Artemisinine derivatives, and uses thereof for treating malaria

Details Artemisinine derivatives, and uses thereof for treating malaria Artemisinine derivatives, and uses thereof for treating malaria

2002-10-25

2008-08-26

Seaman, D. Margaret (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C549S354000, C514S450000

Reexamination Certificate

active

07417155

ABSTRACT:
A new artemisinin derivatives, of following general formula (I):In which:a and b represent a single or a double bond,n1 and n2 represent 0 or 1,R1represents a fluoroalkyl group or a fluoroaryl group,R2represents a hydrogen atom, or a halogen atom, or a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble,R3represents a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble,R4represents H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.

REFERENCES:
Ziffer et al. Journal of Medicinal chemistry, 1995, 38, 4120-4124 (p. 4121, compound 1).
Yu Ming Pu et al., “Synthesis and Antimalarial Activities of Several Fluorinated Artemisinn Derivatives”, Journal Medicinal Chemistry, American Chemical Society, Washington, DC 1995, vol. 38, pp. 4120-4124.
Truong Thi Thanh Nga et al., “Synthesis and Antimalarial Activities of Fluoroalkyl Derivatives of Dihydroartemisinin”, Journal of Medicinal Chemistry, American Chemical Society, Washington, DC,vol. 41, 1998, pp. 4101-4108.
Ahmed Abouabdellah et al., “Synthesis and in vivo Antimalarial Activity of 12α-Trifluoromethyl-Hydroartemisinin”, Bioorganic & Medicinal Chemistry Letters, Oxford, GB, vol. 6, No. 22, Nov. 19, 1996, pp. 2717-2720.

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