TETRAHYDROPYRANE DERIVATIVES FOR NEUROLOGICAL DISEASES Russian patent published in 2015 - IPC C07D309/14 C07D405/04 C07D407/14 A61K31/351 A61K31/4025 A61K31/439 A61K31/4433 A61K31/4412 A61P25/00 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of the general formula

,

wherein R¹/R² independently represent hydrogen, (CR₂)_o-C3-7 cycloalkyl optionally substituted by a lower alkyl or hydroxy, or represent a lower alkyl or tetrahydropyranyl, and o represents 0 or 1; and R can be identical or different, and represent hydrogen or a lower alkyl; or R¹ and R² can form together with a N atom to which they are attached, a heterocycloalkyl group specified in a group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.0]hex-2-yl which are optionally substituted by hydroxy; R³ represents an S-lower alkyl, lower alkyl, lower alkoxy or C3-7 cycloalkyl; R^3′ represents hydrogen, a lower alkyl substituted by a halogen, lower alkyl or lower alkoxy; R⁴ represents a lower alkyl substituted by a halogen; X represents -O- or -CH₂-; X' represents -O- or -CH₂-; provided one of X or X' always represent -O- and the other represents -CH₂-; or a pharmaceutically acceptable acid-additive mixture, a racemic mixture, or a respective enantiomer and/or an optical isomer.

EFFECT: compounds of the general formula (I) are good inhibitors of glycine transporter 1 (GlyT-1) and hence can be used for treating schizophrenia and other neurological conditions, including pain.

13 cl, 1 tbl, 63 ex