Sigma-2 Receptor Modulators With Selective Lactone Scaffolds
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Solution Overview
Problem
There is a need for new Sigma-2 receptor binders and modulators to treat and prevent diseases associated with dysregulation or overexpression of the Sigma-2 receptor, including neuropsychiatric disorders and various types of cancer.
Innovation Solution
Development of novel compounds that bind to the Sigma-2 receptor, including hydrates, solvates, pharmaceutically acceptable salts, and complexes, which can be administered to treat or prevent diseases by modulating Sigma-2 receptor activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing sigma-2 receptor binders are used, then some therapeutic effect is achieved, but they lack sufficient selectivity and potency for treating diseases associated with sigma-2 receptor dysregulation
Solution Approach 1:
The patent applies local quality by introducing specific substituent groups at defined positions on the core chemical structure. Different substituents (R1-R6 groups) are placed at specific locations to enhance sigma-2 receptor binding affinity and selectivity while maintaining appropriate pharmacological properties for treating neuropsychiatric disorders and cancer
Solution Approach 2:
The patent employs parameter changes by systematically varying chemical parameters including substituent types, molecular weight, lipophilicity, and stereochemistry. These parameter modifications optimize the balance between sigma-2 receptor selectivity and therapeutic efficacy, enabling the compounds to effectively treat diseases associated with sigma-2 receptor dysregulation
2Reliability
If novel compounds with high sigma-2 receptor affinity are developed, then therapeutic potential is improved, but chemical complexity and synthesis difficulty increase
Solution Approach 1:
The patent applies segmentation by dividing the molecule into a core structure and separate substituent groups (R1-R6). This modular approach allows independent optimization of each segment's properties and simplifies synthesis by enabling separate preparation of core and substituent components before final assembly
Solution Approach 2:
The patent employs universality by designing a core chemical structure that serves multiple functions: providing the essential sigma-2 receptor binding motif while allowing attachment of various substituents to achieve desired pharmacological properties. This multi-functional core structure simplifies manufacturing by using a common scaffold for different therapeutic applications
Data Source
AI summary
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.