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    THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACIVITY OF CDK, GSK AND AURORA KYNASES
    4.
    发明申请
    THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACIVITY OF CDK, GSK AND AURORA KYNASES 审中-公开
    调节CDK，GSK和AURORA KYNASES的活性的噻唑和异噻唑衍生物

    公开(公告)号：WO2006070192A1

    公开(公告)日：2006-07-06

    申请号：PCT/GB2005/005089

    申请日：2005-12-30

    申请人： ASTEX THERAPEUTICS LIMITED ,  BERDINI, Valerio ,  O'BRIEN, Michael, Alistair ,  PHILLIPS, Theresa, Rachel ,  WYATT, Paul, Graham

    发明人： BERDINI, Valerio ,  O'BRIEN, Michael, Alistair ,  PHILLIPS, Theresa, Rachel ,  WYATT, Paul, Graham

    IPC分类号： C07D417/04 ,  C07D417/14 ,  A61K31/427 ,  A61P35/00

    CPC分类号： C07D417/14 ,  C07D417/04

    摘要： The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR 5 or N; each of Q 1 and Q 2 is a carbon atom; Q 3 is selected from S and CH; Q 4 is selected from CR 2 and S; provided that one of Q 3 and Q 4 is S and the other of Q 3 and Q 4 is not S; wherein when Q 3 is S, there is a double bond between Q 1 and Q 4 and a double bond between Q 2 and the adjacent ring nitrogen atom N; and when Q 4 is S, there is a double bond between Q 1 and Q 2 , and a double bond between Q 3 and the adjacent ring nitrogen atom N; A is a bond or -(CH 2 ) m -(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R 1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R ° is hydrogen or, together with NR g when present, forms a group -(CH 2 ) p - wherein p is 2 to 4; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, 0 and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is as defined in the claims.The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.

    摘要翻译： 本发明提供式（I）化合物或其盐，N-氧化物，互变异构体或溶剂合物，其中X为CR 5或N; Q 1和Q 2中的每一个是碳原子; Q 3和S 3选自S和CH; Q 4 选自CR 2和S; 只要Q 3和Q 4中的一个是S，Q 3和Q 4中的另一个不是 S; 其中当Q 3是S时，在Q 1和Q 2之间存在双键， / SUP>和相邻环氮原子N; 并且当Q 4是S时，Q 1和Q 2之间存在双键，并且Q 3 相邻环氮原子N; A是键或 - （CH 2）m - （B）n - B为C = O，NR（C = O）或O（C = O），其中R 1为氢或任选被羟基取代的C 1-4烃基或C

    PHARMACEUTICAL COMPOUNDS
    7.
    发明申请
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：WO2006008545A2

    公开(公告)日：2006-01-26

    申请号：PCT/GB2005/002888

    申请日：2005-07-22

    申请人： ASTEX THERAPEUTICS LIMITED ,  BERDINI, Valerio ,  EARLY, Theresa, Rachael ,  O'BRIEN, Michael, Alistair ,  WOODHEAD, Andrew, James ,  WYATT, Paul, Graham

    发明人： BERDINI, Valerio ,  EARLY, Theresa, Rachael ,  O'BRIEN, Michael, Alistair ,  WOODHEAD, Andrew, James ,  WYATT, Paul, Graham

    IPC分类号： A61K31/00

    CPC分类号： C07D275/03 ,  C07D277/56 ,  C07D417/12 ,  C07D417/14

    摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): (I) and salts, tautomers, N-oxides or solvates thereof; wherein A is a bond, C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; Q is S or CR 2 ; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R 1 to R 4 are as defined in the claims.

    摘要翻译： 本发明提供一种用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的化合物，具有式（I）：（I）的化合物及其盐，互变异构体，N-氧化物或溶剂合物; 其中A是键，C = O，NR（C = O）或O（C = O），其中R g是氢或C 1〜 任选被羟基或C 1-4烷氧基取代的烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; Q是S或CR <2>; J为S或CH; 假设Q和J中的一个是S，Q和J中的另一个不是S; 当Q是S时，环碳原子“a”和“b”之间有双键，环氮N与J之间有双键; 当J为S时，Q与环碳原子“a”之间存在双键，环氮N与环碳原子“b”之间具有双键。 和R 1至R 4如权利要求中所定义。