PYRIMIDOBENZIMIDAZOLE DERIVATIVES AND APPLICATION THEREOF AS AGONISTS OR ANTAGONISTS OF MELANOCORTIN RECEPTORS Russian patent published in 2010 - IPC C07D495/14 C07D487/14 C07D471/14 C07D491/12 A61K31/519 A61P3/04 A61P19/02 A61P25/24 

FIELD: chemistry.

SUBSTANCE: invention refers to novel compounds with affinity to MC4 receptors, of the general formula (I): , where A is -CH₂- or -C(O)-; R₁ is (C₁-C₈)alkyl; R₂ is (C₁-C₈)alkyl; R₃ is radical of the formula -(CH₂)_s-R'₃; R'₃ is 5-6-member heterocycloalkyl containing one or two nitrogen atoms and possibly one oxygen atom possibly substituted with (C₁-C₆)alkyl or benzyl; or radical of the formula -NW₃W'₃; W₃ is hydrogen atom or (C₁-C₈)alkyl; W'₃ is radical of the formula -(CH₂)_s'-Z₃; Z₃ is hydrogen atom, (C₁-C₈)alkyl; s and s' are independently an integer within 0 to 6; B is 5-6-member monocyclic unsaturated, aromatic or non-aromatic radical which can be condensed with 5-6-member unsaturated, aromatic or non-aromatic radical forming bicyclic condensed system, and B is possibly containing one or more equal or different heteroatoms selected out of O, S and N, and possibly substituted with one or more equal or different radicals selected out of halogen atom, nitro group, cyano group, oxy group, -X_B-Y_B and phenyl possibly substituted with one substitute selected out of halogen atom and (C₁-C₆)alkyl; X_B is a covalent bond, -O-, -S-, -C(O)-, -C(O)-O-; Y_B is (C₁-C₆)alkyl; or pharmaceutically acceptable salt of claimed compounds.

EFFECT: improved obtainment and application efficiency of compounds for production of drug for treatment of diseases related to MC4 receptor activation.

20 cl, 4 dwg, 2 tbl, 81 ex