Beta-AR Agonist and Blocker Combination for ALS Cognition

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current methods for improving cognition and treating neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS), are limited in effectiveness and specificity.

Innovation Solution

Administering a therapeutically effective amount of a β-AR agonist, such as Compound 03-5, optionally in combination with a sub-therapeutic dose of a peripherally acting β-blocker (PABRA), to improve cognitive function and treat neurodegenerative diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a β-AR agonist is administered to improve cognitive function, then cognitive function is improved, but peripheral adverse effects occur

Engineering Contradiction:

Improvecognitive functionVSAvoidperipheral adverse effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention divides the β-AR agonist's effects into two segments: central nervous system effects (desired cognitive improvement) and peripheral effects (undesired adverse effects). By using a peripherally acting β-blocker, the peripheral segment is selectively blocked while the central segment remains active, resolving the contradiction between improving cognition and avoiding peripheral side effects

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The peripherally acting β-blocker serves as an intermediary agent that selectively blocks β-AR agonist activity in peripheral tissues while allowing central nervous system penetration. This intermediary substance enables the desired cognitive effects to occur while filtering out the harmful peripheral effects

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If current treatment methods are used for ALS, then treatment is provided, but effectiveness and specificity are limited

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidspecificity

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention applies local quality by directing the therapeutic effect specifically to the central nervous system where cognitive function resides, while excluding peripheral tissues from the agonist's effects. This localized action pattern provides both effectiveness in improving cognition and specificity by avoiding unwanted peripheral interactions

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The invention changes the parameter of receptor selectivity by combining a β-AR agonist with a peripherally acting β-blocker. This parameter change creates a selective therapeutic profile where the agonist's effects are permitted in the CNS but blocked in peripheral tissues, thereby improving both effectiveness and specificity

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250134835A1Compositions and methods for treating patients with amyotrophic lateral sclerosis (ALS)

Publication Date: 2025.05.01 CURASEN THERAPEUTICS INC

AI summary

In various aspects and embodiments provided are compositions and methods for treating a patient that has ALS (or Lou Gehrig's disease or motor neuron disease). More specifically, the disclosure in some embodiments includes administration of a β-AR agonist (such as a β-agent) and optionally a peripherally acting β-blocker (PABRA) to a patient in need thereof.