Indane Derivatives for Selective Ion Channel Modulation
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Solution Overview
Problem
Current sodium channel and calcium channel blockers for pain management have limited efficacy due to side effects such as CNS disturbances, cardiac arrhythmias, and cardiac failure, and there is a need for more potent compounds with fewer side effects.
Innovation Solution
Development of compounds that inhibit voltage-gated sodium channels and calcium channels, specifically targeting NaV1.1, NaV1.2, NaV1.3, NaV1.4, NaV1.5, NaV1.6, NaV1.7, NaV1.8, NaV1.9, and CaV2.2, which are useful for treating various pain conditions and neurological disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional sodium channel and calcium channel blockers are used for pain management, then pain relief is achieved, but side effects such as CNS disturbances, cardiac arrhythmias, and cardiac failure occur
Solution Approach 1:
The patent applies local quality by developing compounds with selective affinity for specific sodium channel subtypes (NaV1.1, NaV1.2, NaV1.3, NaV1.4, NaV1.5, NaV1.6, NaV1.7, NaV1.8, NaV1.9) and calcium channels (CaV2.2), allowing targeted inhibition at pain-related channels while sparing other channel subtypes that mediate normal physiological functions, thereby reducing systemic side effects while maintaining pain relief efficacy
Solution Approach 2:
The patent employs parameter changes by modifying the chemical structure of channel blocking compounds to alter their pharmacological properties, achieving optimized binding affinity and selectivity for pain-related sodium and calcium channels, which enables effective pain management at lower doses with reduced off-target effects
2Reliability
If existing channel blockers are used to treat various pain conditions and neurological disorders, then therapeutic effect is obtained, but the compounds lack sufficient potency and have limited efficacy
Solution Approach 1:
The patent utilizes parameter changes by systematically optimizing the chemical parameters of the compounds, including molecular weight, lipophilicity, and functional group arrangements, to achieve high potency binding to voltage-gated sodium and calcium channels, thereby enhancing therapeutic effect across multiple pain conditions and neurological disorders
Data Source
AI summary
The present invention relates to indane derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.