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    PHARMACEUTICAL COMPOUNDS
    2.
    发明公开
    PHARMACEUTICAL COMPOUNDS 有权
    药物化合物

    公开(公告)号：EP1845973A1

    公开(公告)日：2007-10-24

    申请号：EP06700879.7

    申请日：2006-01-20

    申请人： Astex Therapeutics Limited

    发明人： CURRY, Jayne Elizabeth ,  LYONS, John Francis ,  SQUIRES, Matthew Simon ,  THOMPSON, Neil Thomas ,  THOMPSON, Kyla Merriom ,  WYATT, Paul Graham

    IPC分类号： A61K31/415 ,  A61K31/4155 ,  A61P35/00 ,  A61K31/4196 ,  A61K31/5685 ,  A61K31/135 ,  A61K31/565 ,  A61K31/4535 ,  A61K31/138 ,  A61K39/395 ,  A61K31/255 ,  A61K31/675 ,  A61K31/195 ,  A61K31/4188

    CPC分类号： A61K31/5685 ,  A61K31/135 ,  A61K31/138 ,  A61K31/195 ,  A61K31/255 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4188 ,  A61K31/4196 ,  A61K31/4535 ,  A61K31/565 ,  A61K31/675 ,  A61K39/395 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or 0(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 , 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

    摘要翻译： 本发明提供了辅助剂和具有式（0）的化合物的组合：或其盐或互变异构体或N-氧化物或溶剂合物; 其中所述辅助剂选自：单克隆抗体，烷化剂，抗癌剂，另外的CDK抑制剂和激素，激素激动剂，激素拮抗剂或激素调节剂; X是基团R1-A-NR4-或5-或6-元碳环或杂环; A是键，SO 2，C = O，NR 9（C = O）或O（C = O），其中R 9是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基和具有3至4个碳原子的杂环基团取代的取代基取代的C 1-8烃基 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团替代; R2是氢; 卤素; C 1-4烷氧基（例如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R3选自氢和具有3至12个环成员的碳环和杂环基团; 并且R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

    THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES
    4.
    发明公开
    THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
    作者CDK，GSK和Aurora激酶MODULLIERENDE噻唑和异噻唑酶活性的影响

    公开(公告)号：EP1836199A1

    公开(公告)日：2007-09-26

    申请号：EP05823660.5

    申请日：2005-12-30

    申请人： Astex Therapeutics Limited

    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 CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or -(CH2)m-(B)n-; B is C=O, NRg(C=O) or O(C=O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R° is hydrogen or, together with NRg when present, forms a group -(CH2)p- wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R3 and R4 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 R5 is hydrogen, a group R2 or a group R10 wherein R10 is as defined in the claims.The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.

    THIAZOLE AND ISOTHIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    5.
    发明公开
    THIAZOLE AND ISOTHIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
    噻唑和异噻唑ALS蛋白激酶抑制剂

    公开(公告)号：EP1781647A2

    公开(公告)日：2007-05-09

    申请号：EP05762253.2

    申请日：2005-07-22

    申请人： Astex Therapeutics Limited

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

    IPC分类号： C07D417/12

    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, NRg(C=O) or O(C=O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; Q is S or CR2; 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 R1 to R4 are as defined in the claims.