308243-45-0Relevant academic research and scientific papers
SHORT-ACTING BENZODIAZEPINES
-
Page/Page column 13, (2008/06/13)
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.
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists
Pacofsky, Gregory J.,Stafford, Jeffrey A.,Cox, Richard F.,Cowan, Jill R.,Dorsey Jr., George F.,Gonzales, Stephen S.,Kaldor, Istvan,Koszalka, George W.,Lovell, George G.,McIntyre, Maggie S.,Tidwell, Jeffrey H.,Todd, Dan,Whitesell, Graham,Wiard, Robert P.,Feldman, Paul L.
, p. 3219 - 3222 (2007/10/03)
The ultrashort-acting benzodiazepine (USA BZD) agonists reported previously have been structurally modified to improve aqueous solubility. Lactam-to-amidine modifications, replacement of the C5-haloaryl ring, and annulation of heterocycles are presented. These analogues retain BZD receptor potency and full agonism profiles.
