申请人:——
公开号:US20040162303A1
公开(公告)日:2004-08-19
Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). 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 4-aminopyrimidine-5-one derivatives.
本发明揭示了新型4-氨基嘧啶-5-酮衍生物。这些化合物抑制细胞周期蛋白依赖性激酶,特别是细胞周期蛋白依赖性激酶4(Cdk4)。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制药组合物以及治疗或控制癌症的方法,尤其是乳腺、肺、结肠和前列腺肿瘤的治疗或控制。此外,还揭示了制备这些新型4-氨基嘧啶-5-酮衍生物的中间体。