Fused Bicyclic FXR Modulators for Lipid Homeostasis
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for hyperlipidemia and related metabolic disorders, such as nonalcoholic steatohepatitis (NASH), are inadequate in effectively lowering triglycerides and non-HDL cholesterol, particularly in patients with cardiovascular disease, diabetes, and metabolic syndrome.
Innovation Solution
Development of compounds, such as those represented by Formulas (I) to (Xa), which act as FXR modulators to regulate bile acid and lipid homeostasis, thereby reducing triglyceride levels and improving lipid profiles.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If current treatments for hyperlipidemia are used, then patient compliance is maintained, but triglyceride and non-HDL cholesterol levels are not effectively lowered
Solution Approach 1:
The patent employs parameter changes by developing novel chemical compounds with modified molecular structures (Formulas I-Xa) that exhibit enhanced FXR modulating activity. These structural modifications include variations in R1-R8 substituents and bicyclic core structures, which change the pharmacological parameters to achieve superior triglyceride and cholesterol lowering effects compared to existing treatments
2Quantity of substance
If FXR modulating compounds are administered, then lipid homeostasis is improved and triglycerides are lowered, but the complexity of treatment regimens increases
Solution Approach 1:
The patent applies universality by designing FXR modulating compounds that simultaneously address multiple lipid abnormalities - lowering triglycerides, reducing non-HDL cholesterol, and improving overall lipid homeostasis. This multi-functional approach allows a single compound to treat several aspects of dyslipidemia, simplifying the treatment regimen despite the molecular complexity of the compounds themselves
Data Source
AI summary
Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.