AMINOTROPANE DERIVATIVES, SYNTHESIS THEREOF AND USE IN THERAPY Russian patent published in 2010 - IPC C07D451/04 A61K31/46 A61K31/55 A61P3/04 A61P3/10 A61P15/00 

FIELD: chemistry.

SUBSTANCE: invention relates to new compounds of formula , in which: R_a and R_a' denote hydrogen, R₁ denotes cycloalkyl; R₂ denotes a group of formula -(CH₂)_x-(CO)_y-Y or -(CO)_y-(CH₂)_x-Y, in which x=0, y=1, Y denotes -N-R₁₁R₁₂;- R₁₁ and R₁₂ denote alkyl; R₃ denotes a halogen atom; R₅ denotes a hydrogen atom; R₄ is selected from: (1) a group of formula : in which each of the rings in formulae (a) and (b) can be substituted in any position with 1-4 R₇ groups which are identical or different from each other, and in which: a=0; p=0, 1, 2 or 3; m=1; X is an oxygen or sulphur atom or a C(R₆)(R₇)- or -N(R₁₀)- group; R₆ is selected from: a hydrogen atom; a -(CH₂)_x-NR₈R₉ group in which x=0, aryl, alkylaryl; R₇ is selected from hydrogen atoms; aryl, alkylaryl groups; -OR group; -NRR' groups; R₈ and R₉ are selected from a hydrogen atom; R₁₀ is selected from: hydrogen atom; aryl, alkylaryl; R and R' denote a hydrogen atom; (2) a group of formula -A-R₁₈, -A-CH=N-R₁₉, in which A denotes a straight or branched alkyl; R₁₈ denotes a halogen atom or a -NH₂ group; R₁₉ denotes hydroxyl; (3) a group of formula : in which r equals 1; s equals 1, and one of U, V and W denotes a nitrogen atom while the others denote a methylene group; or (4) -(CH₂)_r-heteroaryl, where r equals 1; where the heteroaryl denotes a 5-6-member aromatic group containing 1-2 heteroatoms such as nitrogen, oxygen, in form of a base or additive acid salt. The invention also relates to a method for synthesis of formula (I) compounds, to compounds of formulae (IV) and (V), to a medicinal agent, to a pharmaceutical composition, as well as to use of formula (I) compounds.

EFFECT: obtaining new biologically active compounds having melanocortin receptor agonist activity.

11 cl, 28 ex, 1 tbl