NAFLD Treatment via Hepatic Lipid Reduction

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Solution Overview

Problem

There is no established therapy for nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), which involves lipid accumulation in liver cells leading to conditions like fatty liver and cirrhosis, and current weight loss treatments are ineffective due to obesity challenges.

Innovation Solution

A pharmaceutical composition containing a compound of Formula (I), administered as a pharmaceutically acceptable salt, is used to reduce and remove lipid accumulation in liver cells, treating and preventing NAFLD, NASH, and cirrhosis, with potential co-administration with other therapeutic agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If weight loss treatment is prescribed for NASH patients, then obesity is addressed, but the treatment is ineffective because patients seldom maintain significant weight reduction

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidweight maintenance duration
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent introduces a pharmaceutical composition as an intermediary agent that directly addresses lipid accumulation in the liver. Instead of relying solely on weight loss (which patients cannot maintain), the composition acts as a mediator to reduce hepatic steatosis through pharmacological action, bypassing the need for sustained lifestyle changes.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the therapeutic parameter from indirect weight management to direct lipid reduction in liver cells. The pharmaceutical composition targets specific biochemical parameters (lipid accumulation, triglyceride levels) rather than relying on the difficult-to-maintain parameter of body weight reduction.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If no established therapy is used for NASH, then existing treatments avoid potential side effects, but there is no effective treatment for lipid accumulation and liver damage

Engineering Contradiction:
Improvetreatment efficacyVSAvoidlack of therapy
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The pharmaceutical composition enables the liver to self-correct its lipid accumulation problem. The active compounds facilitate the liver's natural lipid metabolism and excretion processes, allowing the organ to remove excess fat without requiring external surgical intervention or aggressive treatment protocols.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The composition serves as a therapeutic intermediary that bridges the gap between no treatment and aggressive unproven therapies. It provides a targeted, mechanism-based approach that directly addresses hepatic steatosis while maintaining a favorable safety profile.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If aggressive weight loss is pursued in obese NASH patients, then lipid accumulation may be reduced, but patient compliance and sustained weight reduction are problematic

Engineering Contradiction:
Improvelipid reductionVSAvoidpatient compliance
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent replaces the mechanical/behavioral system of diet and exercise (which requires high patient compliance) with a pharmacological system. The pharmaceutical composition substitutes for the need for sustained behavioral modification, delivering lipid-reducing effects through chemical intervention rather than mechanical lifestyle changes.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The invention shifts the therapeutic parameter from behavioral compliance (diet/exercise adherence) to pharmacological response. By changing the mode of intervention from patient-dependent behavioral modification to drug-mediated biochemical action, the system achieves lipid reduction independent of patient compliance with lifestyle changes.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9814697B2Composition for nonalcoholic fatty liver disease (NAFLD)
Publication Date: 2017.11.14 ZYDUS LIFESCIENCES LTD
  • US9814697B2 patent drawing
  • US9814697B2 patent drawing
  • US9814697B2 patent drawing

AI summary

The present invention provides a compound of Formula (I) or pharmaceutical acceptable thereof, wherein ‘R’ is herein described. In addition, the invention relates to composition comprising effective therapeutic amount of compound of formula (I) and methods of using the compounds for treating or prevention disorder such as nonalcoholic fatty liver disease (NAFLD) including fatty liver (steatosis), nonalcoholic steatohepatitis (NASH), and cirrhosis (advanced scarring of the liver).