The invention relates to biphenyl derivatives as well as a preparation method and a pharmaceutical composition and application thereof on medicines. And particularly, the invention relates to novel urea-substituted biphenyl derivatives as well as a pharmaceutical composition and a preparation method thereof, and further relates to application to using the biphenyl derivatives and (or) the pharmaceutical composition containing the derivatives as a therapeutic agent, especially as a GPR40 agonist and preparing a drug for treating diseases such as diabetes and metabolic diseases. The novel urea-substituted biphenyl compounds contain urea radicals which have peculiarity and novelty on structure modification of the compounds.