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    PHARMACEUTICAL COMPOUNDS
    3.
    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。

    PHARMACEUTICAL COMPOUNDS
    6.
    发明公开
    PHARMACEUTICAL COMPOUNDS 审中-公开
    药物化合物

    公开(公告)号：EP1968579A1

    公开(公告)日：2008-09-17

    申请号：EP06831505.0

    申请日：2006-12-29

    申请人： Astex Therapeutics Limited

    发明人： BERDINI, Valerio ,  CURRY, Jayne, Elizabeth ,  GALLAGHER, Neil, James ,  GILL, Adrian, Liam ,  LYONS, John, Francis

    IPC分类号： A61K31/4155 ,  A61K31/4184 ,  C07D403/04 ,  A61P35/00

    CPC分类号： C07D403/04 ,  A61K31/4155 ,  A61K31/4184 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/056 ,  C07D513/04

    摘要： The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDKl , Chk (e.g. Cbkl or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c)an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I’), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbBl), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I’) : or a salt, solvate, tautomer or N-oxide thereof; wherein R0’, R1, R1’, R2’, R3’, R4’, A’, X’, E, A and M are as defined in the claims.