DERIVATIVES OF AMIDES AND UREA AS INHIBITORS OF REUPTAKE OF 5-HT AND LIGANDS OF 5-HT1B/1D Russian patent published in 2003 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of amides and urea of the formula (I): R¹-(CH₂)_n-(Y)_q-(Z)_r-CO-NH-R² (I) wherein R¹ means unsubstituted or substituted 3-indolyl, AO, Hal, CN; R² means: (Ia) , (Ib) or (Id) ; m = 1 or 2; n = 0, 1, 2, 3 or 4; Y means 2,4-cyclohexylene, 1,3-pyrrolidinylene, 1,4- piperazinylene or 1,4-piperidinylene ring that can be dehydrogenated partially also; Z means (CH₂)_nNH-,; q = 0 or 1; r = 0 or 1; R³ means A; R⁴ means AO-; Hal means F, Cl, Br, J; A means linear or branched C₁-C₆-alkyl under condition that q and r are not 0 simultaneously, and their physiologically acceptable salts also. Compounds of the formula (I) are antagonists of 5-HT1B/1D, elicit inhibitory effect with respect to reuptake of 5-HT and can be used in pharmaceutical composition in the effective dose. Compounds are prepared, for example, from compound of the formula (II): H₂N-R² and compound of the formula (III): R¹-(CH₂)_n-(Y)_q-(Z)_r-CO-L wherein L means Cl, Br, J, OH, OH-group modified functionally to confer to its reaction capacity [sic] or easily nucleophilically substituting removable group; R¹, R², n, Y, q, Z, r have values indicated above. EFFECT: valuable medicinal properties of compounds. 3 cl, 1 tbl, 11 ex