Azaindole derivatives, process for their preparation, and their use as antitumor agents
    12.
    发明授权
    Azaindole derivatives, process for their preparation, and their use as antitumor agents 失效
    Azaindole衍生物,其制备方法及其作为抗肿瘤剂的用途

    公开(公告)号:US06486322B1

    公开(公告)日:2002-11-26

    申请号:US09968042

    申请日:2001-10-02

    CPC classification number: C07D471/04

    Abstract: Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I): wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR4, —(CH2)nNH2, —(CH2)nNHR4, —(CH2)nNHCOR4, —(CH2)nNHCONR4R5, —(CH2)nNHCOOR4, or —(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from —CONR4R5, —COOR4, —CONHOR4, —SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed. These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

    Abstract translation: 由式(I)表示的新颖的1H-吡咯并[2,3-b]吡啶:其中R是氢或卤素原子或选自-CN,-OH,-OCOR 4, - (CH 2)n NH 2, (CH2)nNHR4, - (CH2)nNHCOR4, - (CH2)nNHCONR4R5, - (CH2)nNHCOOR4或 - (CH2)nNHSO2R4,其中n为0或1,R4和R5如说明书所述; R1是氢或任选取代的烷基; R2是任选取代的选自烷基或芳基的基团; R3是氢或选自-CONR4R5,-COOR4,-CONHOR4,-SO2NHR4,烷基磺酰基氨基羰基或全氟化烷基磺酰基氨基羰基的基团; 或其药学上可接受的盐。这些化合物可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性病症。

    Novel Amino Pyrimidine Derivatives
    13.
    发明申请
    Novel Amino Pyrimidine Derivatives 审中-公开
    新型氨基嘧啶衍生物

    公开(公告)号:US20160235746A1

    公开(公告)日:2016-08-18

    申请号:US15135296

    申请日:2016-04-21

    Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.

    Abstract translation: 本发明描述了与Bruton酪氨酸激酶(Btk)相互作用的新的氨基嘧啶衍生物及其药学上可接受的盐。 因此,新的氨基嘧啶可能有效治疗自身免疫性疾病,炎性疾病,过敏性疾病,气道疾病如哮喘和慢性阻塞性肺疾病(COPD),移植排斥反应,癌症。 的造血起源或实体瘤。

    Azaindole derivatives, process for their preparation, and their use as antitumor agents
    18.
    发明授权
    Azaindole derivatives, process for their preparation, and their use as antitumor agents 失效
    Azaindole衍生物,其制备方法及其作为抗肿瘤剂的用途

    公开(公告)号:US06335342B1

    公开(公告)日:2002-01-01

    申请号:US09597274

    申请日:2000-06-19

    CPC classification number: C07D471/04

    Abstract: Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I): wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR4, —(CH2)nNH2, —(CH2)nNHR4, —(CH2)nNHCOR4, —(CH2)nNHCONR4R5, —(CH2)nNHCOOR4, or —(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from —CONR4R5, —COOR4, —CONHOR4, —SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed. These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

    Abstract translation: 由式(I)表示的新颖的1H-吡咯并[2,3-b]吡啶:其中R是氢或卤素原子或选自-CN,-OH,-OCOR 4, - (CH 2)n NH 2, (CH2)nNHR4, - (CH2)nNHCOR4, - (CH2)nNHCONR4R5, - (CH2)nNHCOOR4或 - (CH2)nNHSO2R4,其中n为0或1,R4和R5如说明书所述; R1是氢或任选取代的烷基; R2是任选取代的选自烷基或芳基的基团; R3是氢或选自-CONR4R5,-COOR4,-CONHOR4,-SO2NHR4,烷基磺酰基氨基羰基或全氟化烷基磺酰基氨基羰基的基团; 或其药学上可接受的盐。 这些化合物可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。

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