NOVEL PIPERAZINES AS ANTIMALARIAL AGENTS Russian patent published in 2011 - IPC C07D295/18 C07D209/04 C07D209/16 C07D213/26 C07D213/38 C07D213/40 C07D213/60 C07D213/74 C07D217/04 C07D217/14 C07D233/54 C07D239/42 C07D277/28 C07D307/14 C07D317/58 A61K31/4965 A61K31/506 A61K31/5377 A61P33/06 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds selected from a group comprising piperazine compounds of formula I: , where X is -CH₂- or a bond; n equals 1; R¹ is alkyl; cycloakyl; hydroxyethyl; benzo[1,3]dioxolyl; phenyl, which can be mono-substituted with a halide, alkyl, alkoxy, -CF₃ or alkylcarbonyl; or phenyl which is di- or tri-substituted with substitutes independently selected from alkyl and halide; pyridyl which can be mono-substituted with a halide, alkyl or -CF₃; furanyl which can be mono-substituted with methyl, hydroxymethyl or bromine, or furanyl which is disubstituted with an alkyl; thienyl which can be mono-substituted with methyl or chromium; pyrimidinyl; isoquinolinyl; benzhydryl; imidazolyl optionally mono-substituted with an alkyl; or thiazolyl; or X is -C(=O)- and R¹ is hydrogen; R² is indolyl, imidazolyl optionally mono-substituted with alkyl; phenyl which can be mono-substituted with a halide, alkyl, hydroxy or cyano, or phenyl which is disubstituted with a halide; pyridyl; benzothienyl; thiazolyl or thienyl; R³ is indolyl, pyridyl which can be mono-substituted with alkoxy, alkoxyalkoxy, NR³¹R³², morpholine, piperadine, oxopiperidinyl, oxopyrrolidinyl, pyridyl or phenyl; or phenyl which is mono-substituted with phenyl, pyridyl, alkyl, alkoxy, dialkylamino, morpholine, N-benzyl-N-alkylamino, (dialkylamino)alkoxy, phenylalkoxy or tetrahydroisoquinolinyl; or R³ denotes the group: , where Z is phenyl or pyridyl; R³¹ is 2-C₁-C₅alkoxyethyl, phenyl, pyridyl, phenylalkyl, hydroxyalkylcarbonyl, alkylcarbonyl, cycloalkylcarbonyl or phenylcarbonyl; R³² is hydrogen or methyl; R³⁵ is alkyl, alkylcarbonyl, phenyl, pyridyl or pyrimidinyl; and R⁴ is phenyl-CH=CH-, where the phenyl can be mono-, di- or tri-substituted with substitutes independently selected from halide, alkyl, alkoxy and -CF₃; or phenyl-CH₂-CH₂, where the phenyl is disubstituted with -CF₃; and to optically pure enantiomers thereof, mixtures of enantiomers, such as, for example, racemates, optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates and mesoforms, such as salts of such compounds. The invention also relates to a pharmaceutical composition, as well as to use of compounds in any of claims 1-4.

EFFECT: obtaining novel biologically active compounds with antimalarial activity.

8 cl, 138 ex, 1 tbl