Antiparasitic Artemisinin Derivatives (Endoperoxides)
Patent Information:
1. Filing Country: China
Application No: 99810650.X
Filing Date: 07 March 2001
Patent No: ZL99810650.X
Issue Date: 24 September 2003
2. Filing Country: USA
Application No: 09/743827
Filing Date: 31 July 2001
Patent No: 6984640
Issue Date: 10 January 2006
Inventor 1: Prof. Richard Kingston, HAYNES
Inventor 2: Dr. William Wai Lun, LAM
Inventor 3: Dr. Ho Wai, CHAN
Inventor 4: Mr. Hing Wo, TSANG
Inventor 5: . Gisela, GREIF
Inventor 6: . Gabriele, SCHMUCK
Inventor 7: . Arnd, VOERSTE
Inventor 8: . Man-Ki, CHEUNG

New antiparasitic qinghaosu derivatives are discovered. The new derivatives of qinghaosu (QHS, or artemisinin) and synthetic trioxane are more active, more stable, and more bioavailable than qinghaosu itself and its current commercially available derivatives. These new derivatives involve alteration of the qinghaosu molecule such that a known decomposition pathway is now no longer available. In addition, certain of the groups attached, specifically amino groups, render the derivatives water soluble, and hence facilitate administration and absorption. Neurotoxicity, one of the biggest potential problems with current derivatives, is also reduced by removing the oxygen atom at C-10. Tests conducted on the derivatives shown that antimalarial activities of several C-10 amino and aryl derivatives are equipotent to, or more potent than, those of artemisinin and dihydroartemisnin, and the C-16 derivatives are less potent. Derivatives have also been tested against Neospora caninum at Bayer Leverkusen and activities have been rated as good against control compounds. Malaria is the world' s most prevalent parasitic disease in humans at the moment. Whilst the current qinghaosu derivatives are successful, there are problems associated with stability, bioavailability, and potential neurotoxicity. Besides, the demand for new qinghaosu-based drugs for animal health against parasitemia functionally related to malaria, and for improved antimalarial drugs for agricultural animals against parasitic diseases, revealed that there are great needs for new antiparasitic qinghaosu derivatives.
Potential Application   Advantage
- Provides a wide range of new drugs against malaria and related parasitic infections in farm animals, including neosporosis and coccidiosis   1. Compound are relatively accessible by conducting straight forward chemical transformation on starting materials that are commercially available in large quantities
2. Families of compounds can be prepared
3. Structural variation of the compounds can be achieved in control
4. Reduced neotoxicity
5. More stable
6. Solve multidrug resistant strains found in antimalarial drugs for agricultural animal
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Contact information :
Ms Shirley Woo
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HKUST R and D Corporation Ltd
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