DERIVATIVES OF DIAZABICYCLIC ALKANES ELICITING NK-ANTAGONISTIC ACTIVITY Russian patent published in 2007 - IPC C07D471/04 C07D487/04 A61K31/4985 A61P29/00 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of diazabicyclic alkanes of the formula (1) and their pharmaceutically acceptable salts and stereoisomers wherein R¹ means phenyl, 3-indolyl or benzo[b]thiophene-3-yl and wherein indicated phenyl group can be substituted with halogen atom; R² and R³ represent independently halogen atom, -CH₃ or -CF₃; R⁴ represents hydrogen atom (H), hydroxyl group (-OH), -CH₂OH, -NH₂, dialkyl-(C₁-C₃)-N, pyrrolidine-1-yl, piperidine-1-yl, morpholine-4-yl or morpholine-4-yl substituted with one or two methyl or methoxymethyl groups, morpholine-4-ylamino-group, morpholine-4-ylmethyl, imidazole-1-yl, thiomorpholine-4-yl, 1,1-dioxothiomorpholine-4-yl or 3-oxa-8-azabicyclo[3.2.1]oct-8-yl; R⁵ means hydrogen atom; R⁴ and R⁵ can represent in common keto-group, 1,3-dioxane-2-yl or 1,3-dioxalane-2-yl; R⁶ represents H, morpholine-4-yl substituted with methyl group or -CH₂OH wherein indicated group -CH₂OH can form ester with organic acid; X represents oxygen atom (O); n = 1 or 2. Proposed compounds possess antagonistic activity with respect to NK₁-receptors. Also, invention describes intermediate compounds used in synthesis of compounds of the formula (I), pharmaceutical composition and using compounds in preparing drugs in treatment, for example, such diseases as chronic pains, inflammatory diseases and disorders of the central nervous system.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

7 cl, 6 ex