SPYRO(2H-1-BENZOPYRANE-2,4'-PIPERIDINE) DERIVATIVES AS GLYCINE TRANSPORT INHIBITORS Russian patent published in 2005 - IPC

FIELD: pharmaceutical chemistry, in particular pharmaceutical compositions.

SUBSTANCE: new spyro(2H-1-benzopyrane-2,4'-piperidine) derivatives of general formula I

and pharmaceutically acceptable salts thereof are disclosed. In formula dotted line is optional bond; Y is 1-4 substituents independently selected from hydrogen, halogen, C1-C4-alkyl, optionally substituted with one or more halogen, C1-C6-alkyloxy, optionally substituted with halogen or C3-C6-cycloalkyl, C2-C6-alkenyloxy, C2-C6-alkinyloxy, C3-C6-cycloalkyloxy, C6-C12-aryloxy, arylalkyloxy, pyridilmethoxy, SR₃, NR₃R₄, OSO₂R₅, and NR₃SO₂R₄; or two Y together may form O-(CH₂)n-O or O-(CF₂)n-O, wherein n is 1 or 2: or Y is condensed C5-C6-aryl group; X is 1-3 substituents independently selected from hydrogen, halogen, hydroxyl, C1-C6-alkoxy, and C1-C4-alkyl; R₁ is hydrogen, C1-C4-alkyl, or C6-C12-aryl; R₂, R₃, and R₄ are independently hydrogen or C1-C4-alkyl; R₅ is C6-C12-aryl. Also disclosed are pharmaceutical compositions including said derivatives and having activity in relation to CNS.

EFFECT: new compounds with valuable pharmacological action.

9 cl, 1 tbl, 83 ex