Matthew J Paul

US Patent:

20040259818, Dec 23, 2004

Filed:

Jul 26, 2004

Appl. No.:

10/477025

Inventors:

Byron Halevy - Watchung NJ, US
Matthew Paul - Scotch Plains NJ, US
Donghui Cui - Chalfont PA, US
Stacey Polsky - Norristown, PA
A. David Rodrigues - Doylestown PA, US
Jose Vega - Westlake Village CA, US
Stanley Vickers - Penllyn PA, US

International Classification:

A61K031/7056
C07H019/22

US Classification:

514/043000, 536/027100

Abstract:

The quaternary ammonium N-glucuronide adduct of 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-yl-methoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine is cleavable by glucuronidase enzymes in the body and can thereby act as a prodrug of a therapeutic agent which is a selective ligand for GABAreceptors, in particular having high affinity for the 2 and/or 3 subunit thereof, and is accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.