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8 条记录 (耗时 0.063 秒)

    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors
    1.
    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

    申请人： 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

    发明人： 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分类号： A61K31/52 ,  A61P35/00 ,  C07D473/34

    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 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.

    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 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。

    Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors
    8.
    发明申请
    Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors 审中-公开
    芳基烷基胺和杂芳基 - 烷基胺作为蛋白激酶抑制剂

    公开(公告)号：US20100210617A1

    公开(公告)日：2010-08-19

    申请号：US11993835

    申请日：2006-06-21

    申请人： Steven John Woodhead ,  Robert Downham ,  Christopher Hamlett ,  Steven Howard ,  Hannah Fiona Sore ,  Marinus Leendert Verdonk ,  David Winter Walker ,  Richard William Arthur Luke

    发明人： Steven John Woodhead ,  Robert Downham ,  Christopher Hamlett ,  Steven Howard ,  Hannah Fiona Sore ,  Marinus Leendert Verdonk ,  David Winter Walker ,  Richard William Arthur Luke

    IPC分类号： A61K31/4155 ,  C07D231/12 ,  C07D403/10 ,  C07D413/10 ,  C07D413/14 ,  C07D401/10 ,  A61K31/415 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/497 ,  A61K31/454 ,  A61P35/00

    CPC分类号： C07D231/12

    摘要： The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R25 is attached; and R4 and R5 each are hydrogen or a substituent as defined in the claims

    摘要翻译： 本发明提供式（II）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中n为0或1; Y1和Y2之一是CH，另一个选自CH，CR8和N; q为0,1或2，条件是当Y1或Y2为CR8时q为0或1; R 10芳环或5至10个环成员的杂芳基; R2a和R3a各自为氢，C1-4烃基或C1-4酰基，其中烃基和酰基部分任选被氟，羟基，氨基，甲基氨基，二甲基氨基或甲氧基取代; 或NR2aR3a形成任选含有选自O和N的第二杂原子环成员的咪唑基或饱和单环4-7元杂环基; R18是氢或甲基; R 19是氢或甲基; R 24是氢或R 24，R 2a，并且插入的氮原子和碳原子一起形成氮杂环丁烷，吡咯烷或哌啶环; R 25是氢或C 1-4烷基，其中C 1-4烷基任选被羟基或氨基取代，条件是羟基或氨基与R 25所连接的氧原子之间至少有两个碳原子; 且R 4和R 5各自为氢或如权利要求中所定义的取代基