S1P Receptor Modulators Block Neo-angiogenesis in Multiple Sclerosis

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Solution Overview

Problem

Current treatments for relapsing-remitting multiple sclerosis are only partially effective in delaying disease progression and do not adequately address the chronic inflammation and neovascularization associated with demyelinating diseases.

Innovation Solution

S1P receptor modulators, such as FTY720, which act as agonists to inhibit neo-angiogenesis by modulating S1P receptors, thereby reducing lymphocyte circulation and promoting their homing into lymphatic tissues, are administered orally to block disease-associated angiogenesis and inhibit relapse phases in MS.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current anti-inflammatory and immunosuppressive treatments are administered, then disease progression is delayed to some extent, but the effectiveness is only partial and does not adequately address chronic inflammation and neovascularization

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidchronic inflammation and neovascularization

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the therapeutic approach by targeting S1P receptors, which modulates lymphocyte trafficking and reduces neovascularization. This parameter change in the mechanism of action addresses both inflammation and neovascularization simultaneously, overcoming the limitations of conventional treatments that only partially delay disease progression

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

S1P receptor modulators exhibit multi-functionality by simultaneously addressing multiple pathological features of MS: they reduce lymphocyte circulation, inhibit neovascularization, and suppress chronic inflammation. This universal approach treats multiple harmful factors with a single therapeutic agent, improving overall treatment effectiveness

Inventive Principle:

Principle #6Universality (Multi-functionality)

2Reliability

If S1P receptor modulators are administered to inhibit neo-angiogenesis and reduce lymphocyte circulation, then relapse phases are inhibited and disease progression is reduced, but generalized immunosuppression may occur

Engineering Contradiction:

Improveinhibition of relapse phasesVSAvoidgeneralized immunosuppression

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The S1P receptor modulators exhibit local quality by selectively affecting lymphocyte trafficking to specific tissues (promoting homing to lymphatic tissues while reducing circulation) rather than causing systemic immunosuppression. This localized modulation of immune cell distribution achieves therapeutic effects without widespread immunosuppression

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

Instead of suppressing the immune system broadly, the invention inverts the approach by actively directing lymphocytes to specific locations (lymphatic tissues) where they are needed, while simultaneously reducing their presence in circulation. This inversion of the traditional immunosuppressive strategy achieves protection against relapses without generalized immunosuppression

Inventive Principle:

Principle #13The other way round (Inversion)

Data Source

PatentEP2959894B1S1p receptor modulators for treating multiple sclerosis

Publication Date: 2022.10.12 NOVARTIS AG

AI summary

The present invention relates uses of an S1 P receptor modulator such as 2-substituted 2-amino-propane-1,3-diol or 2-1 mino-propanol derivatives, e.g. a compound comprising a group of formula (X) for the treatment or prevention of a neo-angiogenesis associated with a demyelinating disease.