Fundacao Oswaldo Cruz-fiocruz

Fundacao Oswaldo Cruz

Marcus Vinicius Nora De Souza

Alessandra Leda Valverde

Antoniana Ursine Krettli

Nubia Boechat

Núbia Boechat

Robson Xavier Faria

Emerson Teixeira Da Silva

Magda Fraguas Serra

The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R, R, R, R, R, and Rin formula (II) are represented by: R=H, CF, CH, OCH, NH, halogen; R=H, CH, NH, halogen, NH&#x2014;CHCH(CH)N(CH)(CHCHOH), CH(OH)-2(CHN), NH&#x2014;R&#x2014;N&#x2014;(CH); R=H, m-OCHCF, NH; R=H, CH, OCH, NH, halogen; R=H, CH, CF, NH, halogen; R=H, CF, CH, NH, halogen, NH&#x2014;R&#x2014;N&#x2014;(CH), NHCH(CH)(CH)NH; R=(CH), (CH), CHCHCH, (CH), (CH), CHCH(CH), (CH), (CH), (CH), (CH); R=CHCH(CH), CHCH(CH)CHCH, (CH), (CH), (CH), (CH)O(CH). This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.

Compounds derived from artesunate, preparation process, pharmaceutical composition and use of the respective medicine

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 R, R, R, R, R, e Rin the general formula (II) are represented by: R&#x2550;H, CF, CH, OCH, NH, halogen; R&#x2550;H, CH, NH, halogen, NH&#x2014;CHCH(CH)N(CH)(CHCHOH), CH(OH)-2(C5HN), NH&#x2014;R&#x2014;N&#x2014;(C2H5); R&#x2550;H, m-OCHCF, NH; R&#x2550;H, CH, OCH, NH, halogen; R&#x2550;H, CH, CF, NH, halogen; R&#x2550;H, CF, CH, NH, halogen, NH&#x2014;R&#x2014;N&#x2014;(CH), NHCH(CH)(CH)NH; R&#x2550;(CH), (CH), CHCHCH, (CH), (CH), CHCH(CH)(CH), (CH), (CH), (CH); R&#x2550;CHCH(CH), CHCH(CH)CHCH, (CH), (CH), (CH), (CH)O(CH). 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.

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Juiz de Fora, Brazil

Marcus Vinicius Nora De Souza