2-AZA-BICYCLO[3,3,0]OCTANE DERIVATIVES Russian patent published in 2013 - IPC C07D417/14 C07D513/04 A61K31/427 A61K31/429 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a 2-aza-bicyclo[3.3.0]octane derivative of formula , with stereogenic centres in a (1S,3S,5S)-configuration, where A is a thiazolyl which is unsubstituted or monosubstituted, where the substitute is independently selected from a group comprising C_1-4alkyl, C_3-6cycloalkyl and NH₂; B is phenyl which is unsubstituted or mono- or disubstituted, where the substitutes are independently selected from a group comprising C_1-4alkyl, trifluoromethyl, NHC(O)CH₃ and halogen; and R¹ is an imidazo[2,1·b]thiazolyl or benzoisoxazolyl group, where said groups are independently unsubstituted or monosubstituted, where the substitutes are independently selected from a group comprising C_1-4alkyl; or R¹ is a 2,3-dihydrobenzofuranyl group; or a pharmaceutically acceptable salt. The 2-aza-bicyclo[3.3.0]octane derivative of formula (I) is as a medicinal agent having the activity of orexin receptor antagonists.

EFFECT: obtaining novel 2-aza-bicyclo[3,3,0]octane derivatives as orexin receptor antagonists.

8 cl, 1 tbl, 26 ex