Small Molecule Compound for Neuroregeneration via Endogenous Stem Cell Activation

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Solution Overview

Problem

Current treatments for neurodegenerative diseases, such as Alzheimer's and Parkinson's, face challenges in effectively activating endogenous neural stem cells to alleviate symptoms and promote neuroregeneration, particularly in crossing in-vivo barriers and addressing neuroinflammation and Aβ production.

Innovation Solution

A novel compound of formula (I) or its isomers, solvates, or pharmaceutically acceptable salts, which are used to manufacture medicaments for preventing, alleviating, or treating neurodegenerative diseases by inhibiting neuroinflammation, reducing Aβ production, and enhancing neural stem cell function, including increasing dopaminergic neurons and striatal dopaminergic nerve fibers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for neurodegenerative diseases, then existing therapeutic approaches can be maintained, but they fail to effectively activate endogenous neural stem cells and cross in-vivo barriers

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidcomplexity of activating endogenous neural stem cells
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent uses small molecule compounds as intermediaries to activate endogenous neural stem cells. These compounds serve as mediators that can cross in-vivo barriers (blood-brain barrier, cellular membranes) and transmit activation signals to neural stem cells, solving the problem of ineffective current treatments without requiring complex cellular transplantation procedures

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the chemical parameters of the treatment by developing novel small molecule compounds with specific structural features (formula I) that enable them to cross biological barriers and interact with neural stem cell receptors, transforming the treatment from ineffective conventional approaches to effective molecular activation

Inventive Principle:
Principle #35Parameter changes

2Reliability

If embryonic neural stem cells are transplanted for cell replacement therapy, then neuroregeneration may be achieved, but safety issues and source controversies arise

Engineering Contradiction:
Improveneuroregeneration capabilityVSAvoidsafety issues and source controversies
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent activates the body's own endogenous neural stem cells to perform neuroregeneration, eliminating the need for external cell transplantation. The endogenous cells self-renew and differentiate to replace damaged neurons, avoiding all safety and ethical issues associated with embryonic stem cell sources while achieving the same regenerative effect

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

Instead of introducing external stem cells from embryonic sources (the conventional approach), the invention inverts the strategy by activating and harnessing the patient's own existing endogenous neural stem cells, thereby reversing the source problem while maintaining the regenerative benefit

Inventive Principle:
Principle #13The other way round (Inversion)

3Ease of operation

If pharmacological means are used to activate endogenous neural stem cells, then ease of operation is improved, but suitable medicaments that can cross in-vivo barriers are difficult to find

Engineering Contradiction:
Improveease of pharmacological activationVSAvoiddifficulty of finding suitable medicaments
Core Design Contradiction:
Ease of operationVSDevice complexity

Solution Approach 1:

The patent modifies the chemical parameters of potential medicaments by designing small molecules with specific physicochemical properties (lipophilicity, molecular weight, structural motifs in formula I) that enable them to cross in-vivo barriers, transforming ordinary compounds into effective neural stem cell activators that are both easy to administer and biologically active

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention identifies and uses specific small molecule compounds as intermediary agents that bridge the gap between oral/pharmacological administration and neural stem cell activation. These intermediary compounds traverse biological barriers and deliver the activation signal, making the process both simple and effective

Inventive Principle:
Principle #24Intermediary (Mediator)

4Object-generated harmful factors

If Aβ accumulates to form oligomers and amyloid plaques, then neuroinflammation and neuronal damage occur, but current treatments cannot effectively reduce Aβ production

Engineering Contradiction:
ImproveAβ production and neuroinflammationVSAvoideffectiveness of current treatments
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The small molecule compounds act as intermediary agents that interfere with the Aβ production pathway. These compounds mediate the reduction of Aβ by interacting with enzymes or pathways involved in Aβ generation, thereby reducing the harmful factor without requiring complex immunotherapies or direct Aβ removal procedures

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention converts the understanding of Aβ pathogenesis into a therapeutic benefit by designing compounds that specifically target and reduce Aβ production. The harmful Aβ accumulation process is countered by pharmacological intervention that exploits knowledge of Aβ metabolism to reduce its formation, turning the pathological insight into a therapeutic mechanism

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentUS11643428B2Therapeutic drug for neurodegenerative disease and application thereof
Publication Date: 2023.05.09 SHANGHAI PHARMACEUTICALS HOLDING CO LTD
  • US11643428B2 patent drawing
  • US11643428B2 patent drawing
  • US11643428B2 patent drawing

AI summary

The present invention relates to a novel therapeutic drug for a neurodegenerative disease and an application thereof. Provided is a novel compound of formula (I). The compound can effectively facilitate the proliferation of neural stem cells in both in vitro and in vivo experiments and can be used as a treatment approach for facilitating neuroregeneration to fight against cognitive decline associated with aging or a neurodegenerative disease.