The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.本發明提供一些新的取代的吡唑酮化合物,其藥學上可接受的鹽,及其藥物製劑,用於調節蛋白激酶的活性,並調節細胞間或細胞內的信號回應。本發明同時也涉及包含本發明化合物的藥物組合物,並使用該藥物組合物治療哺乳動物,特別是人類高增殖性疾病的方法。