3-AZA-BICYCLO[3,3,0]OCTANE COMPOUNDS Russian patent published in 2013 - IPC C07D417/06 C07D417/14 C07D471/04 C07D513/04 A61K31/403 A61K31/426 A61K31/429 A61K31/4427 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of formula , where R¹ and R² are hydrogen, C_1-4alkyl or fluorine; R³ is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C_1-4alkyl, C_1-4alkoxy group, trifluoromethyl, trifluoromethoxy group and halogen; 2,3-dihydrobenzofuranyl; 2,3-dihydrobenzo[1,4]dioxynyl; or isoxazolyl, pyridyl, indazolyl, benzofuranyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl, benzoisothiazolyl, pyrrolo[2,1b]thiazolyl, imidazo[ 1,2-a]pyridinyl or imidazo[2,1-b]thiazolyl, where said groups are unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C₁-₄alkyl, C_1-4alkoxy group, halogen and trifluoromethyl; A is or ; R⁴ is C_1-4alkyl or -NR⁶R⁷; R⁶ is hydrogen or C_1-4alkyl; R⁷ is hydrogen or C_1-4alkyl; and D is a phenyl which is unsubstituted, mono- or disubstituted, where the substitutes are independently selected from a group comprising C_1-4alkyl, C_1-4alkoxy group, trifluoromethyl and halogen; or a pharmaceutically acceptable salt of such a compound. 3-aza-bicyclo[3.3.0]octane derivatives or a pharmaceutically acceptable salt thereof are used as a medicinal agent having the activity of orexin receptor antagonists.

EFFECT: novel 3-aza-bicyclo[3,3,0]octane derivatives as nonpeptide antagonists of human orexin receptors.

9 cl, 1 tbl, 85 ex