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US 2006/0148809 A1Published application
Pyridazine derivatives as ligands for gaba receptors
AssigneeMerck Sharp & Dohme Corp.
InventorsStephen Fletcher, Angus Macleod, Monique Van Niel, Kevin Wilson
Life of this patent
Estimating the term…
Abstract
A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
Claims10
1-9. (canceled)
A compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof:
- wherein:
- Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole;
- or
- Z represents an optionally substituted six-membered heteroaromatic ring selected from pyridine, pyrazine, pyrimidine and pyridazine;
- or
- Z represents an optionally substituted fused bicyclic heteroaromatic moiety selected from benzofuran, benzothiophene, indole, indazole, benzimidazole and pyrazolo(1,5-a)pyridine;
- R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa═NORb;
- and
- Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group.
6 more elements
A compound which is selected from:
- 3-phenyl-5-(pyridin-4-yl)pyridazine;
- 3-(6-phenylpyridazin-4-yl)thiophene-2-carboxylic acid methyl ester;
- 3-phenyl-5-(pyridin-3-yl)pyridazine;
- 5-(6-phenylpyridazin-4-yl)thiophene-2-sulfonic acid amide;
- 3-(6-phenylpyridazin-4-yl)pyrazolo[1,5-α]pyridine;
- 2-[2-(6-phenylpyridazin-4-yl)pyrimidin-4-yl]benzonitrile;
- 2-[6-(6-phenylpyridazin-4-yl)pyridin-2-yl]benzonitrile;
- 5-fluoro-2-[6-(6-phenylpyridazin-4-yl)pyridin-2-yl]benzonitrile;
- 4-fluoro-2-[6-(6-phenylpyridazin-4-yl)pyridin-2-yl]benzonitrile;
- 5-[2-(3-fluorophenyl)pyridin-4-yl]-3-phenylpyridazine;
- 3-phenyl-5-[2-(pyridin-4-yl)pyrimidin-4-yl]pyridazine;
- 3-phenyl-5-(2-trifluoromethylpyrimidin-4-yl)pyridazine;
- and pharmaceutically acceptable salts thereof.
10 more elements
Dependencies are inferred from the claim text.