Substituted Oxopyridine Derivatives Inhibit Factor XIa

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current anticoagulant therapies for thrombotic and thromboembolic disorders are limited by their efficacy, safety profile, and the narrow therapeutic window, leading to unsatisfactory treatment and prophylaxis outcomes.

Innovation Solution

Development of substituted oxopyridine derivatives that specifically inhibit factor XIa, a key enzyme in the coagulation cascade, to treat and prevent thrombotic and thromboembolic disorders without significantly prolonging bleeding times.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional anticoagulant therapies are used to treat thrombotic disorders, then thrombus formation is inhibited, but bleeding risk increases and therapeutic window narrows

Engineering Contradiction:

Improvethrombus inhibition efficacyVSAvoidbleeding risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention segments the coagulation cascade into distinct phases by selectively inhibiting factor XIa, separating the thrombus formation pathway from the bleeding risk pathway. This targeted approach at a specific cascade node (factor XIa) allows thrombus inhibition without the systemic bleeding effects of broad-spectrum anticoagulants

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention changes the parameter of coagulation factor specificity by designing compounds that selectively target factor XIa with high affinity, altering the selectivity parameter of anticoagulant therapy. This specificity parameter change enables differentiation between pathological thrombus formation and physiological hemostasis

Inventive Principle:

Principle #35Parameter changes

2Reliability

If factor XIa inhibition is achieved to reduce thrombus formation, then anticoagulant effect is improved, but bleeding time may be prolonged

Engineering Contradiction:

Improveanticoagulant effectVSAvoidbleeding time

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The invention applies partial action by selectively inhibiting only factor XIa while leaving other coagulation factors unaffected. This partial inhibition at a specific cascade node provides sufficient anticoagulant effect for thrombus prevention while maintaining normal bleeding time through preservation of other hemostatic pathways

Inventive Principle:

Principle #16Partial or excessive action

3Reliability

If broad-spectrum anticoagulants are used to prevent thromboembolism, then prophylaxis efficacy is improved, but safety profile deteriorates

Engineering Contradiction:

Improveprophylaxis efficacyVSAvoidsafety side effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention introduces factor XIa as an intermediary target in the coagulation cascade. By blocking this intermediate step rather than using broad-spectrum anticoagulants, the patent achieves prophylaxis efficacy while minimizing safety side effects through selective action at a cascade node that does not critically impact normal hemostasis

Inventive Principle:

Principle #24Intermediary (Mediator)

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

The compounds effectively inhibit factor XIa, reducing thrombus formation and stabilization while minimizing the risk of bleeding, thus offering a promising therapeutic option for thrombotic and thromboembolic disorders.

Implementation Method 1

The compounds effectively inhibit factor XIa, reducing thrombus formation and stabilization

Methodology Applied

Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS20250051303A1Substituted oxopyridine derivatives for the treatment and/or prophylaxis of thrombotic or thromboembolic disorders and/or thrombotic or thromboembolic complications

Publication Date: 2025.02.13 BAYER AG

AI summary

The invention relates to the use of substituted oxopyridine derivatives for the treatment and/or prophylaxis of thrombotic or thromboembolic disorders and/or thrombotic or thromboembolie complications.