Formula I Compounds for Brain Exposure in Neurodegenerative Treatment
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Solution Overview
Problem
Current treatments for neurodegenerative disorders, particularly Alzheimer's disease, lack effective targets to substantially alter the clinical course, and no cure has been identified.
Innovation Solution
Development of compounds with specific structural formulas, including phenyl or pyridyl groups optionally substituted with various moieties, for use in pharmaceutical compositions to treat or prevent neurodegenerative disorders, demonstrating good brain exposure and efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for Alzheimer's disease are used, then existing therapeutic approaches are maintained, but no substantial change in clinical course is achieved
Solution Approach 1:
The patent applies parameter changes by developing novel chemical compounds with specific molecular structures (Formula I) that differ from existing treatments. The compounds feature variable parameters including n (1, 2, or 3), substituent groups (R1, R2a, R2b, R3, R4), and heterocyclic ring structures, allowing optimization of brain penetration and therapeutic efficacy to substantially change the clinical course of Alzheimer's disease
2Reliability
If compounds with complex structural formulas are developed, then brain exposure and efficacy are improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the complex molecule into distinct modular components: a core heterocyclic ring structure (pyrazolo[4,3-c]pyridine), substituent groups (R1-R4), and variable parameters (n). This modular structure allows systematic synthesis and optimization of brain-penetrating compounds while maintaining manufacturability through standardized chemical building blocks
Data Source
AI summary
The present invention discloses compounds according to Formula I:wherein R1, R2a, R2b, R3, X, Y, and the subscript n are as defined herein.The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving neurodegenerative disorders by administering the compound of the invention.