COMPOUNDS OF SUBSTITUTED DIAZEPANES AS ANTAGONISTS OF OREXIN RECEPTORS Russian patent published in 2015 - IPC C07D401/14 C07D403/14 C07D413/14 C07D471/04 C07D487/04 C07D491/48 C07D491/52 C07D495/04 A61K31/551 A61P3/04 A61P25/20 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to formula I compounds or their pharmaceutically acceptable salts. The invention compounds possess properties of an orexin receptor antagonist. In formula: I:

R¹ is phenyl, substituted with triazolyl, and optionally C_1-6alkyl, -(C=O)-O-C_1-6alkyl, -CO₂H, C_1-6alkyl, substituted with hydroxyl; R² is heteroaryl, selected from quinazolinyl, 1,3-benzoxazolyl, quinoxalinyl, thieno[2,3-d]pyrimidinyl, pyrido[2,3-d]pyrimidinyl, furo[2,3-d]pyrimidinyl, pyrimidinyl, pyridinyl, pyrazolo[3,4-d]pyrimidinyl, substituted with R^2a, R^2b; R^2a, R^2b are independently selected from a group, consisting of a halogen, -C_1-6alkyl, -O-C_1-6alkyl, -C_1-6alkyl, substituted with a halogen, -C_1-6alkyl, substituted with hydroxyl, -NH₂, =O, on condition that at least one of R^2a, R^2b is a halogen or C_1-6alkyl or where adjacent R^2a and R^2b can be bound together with the formation of a cycloalkyl or cycloalkoxy ring, cycloalkyl is non-substituted or is substituted with =O; R³ represents -C_1-6alkyl. The invention also relates to a pharmaceutical composition, containing the invention compound.

EFFECT: obtained are the novel compounds, possessing properties of the orexin receptor antagonist.

7 cl, 1 tbl