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    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors
    13.
    发明申请
    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors 审中-公开
    正电子缩合吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂

    公开(公告)号：US20090099213A1

    公开(公告)日：2009-04-16

    申请号：US11577962

    申请日：2005-10-25

    Applicant: Valerio Berdini ,  Robert George Boyle ,  Gordon Saxty ,  Marinus Leendert Verdonk ,  Steven John Woodhead ,  Paul Graham Wyatt ,  Hannah Fiona Sore ,  John Caldwell ,  Ian Collins ,  Tatiana Faria Da Fonseca ,  Alastair Donald

    Inventor： Valerio Berdini ,  Robert George Boyle ,  Gordon Saxty ,  Marinus Leendert Verdonk ,  Steven John Woodhead ,  Paul Graham Wyatt ,  Hannah Fiona Sore ,  John Caldwell ,  Ian Collins ,  Tatiana Faria Da Fonseca ,  Alastair Donald

    IPC: A61K31/52 ,  A61P35/00 ,  C07D473/34

    CPC classification number: C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04

    Abstract: 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 C1-4alkyl; 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.

    Abstract translation: 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 CR5; J1-J2是N-C（R6），（R7）C-N，（R8）N-C（O），（R8）2C-C（O），N-N或（R7）C-C（R6） A是在R 1和NR 2 R 3之间延伸的最大链长度为5个原子并且在E和NR 2 R 3之间延伸的4个原子的最大链长度的任选取代的饱和C 1-7烃连接基团，连接基团中的一个碳原子是任选的 用氧或氮代替; E是单环或双环碳环或杂环基或非环基X-G，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; R1是氢或芳基或杂芳基; R2和R3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NR2R3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NR2R3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; 且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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