公开(公告)号：EP1183243A1

公开(公告)日：2002-03-06

申请号：EP00930686.1

申请日：2000-05-12

申请人： GLAXO GROUP LIMITED

发明人： FELDMAN, Paul L.,Glaxo Wellcome Inc. ,  JUNG, David Kendall,Glaxo Wellcome Inc. ,  KALDOR, IstvanGlaxo Wellcome Inc. ,  PACOFSKY, Gregory J.,Glaxo Wellcome Inc. ,  STAFFORD, Jeffrey A.,Glaxo Wellcome Inc. ,  TIDWELL, Jeffrey H.,Glaxo Wellcome Inc.

IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D243/22 ,  C07D243/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D487/04 ,  A61K31/55

CPC分类号： C07D401/04 ,  C07D243/20 ,  C07D243/22 ,  C07D243/24 ,  C07D401/12 ,  C07D403/12 ,  C07D487/04

摘要： It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.