1-[Styryl]- and 1-[2'-(heteroaryl)-ethenyl]-isoquinoline derivatives, a process for preparing them as well as medicaments containing them and the use of them
申请人:EGIS GYOGYSZERGYAR RT.
公开号:EP0680953A1
公开(公告)日:1995-11-08
A subject-matter of the invention are 1-[styryl]- and 1-[2'-(heteroaryl)-ethenyl]-isoquinoline derivatives having the formula
wherein
nis 1, 2, 3 or 4,
Rwhich represent(s) hydrogen, C₁₋₇-alkyl, C₁₋₇-alkoxy or hydroxy, or two substituents R form together a C₁₋₇-alkylenedioxy group attached to two adjacent ring carbon atoms,
R₁represents hydrogen or C₁₋₇-alkyl and
Arstands for an aryl or heteroaryl group containing one or two oxygen, nitrogen and/or sulfur atom(s), optionally carrying one or more substituent(s) selected from halogen, trihalomethyl, hydroxy, C₁₋₇-alkyl, C₁₋₇-alkoxy, C₁₋₇-alkylenedioxy (attached to two adjacent ring carbon atoms), cyano, nitro, amino, mono- and di-(C₁₋₇-alkyl)-amino,
as well as acid addition salts thereof.
Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use both of the novel and of the known compounds for preparing medicaments having an anxiolytic effect.
本发明的主题是具有以下式子的1-[苯乙烯基]-和1-[2'-(杂环芳基)-乙烯基]-异喹啉衍生物,其中n为1、2、3或4,R代表氢、C₁₋₇-烷基、C₁₋₇-烷氧基或羟基,或两个R取代基共同形成连接到相邻环碳原子的C₁₋₇-烷二氧基基团,R₁表示氢或C₁₋₇-烷基,Ar表示含有一个或两个氧、氮和/或硫原子的芳基或杂芳基基团,可选地携带一种或多种取代基,所述取代基选择自卤、三卤甲基、羟基、C₁₋₇-烷基、C₁₋₇-烷氧基、连接到相邻环碳原子的C₁₋₇-烷二氧基、氰基、硝基、氨基、单-和双-(C₁₋₇-烷基)-氨基,以及它们的酸加合物。此外,本发明涉及制备这些化合物的方法,以及含有它们的药物和使用新化合物和已知化合物制备具有抗焦虑作用的药物。