The present invention is involved in substituted urea derivatives and pharmaceutical uses thereof. Specifically, the present invention provides the mentioned substituted urea derivatives, and its stereoisomer, geometric isomer, tautomer, nitroxide, hydrate, solvate, metabolism product, ester, and pharmaceutically acceptable salt or its prodrug. The present invention also provides the medicament composition comprising the mentioned substituted urea derivatives, and uses of the mentioned substituted urea derivatives or medicament composition in the protection, treatment, curing, or relief of the proliferative diseases of patients, and its use in regulating the activity of protein kinase.本發明涉及取代脲衍生物及其在藥物中的應用,具體地,本發明提供了所述取代脲衍生物以及其立體異構體、幾何異構體、互變異構體、氮氧化物、水合物、溶劑化物、代謝產物、酯、藥學上可接受的鹽或它的前藥。本發明還提供了包含所述取代尿素衍生物的藥物組合物,以及所述取代脲衍生物或所述藥物組合物用於防護、處理、治療或減輕患者增殖性疾病以及用於調節蛋白激酶活性的用途。