Purine A2aR Antagonist Compounds for Broad Disease Treatment
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Solution Overview
Problem
There is a need for effective adenosine A2a receptor (A2aR) antagonists to treat neurological diseases, fibrosis-related diseases, and cancer, as existing treatments are inadequate.
Innovation Solution
Development of specific purine compounds, including 8-[(E)-2-[3,4-bis(difluoromethoxy)phenyl]vinyl]-1,3-diethyl-7-methyl-purine-2,6-dione, 8-[(E)-2-[3,4-dimethoxyphenyl]vinyl]-1,3-diethyl-7-methyl-6-thioxo-purin-2-one, and Istradefylline, which act as A2aR antagonists, and their pharmaceutical compositions for treating conditions such as depression, anxiety, multiple sclerosis, NASH, scleroderma, ADHD, Alzheimer's, and Parkinson's.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing A2aR antagonists are used, then some neurological conditions may be treated, but treatment effectiveness is inadequate for multiple disease types
Solution Approach 1:
The patent develops A2aR antagonist compounds with broad-spectrum therapeutic activity across multiple disease categories including neurological disorders (Parkinson's, Alzheimer's, depression, anxiety), fibrosis-related diseases (NASH, scleroderma), and cancer. The compounds demonstrate universal applicability by targeting the A2aR pathway which plays regulatory roles in diverse physiological systems including immune function, motor control, and inflammation.
2Productivity
If existing treatments are used, then some symptoms may be managed, but adequate therapeutic benefits are not achieved
Solution Approach 1:
The patent employs structural modification of purine compounds to optimize A2aR antagonistic activity. Specific chemical parameters including substitution patterns (difluoromethoxy groups at positions 3,4), vinyl linkages, and purine core structures are adjusted to enhance binding affinity and pharmacological effectiveness, thereby improving therapeutic benefits while maintaining treatment reliability.
Data Source
AI summary
Novel and known substituted purine compounds and salts thereof act as adenosine A2a receptor (A2aR) antagonists for cancer immunotherapy, depression, anxiety, multiple sclerosis, NASH, scleroderma, ADHD, Alzheimer's and Parkinsons. Pharmaceutical compositions comprising such compounds, and methods of their use in treating depression are also taught.