The present disclosure provides boron-containing diacylhydrazines having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, 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.
本公开提供具有式(I)的含
硼二酰
肼化合物及其药学上可接受的盐和溶剂化物,其中A、R4和R5如规范中所述。本公开还提供了含
硼二酰
肼化合物在
蜕皮激素受体基础上的诱导
基因表达系统的用途。因此,本公开适用于
基因治疗、疾病治疗、大规模蛋白质和
抗体生产、基于细胞的筛选分析、功能
基因组学、蛋白质组学、代谢组学和调节转
基因生物的特征等应用中,其中对
基因表达
水平的控制是可取的。