US 7,528,127 B2 · Short-acting benzodiazepines

Abstract

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.

Claims10

Dependent claims

A compound of formula (I):

wherein
W is H, a C1-C4 branched alkyl, or straight chained alkyl;
X is CH2, NH or NCH3;
n is 1 or 2;
Y is O or CH2;
m is 0 or 1, provided that if X is CH2, n is 1 and m is 0, then R1 is not CH2CH3;
R1 is H, a C1-C7 straight chain alkyl, a C3-C7 branched chain alkyl, a C1-4haloalkyl, a C3-C7 cycloalkyl, an aryl, a heteroaryl, an aralkyl, or a heteroaralkyl;
R2 is phenyl, 2-halophenyl or 2-pyridyl,
R3 is H, Cl, Br, F, I, CF3 or NO2;
R8 is hydrogen, C1-4alkyl or C1-3hydroxyalkyl;
U is CR9 where R9 is H, C1-3hydroxyalkyl, C1-4alkoxy, or C1-4alkyl;
and V is CH;
or a pharmaceutically acceptable salt or solvate thereof.

10 more elements

Dependencies are inferred from the claim text.

Short-acting benzodiazepines

Life of this patent

Short-acting benzodiazepines

Life of this patent

Abstract

Claims10