申请人:Hoffmann-La Roche Inc.
公开号:US07423051B2
公开(公告)日:2008-09-09
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.
本发明揭示了公式中R1和R2如下所定义的新颖2,6-二氨基吡啶衍生物。这些化合物抑制细胞周期依赖性激酶。这些化合物及其药学上可接受的盐和酯具有抗增殖活性,并可用于治疗或控制癌症,尤其是实体肿瘤。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,尤其是乳腺癌、肺癌、结肠癌和前列腺肿瘤的治疗或控制。还揭示了在制备这些新颖的2,6-二氨基吡啶衍生物中有用的中间体。