(Phenylmethylene)-2-(alkyl)-1- omega-(amino)-alkoxyimino -cycloalkane 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:EP0619298A2
公开(公告)日:1994-10-12
A subject-matter of the invention are (phenylmethylene)-2-(alkyl)-1-[ω-(amino)-alkoxyimino]-cycloalkane derivatives of general formula
wherein
Rrepresents hydrogen, C₁₋₄ alkyl or hydroxyl,
R₁stands for C₁₋₁₂ alkyl,
R₂ and R₃independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl group,
or
R₂ and R₃together 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,
R₄ and R₅independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group, or together represent a 3,4-methylenedioxy group,
nis an integer from 2 to 5
and
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 effects.
本发明的一个主题是通式为(苯基亚甲基)-2-(烷基)-1-[ω-(氨基)-烷氧基亚氨基]-环烷烃衍生物
其中
R 代表氢、C₁₋₄ 烷基或羟基、
R₁ 代表 C₁₋₁₂ 烷基、
R₂ 和 R₃ 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
R₂ 和 R₃ 与它们所连接的氮原子一起形成一个 4-7 元杂环,该杂环可选择包含氧、硫或另一个氮原子,后者可选择带有苯基、苄基或 C₁₋₄烷基取代基、
R₄ 和 R₅ 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、
n 是 2 到 5 的整数
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作用的药物。