The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.本發明提供具有式I之含硼的二醯基肼類化合物：及其醫藥上可接受之鹽類和溶劑合物，其中R1、R2、R3、R4和R5係如說明書中所提出之定義。本發明亦提供含硼的二醯基肼類化合物於以蛻皮激素受體為基底之誘發基因表現系統中的用途。因此，本發明可用於以下希望控制基因表現程度的應用：諸如基因療法、疾病的治療、蛋白質和抗體的大規模生產、以細胞為基礎之篩選檢定、功能性基因體、蛋白質體(proteomic)、代謝體(mefabolomic)、及基因轉殖有機體之表徵的調節。
