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    SYNTHESIS AND SCREENING OF LIGANDS USING X-RAY CRYSTALLOGRAPHY
    4.
    发明授权
    SYNTHESIS AND SCREENING OF LIGANDS USING X-RAY CRYSTALLOGRAPHY 有权
    合成和筛选配体利用X射线晶体学

    公开(公告)号：EP1576375B1

    公开(公告)日：2007-02-14

    申请号：EP03782663.3

    申请日：2003-12-22

    申请人： Astex Therapeutics Limited

    发明人： JHOTI, Harren ,  CONGREVE, Miles, Stuart ,  O'REILLY, Marc ,  WYATT, Paul, Graham

    IPC分类号： G01N33/68

    CPC分类号： C40B30/04 ,  G01N23/20 ,  G01N33/6803

    摘要： A method for identifying a ligand of a target macromolecule is disclosed, comprising the steps of: soaking one or more crystals of the target macromolecule in a solution containing a collection of compounds generated in situ or separate from the crystal, where the solution has been prepared without the purification of the synthesized collection of compounds; obtaining an X-ray crystal diffraction pattern of the soaked macromolecule crystal; and using said X-ray crystal diffraction pattern to identify any compound bound to the macromolecule crystal, said compound being a ligand of the target macromolecule.

    PHARMACEUTICAL COMPOUNDS
    10.
    发明公开
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：EP2049516A2

    公开(公告)日：2009-04-22

    申请号：EP07766227.8

    申请日：2007-07-13

    申请人： Astex Therapeutics Limited ,  Novartis AG

    发明人： CONGREVE, Miles, Stuart ,  GILL, Adrian, Liam ,  HOWARD, Steven ,  MORTENSON, Paul, Neil ,  BESONG, Gilbert, Ebai

    IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D497/04 ,  A61K31/4155 ,  A61P35/00 ,  A61P31/10 ,  A61P31/12 ,  A61P37/00 ,  A61P25/28

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D401/14 ,  C07D513/04

    摘要： The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R1 is an optionally substituted monocyclic or bicyclic aryl or heteroaryl group containing 0-2 heteroatoms selected from O, N and S wherein the optional substituents are selected from halogen, C1-4 alkyl, C1-4 alkoxy, C3-4 cycloalkyl and cyano, and wherein the C1-4 alkyl and C1-4 alkoxy groups are each optionally further substituted by C1-2 alkoxy or one or more halogen atoms; and E is a group E1, E2, E3 or E4: formulae E1, E2, E3, E4 wherein n, q, A5 B, T, U, V, W, Z, R2, R5, R6 and R7 are as defined in the claims.

    摘要翻译： 本发明提供式（I）的细胞周期蛋白依赖性激酶（例如cdk-4激酶）抑制剂或其盐，互变异构体，溶剂化物或N-氧化物; 其中R 1为任选取代的含有0-2个选自O，N和S的杂原子的单环或双环芳基或杂芳基，其中任选取代基选自卤素，C 1-4烷基，C 1-4烷氧基，C 3-4环烷基和氰基 并且其中所述C 1-4烷基和C 1-4烷氧基各自任选进一步被C 1-2烷氧基或一个或多个卤素原子取代; 和E是基团E1，E2，E3或E4：式E1，E2，E3，E4其中n，q，A5 B，T，U，V，W，Z，R2，R5，R6和R7如 索赔。