Chalcone Composition for Blood Clotting Without Immunogenicity

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Solution Overview

Problem

Current therapies for treating bleeding and bleeding disorders, such as hemophilia, are limited by immunogenicity, the need for injection, and increased risk of unwanted blood clotting.

Innovation Solution

The use of chalcones, a class of compounds identified through bioassay-guided fractionation and synthetic methods, which can reduce blood clotting time and increase blood clotting efficiency without causing immunogenicity or unwanted clotting.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If factor protein therapies are administered to treat bleeding disorders, then blood clotting function is improved, but the body generates antibodies that destroy these foreign proteins rendering the therapy ineffective

Engineering Contradiction:

Improveblood clotting functionVSAvoidimmune response antibodies

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent uses small molecule compounds that copy or mimic the functional effect of clotting factor proteins without being the actual proteins. These small molecules can activate clotting mechanisms indirectly, achieving the desired therapeutic effect while avoiding immune recognition and antibody formation against foreign proteins.

Inventive Principle:

Principle #26Copying

2Reliability

If non-factor protein therapies such as bispecific antibodies are used to boost blood clotting mechanisms, then clotting effectiveness is improved, but the risk of unwanted blood clotting increases

Engineering Contradiction:

Improveblood clotting effectivenessVSAvoidunwanted blood clotting

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The small molecule compounds activate clotting mechanisms partially or moderately rather than fully amplifying the clotting cascade. This controlled activation achieves sufficient clotting effectiveness while avoiding excessive clot formation and thrombosis risks associated with stronger clotting boosters.

Inventive Principle:

Principle #16Partial or excessive action

3Duration of action of stationary object

If gene therapies are administered to replace missing factor proteins, then long-term blood clotting function is improved, but severe side effects have been observed in clinical trials

Engineering Contradiction:

Improvelong-term blood clotting functionVSAvoidsevere side effects

Core Design Contradiction:

Duration of action of stationary objectVSObject-generated harmful factors

Solution Approach 1:

Instead of attempting permanent genetic modification with viral vectors, the patent employs small molecule compounds that act temporarily but safely. These molecules can be administered repeatedly over time, providing sustained treatment without the severe side effects associated with gene therapy, allowing the body to clear them without long-term consequences.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

4Reliability

If desmopressin is administered to release von Willebrand's antigen from platelets, then blood clotting is improved in mild cases, but effectiveness is drastically reduced in moderate and severe cases

Engineering Contradiction:

Improveblood clotting responseVSAvoideffectiveness across disease severity

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The small molecule compounds work through a different mechanism that is not limited by the severity of factor deficiency. By targeting alternative pathways or using a different mode of action, these compounds can effectively treat bleeding disorders across the full spectrum from mild to severe cases, unlike desmopressin which only works in mild cases.

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

Chalcones effectively reduce blood clotting time and enhance blood clotting efficiency in both regular and hemophilic blood models, offering a potential non-immunogenic and orally active treatment for bleeding disorders.

Implementation Method 1

one of the mechanisms by which chalcones work is to reduce the inhibitory activity of antithrombin on thrombin-driven blood clotting, thereby increasing the effectiveness of the thrombin mechanism in blood clotting

Methodology Applied

Scientific EffectAntithrombin inhibition:

Data Source

PatentUS12343317B2Compositions and methods for treating bleeding and bleeding disorders

Publication Date: 2025.07.01 YEWSAVIN

AI summary

Various embodiments of the invention utilize chalcones to treat blood, bleeding, and/or bleeding disorders. As described herein, chalcones significantly reduce blood clotting time in normal/hemophilic blood and normal/hemophilic animal models. As also described herein, chalcones reduce blood clotting time and increase blood clotting efficiency without any apparent risk of immunogenicity or unwanted blood clots. As also described herein, chalcones reduce the inhibitory activity of antithrombin on thrombin-driven blood clotting, thereby increasing the effectiveness of the thrombin mechanism in clotting blood.