Formula I Compounds Inhibit Factor IXa to Reduce Thrombosis Risk

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Solution Overview

Problem

Current treatments for conditions associated with thrombosis, embolism, and hypercoagulability lack effective inhibitors for blood coagulation factor IXa, leading to increased risks of thrombus formation and complications such as hemophilia B and excessive thrombosis.

Innovation Solution

Development of novel compounds of formula I, which inhibit blood coagulation factor IXa, comprising specific aryl and Het groups, and their preparation processes, allowing for prophylactic and therapeutic use in humans to prevent and treat thrombotic disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for thrombosis are used, then existing therapeutic options are available, but effective inhibition of factor IXa is lacking leading to increased thrombus formation risk

Engineering Contradiction:

Improveeffectiveness of thrombosis treatmentVSAvoidavailability of factor IXa inhibitors

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent segments the coagulation cascade pathway by specifically targeting factor IXa as a distinct inhibition point. The compounds are designed to selectively bind to and inhibit factor IXa, separating this specific therapeutic need from general anticoagulation treatments. This segmentation allows for precise intervention in the coagulation process at the factor IXa step, addressing the unmet need for effective factor IXa inhibition while maintaining reliability in thrombosis treatment.

Inventive Principle:

Principle #1Segmentation

2Productivity

If factor IXa activity is not regulated, then natural coagulation process continues, but thrombus formation risk increases significantly

Engineering Contradiction:

Improvenatural coagulation functionVSAvoidthrombus formation risk

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces compounds of formula I as intermediary substances that mediate between the natural coagulation process and thrombus prevention. These compounds act as mediators by binding to factor IXa and preventing its pro-thrombotic activity, while still allowing regulated coagulation to occur. The intermediary compounds enable the system to maintain natural coagulation function where needed while blocking harmful thrombus formation, thus resolving the contradiction between maintaining productivity and preventing harm.

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentEP2069289B1ISOSERINE DERIVATIVES FOR USE AS COAGULATION FACTOR IXa INHIBITORS

Publication Date: 2013.10.02 SANOFI SA(FR)

AI summary

The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood coagulation factor IXa, to methods for producing the same and to the use thereof as drugs.