Deuterated hydroxychloroquine derivative and pharmaceutical composition containing deuterated hydroxychloroquine derivative
Through the preparation of deuterated hydroxychloroquine derivatives, the toxic side effects and metabolites related problems of hydroxychloroquine are solved, the efficacy and safety of the drug are improved, and the pharmacodynamic and pharmacokinetic performance are achieved.
Patent Information
- Application Number
- CN202010888546.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2020-08-28
- Publication Date
- 2020-11-27
- Estimated Expiration
- 2040-08-28
AI Technical Summary
Hydroxychloroquine has toxic side effects, especially retinal toxicity, which is related to the dose, and the blood concentration of its metabolite DCQ is related to the risk of adverse eye events in the patient. The blood concentration of the active metabolite DHCQ is related to the efficacy, but the drug concentration varies greatly , compounds with better pharmacodynamic/pharmacokinetic properties need to be developed.
Deuterated hydroxychloroquine derivative and its pharmaceutical composition are provided, which reduces toxic metabolites, improves pharmacodynamic and pharmacokinetic performance, improves therapeutic efficacy, and reduces toxic side effects by increasing active metabolites. This compound has better stability and drug preparation by the deuterated compound 2-{[4-(7-chloro-quinoline-4-ylamino)-pentyl]-ethyl-amino}-4D-ethanol Generation dynamics characteristics.
Deuterated hydroxychloroquine derivatives are more stable in liver microsomal enzymes, with increased active metabolites and decreased inactive metabolites, significantly improving pharmacodynamic/pharmacokinetic characteristics, improving drug efficacy, and reducing toxic side effects.