申请人:Takeda Chemical Industries, Ltd.
公开号:US04255576A1
公开(公告)日:1981-03-10
The present invention relates to novel 1-azaxanthone derivatives, which are shown by the following formula: ##STR1## wherein m is 1 or 2 R'.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxycarbonyl, hydroxy, C.sub.1-4 alkoxy, amino or C.sub.1-3 alkylamino; each of R.sub.2 is independently C.sub.1-6 alkyl, C.sub.1-4 alkoxy, halogen, nitro, hydroxy, carboxy, amino, C.sub.1-3 alkylamino or di(C.sub.1-3 alkyl) amino; or when m is 2, the two R.sub.2 groups may be independently as defined above or may form together with adjacent rings carbon atoms the butadienylene group; R.sub.3 is cyano, C.sub.1-6 alkoxycarbonyl, carboxamide, N-C.sub.1-3 alkylcarboxamide or N,N-di(C.sub.1-3 alkyl) carboxamide. The novel derivatives are useful as intermediates for 1-azaxanthone-3-carboxylic acid derivatives having effective antiallergic and bronchodilating activities.
本发明涉及新型1-氮杂黄酮衍生物,其由以下式表示:##STR1## 其中m为1或2,R'.sub.1为氢、C.sub.1-6烷基、苯基、C.sub.1-6烷氧羰基、羟基、C.sub.1-4烷氧基、氨基或C.sub.1-3烷基氨基;每个R.sub.2独立地为C.sub.1-6烷基、C.sub.1-4烷氧基、卤素、硝基、羟基、羧基、氨基、C.sub.1-3烷基氨基或二(C.sub.1-3烷基)氨基;或当m为2时,两个R.sub.2基团可以独立地定义如上,或者可以与相邻环的碳原子一起形成丁二烯基团;R.sub.3为氰基、C.sub.1-6烷氧羰基、羧酰胺、N-C.sub.1-3烷基羧酰胺或N,N-二(C.sub.1-3烷基)羧酰胺。这些新型衍生物可用作具有有效抗过敏和支气管扩张活性的1-氮杂黄酮-3-羧酸衍生物的中间体。