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Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof

机译:大环胰岛素降解酶(IDE)抑制剂及其用途

摘要

Macrocyclic compounds that specifically inhibit insulin degrading enzyme (IDE) are provided. Pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, polymorphs, tautomers, isotopically enriched forms, and prodrugs of the macrocyclic IDE inhibitors are also described. Pharmaceutical compositions are also provided. In vivo and in vitro methods of using the IDE inhibitor, and pharmaceutical compositions comprising the IDE inhibitor, for example, for the inhibition of IDE in a subject exhibiting aberrant IDE activity, impaired insulin signaling, or insulin resistance, for example, a subject having diabetes, are also provided.
机译:提供了特异性抑制胰岛素降解酶(IDE)的大环化合物。还描述了大环IDE抑制剂的药学上可接受的盐,溶剂化物,水合物,立体异构体,多晶型物,互变异构体,同位素富集形式和前药。还提供了药物组合物。使用IDE抑制剂的体内和体外方法,以及包含IDE抑制剂的药物组合物,例如,用于在表现出异常IDE活性,受损的胰岛素信号传导或胰岛素抵抗的受试者中例如抑制IDE,还提供了糖尿病。

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