The present invention relates generally to novel allosteric regulators of proteasome activity, methods for preparation and use, and pharmaceutical compositions thereof. Specifically piperidine-2-carboxylic acid derivatives containing 1-oxo-aroyl group and a lipophilic ester side chain are disclosed as allosteric inhibitors of proteasome 2S activity, and as therapeutic agents for the treatment of proteasome-associated disorders in a subject.
本发明一般涉及
蛋白酶体活性的新型异位调节剂、制备和使用方法及其药物组合物。具体而言,本发明公开了含有 1-氧代-芳酰基和亲油酯侧链的
哌啶-2-
羧酸衍
生物,作为
蛋白酶体 2S 活性的异构
抑制剂,以及用于治疗受试者
蛋白酶体相关疾病的治疗剂。