Non-peptide tachykinin receptor antagonists

A method of treating a condition associated with an excess of tachykinins which comprises administering to a mammal in need thereof an effective amount of a compound of the formula ##STR34## wherein R.sup.a is 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;

• R.sup.1 is pyrrolidinyl, morpholinyl, indolinyl, indolyl, benzothienyl, benzofuranyl, quinolinyl, tetrahydropyridinyl, isoquinolinyl, reduced quinolinyl, or reduced isoquinolinyl,
• which 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 which 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 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 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;
• R.sup.2 is hydrogen, acetyl or methylsulfonyl;
• or a pharmaceutically acceptable salt or solvate thereof.

A pharmaceutical formulation comprising an effective amount of a compound of the formula ##STR35## wherein R.sup.a is 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;

• R.sup.1 is pyrrolidinyl, morpholinyl, indolinyl, indolyl, benzothienyl, benzofuranyl, quinolinyl, tetrahydropyridinyl, isoquinolinyl, reduced quinolinyl, or reduced isoquinolinyl,
• which 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 which 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 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 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;
• R.sup.2 is hydrogen, acetyl or methylsulfonyl;
• or a pharmaceutically acceptable salt or solvate thereof, in combination with one or ore pharmaceutically acceptable carriers, diluents, or excipients therefor.