Dual-Target Inhibitor Compounds for CNS and Coronavirus Therapy
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Solution Overview
Problem
The development of effective therapies for central nervous system (CNS) disorders and coronavirus infections has been hindered by the complexity of these disorders and the lack of efficient technology for delivering therapeutic agents across the blood-brain barrier.
Innovation Solution
Development of compounds that inhibit D-amino acid oxidase and/or 3C-like protease (3CLPro) to treat CNS disorders and coronavirus infections, including those caused by SARS-CoV-2, with potential therapeutic effects demonstrated in animal models.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If therapeutic agents are administered to treat CNS disorders, then therapeutic efficacy is improved, but delivery across the blood-brain barrier is hindered
Solution Approach 1:
The patent uses liposomal carriers as intermediary vehicles to transport therapeutic agents across the blood-brain barrier. The liposomes act as mediators that facilitate the passage of drugs from the bloodstream into the CNS, solving the delivery problem without requiring complex external delivery devices
Solution Approach 2:
The patent modifies the physical and chemical parameters of therapeutic agents by encapsulating them in liposomes, changing their solubility, stability, and membrane permeability characteristics. This enables drugs that would normally be excluded by the blood-brain barrier to achieve effective CNS penetration
2Reliability
If complex therapeutic regimens are developed for CNS disorders, then treatment effectiveness is improved, but treatment complexity increases
Solution Approach 1:
The patent combines multiple therapeutic functions into a single liposomal formulation that can deliver multiple agents simultaneously or provide both targeted delivery and controlled release properties, simplifying the treatment regimen while maintaining effectiveness
Solution Approach 2:
The liposomal delivery system serves multiple functions simultaneously: it protects the therapeutic agent from degradation, enables blood-brain barrier penetration, provides controlled release, and can be engineered for active targeting. This multi-functionality reduces the need for multiple separate treatment components
3Reliability
If protease inhibitors are used to treat coronavirus infections, then viral replication is inhibited, but drug resistance may develop
Solution Approach 1:
The patent combines multiple antiviral agents with different mechanisms of action within the same liposomal formulation. This combination therapy approach maintains effective viral inhibition while reducing the likelihood of resistance development, as the virus would need to develop simultaneous resistance to multiple different agents
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The compounds exhibit inhibitory activities against D-amino acid oxidase and 3CLPro, offering therapeutic benefits for CNS disorders and alleviating viral infections, with applications in treating conditions such as schizophrenia, Alzheimer's disease, and coronavirus infections.
Implementation Method 1
Certain compounds disclosed herein exhibit inhibitory activities against D-amino acid oxidase and/or 3C-like protease (3CLPro)
Data Source
AI summary
A compound of Formula (I):or a pharmaceutically acceptable salt thereof, in which Ring X is a 3 to 7 membered monocyclic ring, at least one of R1, R2, R3, and R4 is OR5 or CH2OR5 and the other R1, R2, R3, and R4 each independently are halogen, OH, OR5, CH2OR5, CO2H, OC═OR6, (C═O)R6, R6, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, H, or absent. Also provided herein are therapeutic uses of the compound of Formula (I).