This application provides quinoline derivatives with indoleamine-2,3-dioxygenase inhibitory activity. Specifically, this application provides a compound of general formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, The preparation method and the use in the preparation of drugs for immune regulation and prevention and/or treatment of diseases related to abnormal IDO expression and/or abnormal tryptophan metabolism. The application also relates to the combined medication of the quinoline derivative and the HDAC inhibitor and its use in the preparation of anti-tumor drugs.本申請提供具有吲哚胺-2,3-雙加氧酶抑制活性的喹啉衍生物,具體地,本申請提供通式(I)化合物或其藥學上可接受的鹽,其藥物組合物,製備方法和在製備免疫調節及預防和/或治療與IDO表達異常和/或色氨酸代謝異常有關的疾病的藥物中的用途。本申請還涉及該喹啉衍生物與HDAC抑制劑的聯合用藥及其在製備抗腫瘤藥物中的用途。