噁唑酮类化合物及其药物组合物和应用
By designing reversible oxazolone compounds to inhibit MAGL enzymes, the side effects of existing MAGL inhibitors have been resolved, achieving highly effective treatment with low side effects, and making it suitable for drug applications in a variety of diseases.
CN117567450BActive Publication Date: 2026-07-17CHINA PHARM UNIV
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- CHINA PHARM UNIV
- Filing Date
- 2023-11-21
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
Existing MAGL inhibitors, due to their irreversible mechanism of action, lead to long-term activation of CB receptors, resulting in side effects such as CB1 desensitization, tonic syncope, and motor weakness, which are not conducive to clinical application.
Method used
An oxazolone compound and its pharmaceutically acceptable salt were designed and synthesized to prepare a pharmaceutical composition for the treatment of related diseases by reversibly inhibiting MAGL enzyme.
Benefits of technology
This compound exhibits an enzyme inhibition rate of over 50% at micromolar concentrations, with an IC50 value reaching nanomolar concentration levels, optimally below 5 nM, significantly reducing side effects and improving therapeutic efficacy.
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Figure CN117567450B_ABST
Abstract
本发明公开了一种噁唑酮类化合及其药物组合物和应用。该类化合物结构如式I，还包含其顺反异构体、药学上可接受的盐或它们的混合物。本发明设计的化合物对单酰基甘油酯酶具有优异的抑制活性，在微摩尔浓度水平的酶抑制率达到50％以上，酶抑制IC50值达到纳摩尔浓度水平。可制备为治疗抑郁症、焦虑症、帕金森病、阿尔兹海默症、肌萎缩性侧索硬化、多发性硬化、神经疼痛、炎性疼痛、癌性疼痛、癫痫、癌症、脂肪肝、非酒精性脂肪肝炎、胆汁淤积、炎性肠病的药物，应用广泛。
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