DERIVATIVES OF AMINOPIPERIDINE, THEIR PRODUCTION AND USE IN THERAPY Russian patent published in 2009 - IPC C07D451/04 C07D453/02 C07D401/14 C07D405/12 C07D401/12 C07D211/58 A61K31/4468 A61K31/439 A61P3/04 A61P3/10 A61P9/00 A61P15/00 A61P25/32 A61P29/00 

FIELD: medicine.

SUBSTANCE: invention is related to new compounds of formula (I): , in which: R_a and R_a', identical or different, mean atom of hydrogen or alkyl, R₁ means atom of hydrogen or alkyl, cycloalkyl, heterocycloalkyl or aryl, R₂ means group of formula -(CH₂)_x-(CO)_y-Y or -(CO)_y-(CH₂)_x-Y, in which, x = 0, 1, 2, 3 or 4, y = 0 or 1, Y means atom of hydrogen or the following group: hydroxyl, alkyl, cycloalkyl, alkyloxyl, aryl, heteroaryl or -NR₁₁R₁₂, besides, Y is not an atom of hydrogen, when x=y=0, R₁₁ and R₁₂, identical or different, mean atom of hydrogen or the following group: alkyl, cycloalkyl, alkyloxyl or -NR₁₃R₁₄, or R₁₁ and R₁₂ together with atom of nitrogen, to which they are connected, create mono- or bicyclic structure, which contains 4-10 links and unnecessarily contain additionally 1-3 heteroatoms and/or 1-3 ethylene unsaturated links, besides this cycle is not necessarily substituted in any of positions with 1-3 groups, selected from atoms of halogen and hydroxyl, alkyl, cycloalkyl and alkyloxygroups; R₁₃ and R₁₄, identical or different, mean atom of hydrogen or alkyl, R₃ means 1-3 groups, identical or different, available in any position of cyclic structure, to which they are connected, and selected from atoms of halogen; R₅ means atom of hydrogen, R₄ is selected from groups of formulae (a), (b), (c), which are not necessarily substituted with aryl group, described below: (a), (b), (c), in which p=0,1,2 or 3; m=0,1 or 2, and either a) X means link -N(R₁₀)-, in which R₁₀ is selected from: -CO-alkyl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-aryl, -CO-heteroaryl, - or R₁₀ with atom of nitrogen, with which it is connected, and with atom of carbon, available in any position of cyclic structure of formula (a), but not with neighboring to mentioned atom of nitrogen, creates bridge, containing 3-5 links, or, b) X means link -C(R₆)(R₇)-, where R₆ is selected from the following: atom of hydrogen, atom of halogen, group -(CH₂)_x-OR₈, -(CH₂)_x-NR₈R₉, -(CH₂)_x-CO-NR₈R₉ or -(CH₂)_x-NR₈-COR₉, in which x=0,1,2,3 or 4, alkyl, cycloalkyl, heterocycloalkyl, aryl, heterocycloalkyl, condensed with aryl, besides, alkyl, cycloalkyl or aryl groups are not necessarily substituted with 1 or several groups, selected from groups: R, R', -OR, -NRR', -COR; R₇ is selected from atoms of hydrogen and halogen and the following groups: alkyls, -OR, -NRR', -NR-CO-R', -NR-COOR', -R₈ and R₉ are selected, independently from each other, from atom of hydrogen and the following groups: alkyls, cycloalkyls, aryls, -CO-alkyls, besides, alkyls and aryls are unnecessarily substituted with one or several groups, selected from groups: R, R', -OR, or R₈ and R₉ together create heterocycloalkyl,- R and R' mean, independently from each other, atom of hydrogen or alkyl, cycloalkyl, besides, mentioned hetero aryl groups represent aromatic groups, including from 5 to 10 links and including from 1 to 4 heteroatoms, such as atom of nitrogen, oxygen and/or sulfur; besides mentioned heterocycloalkyl groups represent cycloalkyl groups, including from 5 to 6 links and including from 1 to 4 heteroatoms, such as atom of nitrogen, oxygen or sulfur; in the form of base or acid-additive salt, and also in the form of hydrate or solvate. Invention is also related to medicinal agent, to pharmaceutical composition, to application, to method of production, and also to compounds of formulas (VI), (XVIII), (XIX).

EFFECT: new biologically active compounds have activity of agonists of melanocortin receptors.

27 cl, 16 ex, 1 tbl