申请人:Roussel Uclaf
公开号:US05053416A1
公开(公告)日:1991-10-01
Compounds of formula (I) ##STR1## in which X represents oxygen or sulphur, R.sub.1 represents hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, an alkenyl or alkynyl containing up to 6 carbon atoms, hydroxyl, an OCOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, an OCONHalk.sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon atoms, a CO.sub.2 alk.sub.3 radical in which alk.sub.3 represents alkyl or alkenyl containing up to 6 carbon atoms, an Oalk.sub.4 radical in which alk.sub.4 represents alkyl containing up to 6 carbon atoms, an OCOAr.sub.1, OCONHAr.sub.2 or CO.sub.2 Ar.sub.3 radical in which Ar.sub.1, Ar.sub.2 or Ar.sub.3 represents aryl containing up to 14 carbon atoms, R.sub.2 represents hydrogen, a linear, branched or cyclic alkyl containing up to 6 carbon atoms, alkenyl or alkynyl containing up to 6 carbon atoms, an alkoxyalkyl alk'.sub.1 Oalk'.sub.2 radical in which alk'.sub.1 and alk'.sub.2 represent alkyl containing up to 6 carabon atoms, hydroxyalkyl in which the alkyl contains up to 6 carbon atoms or aryl containing up to 14 carbon atoms, as well as their addition salts with organic or mineral acids, which compounds are useful in the treatment of patients suffering from Alzheimer's disease, senile dementia or memory disorders of the aged; also, compositions containing the same, method of use, method of preparation, and intermediates therefor.
化合物的式子(I) ##STR1## 其中X代表氧或硫,R.sub.1代表氢,线性、支链或环烷基,含有高达8个碳原子,烯基或炔基,含有高达6个碳原子,羟基,OCOalk.sub.1基团,其中alk.sub.1代表含有高达6个碳原子的烷基,OCONHalk.sub.2基团,其中alk.sub.2代表含有高达6个碳原子的烷基,CO.sub.2 alk.sub.3基团,其中alk.sub.3代表含有高达6个碳原子的烷基或烯基,Oalk.sub.4基团,其中alk.sub.4代表含有高达6个碳原子的烷基,OCOAr.sub.1,OCONHAr.sub.2或CO.sub.2 Ar.sub.3基团,其中Ar.sub.1,Ar.sub.2或Ar.sub.3代表含有高达14个碳原子的芳基,R.sub.2代表氢,线性、支链或环烷基,含有高达6个碳原子,烯基或炔基,含有高达6个碳原子,alkoxyalkyl alk'.sub.1 Oalk'.sub.2基团,其中alk'.sub.1和alk'.sub.2代表含有高达6个碳原子的烷基,含有高达6个碳原子的烷基的羟基烷基或含有高达14个碳原子的芳基,以及它们与有机或无机酸的加成盐,这些化合物在治疗患有阿尔茨海默病、老年性痴呆或老年人记忆障碍的患者中有用;此外,还包括含有相同化合物的组合物,使用方法,制备方法和中间体。