7-Amino-pyrazolo[1,5-a]pyrimidine derivatives as cyclin dependent kinase inhibitors

摘要

Disclosed are specific 7-amino-pyrazolo[1,5-a]pyrimidine compounds as represented by the general formula (I), wherein R2 is a group such as alkyl, cycloalkyl, or bromo; R3 is a group such as phenyl, an alkylamino group, or a nitrogen linked heterocycle; R4 is hydrogen; and R is an arylmethyl group or a heteroarylmethyl group. Some of the specific compounds disclosed herein include 3-ethyl-5-(2-(hydroxyethyl)-piperidin-1-yl)-7-[{ (pyridin-3-yl)methyl} amino]-pyrazolo[1,5-a]pyrimidine; 3-ethyl-5-[{ 2-(hydroxymethyl)-cyclohexy} amino]-7-[{ (2-amino-pyrimidin-5-yl)methyl} amino]-pyrazolo[1,5-a]pyrimidine, 5-ethoxy-3-[{ (3-ethyl-5-phenyl-pyrazolo[1,5-a]pyrimidin-7-yl)amino} methyl]-pyridine N-oxide, 3-[{ (3-cyclopropyl-5-(2-(hydroxyethyl)-piperidin-1-yl)-pyrazolo[1,5-a]pyrimidin-7-yl)amino} methyl]-pyridine N-oxide and 3-[{ (3-ethyl-5-(2-(hydroxyethyl)-piperidin-1-yl)-pyrazolo[1,5-a]pyrimidin-7-yl)amino} methyl]-pyridine N-oxide. Further disclosed is a pharmaceutical composition which comprises at least one compound as defined above or a pharmaceutically acceptable salt or solvate thereof in combination with at least one pharmaceutically acceptable carrier for the treatment of cancer, squamous cell carcinoma, leukemia, fibrosarcoma, melanoma, seminoma, teratocarcinoma, osteosarcoma, xenoderoma pigmentosum, keratoctanthoma, thyroid follicular cancer, Kaposi's sarcoma etc.