New 4-substituted derivatives of pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine and uses thereof

The present invention refers to 4-amino-substituted pyrazolo[3,4-d]pyrimidine derivatives, belonging to a new class of dual Src-Abl inhibitors, showing effects derived from targeting both Src (sarcoma) and Abl (Abelson) kinases. Such compounds proven to inhibit Src phosphorylation in a cell-free assay, thus significantly reducing the growth of human osteogenic sarcoma (SaOS-2) cells. They were also able to reduce bone resorption when used to treat mouse osteoclasts, without interfering with normal osteoblast growth. On the other hand by targeting Abl, they showed cytotoxic effects on Bcr (Breakpoint cluster region)-Abl-transduced cell lines (BaF3) resistant to Imatinib. The compounds of the invention have therapeutic applications in particular for bone related diseases and or chronic myeloid leukemia (CML).