| 摘要 |
PCT No. PCT/EP93/02742 Sec. 371 Date Apr. 5, 1995 Sec. 102(e) Date Apr. 5, 1995 PCT Filed Oct. 6, 1993 PCT Pub. No. WO94/08985 PCT Pub. Date Apr. 28, 1994Described are 2H-1-benzopyran-2-ones (coumarin derivates) of general formula (I), <IMAGE> (I) wherein R1 is a hydroxyl group, a lower-alkoxy group, a cycloalkoxy group with 4 to 6 C-atoms or the alkyl- or arylsulphonyloxy group R6-SO2O-; R2 and R3, independently of each other, are hydrogen atoms, hydroxyl groups, lower-alkoxy groups or cycloalkoxy groups with 4 to 6 C-atoms; R4 is a hydrogen atom, a lower-alkyl group with 1 to 4 C-atoms or a phenyl group; Y is a nitrogen atom, a CH group or a COH group; R5 is a phenyl, naphtyl, pyridinyl or pyrimidinyl group which may optionally be substituted by one or two C1-C5 alkyl groups, by one or two halogen atoms, by a halogen and C1-C5 alkyl together, by perfluoroalkyl with 1 to 3 C-atoms, by C1-C5 alkoxy, by hydroxy, by methylenedioxy or by nitro; R6 is a lower-alkyl group, a cycloalkyl group with 4 to 6 C-atoms or a phenyl group which may optionally be substituted by one or two C1-C5 alkyl groups, by one or two halogen atoms, or by perfluoroalkyl with 1 to 3 C-atoms; and n=1 to 4; plus their addition compounds with physiologically tolerated acids. Also described are methods of preparing these compounds, novel intermediates in their preparation and methods of preparing such intermediates. The novel coumarin derivatives described possess a neuroprotective and psychopharmacological action. The invention also concerns pharmaceuticals containing these compounds.
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