Adenosine A2A Receptor Ligands for Neurological Disorder Treatment
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Solution Overview
Problem
Current treatments for central nervous system disorders such as Parkinson's disease, Alzheimer's disease, and ADHD lack effective solutions for modulating adenosine A2A receptor signaling pathways, which are crucial for neuronal protection and function.
Innovation Solution
Development of compounds with high affinity for adenosine A2A receptors that act as antagonists, potentially offering therapeutic benefits by partially or totally inactivating these receptors, thereby addressing various neurological disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for CNS disorders are used, then existing therapeutic options are maintained, but effective modulation of adenosine A2A receptor signaling pathways is lacking
Solution Approach 1:
The patent develops novel compounds with optimized molecular structures (Formula I) that specifically target adenosine A2A receptors, changing the pharmacological parameters of receptor modulation. These compounds exhibit high affinity and selectivity for A2A receptors, enabling effective signaling pathway modulation that current treatments cannot achieve.
2Reliability
If high affinity compounds for adenosine A2A receptors are developed, then therapeutic benefits for neurological disorders are achieved, but compound specificity and selectivity must be maintained
Solution Approach 1:
The patent employs local quality by designing compounds with specific substituent patterns at defined positions in the molecular structure (Formula I). Different substituents at specific positions confer selectivity for A2A receptors over other adenosine receptor subtypes, while maintaining high affinity binding. This localized structural optimization ensures both therapeutic effectiveness and receptor specificity.
3Reliability
If adenosine A2A receptor antagonists are used, then neuronal protection and function are improved, but potential side effects from receptor inactivation must be managed
Solution Approach 1:
The patent employs partial action by developing antagonists that selectively block A2A receptors without completely inactivating all adenosine signaling pathways. The compounds provide sufficient receptor modulation to achieve neuronal protection and therapeutic benefits while maintaining enough adenosine signaling activity to avoid excessive side effects, achieving a balanced therapeutic window.
Data Source
AI summary
The present invention provides new compounds with high affinity for adenosine A2A receptors. It also provides antagonists of adenosine A2A receptors and their use as medicaments for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors signalling pathways could be beneficial such as Alzheimer's disease, Parkinson's disease, attention deficit and hyperactivity disorders (ADHD), Huntington's disease, neuroprotection, schizophrenia, anxiety and pain. The present invention further relates to pharmaceutical compositions containing such new compounds with high affinity for adenosine A2A receptors and their use for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors could be beneficial.