The present invention relates to compounds (I) capable of inhibiting the Mst1/2 protein kinase activity, a preparation method therefor, a pharmaceutical composition comprising the compounds, and uses of the compounds and the pharmaceutical composition comprising the compounds in the preparation of drugs for prompting repair and regeneration of tissues and organs, prompting stem cell proliferation and somatic cell dedifferentiation, immunosuppression, and preventing or treating diseases related to nervous disorders and local ischemia.