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17 条记录 (耗时 0.076 秒)

    Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors
    4.
    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

    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors
    10.
    发明申请
    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors 有权
    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：US20090247538A1

    公开(公告)日：2009-10-01

    申请号：US11577963

    申请日：2005-10-25

    申请人： Valerio Berdini ,  Robert George Boyle ,  Gordon Saxty ,  David Winter Walker ,  Steven John Woodhead ,  Paul Graham Wyatt ,  Alastair Donald ,  John Caldwell ,  Ian Collins ,  Tatiana Faria Da Fonseca

    发明人： Valerio Berdini ,  Robert George Boyle ,  Gordon Saxty ,  David Winter Walker ,  Steven John Woodhead ,  Paul Graham Wyatt ,  Alastair Donald ,  John Caldwell ,  Ian Collins ,  Tatiana Faria Da Fonseca

    IPC分类号： A61K31/52 ,  C07D473/34 ,  C07D487/04 ,  A61K31/519 ,  C12N9/99 ,  C12Q1/48

    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 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); 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; Q1 is a bond or a saturated C1-3 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 CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 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 Q2 is other than a bond; G is hydrogen, NR2R, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.

    摘要翻译： 本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N-C（R6），（R7）C-N，（R8）N-C（O），（R8）2C-C（O），N-N或（R7）C-C（R6） 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; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R1或Q1的碳原子连接的C 1-4亚烷基链，形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2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Q2不是键; G为氢，NR2R，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢且G是NR 2 R 3时，则Q2是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。