2-Substituted amino-4(1H)-pyrimidone derivatives, their production, and medical compositions containing them
申请人:YAMANOUCHI PHARMACEUTICAL CO. LTD.
公开号:EP0186275A2
公开(公告)日:1986-07-02
A 2-substituted amino-4 (1H)-pyrimidone derivative shown by the general formula
wherein R' and R2, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; R3 represents an alkyl group, an alkenyl group, an alkynyl group, a halogen-substituted alkyl group, a halogen-substituted alkenyl group, a halogen-substituted alkynyl group, or an alkyl group interrupted by an oxygen atom or a sulfur atom; R4 represents a hydrogen atom or a lower alkyl group; m is an integer of 1 or 3 and n is an integer of 2 or 4 (with said R4 being a lower alkyl group when R' and R2 are hydrogen atoms, R3 is an alkyl group, m is 2 and n is 3) or an acid addition salt thereof.
The compounds of this invention have both histamine H2-receptor antagonist activity and gastric cytoprotective activity and are very useful as drugs for gastric diseases.
通式如下的 2-取代氨基-4(1H)-嘧啶酮衍生物
其中 R'和 R2(可以相同或不同)各自代表氢原子或低级烷基;R3 代表烷基、烯基、炔基、卤素取代的烷基、卤素取代的烯基、卤素取代的炔基、或被氧原子或硫原子打断的烷基;R4 代表氢原子或低级烷基;m 为 1 或 3 的整数,n 为 2 或 4 的整数(当 R' 和 R2 为氢原子,R3 为烷基,m 为 2,n 为 3 时,所述 R4 为低级烷基)或其酸加成盐。
本发明的化合物同时具有组胺 H2 受体拮抗剂活性和胃细胞保护活性,作为治疗胃病的药物非常有用。