- SHORT-ACTING BENZODIAZEPINES
-
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.
- -
-
Page/Page column 31
(2008/06/13)
-
- Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists
-
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.
- 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)
-