PYRIDYL IMIDAZOBENZODIAZEPINE PROPIONATE COMPOUND AND SYNTHESIS AND USE THEREOF

    公开(公告)号:EP3730495A1

    公开(公告)日:2020-10-28

    申请号:EP18894266.8

    申请日:2018-12-28

    发明人: QI, Youmao

    摘要: Disclosed are a pyridyl imidazobenzodiazepine propionate (compound 1) and the synthesis and use thereof. Also provided are intermediates for the preparation. Compound 1 provided by the present invention has an obvious venous anesthesia activity equivalent to that of the positive control drug remimazolam p-toluenesulfonate or remimazolam besylate. In addition, compound 1 can be significantly reduced in mouse model experiments, and same can even overcome common limb jitters, head tilting, opisthotonus and other side effects caused by the remimazolam besylate or remimazolam p-toluenesulfonate as a drug during development in preclinical animal experiments, thereby allowing same to be used in the preparation of intravenous anesthetics. The structural general formula of compound 1 is as follows, wherein each group and substituent are as defined in the description.