The invention relates to uses of 2-[(4-formyl-pyrazol-5-yl)-thio]acetic acid derivatives in the preparation of Caspase-3 inhibitors, and concretely relates to use of compounds of general formula (I) or pharmaceutically acceptable salts thereof in the preparation of medicines used for preventing and/or treating excessive apoptosis related diseases, and the preparation of Caspase inhibitors, especially Caspase-3 inhibitors.