 , Q 1 , Q 2 , E, G, T, R 4 , J 1 and J 2 are as defined in the claims; or (II) a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein R 1 , R 2 , R 3 , R 4 , E, A, T, J 1 and J 2 are as defined in the claims.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的组合，所述组合包含（或由其基本上由）辅助化合物组成，和：（I）下式化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中 R 1，Q 1，Q 2，E，G，T，R 4，J 4， 1＆lt; 2＆gt;和＆lt; 2＆gt;如权利要求中所定义; 或（II）具有式（I）的化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中R 1，R 2，R 2， 3，R 4，E，A，T，J 1和J 2如权利要求中所定义。

3. 发明申请

WO2006136837A3 PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：包含作为蛋白激酶调节剂的吡唑衍生物的药物组合
公开(公告)号：WO2006136837A3
公开(公告)日：2007-02-15
申请号：PCT/GB2006002297
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , 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
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 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 a with respect to the NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom a 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。

4. 发明申请

WO2007125321A3 PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：作为药物化合物的嘌呤和多巴林衍生物
公开(公告)号：WO2007125321A3
公开(公告)日：2007-12-27
申请号：PCT/GB2007001518
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , 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： A61K31/52 , A61K31/4523 , A61K31/519 , A61K31/522 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D471/04 , C07D473/34 , C07D487/04
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 a 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。}

5. 发明申请

WO2007125315A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125315A3
公开(公告)日：2007-12-27
申请号：PCT/GB2007001510
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , 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 , A61K31/407 , A61K31/4188 , A61P9/00 , A61P35/00 , A61P37/00 , C07D473/00 , C07D473/34 , C07D487/04
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：本发明提供具有式（I）的化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是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 ）; A是在R 1和R 2之间延伸的最大链长为5个原子的任选取代的饱和C 1 -C 7烃连接基团连接基团中的一个碳原子是任选的，并且在E和NR 2 R 3之间延伸的最大链长为4个原子用氧或氮代替; E是单环或双环碳环或杂环基或非环基XG，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链其中一个碳原子任选被O，S或NH取代; R 1是氢或芳基或杂芳基; R 2和R 3各自为氢，任选取代的C 1-4 - 烃基或任选取代的C 1-4 - >酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 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，烷基; 或NR 2 R 3和连接基团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的疾病或病症被指示和/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。}

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