Macrocyclic inhibitors of atp citrate lyase

EP4801897A1Pending Publication Date: 2026-09-09ESPERION THERAPEUTICS INC
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Patent Information

Application Number
EP2024805729
Authority / Receiving Office
EP · EP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-11-01
Filing Date
2024-10-31
Publication Date
2026-09-09

AI Technical Summary

Technical Problem

Current treatment options for metabolic and cardiovascular diseases associated with cholesterol and triglyceride metabolism are inadequate, and there is a need for new therapeutic strategies that target ATP-citrate lyase (ACLY) activity.

Method used

Development of macrocyclic inhibitors of ATP citrate lyase (ACLY) as therapeutic agents to treat conditions such as nonalcoholic fatty liver disease (NAFLD), type-2 diabetes, chronic kidney disease, inflammation, autoimmunity, and cancer.

Benefits of technology

The ACLY inhibitors effectively modulate ACLY activity, providing therapeutic benefits for various metabolic and cardiovascular disorders by inhibiting cholesterol synthesis and suppressing fatty acid biosynthesis.

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Abstract

The application relates to macrocyclic compounds of formula (I) which act as inhibitors of ATP citrate lyase (ACLY) useful for the treatment of conditions, diseases, and disorders associated with aberrant levels of lipids such as liver diseases, type-2 diabetes, inflammation, chronic kidney disease, autoimmunity and cancer.
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