首页> 外国专利> 1,3,4-oxadiazol-2(3H)-one Derivates, their preparation and their use as monoamine oxidase inhibitors.

1,3,4-oxadiazol-2(3H)-one Derivates, their preparation and their use as monoamine oxidase inhibitors.

机译:1,3,4-恶二唑-2(3H)-one衍生物,其制备及其作为单胺氧化酶抑制剂的用途。

摘要

The invention relates to 1,3,4-oxadiazol-2(3H)-one derivatives, of general formula (I) IMAGE in which R1 represents either a hydrogen atom or a linear or branched (C1-4)alkyl group, which is substituted by a hydroxyl, phenoxy, (C1-4)alkoxy, (C1-4)alkylthio, mercapto, (C1-4)alkoxy(C1-4)alkoxy, di(C1-4)alkylamino or N-(C1-4)alkyl-N-propynylamino group, or a (C3-4)alkynyl group, and R2 represents either a linear or branched (C1-8)alkyl group, which is substituted by one or a number of halogen atoms and/or a hydroxyl, 1-imidazolyl or 3-tetrahydropyranyl group, or a trifluoro(C3-5)alkenyl group, in the form of pure enantiomers or of mixtures of enantiomers, including racemic mixtures, and their addition salts with pharmaceutically acceptable acids. Application of them as monoamine oxidase, in particular MAO-B, inhibitors.
机译:本发明涉及通式(I)的1,3,4-恶二唑-2(3H)-一衍生物,其中R1代表氢原子或直链或支链(C1-4)烷基,被羟基,苯氧基,(C1-4)烷氧基,(C1-4)烷硫基,巯基,(C1-4)烷氧基(C1-4)烷氧基,二(C1-4)烷氨基或N-(C1 -4)烷基-N-丙炔基氨基或(C3-4)炔基,并且R2代表直链或支链(C1-8)烷基,其被一个或多个卤素原子和/或纯对映异构体或对映异构体混合物(包括外消旋混合物)及其与药学上可接受的酸的加成盐形式的羟基,1-咪唑基或3-四氢吡喃基或三氟(C3-5)烯基。它们作为单胺氧化酶,特别是MAO-B抑制剂的应用。

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