申请人:WARNER-LAMBERT COMPANY
公开号:EP0175541A1
公开(公告)日:1986-03-26
Aminoalkoxybenzopyranones of the formula
or a pharmaceutically acceptable acid addition salt thereof; wherein
n is an integer from 2-5;
R is hydrogen, lower alkyl, trofluoromethyl, or lower alkoxy;
R1 is a radical of the formula
in which --- represents a single or double bond, Ar is phenyl or phenyl substituted by lower alkyl, lower alkoxy, lower thioalkoxy, halogen, or trifluoromethyl, and in which Het is chosen from the following heterocyclic radicals (a) 2-, 3-, or 4-pyridinyl or 2-, 3-, or 4-pyridinyl substituted by lower alkyl, lower alkoxy, or halogen, (b) 2-, 4-, or 5-pyrimidinyl, or 2-, 4-, or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy, or halogen, (c) 2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy, or halogen, (d) 2- or 3-thienyl, or 2- or 3-thienyl substituted by lower alkyl or halogen, (e) 2- or 3-furanyl, or 2-or 3-furanyl substituted by lower alkyl or halogen, or (f) 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen; with the exclusion of the compound in which n is 3, R is methyl, and R, is a radical of the formula
Also described are processes for producing the compounds, and pharmaceutical compositions comprising the compounds.
式中的氨基烷氧基苯并吡喃酮
或其药学上可接受的酸加成盐; 其中
n 是 2-5 之间的整数
R 是氢、低级烷基、三氟甲基或低级烷氧基;
R1 是式中的一个基团
其中 --- 代表单键或双键,Ar 是苯基或被低级烷基、低级烷氧基、低级硫代烷氧基、卤素或三氟甲基取代的苯基,其中 Het 选自以下杂环基 (a) 2-、3-或 4-吡啶基或被低级烷基、低级烷氧基或卤素取代的 2-、3-或 4-吡啶基, (b) 2-、4-或 5-嘧啶基或被低级烷基、低级烷氧基或卤素取代的 2-、4-、(c) 2-吡嗪基,或被低级烷基、低级烷氧基或卤素取代的 2-吡嗪基, (d) 2-或 3-噻吩基,或被低级烷基或卤素取代的 2-或 3-噻吩基, (e) 2-或 3-呋喃基,或被低级烷基或卤素取代的 2-或 3-呋喃基,或 (f) 2-或 5-噻唑基,或被低级烷基或卤素取代的 2-或 5-噻唑基;其中 n 为 3、R 为甲基、R 为式中自由基的化合物除外。
还描述了生产这些化合物的工艺和包含这些化合物的药物组合物。