申请人:Ube Industries, Ltd.
公开号:US05610303A1
公开(公告)日:1997-03-11
A pyrimidine derivative represented by the formula (II) or (III): ##STR1## (wherein R.sup.1 and R.sup.2 each represent H, a halogen, amino, nitro, an unsubstituted or substituted alkyl, an alkoxy or an alkoxycarbonyl, or R.sup.1 and R.sup.2 are bonded together to form an unsubstituted or substituted alkylene; R.sup.3 represents an aralkyl or a hetero aromatic ring type-alkyl, R.sup.4 represents H or acyl, R.sup.5 represents H, OH or an alkoxy, R.sup.6 represents H, a halogen, an alkyl or an alkoxy, X represents --CH=, --CH=CH--(CH.sub.2).sub.p --, --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --(CH.sub.2).sub.p --, Y represents =CH-- (CH.sub.2).sub.p --, --CH.sub.2 --(CH.sub.2).sub.p --, a single bond or a double bond, p represents 0 or 1, and . . . represents a single bond or a double bond), and a salt thereof have selective acetylcholinesterase-inhibiting activities and selective A type monoamine oxidase-inhibiting activities, and are useful as an antidepressant and an agent for curing senile dementia.
式(II)或(III)表示的嘧啶衍生物:##STR1##(其中,R.sup.1和R.sup.2每个代表H,卤素,氨基,硝基,未取代或取代的烷基,烷氧基或烷氧羰基,或R.sup.1和R.sup.2结合形成未取代或取代的亚烷基; R.sup.3代表芳基烷基或杂环芳基烷基,R.sup.4代表H或酰基,R.sup.5代表H,OH或烷氧基,R.sup.6代表H,卤素,烷基或烷氧基,X代表--CH=,--CH=CH--(CH.sub.2).sub.p --,--CH.sub.2--或--CH.sub.2CH.sub.2--(CH.sub.2).sub.p --,Y代表=CH--(CH.sub.2).sub.p --,--CH.sub.2--(CH.sub.2).sub.p --,单键或双键,p代表0或1,而“...”代表单键或双键),以及其盐具有选择性乙酰胆碱酯酶抑制活性和选择性A型单胺氧化酶抑制活性,可用作抗抑郁剂和治疗老年痴呆症的药物。