Patent ID: 6303610
Filing Date: 2001-10-16
Classification: A61K,A61P

Abstract:
A method for the treatment of gout, which method comprises administering to a mammal in need of said treatment an effective amount of a compound of the formula I ##STR33##whereinm is 0 or 1;n is 0 or 1;o is 0, 1, or 2;p is 0 or 1;R is phenyl, 2- or 3-indolyl, 2- or 3-indolinyl, benzothienyl, benzofuranyl, or naphthyl;any one of which groups may be substituted with one or two halo, C.sub.1 -C.sub.3 alkoxy, trifluoromethyl, C.sub.1 -C.sub.4 alkyl, phenyl-C.sub.1 -C.sub.3 alkoxy, or C.sub.1 -C.sub.4 alkanoyl groups;R.sup.1 is trityl, phenyl, diphenylmethyl, phenoxy, phenylthio, piperazinyl, hexamethyleneiminyl, piperidinyl, pyrrolidinyl, morpholinyl, indolinyl, indolyl, benzothienyl, benzofuranyl, quinolinyl, isoquinolinyl, tetrahydropyridinyl, reduced quinolinyl, reduced isoquinolinyl, phenyl-(C.sub.1 -C.sub.4 alkyl)-, phenyl-(C.sub.1 -C.sub.4 alkoxy)-, quinolinyl-(C.sub.1 -C.sub.4 alkyl)-, isoquinolinyl-(C.sub.1 -C.sub.4 alkyl)-, reduced quinolinyl-(C.sub.1 -C.sub.4 alkyl)-, reduced isoquinolinyl-(C.sub.1 -C.sub.4 alkyl)-, benzoyl-(C.sub.1 -C.sub.3 alkyl)-, C.sub.1 -C.sub.4 alkyl, or --NH--CH.sub.2 -R.sup.5 ;any one of which R.sup.1 groups may be substituted with halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, amino, C.sub.1 -C.sub.4 alkylamino, or di(C.sub.1 -C.sub.4 alkyl) amino;or any one of which R.sup.1 groups may be substituted with phenyl, piperazinyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl, C.sub.1 -C.sub.4 alkyl, piperidinyl, pyridinyl, pyrimidinyl, C.sub.2 -C.sub.6 alkanoylamino, pyrrolidinyl, C.sub.2 -C.sub.6 alkanoyl, or C.sub.1 -C.sub.4 alkoxycarbonyl;any one of which groups may be substituted with halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, or C.sub.2 -C.sub.4 alkanoylamino;or R.sup.1 is amino, a leaving group, hydrogen, C.sub.1 -C.sub.4 alkylamino, or di(C.sub.1 -C.sub.4 alkyl)amino;R.sup.5 is pyridyl, anilino-(C.sub.1 -C.sub.3 alkyl)-, or anilinocarbonyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, arylsulfonyl, C.sub.1 -C.sub.4 alkylsulfonyl, carboxy-(C.sub.1 -C.sub.3 alkyl)-, C.sub.1 -C.sub.3 alkoxycarbonyl-(C.sub.1 -C.sub.3 alkyl)-, or --CO--R.sup.6 ;R.sup.6 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 haloalkyl, phenyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 hydroxyalkyl, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, or --(CH.sub.2).sub.q --R.sup.7 ;q is 0 to 3;R.sup.7 is phenoxy, phenylthio, piperazinyl, piperidinyl, pyrrolidinyl, morpholinyl, indolinyl, indolyl, benzothienyl, benzofuranyl, quinolinyl, isoquinolinyl, reduced quinolinyl, reduced isoquinolinyl, phenyl-(C.sub.1 -C.sub.4 alkyl)-, quinolinyl-(C.sub.1 -C.sub.4 alkyl)-, isoquinolinyl-(C.sub.1 -C.sub.4 alkyl)-, reduced quinolinyl-(C.sub.1 -C.sub.4 alkyl)-, reduced isoquinolinyl-(C.sub.1 -C.sub.4 alkyl)-, benzoyl-C.sub.1 -C.sub.3 alkyl;any one of which R.sup.7 groups may be substituted with halo, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, or C.sub.2 -C.sub.4 alkanoylamino;or any one of which R.sup.7 groups may be substituted with phenyl, piperazinyl, C.sub.3 -C.sub.8 cycloalkyl, benzyl, piperidinyl, pyridinyl, pyrimidinyl, pyrrolidinyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkoxycarbonyl;any of which groups may be substituted with halo, trifluoromethyl, amino, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, or C.sub.2 -C.sub.4 alkanoylamino;or R.sup.7 is carboxy, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylcarbonyloxy, amino, C.sub.1 -C.sub.4 alkylamino, di(C.sub.1 -C.sub.4 alkyl)amino, C.sub.1 -C.sub.6 alkoxycarbonylamino;R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.3 is phenyl, phenyl-(C.sub.1 -C.sub.6 alkyl)-, C.sub.3 -C.sub.8 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl, C.sub.1 -C.sub.8 alkyl, naphthyl, C.sub.2 -C.sub.8 alkenyl, or hydrogen;any one of which groups except hydrogen may be substituted with one or two halo, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio, nitro, trifluoromethyl, or C.sub.1 -C.sub.3 alkyl groups;andR.sup.4 is hydrogen or C.sub.1 -C.sub.3 alkyl;with the proviso that if R.sup.1 is hydrogen or halo, R.sup.3 is phenyl, phenyl-(C.sub.1 -C.sub.6 alkyl)-, C.sub.3 -C.sub.8 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl, or naphthyl;or a pharmaceutically acceptable salt or solvate thereof.