BBSCB Protection via Muvritinib and Bismuth Compounds
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Solution Overview
Problem
Current therapeutic agents are ineffective in clinically preventing or treating disorders associated with disruption of the blood brain spinal cord barrier (BBSCB), which leads to secondary injuries and exacerbates CNS diseases such as spinal cord injury.
Innovation Solution
The use of mubritinib, brexpiprazole, papaverine, and bismuth-containing compounds, or their pharmaceutically acceptable salts, as protective agents for vascular endothelial cells and the BBSCB, thereby preventing disruption and maintaining barrier function.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If methylprednisolone sodium succinate is used to suppress secondary injury, then some suppressive effect is achieved, but its efficacy is questioned and more effective agents are desired
Solution Approach 1:
The patent changes the chemical parameter by replacing methylprednisolone sodium succinate with compounds having different chemical structures and mechanisms of action (mubritinib, brexpiprazole, papaverine, bismuth-containing compounds), thereby achieving improved therapeutic efficacy while maintaining the protective effect on BBSCB
Solution Approach 2:
The patent identifies and utilizes the protective effect on BBSCB that is common to multiple different compounds (mubritinib, brexpiprazole, papaverine, bismuth-containing compounds), copying this beneficial effect across different chemical classes to achieve reliable therapy
2Reliability
If existing BBSCB protective agents (cilostazol, metformin, rosiglitazone) are used, then protective effects are observed in basic research, but no clinically effective agent has been established
Solution Approach 1:
The patent performs preliminary identification and validation of compounds with BBSCB protective effects (mubritinib, brexpiprazole, papaverine, bismuth-containing compounds) through in vitro and in vivo studies, establishing their efficacy before clinical application, thereby preparing effective agents in advance for clinical use
Solution Approach 2:
The patent identifies compounds that can protect BBSCB across different pathological conditions (spinal cord injury, stroke, neurodegenerative diseases), making these agents universally applicable to multiple CNS disorders, thereby increasing the quantity of clinically effective agents
3Object-affected harmful factors
If the BBSCB is disrupted, then permeability increases and cytotoxic substances leak into CNS, but maintaining barrier function requires effective protective agents
Solution Approach 1:
The patent applies compounds (mubritinib, brexpiprazole, papaverine, bismuth-containing compounds) that prevent BBSCB disruption before it occurs or at early stages, thereby maintaining barrier function and preventing the harmful effects of increased permeability and cytotoxic substance leakage
Solution Approach 2:
The patent utilizes compounds that act as intermediaries between the blood and CNS, protecting the BBSCB from disruption by cytotoxic substances and inflammatory cells, thereby maintaining the barrier function without completely blocking beneficial exchanges
Data Source
AI summary
The present invention relates to an agent for protection of vascular endothelial cells, an agent for protection of blood brain spinal cord barrier, and an agent for protection of central nervous system, containing at least one compound selected from the group consisting of muvritinib, brexpiprazole, papaverine, bismuth-containing compounds, and pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition for the treatment of diseases associated with blood brain spinal cord barrier disruption, containing at least one compound selected from the group consisting of muvritinib, brexpiprazole, papaverine, bismuth-containing compounds, and pharmaceutically acceptable salts thereof.