The present invention relates to naphthylurea derivatives. Such substances can significantly inhibit VEGFR2 and PDGFR-?receptor tyrosine kinase phosphorylation at nanomolar concentration levels. It is a novel type of tyrosine kinase inhibitors which can be used in the treatment of tyrosine kinase-mediated diseases or symptoms such as malignancies and ocular diseases accompanied with pathologic neovascularization.