Pyrazolobenzodiazepines
    5.
    发明授权
    Pyrazolobenzodiazepines 失效
    吡唑并苯并二氮杂

    公开(公告)号:US06440959B1

    公开(公告)日:2002-08-27

    申请号:US09548091

    申请日:2000-04-12

    IPC分类号: A61K31551

    CPC分类号: C07D487/04 C07D243/22

    摘要: Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.

    摘要翻译: 公开了具有下式的新的吡唑并苯并二氮杂类及其药学上可接受的盐,其中R 1,R 2,R 3和R 4如本文所定义。 这些化合物抑制细胞周期蛋白依赖性激酶(CDK),特别是CDK2。 这些化合物及其药学上可接受的盐和所述化合物的前药是可用于治疗或控制细胞增殖性疾病,特别是癌症的抗增殖剂,更特别地,治疗或控制乳腺癌,结肠癌,肺癌和前列腺肿瘤 。 还公开了含有式I化合物的药物组合物以及可用于制备式I化合物的中间体。

    Naphthostyrils
    7.
    发明授权
    Naphthostyrils 失效
    萘妥拉明

    公开(公告)号:US06531598B1

    公开(公告)日:2003-03-11

    申请号:US10224022

    申请日:2002-08-20

    IPC分类号: C07D41314

    摘要: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

    摘要翻译: 公开了新颖的式萘普通抗坏血酸的这些化合物抑制细胞周期蛋白依赖性激酶(CDK),特别是CDK2。 这些化合物及其药学上可接受的盐和酯是可用于治疗或控制细胞增殖性疾病,特别是癌症的抗增殖剂。 还公开了含有这些化合物的药物组合物,使用这种组合物治疗和/或预防癌症的方法,以及可用于制备式I化合物的中间体。

    4-alkenyl-and 4-alkynyloxindoles
    10.
    发明授权
    4-alkenyl-and 4-alkynyloxindoles 失效
    4-链烯基和4-炔氧基吲哚

    公开(公告)号:US06303793B1

    公开(公告)日:2001-10-16

    申请号:US09566054

    申请日:2000-05-05

    IPC分类号: C07D20934

    摘要: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.

    摘要翻译: 公开了具有下式的新的4-烯基 - 和4-炔基羟基吲哚及其药学上可接受的盐,其中R1,R2,R3,a,b和X如本文所定义。 这些化合物抑制细胞周期蛋白依赖性激酶(CDK),特别是CDK2。 这些化合物及其药学上可接受的盐和所述化合物的前药是用于治疗或控制细胞增殖性疾病,特别是癌症的抗增殖剂,更具体地,涉及乳腺癌和结肠肿瘤的治疗或控制。 还公开了含有式I和II化合物的药物组合物以及可用于制备式I和II化合物的中间体。