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19 条记录 (耗时 0.035 秒)

    Pyrazolobenzodiazepines
    1.
    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

    申请人： Qingjie Ding ,  Jin-Jun Liu ,  Vincent Stewart Madison ,  Giacomo Pizzolato ,  Chung-Chen Wei ,  Peter Michael Wovkulich

    发明人： Qingjie Ding ,  Jin-Jun Liu ,  Vincent Stewart Madison ,  Giacomo Pizzolato ,  Chung-Chen Wei ,  Peter Michael Wovkulich

    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。

    2,6-diaminopyridine derivatives
    10.
    发明授权
    2,6-diaminopyridine derivatives 失效
    2,6-二氨基吡啶衍生物

    公开(公告)号：US07423051B2

    公开(公告)日：2008-09-09

    申请号：US11165912

    申请日：2005-06-24

    申请人： David Joseph Bartkovitz ,  Xin-Jie Chu ,  Allen John Lovey ,  Peter Michael Wovkulich

    发明人： David Joseph Bartkovitz ,  Xin-Jie Chu ,  Allen John Lovey ,  Peter Michael Wovkulich

    IPC分类号： A61K31/4545 ,  C07D401/12

    CPC分类号： C07D213/73

    摘要： Novel 2,6-diaminopyridine derivatives of formula wherein R1 and R2 are as defined below, are disclosed. These compounds inhibit cyclin-dependent kinases. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 2,6-diaminopyridine derivatives.

    摘要翻译： 公开了下述新的2,6-二氨基吡啶衍生物，其中R 1和R 2定义如下。 这些化合物抑制细胞周期蛋白依赖性激酶。 这些化合物及其药学上可接受的盐和酯具有抗增殖活性，并且可用于治疗或控制癌症，特别是实体瘤。 本发明还涉及含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是乳腺癌，肺癌，结肠癌和前列腺肿瘤的治疗或控制。 还公开了可用于制备这些新型2,6-二氨基吡啶衍生物的中间体。