申请人:Nerviano Medical Sciences S.R.L.
公开号:US08207180B2
公开(公告)日:2012-06-26
The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.
本发明提供了式(I)或其药学上可接受的盐的三环吲哚和(4,5-二氢)吲哚,其中环A代表融合的吡唑、吡啶或嘧啶,表示单一或双重碳-碳键,而R1、R2和R3如规范中所定义。本发明的进一步目的是提供式(I)化合物的制备方法、包含它们的制药组合物以及治疗细胞增殖障碍的方法。事实上,式(I)化合物在治疗与蛋白激酶活性失调有关的疾病,特别是Cdc7和AKT激酶活性,如癌症方面是有用的。