TRIPHENYLPHOSPHONIUM-BONDED SALICYLAMIN DERIVATIVES
Patent Information
- Application Number
- DE602020048328
- Authority / Receiving Office
- DE · DE
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2019-01-25
- Filing Date
- 2020-01-27
- Publication Date
- 2025-03-26
- Estimated Expiration
- 2040-01-27
AI Technical Summary
Current treatments for neurodegenerative and cardiovascular diseases related to oxidative stress and inflammation are limited by the need for high doses of salicylamine, which can lead to toxic levels of salicylic acid, and inefficiencies in targeting mitochondria, where oxidative damage occurs.
Development of salicylamine derivatives conjugated with triphenylphosphonium (TPP) salts, which are specifically targeted to mitochondria, allowing for lower effective doses and reducing exposure to systemic toxicity by leveraging the mitochondrial membrane potential for enhanced delivery.
The TPP-conjugated salicylamine derivatives effectively inhibit γ-ketoaldehyde protein adducts, providing therapeutic benefits for oxidative stress and inflammation with reduced toxicity and improved dosing requirements, while maintaining high concentrations at the mitochondrial site of action.