Endothelium-Stabilizing Compounds for Therapy-Induced Hemorrhage

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Solution Overview

Problem

Thrombolytic and anticoagulant therapies often induce hemorrhage and vascular instability, such as localized edema and disruption of the blood-brain barrier function, which are not effectively addressed by existing treatments.

Innovation Solution

Administering a therapeutically effective amount of compounds, such as those represented by Formulae I, II, III, or IV, to prevent and treat hemorrhage and vascular instability induced by these therapies.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If thrombolytic and anticoagulant therapies are administered to prevent blood clot formation and dissolve blood clots, then blood clot prevention and dissolution is improved, but hemorrhage and vascular instability occur

Engineering Contradiction:

Improveblood clot prevention and dissolution efficacyVSAvoidhemorrhage and vascular instability

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies this principle by using the same vascular endothelium-targeted mechanism to counteract the harmful effects of thrombolytic therapy. The compound J147 stabilizes vascular endothelium to prevent hemorrhage, converting the potential harm of vascular instability into a protective effect through endothelium stabilization.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent introduces vascular endothelium-stabilizing compounds as intermediaries between thrombolytic therapy and the vascular system. These compounds act as mediators that protect the vascular endothelium from the destabilizing effects of thrombolytics while allowing the thrombolytic therapy to function.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Productivity

If thrombolytic therapy is used to dissolve blood clots, then clot dissolution is improved, but disruption of blood brain barrier function occurs

Engineering Contradiction:

Improveclot dissolution efficacyVSAvoidblood brain barrier function

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The patent converts the harmful disruption of blood-brain barrier into a beneficial protective effect by using vascular endothelium-stabilizing compounds. These compounds protect the blood-brain barrier from thrombolytic-induced disruption while allowing clot dissolution to proceed.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent applies prior cushioning by administering vascular endothelium-stabilizing compounds before or during thrombolytic therapy to pre-protect the blood-brain barrier. This preemptive stabilization prevents barrier disruption before it can occur.

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

Data Source

PatentUS12496281B2Compounds for prevention and treatment of hemorrhage and vasculature instability

Publication Date: 2025.12.16 ABREXA PHARMACEUTICALS INC

AI summary

Hemorrhage and vascular instability can be induced by thrombolytic and anti-coagulant therapies. Presented herein, in certain aspects, are methods for the treatment and/or prevention of hemorrhage and vascular instability that comprise administering a compound disclosed herein to a subject in need thereof.