申请人:A.H. ROBINS COMPANY, INCORPORATED
(a Delaware corporation)
公开号:EP0295833A1
公开(公告)日:1988-12-21
Novel aromatic-spiropiperidineoxazepinones and thiones exhibiting antihistamine activity are disclosed having the formula:
wherein A represents an aromatic ring, selected from benzo when Z is carbon or pyrido[3,2-f] when Z is nitrogen either of which rings may be optionally substituted on carbon;
B is selected from oxygen or sulfur;
R¹ is selected from the group consisting of loweralkyl, cycloalkyl, cycloalkyl-loweralkyl or phenyl-loweralkyl of which phenyl may be optionally substituted;
R is selected from the group consisting of loweralkyl, cycloalkyl or phenyl-loweralkyl of which phenyl may be optionally substituted and the pharmaceutically acceptable salts thereof and novel chemical intermediates in the preparation thereof.
本发明公开了具有抗组胺活性的新型芳香-硫代哌啶氧氮杂环庚酮和硫酮,其式如下
其中 A 代表芳香环,当 Z 为碳时,选自苯并环,当 Z 为氮时,选自吡啶并[3,2-f]环;
B 选自氧或硫;
R¹ 选自低烷基、环烷基、环烷基-低烷基或苯基-低烷基组成的组,其中苯基可被任选取代;
R¹选自低级烷基、环烷基或苯基-低级烷基(其中苯基可被任选取代)组成的组,以及它们的药学上可接受的盐和制备它们的新型化学中间体。