S1P and ATX Modulating Compounds for Demyelination

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Solution Overview

Problem

Current treatments for demyelination disorders, such as multiple sclerosis and other autoimmune and inflammatory conditions, are limited in effectiveness, often merely postponing disability rather than providing lasting solutions, and there is a need for new therapeutic approaches that can specifically target S1P and ATX pathways to modulate cellular responses.

Innovation Solution

Development of compounds, represented by formulas (I), (II), and (III), which act as S1P modulating agents and/or ATX modulating agents, specifically as S1P4 antagonists or ATX inhibitors, to selectively target S1P receptors and ATX activity, potentially reducing symptoms of conditions mediated by S1P and ATX activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for demyelination disorders are used, then symptoms may be temporarily managed, but lasting effectiveness is limited and disability is merely postponed

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidduration of symptom relief
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent modifies the chemical structure of S1P and ATX pathway modulators by changing molecular parameters (formulae I, II, III with specific substituents) to achieve superior therapeutic effectiveness and prolonged duration of action compared to conventional treatments. The compounds are designed with specific pharmacological properties that enable sustained modulation of S1P receptors and ATX activity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces novel intermediary compounds that selectively modulate the S1P and ATX pathways. These compounds act as mediators between the disease pathology and therapeutic response, providing sustained symptom relief through prolonged activation or inhibition of S1P receptors and ATX enzymes, thereby extending the duration of therapeutic action.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If existing treatments are used, then some symptom relief is achieved, but they do not specifically target S1P and ATX pathways

Engineering Contradiction:
Improvepathway specificityVSAvoidtherapeutic effectiveness
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies local quality by designing compounds with specific molecular structures (formulae I, II, III) that are selectively active at S1P receptors and ATX enzymes. The compounds exhibit localized pharmacological activity at specific pathway components, providing targeted modulation rather than non-specific symptom relief, thereby improving both pathway specificity and therapeutic effectiveness.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent segments the therapeutic approach by developing separate but complementary compounds targeting S1P receptors and ATX enzymes. This segmentation allows independent optimization of each pathway's modulation, enabling precise control over S1P signaling and ATX activity while maintaining overall therapeutic effectiveness.

Inventive Principle:
Principle #1Segmentation

3Duration of action of stationary object

If conventional treatments are used, then treatment is provided, but they do not offer lasting solutions for demyelination disorders

Engineering Contradiction:
Improveduration of symptom reliefVSAvoidlasting therapeutic solution
Core Design Contradiction:
Duration of action of stationary objectVSReliability

Solution Approach 1:

The patent ensures continuity of useful action through compounds that provide sustained modulation of S1P and ATX pathways. The compounds are designed to maintain therapeutic activity over extended periods, eliminating the need for frequent dosing adjustments and providing continuous symptom relief rather than temporary improvement, thereby achieving lasting therapeutic solutions.

Inventive Principle:
Principle #20Continuity of useful action

Data Source

PatentUS9944666B2Compounds that are S1P modulating agents and/or ATX modulating agents
Publication Date: 2018.04.17 BIOGEN MA INC
  • US9944666B2 patent drawing
  • US9944666B2 patent drawing
  • US9944666B2 patent drawing

AI summary

Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).