1-(Phenyl)-3-[omega-(amino)-alkoxyimino]-alk-1-ene 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:EP0619299A2
公开(公告)日:1994-10-12
A subject-matter of the invention are 1-(Phenyl)-3-[ω-(amino)-alkoxyimino]-alk-1-ene derivatives of general formula
wherein
R₁ and R₂independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group or together represent a 3,4-methylenedioxy group,
Rstands for C₁₋₈ alkyl,
R₃represents hydrogen, C₁₋₄ alkyl or hydroxy,
R₄ and R₅independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl or C₃₋₆ cycloalkyl group,
óóóor
R₄ and R₅together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter optionally may carry a phenyl, benzyl or C₁₋₄ alkyl substituent
óóóand
Arepresents a valency bond or a -CH₂-group,
as well as stereo and optically active isomers and their mixtures, acid-addition salts and quaternary ammonium derivatives thereof.
Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use of them for preparing medicaments, particularly having ulcus and gastric-acid-secretion inhibiting and anxiolytic effects.
本发明的一个主题是通式为 1-(苯基)-3-[ω-(氨基)-烷氧基亚氨基]-烷-1-烯衍生物
其中
R₁ 和 R₂ 各自代表氢、卤素或 C₁₋₄ 烷氧基,或共同代表 3,4-亚甲二氧基、
R 代表 C₁₋₈ 烷基、
R₃ 代表氢、C₁₋₄ 烷基或羟基、
R₄ 和 R₅ 各自独立地代表氢、任选被羟基取代的 C₁₋₁₂ 烷基或 C₂₋₁₂ 烯基或 C₃₋₆ 环烷基、
或
R₄ 和 R₅ 与它们所连接的氮原子一起形成一个 4 至 7 元杂环,可选地包括一个氧原子、硫原子或另一个氮原子,后者可选地带有一个苯基、苄基或 C₁₋₄ 烷基取代基。
和
代表价键或 -CH₂ 基团、
以及立体异构体和光学活性异构体及其混合物、酸加成盐和季铵衍生物。
此外,本发明还涉及到制备这些化合物的工艺以及含有这些化合物的药物,以及使用这些化合物制备药物,特别是具有抑制溃疡和胃酸分泌以及抗焦虑作用的药物。