Novel antimalarial drugs

By developing tetrahydroisoquinoline derivatives with higher metabolic stability, the problems of drug resistance and poor adherence to multiple-dose treatments in existing antimalarial drugs have been solved, achieving the antimalarial effect of low-dose single-dose treatment.

JP7883235B2Inactive Publication Date: 2026-07-01UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION +1

Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
Filing Date
2021-04-08
Publication Date
2026-07-01
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Existing antimalarial drugs suffer from drug resistance issues, and existing candidate drugs are not effective in single-dose treatment, making it difficult to meet the treatment requirements of the World Health Organization. Furthermore, multiple-dose treatment leads to poor patient compliance.

Method used

A series of tetrahydroisoquinoline derivatives were developed, and by optimizing their inhibitory effect on parasite ATP4' enzyme, the metabolic stability of the drug was improved. The effective dose for single-dose treatment is expected to be less than 500 mg, reducing the frequency of administration.

Benefits of technology

Tetrahydroisoquinoline derivatives have shown significant antimalarial activity, improved metabolic stability, and are expected to be effective with single-dose treatment, thus enhancing patient compliance.

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Patent Text Reader

Abstract

The present invention relates to novel derivatives useful in the manufacture of medicaments for preventing or treating malaria. In particular, the present invention relates to dihydroisoquinoline derivatives useful in the preparation of pharmaceutical formulations for the inhibition of malaria parasite proliferation.
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