Autophagy-Inducing Compound Design for Selective CNS Therapy

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Solution Overview

Problem

There is a need for more selective autophagy inducers that can effectively treat and prevent diseases related to autophagy, particularly in the central nervous system, as existing treatments are not sufficiently targeted or effective.

Innovation Solution

Development of compounds according to Formula (I) or their salts, solvates, and hydrates, which induce and stimulate the process of autophagy, specifically designed to address conditions such as cancer, age-related diseases, and viral infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing autophagy inducers are used, then some therapeutic effect is achieved, but selectivity and effectiveness in the central nervous system are insufficient

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidselectivity for CNS diseases
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by designing compounds with specific molecular structures (Formula I) that have enhanced properties for crossing the blood-brain barrier and targeting CNS tissues. The compounds contain specific functional groups and structural features that confer selective affinity for neural tissues, thereby improving therapeutic effectiveness specifically in the central nervous system while maintaining autophagy induction capability.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by modifying key molecular parameters of autophagy inducers, including molecular weight, lipophilicity, and structural configuration. These parameter optimizations enable the compounds to better penetrate the blood-brain barrier and achieve selective accumulation in CNS tissues, resolving the contradiction between general therapeutic effect and CNS-specific selectivity.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If broad-spectrum autophagy inducers are used, then multiple disease types are covered, but specificity for targeted diseases is reduced

Engineering Contradiction:
Improvebroad disease coverageVSAvoiddisease targeting precision
Core Design Contradiction:
Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent applies segmentation by dividing the broad spectrum of autophagy-related diseases into specific categories (CNS diseases, viral infections, cancer, metabolic disorders). For each category, the patent optimizes compound properties to achieve selective targeting while maintaining the core autophagy induction mechanism. This allows the compound to cover multiple disease types with enhanced precision for each specific indication.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs universality by designing a core molecular scaffold (Formula I) that maintains universal autophagy induction capability across different disease types, while allowing for specific functional modifications that enable targeted action in different disease contexts. This multi-functional design achieves both broad coverage and disease-specific precision.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP4653432A1Autophagy inducing compounds and uses thereof in the prevention or therapy of diseases
Publication Date: 2025.11.26 SAMSARA THERAPEUTICS INC
  • EP4653432A1 patent drawing
  • EP4653432A1 patent drawing
  • EP4653432A1 patent drawing

AI summary

The invention relates to pharmaceutical compositions and methods of preventing and/or treating autophagy related diseases and disorders. The present invention relates to compounds according to Formula (I) or salts, solvates and/or hydrates thereof, wherein said compounds induce and/or stimulate the process of autophagy, as well as uses of the compounds in the treatment and prevention of autophagy related diseases and disorders. Examples are cancer, age-related diseases, and viral infection.