Compounds derived from artesunate, preparation process,...

Details Compounds derived from artesunate, preparation process,... Compounds derived from artesunate, preparation process,...

2005-04-12

2011-12-06

Seaman, D M (Department: 1625)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S163000, C514S312000

Reexamination Certificate

active

08071777

ABSTRACT:
The present invention refers to new compounds derived from artesunate salts with quinolines represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III) depending on the radicals substituted in X (formula II), the relation X to Y (formula III) may vary from 1:1 to 1:7, because the amount of Y depends on the amount of N available in X for the formation of the salt. The radicals R1, R2, R3, R4, R5, e R6in the general formula (II) are represented by: R1═H, CF3, CH3, OCH3, NH2, halogen; R2═H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3═H, m-OC6H4CF3, NH2; R4═H, CH3, OCH3, NH2, halogen; R5═H, CH3, CF3, NH2, halogen; R6═H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7═(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3(CH2)6, (CH2)8, (CH2)10, (CH2)12; R8═CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. The present invention also refers to a process of preparation of these general formula (I) compounds, and the pharmaceutical compositions, in which these compounds are included especially their use as medicine for treatment or prevention or inhibition of malaria or other parasitic diseases such as: kaodzera, Chagas disease, leishmaniasis, amoebiasis, giardiasis, trichommoniasis, toxoplasmosis, schistosomiasis, as well as other helminthiases.

REFERENCES:
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de Pilla Varotti, Antimic Agents and Chemo, vol. 52(11), pp. 3868-3874, Nov 2008.
Herwaidt, Antimic Agents and Chemo, Jul. 1988, pp. 953-956, vol. 32(7).
Wetsteyn, Br J Clin Pharmac, vol. 39, pp. 696-699, 1995.

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