The present invention relates to imidazoline derivatives, the preparation method and medical use thereof. Specifically, the present invention relates to a novel imidazoline derivative represented by formula (I), a preparation method thereof, a pharmaceutical composition containing the same, a use as a therapeutic agent especially as an androgen receptor antagonist and in the preparation of a medicament for the treatment of prostate cancer and so on, wherein all substituents of formula (I) are defined as those in the specification.本發明涉及咪唑啉類衍生物、其製備方法及其在醫藥上的應用。具體而言,本發明涉及一種通式(I)所示的新的咪唑啉類衍生物、其製備方法及含有該衍生物的醫藥組成物以及其作為治療劑,特別是作為雄激素受體拮抗劑和在製備治療前列腺癌等疾病的藥物中的用途,其中通式(I)的各取代基與說明書中的定義相同。