Cefin 1 and related compounds for the treatment of diseases and disorders that can be treated by AMPK activation and / or CHOP inhibition

Cefin-1 activates AMPK and inhibits CHOP to treat metabolic disorders and diseases by enhancing pAMPK/AMPK and pCHOP/CHOP ratios, addressing conditions such as metabolic syndrome and ALS.

JP2026510456APending Publication Date: 2026-04-06KYOTO PREFECTURAL PUBLIC UNIV CORP
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Patent Information

Application Number
JP2025553681
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-03-16
Filing Date
2024-03-15
Publication Date
2026-04-06

AI Technical Summary

Technical Problem

Current treatments for diseases and disorders such as metabolic syndrome, type 2 diabetes, cancer, and fibrosis are inadequate in effectively activating AMP-activated protein kinase (AMPK) and inhibiting C/EBP homologous protein (CHOP), which are associated with various health benefits and pathologies.

Method used

The use of cefin-1, a benzyliden guanidine derivative, to activate AMPK and/or inhibit CHOP by increasing the phosphorylated AMPK (pAMPK)/AMPK and/or phosphorylated CHOP (pCHOP)/CHOP ratios in cells, thereby addressing these diseases and disorders.

Benefits of technology

Cefin-1 effectively activates AMPK and inhibits CHOP, leading to therapeutic benefits including suppression of fatty acid and cholesterol synthesis, increased glucose uptake, and treatment of conditions like metabolic syndrome, non-alcoholic fatty liver disease, cancer cachexia, and amyotrophic lateral sclerosis (ALS).

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Abstract

Methods for treating diseases and disorders treatable by AMPK activation with cefin-1 and related compounds, such as metabolic syndrome, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis (NASH), obesity, type 2 diabetes, insulin resistance, glucose intolerance, chronic pain, muscle loss, neuromuscular disorders, heart failure, cardiac hypertrophy, diabetic cardiomyopathy, cardiac reperfusion injury, chronic kidney disease, polycystic kidney disease, diabetic nephropathy, cardiovascular disease, inflammatory bowel disease, arthritis, hypertension, peripheral vascular disease, nephrogenic diabetes insipidus, glaucoma, eye diseases or disorders, ocular angiogenesis, β-hemochromocytic disorder, cancer, fibrosis, cancer cachexia, and mitochondrial diseases.
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