3-AMINO-1-ARYLPROPYLINDOLES APPLIED AS INHIBITOR MONOAMINE REUPTAKE Russian patent published in 2010 - IPC C07D209/04 C07D209/14 C07D209/42 C07D231/56 A61K31/4045 

FIELD: chemistry.

SUBSTANCE: invention refers to new 3-amino-1-arylpropylindoles of formula I: or to its pharmaceutically acceptable salts, where: p is equal to 1 or 2; Ar means: indolyl, 2,3-dihydroindolyl, indazolyl, benzimidazolyl, benzofuranyl, and each can be substituted; R¹ means: phenyl, naphthyl, thienyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, thiazolyl, isoxazolyl, pyrazolyl, quinolinyl, aryl-C_1-6alkyl where each can be substituted; C_3-6cycloalkyl; branched C_1-6alkyl; R² and R³ each independently stands for: H, C_1-6alkyl; OH-C_1-6alkyl; benzyl; or R² and R³ together with nitrogen atom whereto attached can form optionally substituted tetra-heptamerous ring, optionally with additional heteroatom chosen from N, O; R^a means H, C_1-6alkyl; R^b means H, C_1-6alkyl; OH; R^c and R^d each independently means H, C_1-6alkyl; Or one of R² and R³ together with one of R^a and R^b and atoms whereto attached can form penta- or hexamerous ring, optionally with additional heteroatom chosen from O, N; or one of R² and R³ together with one of R^c and R^d together with atoms whereto attached, can form tetra-hexamerous ring, optinally with additional heteroatom chosen from O, N; R^c means H, C_1-6alkyl; provided when p =1, R^a, R^b, R^c and R^d mean H, Ar means indole-1-yl and R¹ means C₆H₅, then R² and R³ do not mean CH₃ and do not form hexamerous ring, and when Ar means indole-3-yl, p =1, R^a, R^b, R^c and R^d means H and R¹ means C₆H₅-, 3-OCH₃C₆H₅- then R² and R³ do not mean simultaneously H, and when p =1, R^a, R^b, R^c and Rd mean H, Ar means indolyl and R1 means thienyl, pyridinyl, quinolinyl, then one of R² and R³ means H, and another means C_1-6alkyl where possible substitutes are presented in cl.1 of.

EFFECT: compounds express activity of double inhibition serotonin reuptake, possibility to use thereof in making a pharmaceutical composition and a medical product.

32 cl, 7 tbl, 16 ex