Antimalarial quinolin derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 215/46 (2006.01) A61K 31/47 (2006.01) A61K 31/4706 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2237997

N1-Aralkyl-N2-quinolin-4-yl-diamine derivatives of general formula (I), wherein R1 signifies halogen or trifluoromethyl; R2 signifies hydrogen, halogen or trifluoromethyl; A signifies (a) or (C5-C6)-cycloalkylene; n signifies 1-4; R3 and R4 each independently signify hydrogen or methyl; p signifies 0-3 and B signifies aryl, as well as pharmaceutically acceptable salts of basic compounds of general formula (I), for use as therapeutically active substances, especially as active substances against malaria.

On décrit des dérivés N¿1?-aralkyl-N¿2?-quinolin-4-yl-diamine, ainsi que des sels de composés basiques, acceptables sur le plan pharmacologique, répondant à la formule générale (I), dans laquelle R?1¿ représentent halogène ou trifluorométhyle, R?2¿ représente hydrogène, halogène ou trifluorométhyle, A représente (a) ou cycloalkylène C¿5?-C¿6?, n vaut 1 à 4, R?3¿ et R?4¿ représentent chacun indépendamment hydrogène ou méthyle, p vaut 0 à 3 et B représente aryle. Ces composés sont utiles en tant que substances actives sur le plan thérapeutique, notamment en tant que principes actifs contre le paludisme.

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