申请人:U C B S.A.
公开号:US04956367A1
公开(公告)日:1990-09-11
New 2-amino-4-morpholino-6-propyl-1,3,5-triazines having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, aralkyl or acetyl, R.sub.2 is hydroxyl, hydroxyalkyl, alkoxyalkyl, dialkylamino, arylhydroxyalkyl, (hydroxy-cycloalkyl)alkyl, alkanoyloxyalkyl, benzoyloxyalkyl, phenylacetyloxyalkyl, aminocarbonyloxyalkyl, COR.sub.3 or CONR.sub.4 R.sub.5, or NR.sub.1 R.sub.2 =(hydroxyalkyl)alkyleneimino, R.sub.3 =alkyl, aryl, haloaryl, alkylaryl, alkoxyaryl, aralkyl or aryloxy, R.sub.4 =R.sub.5 =hydrogen or alkyl, alkyl, alkoxy and alkanoyloxy having 1 to 4 carbon atoms, cycloalkyl and alkyleneimino having 4 to 6 carbon atoms. Moreover, when R.sub.1 is acetyl, R.sub.2 is acetoxyalkyl. Processes for the preparation thereof and pharmaceutical compositions containing the same are also given. In particular, these compounds are useful for the treatment of cognitive and behavioral disorders associated with aging and dementia syndromes, e.g. those associated with Alzheimer's disease.
新的2-氨基-4-吗啡基-6-丙基-1,3,5-三嗪具有以下式子:##STR1## 其中,R.sub.1是氢,烷基,芳基烷基或乙酰基,R.sub.2是羟基,羟基烷基,烷氧基烷基,二烷基氨基,芳基羟基烷基,(羟基-环烷基)烷基,烷酰氧基烷基,苯甲酰氧基烷基,苯乙酰氧基烷基,氨基羰氧基烷基,COR.sub.3或CONR.sub.4R.sub.5,或NR.sub.1R.sub.2=(羟基烷基)烷基亚氨基,R.sub.3=烷基,芳基,卤代芳基,烷基芳基,烷氧基芳基,芳基烷基或芳氧基,R.sub.4=R.sub.5=氢或烷基,烷基,烷氧基和烷酰氧基具有1至4个碳原子,环烷基和具有4至6个碳原子的烷基亚氨基。此外,当R.sub.1为乙酰基时,R.sub.2为乙酰氧基烷基。还给出了制备这些化合物和含有它们的制药组合物的方法。特别是,这些化合物对于治疗与老化和痴呆综合症相关的认知和行为障碍,例如与阿尔茨海默病相关的障碍,非常有用。