Patent TW-412512-B (TW)
Title: Non-peptide tachykinin receptor antagonists
Inventor: CHO SUNG-YONG STEPHEN
IPC: C07D409/12
Filed: 1994-11-16
Granted: 2000-11-21
Abstract: A compound of the formula, wherein m 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 R groups may be substituted with one or two halo, C1-C3 alkoxy, trifluoromethyl, C1-C4 alkyl, phenyl-C1-C3 alkoxy, or C1-C4 alkanoyl groups; R1 is trityl, phenyl, diphenylmethyl, phenoxy, phenylthio, hexamethyleneiminyl, piperazinyl, piperidinyl, pyrrolidinyl, morpholinyl, indolinyl, indolyl, benzothienyl, benzofuranyl, quinolinyl, tetrahydropyridinyl, isoquinolinyl, reduced quinolinyl, reduced isoquinolinyl, phenyl-(C1-C4 alkyl)-, phenyl-(C1-C4 alkoxy)-, quinolinyl-(C1-C4 alkyl)-, isoquinolinyl-(C1-C4 alkyl)-, reduced quinolinyl-(C1-C4 alkyl)-, reduced isoquinolinyl-(C1-C4 alkyl)-, benzoyl-(C1-C3 alkyl)-, C1-C4 alkyl, or -NH-CH2-R5; any one of which R1 groups may be substituted with halo, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, amino, C1-C4 alkylamino, or di(C1-C4 alkyl)amino; or any one of which R1 groups may be substituted with phenyl, piperazinyl, C3-C8 cycloalkyl, benzyl, C1-C4 alkyl, piperidinyl, pyridinyl, pyrimidinyl, C2-C6 alkanoylamino, pyrrolidinyl, C2-C6 alkanoyl, or C1-C4 alkoxycarbonyl; any one of which groups may be substituted with halo, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, amino, C1-C4 alkylamino, di(C1-C4 alkyl)amino, or C2-C4 alkanoylamino; or R1 is amino, a leaving group, hydrogen, C1-C4 alkylamino, or di(C1-C4 alkyl)amino; R5 is pyridyl, anilino-(C1-C3 alkyl)-, or anilinocarbonyl; R2 is hydrogen, C1-C4 alkyl, arylsulfonyl, C1-C4 alkylsulfonyl, carboxy-(C1-C3 alkyl)-, C1-C3 alkoxycarbonyl-(C1-C3 alkyl)-, or -CO-R6; R6 is hydrogen, C1-C4 alkyl, C1-C3 haloalkyl, phenyl, C1-C3 alkoxy, C1-C3 hydroxyalkyl, amino, C1-C4 alkylamino, di(C1-C4 alkyl)amino, or -(CH2)q-R7; q is 0 to 3; R7 is phenoxy, phenylthio, piperazinyl, piperidinyl, pyrrolidinyl, morpholinyl, indolinyl, indolyl, benzothienyl, benzofuranyl, quinolinyl, isoquinolinyl, reduced quinolinyl, reduced isoquinolinyl, phenyl-(C1-C4 alkyl)-, quinolinyl-(C1-C4 alkyl)-, isoquinolinyl-(C1-C4 alkyl)-, reduced quinolinyl-(C1-C4 alkyl)-, reduced isoquinolinyl-(C1-C4 alkyl)-, benzoyl-C1-C3 alkyl; any one of which R7 groups may be substituted with halo, trifluoromethyl, C1-C4 alkoxy, amino, C1-C4 alkylamino, di(C1-C4 alkyl) amino, or C2-C4 alkanoylamino; or any one of which R7 groups may be substituted with phenyl, piperazinyl, C3-C8 cycloalkyl, benzyl, piperidinyl, pyridinyl, pyrimidinyl, pyrrolidinyl, C2-C6 alkanoyl, C1-C4 alkyl, or C1-C4 alkoxycarbonyl; any of which groups may be substituted with halo, trifluoromethyl, amino, C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino, di(C1-C4 alkyl) amino, or C2-C4 alkanoylamino; or R7 is carboxy, C1-C4 alkoxycarbonyl, C1-C4 alkylcarbonyloxy, amino, C1-C4 alkylamino, di(C1-C4 alkyl)amino, C1-C6 alkoxycarbonylamino; R8 is hydrogen or C1-C6 alkyl; R3 is phenyl, phenyl-(C1-C6 alkyl)-, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, C1-C8 alkyl, naphthyl, C2-C8 alkenyl, or hydrogen; any one of which group except hydrogen may be substituted with one or two halo, C1-C3 alkoxy, C1-C3 alkylthio, nitro, trifluoromethyl, or C1-C3 alkyl groups; and R4 is hydrogen or C1-C3 alkyl; with the proviso that if R1 is hydrogen or halo, R3 is phenyl, phenyl-(C1-C6 alkyl)-, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, or naphthyl; or a pharmaceutically acceptable salt or solvate thereof.