CYCLOPROPYLAMIDE DERIVATIVES AS N-HISTAMINE RECEPTOR MODULATORS Russian patent published in 2012 - IPC C07D207/06 C07D401/10 C07D403/10 C07D417/10 A61K31/4025 A61K31/4439 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new cyclopropylamine derivatives of formula: or its pharmaceutically acceptable salt, wherein: one of R₁ and R₂ means a group of formula -L₂-R_6a-L₃-R_6b; the other of R₁ and R₂ means H, C_1-10alkyl, C_1-10alkoxy, halogen, CN; each R₃, R_3a R_3b independently means H, C_1-6alkyl, trifluoromethyl, C_1-10alkoxy, CN; R₄ and R₅ taken together with a nitrogen atom whereto each attached form a non-aromatic cycle of formula: R₇, R₈, R₉ and R₁₀ each H, C_1-10alkyl; R_6a means cyanophenyl, phenyl, pyrazolyl, pyridazinyl, pyridinyl, pyrimidinyl, [1,2,3]triazolyl, [1,2,4]triazolyl, azepanyl, azetidinyl, azetidin-2-onyl, pyridazin-3(2H)-onyl, pyridin-2(1H)-onyl, pyrimidin-2(1H)-onyl, pyrrolidin-2-onyl, benzothiazolyl wherein the pyridinyl and pyrimidinyl groups optionally contain 1-3 substitutes specified in a group consisting of C_1-10alkyl and C_1-10alkoxy; R_6b means H; L means - [C(R₁₆)(R₁₇)]_k; L₂ means a bond, C_2-10alkylene, -O-, -C(=O)-, -NH-, -N(R₁₆)C(=O), -C(=O)N(R₁₆) and -N(C_1-6alkyl)-;L₃ means a bond; R₁₅ means H, C_1-6alkyl, C_1-6alkoxycarbonyl, amido and formyl R₁₆ , R₁₇ in each specific case means H, C_1-6alkyl; R_x and R_y in each specific case independently mean H, C_1-6alkyl, C_1-6alkoxy, C_1-6alkylamino, fluorine, diC_1-6alkylamino; k is equal to 1, 2 or 3; m is equal to 2.

EFFECT: compounds show H3 receptor inhibitory activity that makes them applicable in a pharmaceutical composition.

10 cl, 7 dwg, 44 ex