This invention relates to 4-aminobutyric acid derivatives substituted by biaryl, process for preparing and their use thereof. Particularly, the invention relates to 4-aminobutyric acid derivatives substituted by biaryl as formular (I), process for preparing and their use thereof, the intermediate for preparing 4-aminobutyric acid derivatives substituted by biaryl by cyclization and pharmaceutical composition including 4-aminobutyric acid derivatives substituted by biaryl. These 4-aminobutyric acid derivatives substituted by biaryl have inhibition activity to NEP, which can be used as NEP inhibitor.本發明涉及聯芳基取代的4-胺基丁酸衍生物及其製備方法和用途。具體而言，本發明涉及如式(I)所示的聯芳基取代的4-胺基丁酸衍生物及其製備方法和用途，經環合反應製備聯芳基取代的4-胺基丁酸衍生物的中間體以及含有聯芳基取代的4-胺基丁酸衍生物的醫藥組成物。這些聯芳基取代的4-胺基丁酸衍生物具有NEP抑制活性，可以作為NEP抑制劑。□
