Monoacylglycerol lipase (MAGL) inhibitors for the treatment of pain and related medical disorders

Novel heterocyclic molecules inhibit MAGL to modulate the endocannabinoid system, addressing neuroinflammation and providing therapeutic benefits for pain and related disorders, including neurodegenerative diseases and chronic pain.

JP2026518409APending Publication Date: 2026-06-08YICHANG HUMANWELL PHARMA CO LTD
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Patent Information

Application Number
JP2025558484
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-04-14
Filing Date
2024-04-11
Publication Date
2026-06-08

AI Technical Summary

Technical Problem

Current treatments for pain and related disorders, such as chronic pain, anxiety, and depression, do not effectively modulate the endocannabinoid system to address neuroinflammation and neurodegeneration, as they fail to inhibit the monoacylglycerol lipase (MAGL) enzyme effectively.

Method used

Development of novel small heterocyclic molecules that act as MAGL inhibitors, including compounds of formula (I), (II), (III), and (IV), which can inhibit MAGL activity, thereby modulating the endocannabinoid system to reduce neuroinflammation and provide therapeutic benefits for various disorders.

Benefits of technology

The novel MAGL inhibitors demonstrate significant MAGL inhibitory activity, offering effective pain relief and therapeutic effects against neuroinflammation, neurodegenerative diseases, pain, cancer, and psychiatric disorders, including conditions like multiple sclerosis, Alzheimer's disease, Parkinson's disease, and chronic pain.

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Abstract

This invention discloses a novel class of monoacylglycerol lipase (MAGL) small molecule inhibitors, as well as their pharmaceutically acceptable compositions, methods of preparation, and uses. The MAGL small molecule inhibitors are represented by formula (I), having the specific substituents and definitions described herein. The disclosed MAGL small molecule inhibitors exhibit excellent MAGL enzyme inhibitory activity. This invention includes these compounds or their pharmaceutically acceptable compositions for the treatment and / or prevention of MAGL-related conditions such as multiple sclerosis, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, neurotoxicity, stroke, epilepsy, anxiety, migraine, depression, hepatocellular carcinoma, colorectal cancer lesions, ovarian cancer, neuropathic pain, chemotherapy-induced neuropathy, acute pain, chronic pain, and / or pain-related spasticity.
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Citation Information

Patent Citations

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    EP3328849A1

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  • US10,093,630

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  • Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders

    US20090082435A1