Anti-malarial agents

摘要

The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation. In one embodiment, the invention provides aminopyrazine derivatives having the following formula:;

主权项

1. An aminopyrazine according to Formula (I), wherein X is CR1 or N; Y is selected from CF3, —C(O)—NR3R4; O—R6; SO2R6; R1 is selected from H and halogen; R2 is selected from SO2—R5 and —C(O)—R10; R3 and R4 are independently selected from H and optionally substituted C1-C6 alkyl; R5 is selected from —NR7R8 and R9; R6 is optionally substituted C1-C6 alkyl; R7 and R8 are independently selected from H and optionally substituted C1-C6 alkyl; R9 is an optionally substituted C1-C6 alkyl; R10 is —NR11R12; R11 and R12 are independently selected from H and optionally substituted C1-C6 alkyl or NR11R12 form together an optionally substituted heterocycloalkyl; or a pharmaceutically acceptable salt, hydrate, solvate, or polymorph, tautomer, geometrical isomer, or an optically active form thereof.