Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.本發明係揭示一種經取代的5-(3,5-二甲基異唑-4-基)二氫吲哚-2酮化合物,包括至少一個4經取代的5-(3,5-二甲基異唑-4-基)二氫吲哚-2酮化合物之醫藥組成物,其製備方法,及其用於抑制布羅莫結構域之BET家族和治療由此引起疾病,如特定癌症之用途。