Phosphorylcholine Conjugates Replace Parasitic Agents in Autoimmune Therapy

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Solution Overview

Problem

There is a need for safe and stable small molecules with minimal adverse side effects to treat autoimmune diseases associated with abnormal inflammation, as using parasitic agents for immunomodulation raises ethical and safety concerns.

Innovation Solution

Phosphorylcholine-conjugates, specifically those comprising tuftsin derivatives like Thr-Lys-Pro-Arg-Gly-Tyr-Phosphorylcholine, exhibit immunomodulatory effects on autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus by inhibiting disease progression and promoting anti-inflammatory responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If parasitic agents are used for immunomodulation to treat autoimmune diseases, then therapeutic efficacy is improved, but ethical and safety concerns arise

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidethical and safety concerns
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the beneficial immunomodulatory component (phosphorylcholine) from the parasitic agent and uses it as a standalone therapeutic molecule. This eliminates the ethical and safety concerns associated with using whole parasitic agents while preserving the therapeutic efficacy through the isolated active component.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent creates a synthetic copy of the immunomodulatory molecule (phosphorylcholine-conjugates) that mimics the structure and function of the natural parasitic-derived molecule. This synthetic copy provides the same therapeutic benefits without the ethical and safety issues of using actual parasitic agents.

Inventive Principle:
Principle #26Copying

2Object-affected harmful factors

If small molecules are developed to replace parasitic agents, then safety and ethical issues are resolved, but immunomodulatory effectiveness must be maintained

Engineering Contradiction:
Improvesafety and ethical issuesVSAvoidimmunomodulatory effectiveness
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent modifies the phosphorylcholine molecule by conjugating it to various carriers (proteins, polysaccharides, lipids) to optimize its immunomodulatory effectiveness. These parameter changes in molecular structure and composition enhance the therapeutic effect while maintaining the safety profile of the small molecule approach.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite structures by conjugating phosphorylcholine with various carriers to form phosphorylcholine-conjugates. These composite materials combine the safety of small molecules with the enhanced immunomodulatory capabilities achieved through conjugation, thereby maintaining effectiveness while ensuring safety.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS12350308B2Phosphorylcholine conjugates and uses thereof
Publication Date: 2025.07.08 TPCERA LTD
  • US12350308B2 patent drawing
  • US12350308B2 patent drawing
  • US12350308B2 patent drawing

AI summary

The present invention provides phosphorylcholine conjugates and pharmaceutical compositions comprising same for the prevention or treatment of autoimmune diseases. In particular, the conjugates of the present invention are effective in treating autoimmune diseases associated with pathological inflammation.