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    • 42. 发明授权
    • 4-alkenyl-and 4-alkynyloxindoles
    • 4-链烯基和4-炔氧基吲哚
    • US06303793B1
    • 2001-10-16
    • US09566054
    • 2000-05-05
    • Yi ChenApostolos DermatakisJin-Jun LiuKin-Chun Luk
    • Yi ChenApostolos DermatakisJin-Jun LiuKin-Chun Luk
    • C07D20934
    • C07D401/14C07D403/06C07D403/14C07D405/14C07D409/14
    • 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.
    • 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。