Functionalized Long-Chain Carboxylic Acids for Lipid and Inflammation Control
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Solution Overview
Problem
Current treatments for conditions such as hepatocellular carcinoma, liver diseases, lipid-and-metabolic disorders, and cardiovascular disorders are limited, often ineffective, and can cause significant side effects, while existing therapies for gastrointestinal cancers pose diagnostic and therapeutic challenges.
Innovation Solution
Development of compounds of specific Formulae (IA) through (IIIB) and their pharmaceutically acceptable salts and solvates, administered with a carrier, to treat or prevent diseases including liver diseases, cancers, lipid-and-metabolic disorders, and cardiovascular disorders, by reducing inflammatory markers and lipid levels, and modulating metabolic pathways.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If statins are used to lower LDL-C and reduce inflammation, then lipid levels and inflammation are improved, but triglyceride concentrations are not effectively lowered
Solution Approach 1:
The patent employs parameter changes by transitioning from statin monotherapy to combination therapy with fibrates, altering the treatment approach to simultaneously address both LDL-C and triglyceride levels. This combination strategy changes the therapeutic parameters to achieve broader lipid profile improvement.
2Quantity of substance
If high dose statin therapy is administered to maximize LDL-C reduction, then lipid control is improved, but muscle pain and muscle toxicity risk increase
Solution Approach 1:
The patent introduces an intermediary approach by combining statins with fibrates, where the fibrate acts as an adjunctive agent that enhances triglyceride lowering while allowing statin dosage optimization. This intermediary therapy aims to achieve comprehensive lipid control with potentially reduced muscle toxicity risk through synergistic effects.
3Quantity of substance
If fibrates are administered in combination with statins to lower triglycerides, then triglyceride levels are improved, but drug-drug interactions increase statin blood levels and muscle toxicity risk
Solution Approach 1:
The patent applies feedback principles by emphasizing close monitoring of statin blood levels and muscle enzyme markers when combining statins with fibrates. This feedback mechanism allows for dosage adjustments to maintain therapeutic efficacy while minimizing the risk of elevated statin levels and muscle toxicity.
4Quantity of substance
If fish oil is used to lower triglyceride levels, then triglyceride control is improved, but multiple daily administrations and fish oil aftertaste occur
Solution Approach 1:
The patent considers alternative lipid-lowering agents that may offer more convenient dosing regimens compared to fish oil. By exploring different therapeutic options with potentially once-daily or less frequent administration, the patent seeks to improve patient compliance while achieving triglyceride control.
Data Source
AI summary
This invention provides compounds of Formulae (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH), (IJ), (IK), (IL), (II), (III), (IIIA), and (IIIB); pharmaceutically acceptable salts and solvates thereof; and compositions thereof. This invention further provides methods for treating a disease, including but not limited to, liver disease or an abnormal liver condition; cancer (such as hepatocellular carcinoma or cholangiocarcinoma); a malignant or benign tumor of the lung, liver, gall bladder, bile duct or digestive tract; an intra- or extra-hepatic bile duct disease; a disorder of lipoprotein; a lipid-and-metabolic disorder; cirrhosis; fibrosis; a disorder of glucose metabolism; a cardiovascular or related vascular disorder; a disease resulting from steatosis, fibrosis, or cirrhosis; a disease associated with increased inflammation (such as hepatic inflammation or pulmonary inflammation); hepatocyte ballooning; a peroxisome proliferator activated receptor-associated disorder; an ATP citrate lyase disorder; an acetyl-coenzyme A carboxylase disorder; obesity; pancreatitis; or renal disease.