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1. 发明申请

WO2006046024A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046024A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004119
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
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
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 CR 5 ; J l -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.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（I）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 >; 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 2，R 3，R 4，R 4， SUP＆gt;和R＆gt; 8如权利要求中所定义。}

2. 发明申请

WO2006046023A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046023A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004115
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , 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
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 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.
摘要翻译：本发明提供了一种用于预防或治疗由蛋白激酶B介导的疾病状态或病症的化合物，其具有式（I）：或其盐，溶剂合物，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 ）; 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所定义的各种取代基。}}

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