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    CHEMICAL COMPOUNDS
    3.
    发明申请
    CHEMICAL COMPOUNDS 审中-公开
    化学化合物

    公开(公告)号：WO2003024967A2

    公开(公告)日：2003-03-27

    申请号：PCT/EP2002/011131

    申请日：2002-09-17

    Applicant: AVENTIS PHARMA S.A. ,  RATCLIFFE, Andrew, James ,  WALSH, Rodger, John, Aitchison ,  MAJID, Tahir, Nadeem ,  THURAIRATNAM, Sukanthini ,  AMENDOLA, Shelly ,  ALDOUS, David, John ,  SOUNESS, John, Edward ,  NEMECEK, Conception ,  WENTZLER, Sylvie ,  VENOT, Corinne

    Inventor： RATCLIFFE, Andrew, James ,  WALSH, Rodger, John, Aitchison ,  MAJID, Tahir, Nadeem ,  THURAIRATNAM, Sukanthini ,  AMENDOLA, Shelly ,  ALDOUS, David, John ,  SOUNESS, John, Edward ,  NEMECEK, Conception ,  WENTZLER, Sylvie ,  VENOT, Corinne

    IPC: C07D487/00

    CPC classification number: A61K31/495 ,  C07D487/04 ,  Y02A50/411

    Abstract: The present invention concerns compounds of general formula (I): in which: R1 represents hydrogen, R4, -C(=Y)-NHR4, -SO2NHR4, -C(=Z1)-R4, -SO2-R4 or -C(=Z1)-OR4; R2 represents hydrogen, cyano, halogen or -C°C-R5;R3 represents hydrogen, acyl, alkoxycarbonyl, alkyl, aroyl, aryl, aryloxycarbonyl, carboxy, cycloalkenyl, cycloalkyl, heteroaroyl, heteroaryl, heterocycloalkyl or -C(=O)-NY1Y2; R4 represents optionally substituted alkyl, cycloalkyl, cycloalkenyl ,heterocycloalkyl, aryl or heteroaryl R5 represents hydrogen or alkyl;R6 represents alkyl, acyl, alkoxycarbonyl, alkylsulfonyl, aryl, arylsulfonyl, aroyl, cycloalkyl, cycloalkenyl, heteroaryl, heteroarylsulfonyl, heteroaroyl and heterocycloalkyl;R7 represents optionally substituted alkyl, cycloalkyl or cycloalkylalkyl, R8 represents hydrogen, alkyl, alkenyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl;R9 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; R10 represents hydrogen or lower alkyl;R11 represents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; or alkyl optionally substituted by -NY1Y2;R12 represents aryl or heteroaryl; or alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl or heterocycloalkylalkyl each optionally substituted Y represents O, S or NCN;Y1 and Y2 (Y3 and Y4) are independently in particular hydrogen, alkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycloalkyl; or the group -NY1Y2 may form 5-7 membered ring or the group -NY3Y4 (-NY5Y6) may form a cyclic amine;Z (Z1)represents O or S; Z2 represents O or S(O)p;n is zero or an integer 1 or 2; m is 1 or 2;p is 1 or 2;and their corresponding N-oxides, their prodrugs; their pharmaceutically acceptable salts and solvates (e.g. hydrates), also together with one or more pharmaceutically acceptable carriers or excipients, such novel indolizines derivatives with inhibitory effects towards kinase proteins and especially for use for preventing or treating diseases that may be modulated by the inhibition of such kinase proteins and particularly solid tumours.

    Abstract translation: 本发明涉及通式（I）的化合物：其中：R1表示氢，R4，-C（= Y）-NHR4，-SO2NHR4，-C（= Z1）-R4，-SO2-R4或-C = Z1）-OR 4; R 2表示氢，氰基，卤素或-C≡C-R 5; R 3表示氢，酰基，烷氧基羰基，烷基，芳酰基，芳基，芳氧基羰基，羧基，环烯基，环烷基，杂芳酰基，杂芳基，杂环烷基或-C（= O） - NY1Y2; R 4表示任选取代的烷基，环烷基，环烯基，杂环烷基，芳基或杂芳基R 5表示氢或烷基; R 6表示烷基，酰基，烷氧基羰基，烷基磺酰基，芳基，芳基磺酰基，芳酰基，环烷基，环烯基，杂芳基，杂芳基磺酰基，杂芳酰基和杂环烷基; R 8代表烷基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烷基烷基; R 9代表任选取代的烷基，环烷基或环烷基烷基，R 8代表氢，烷基，烯基，芳基， R 10表示氢或低级烷基; R 11表示烷基，芳基，芳基烷基，环烷基，环烷基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烷基烷基; 或任选被-NY 1 Y 2取代的烷基; R 12表示芳基或杂芳基; 或任选被取代的Y代表O，S或NCN的烷基，环烷基，环烷基烷基，杂环烷基或杂环烷基烷基; Y 1和Y 2（Y 3和Y 4）独立地是氢，烷基，芳基，环烷基，环烯基，杂芳基或杂环烷基; 或-NY1Y2基可以形成5-7元环，或者-NY3Y4（-NY5Y6）可以形成环状胺; Z（Z1）表示O或S; Z2表示O或S（O）p; n为零或整数1或2; m为1或2; p为1或2;及其相应的N-氧化物，其前药; 其药学上可接受的盐和溶剂合物（例如水合物），还与一种或多种药学上可接受的载体或赋形剂一起，具有对激酶蛋白具有抑制作用的新型中氮茚衍生物，特别是用于预防或治疗可能受抑制作用 这种激酶蛋白，特别是实体瘤。

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