Back to results
US 6,476,030 B1Granted
Pyrazolo-triazine derivatives as ligands for GABA receptors
AssigneeMerck Sharp & Dohme Corp.
InventorsWilliam Robert Carling, Andrew Mitchinson, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
Life of this patent
Estimating the term…
Abstract
Compounds according to Formula (I): or a salt or prodrug thereof, have good affinity as ligands for the alpha2 and/or alpha3 subunit of the human GABAA receptor and are useful for treatment of disorders of the central nervous system, including anxiety and convulsions.
Claims9
A compound of formula I, or a salt thereof:
- wherein
- Z represents halogen;
- or C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, C6-8 bicycloalkyl, di(C1-6)alkylamino, phenyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridinyl, quinolinyl, isoquinolinyl, pyridazinyl, pyrimidinyl, pyrazinyl, quinoxalinyl, furyl, benzofuryl, dibenzofuryl, thienyl, benzthienyl, pyrrolyl, indolyl, pyrazolyl, indazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, benzimidazolyl, oxadiazolyl, thiadiazolyl, triazolyl or tetrazolyl, which may be optionally substituted with a substitutent selected from C1-6 alkyl, phenylC1-6 alkyl, halogen, cyano, hydroxy, hydroxymethyl, C1-6 alkoxy and C3-7 cycloalkylC1-6 alkyl;
- R1 represents C3-7 cycloalkyl, phenyl, furyl, thienyl, pyridinyl or pyrazinyl, which may be optionally substituted with a substitutent selected from C1-6 alkyl, phenylC1-6 alkyl, halogen, cyano, hydroxy, hydroxymethyl, C1-6 alkoxy and C3-7 cycloalkylC1-6 alkyl;
- and
- R2 represents C3-7 cycloalkyl(C1-6)alkyl, phenyl(C1-6 alkyl), azetidinyl(C1-6 alkyl), pyrrolidinyl(C1-6 alkyl), piperidinyl(C1-6 alkyl), piperazinyl(C1-6 alkyl), morpholinyl(C1-6 alkyl), thiomorpholinyl(C1-6 alkyl), pyridinyl(C1-6 alkyl), quinolinyl(C1-6 alkyl), isoquinolinyl(C1-6 alkyl), pyridazinyl(C1-6 alkyl), pyrimidinyl(C1-6 alkyl), pyrazinyl(C1-6 alkyl), quinoxalinyl(C1-6 alkyl), furyl(C1-6 alkyl), benzofuryl(C1-6 alkyl), dibenzofuryl(C1-6 alkyl), thienyl(C1-6 alkyl), benzthienyl(C1-6 alkyl), pyrrolyl(C1-6 alkyl), indolyl(C1-6 alkyl), pyrazolyl(C1-6 alkyl), indazolyl(C1-6 alkyl), oxazolyl(C1-6 alkyl), isoxazolyl(C1-6 alkyl), thiazolyl(C1-6 alkyl), isothiazolyl(C1-6 alkyl), imidazolyl(C1-6 alkyl), benzimidazolyl(C1-6 alkyl), oxadiazolyl(C1-6 alkyl), thiadiazolyl(C1-6 alkyl), triazolyl(C1-6 alkyl) or tetrazolyl(C1-6 alkyl), which may be optionally substituted with a substitutent selected from C1-6 alkyl, phenylC1-6 alkyl, halogen, cyano, hydroxy, hydroxymethyl, C1-6 alkoxy and C3-7 cycloalkylC1-6 alkyl.
3 more elements
A compound represented by formula IIB, and pharmaceutically acceptable salts thereof:
- wherein
- Q represents the residue of a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, pyridinyl, furyl or thienyl ring;
- R3a represents hydrogen, methyl, fluoro, chloro, trifluoromethyl, cyano or amino;
- R3b represents hydrogen or fluoro;
- and
- R4 represents hydrogen, methyl, ethyl, n-propyl, isopropyl, fluoroethyl or difluoroethyl.
3 more elements
A compound selected from:
- 7-(2-fluorophenyl)-2-(2-methyl-2H-[1,2,4]triazol-3-ylmethoxy)-3-phenyl-pyrazolo[1,5-d][1,2,4]triazine;
- and salts thereof.
Dependencies are inferred from the claim text.