首页> 外国专利> 6,7-ASYMMETRICALLY DISUBSTITUTED QUINOXALINECARBOXYLIC ACID DERI VATIVES, ADDITION SALTS THEREOF, AND PROCESSES FOR THE PREPARATION OF BOTH

6,7-ASYMMETRICALLY DISUBSTITUTED QUINOXALINECARBOXYLIC ACID DERI VATIVES, ADDITION SALTS THEREOF, AND PROCESSES FOR THE PREPARATION OF BOTH

机译:6,7-非对称取代的喹喔啉羧酸衍生物,其另外的盐以及两者的制备方法

摘要

The present invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor, having 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives and their addition salts as effective ingredients, and processes for preparing them, and relates to 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives represented by a general formula (1) [wherein, Q denotes a halogen atom, lower alkyl group which may be substituted with halogen atom, general formula (2)        Ar-P-     (2)(wherein Ar denotes a phenyl group or naphthyl group which may have one or more substituents, and P denotes a lower alkylene, lower alkenylene, lower alkynylene, oxygen or sulfur atom), or general formula (3);        L-A-     (3)R denotes a nitro group, trifluoromethyl group, amino group which may be substituted, or general formula (7),R1 denotes an aralkyl group, phenyl group, naphthyl group, 5- or 6-membered heterocycle and its condensed ring (these may have one or more substituents on aromatic ring or heterocycle), hydrogen atom, lower alkyl group which may be substituted with halogen atom or cycloalkyl group, and R2 denotes a hydroxyl group, lower alkoxy group or general formula (6) ], and their addition salts.
机译:本发明提供了具有对抗性氨基酸受体,特别是AMPA受体,具有6,7-不对称双取代喹喔啉羧酸衍生物及其加成盐作为有效成分的拮抗剂,及其制备方法,涉及6,7-通式(1)表示的不对称二取代喹喔啉羧酸衍生物 <图像文件=“ IMGA0001.GIF” he =“ 40” id =“ ia01” imgContent =“ chem” imgFormat =“ GIF” wi =“ 82” /> [其中,Q表示卤素原子,可以被卤素原子取代的低级烷基,通式(2) Ar-P-(2)(其中Ar表示可具有一个或多个取代基的苯基或萘基,P表示低级亚烷基,低级亚烯基,低级亚炔基,氧或硫原子)或通式(3); L-A-(3) R表示硝基,三氟甲基,可以被取代的氨基或通式(7), <图像文件=“ IMGA0002.GIF” he =“ 27” id =“ ia02” imgContent =“ chem” imgFormat =“ GIF” wi =“ 78” /> <! -EPO -> R 1 表示芳烷基,苯基,萘基,5元或6元杂环及其稠环(在芳香环或杂环上可具有一个或多个取代基),氢原子,可被卤素原子或环烷基取代的低级烷基,R 2 表示羟基,低级烷氧基或通式(6) <图像文件=“ IMGA0003.GIF” he =“ 25” id =“ ia03” imgContent =“ chem” imgFormat =“ GIF” wi =“ 104” /> ],及其加成盐。

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