Boronic Acid Compounds for Cytokine Modulation
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Solution Overview
Problem
Current treatments for inflammatory-related diseases such as inflammatory bowel disease, psoriasis, rheumatoid arthritis, multiple sclerosis, neurodegenerative disorders, and post-radiotherapy inflammation are inadequate due to unsatisfactory efficacy and significant side effects, with a lack of understanding in the underlying disease mechanisms and ineffective modulation of cytokines.
Innovation Solution
A compound with a specific formula is developed to decrease the release of cytokines and chemokines, potentially treating conditions by administering a therapeutically effective amount, thereby modulating inflammatory responses.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments (corticosteroids, immunosuppressive agents) are used for inflammatory diseases, then some therapeutic effect is achieved, but significant side effects occur and efficacy is unsatisfactory
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of boronic acid compounds to optimize their biological activity. Specifically, the invention varies substituents at different positions (R1-R6) on the boronic acid core structure to achieve compounds with improved cytokine modulation efficacy and reduced side effects compared to conventional treatments
Solution Approach 2:
The boronic acid compounds act as intermediaries that selectively modulate cytokine pathways. The compounds interfere with the interaction between cytokines and their receptors or with intracellular signaling molecules, thereby providing therapeutic effect with potentially greater specificity and fewer side effects than broad-spectrum immunosuppressants
2Duration of action of moving object
If current immunosuppressive therapies are administered, then inflammatory symptoms are controlled, but the treatments have slow onset of action and only moderate efficacy
Solution Approach 1:
The patent employs parameter changes by optimizing the pharmacokinetic properties of boronic acid compounds through structural modification. The varying substituent patterns (R1-R6) are designed to improve drug absorption, distribution, and metabolic stability, thereby achieving faster onset of action while maintaining or enhancing therapeutic efficacy
3Duration of action of stationary object
If long-term immunosuppressive therapy is used, then disease symptoms are managed, but liver damage and bone marrow suppression occur
Solution Approach 1:
The boronic acid compounds serve as selective intermediaries that target specific cytokine pathways involved in inflammatory diseases. This selective mechanism of action allows for long-term therapy with reduced off-target effects compared to conventional immunosuppressants, thereby minimizing liver damage and bone marrow suppression
Solution Approach 2:
The patent applies local quality by designing compounds with specific molecular features that enable selective interaction with target cytokines or receptors. The varied substituent patterns (R1-R6) on the boronic acid core create compounds with different binding affinities and specificities, allowing optimization for particular inflammatory conditions while reducing systemic toxicity
Data Source
AI summary
This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.