Arylkalkyl-amines and -amides having anticonvulsant and neuroprotective properties
申请人:Astra Aktiebolag
公开号:EP0356035A2
公开(公告)日:1990-02-28
There is provided the use of a compound of formula I in the preparation of a medicament for use in the prevention or treatment of neurological disorders,
wherein,
Ar₁ and Ar₂, which may be the same or different, independently represent phenyl substituted by one or more of amino, nitro chlorine, bromine, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano; in addition one of Ar₁ or Ar₂ may also represent phenyl;
R₁ represents hydrogen or C1 to 6 alkyl;
R₂ represents hydrogen or COCH₂NH₂;
R₃ represents hydrogen or C1 to 6 alkyl;
provided that when R₂ represents hydrogen, then one or both of Ar₁ and Ar₂ may also represent phenyl, fluorophenyl or 2-, 3- or 4- pyridinyl and R₁ may also represent C1 to 6 alkoxycarbonyl or trifluoromethyl;
or a pharmaceutically acceptable salt thereof.
Some of the compounds of formula I are novel, and there are provided processes for making these, together with processes for making pharmaceutical compositions containing the novel compounds.
提供了式 I 化合物在制备用于预防或治疗神经系统疾病的药物中的用途、
其中
Ar₁和Ar₂可以相同或不同,独立地代表被氨基、硝基氯、溴、羟基、C1~6 烷氧基、C1~6 烷基或氰基中的一个或多个取代的苯基;此外,Ar₁或Ar₂中的一个也可以代表苯基;
R₁ 代表氢或 C1 至 6 烷基;
R₂ 代表氢或 COCH₂NH₂;
R₃ 代表氢或 C1 至 6 烷基;
但当 R₂ 代表氢时,Ar₁ 和 Ar₂ 中的一个或两个也可代表苯基、氟苯基或 2-、3- 或 4-吡啶基,R₁ 也可代表 C1-6 烷氧羰基或三氟甲基;
或其药学上可接受的盐。
式 I 的某些化合物是新型的,提供了制造这些化合物的工艺以及制造含有新型化合物的药物组合物的工艺。