Triazolo-pyridazine derivatives as ligands for GABA receptors
AssigneeMerck & Co., Inc.
InventorsWilliam Robert Carling, Jose Luis Castro Pineiro, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
Life of this patent
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Abstract
A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro- or trifluoro-substituted phenyl ring at the 3-position, a triazolyl-methoxy moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
Claims15
A compound of formula I, or a pharmaceutically acceptable salt thereof:
- 15
- wherein
- Y represents hydrogen and Z represents fluoro, or Y represents fluoro and Z represents hydrogen or fluoro;
- and
- R1 represents methyl or ethyl.
A compound as claimed in any one of the preceding claims wherein R1 represents methyl.
A compound selected from:
- 3-(2,5-difluorophenyl)-7-(1,1-dimethylethyl)-6-(2-methyl-2H-1,2,4-triazol-3-ylmethoxy)-1,2,4-triazolo[4,3-b]pyridazine;
- 3-(2,5-difluorophenyl)-7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-1,2,4-triazolo[4,3-b]pyridazine;
- and pharmaceutically acceptable salts thereof.
A compound selected from:
- 3-(2,6-difluorophenyl)-7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-1,2,4-triazolo[4,3-b]pyridazine;
- and pharmaceutically acceptable salts thereof.
A compound selected from:
- 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2,3,6-trifluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine;
- 7-(1,1-dimethylethyl)-6-(2-methyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2,3,6-trifluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine;
- 7-(1,1-dimethylethyl)-6-(1-methyl-1H-1,2,4-triazol-3-ylmethoxy)-3-(2,3,6-trifluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine;
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.