PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, METHOD OF OBTAINING THEREOF AND THEREOF-CONTAINING PHARMACEUTICAL COMPOSITION Russian patent published in 2015 - IPC C07D401/04 C07D401/14 C07D413/14 A61K31/444 A61K31/496 A61K31/5377 A61P1/18 A61P3/04 A61P3/06 A61P3/08 A61P9/00 A61P37/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: in formula 1 X represents N or CR, and Y represents N or CH on condition that X and Y are not simultaneously carbon; Z represents N or CH; R₁ and R₂ represent independently hydrogen, (C3-C10)cycloalkyl, norbornyl, adamantyl or noradamantyl, or R₁ and R₂ can be bound with each other together with nitrogen atoms, to which they are bound, with the formation of (C5-C10) saturated or unsaturated heterocycle or condensed heterocycle, on condition that R₁ and R₂ are not simultaneously hydrogen; L represents a single bond, -CO-, -SO₂-, -(CR₂₁R₂₂)-(CH₂)_c- (c represents an integer number 0-5), , -CO(CR₂₁R₂₂)_d- (d represents an integer number 1-6), (C3-C10)cycloalkylene, (C6-C20)arylene or 5-6-membered heteroarylene, including one or two heteroatoms, selected from N; R₂₁ and R₂₂ represent independently hydrogen or (C1-C10)alkyl, R represents hydrogen or hydroxyl; R₄ and R₅ independently represent hydrogen or (C1-C10)alkyl, or R₄ and R₅, bound together form a 6-membered unsaturated carbocycle; R₆ and R₇ represent independently hydrogen, (C1-C10)alkyl or halogen; R₃₁-R₃₈, R₄₁-R₄₃ and R₄₆ represent independently hydrogen or (C1-C10)alkyl; and m and n independently represent an integer number 0-3 on condition that m+n represent an integer number 2 or larger. Values of radical R₃ and additional substituents of cyclic groups R₁-R₃, L are given in the invention formula. The invention also relates to pharmaceutical composition, containing the said compounds, and to the 11β-HSD1 inhibitor.

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EFFECT: invention relates to amide compounds of structural formula 1, which possess inhibiting activity with respect to 11β-HSD1 enzyme.

9 cl, 24 tbl, 296 ex