摘要 |
The quaternary ammonium N-glucuronide adduct of 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-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 GABAA receptors, in particular having high affinity for the alpha 2 and/or alpha 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.
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申请人 |
MERCK & CO., INC.;ARISON, BYRON, HALEVY;BRAUN, MATTHEW, PAUL;CUI, DONGHUI;POLSKY, STACEY, LYNN;RODRIGUES, A., DAVID;VEGA, JOSE, MIGUEL;VICKERS, STANLEY |
发明人 |
ARISON, BYRON, HALEVY;BRAUN, MATTHEW, PAUL;CUI, DONGHUI;POLSKY, STACEY, LYNN;RODRIGUES, A., DAVID;VEGA, JOSE, MIGUEL;VICKERS, STANLEY |