EP0714891A1 — Heterocyclic tachykinin receptor antagonists

USPTO Abstract

This invention provides a novel series substituted piperidines, pyrrolidines, and hexamethyleneimines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds. The compounds have the formula wherein:    p is 1, 2, or 3;    m and n are independently 0-6;    X is         N-R a , or CH-NR b R c ,    where R a , R b , and R c are independently selected from the group consisting of hydrogen and C 1 -C 6 alkyl;    R 1 and R 2 are independently hydrogen, halo, trifluoromethyl, trichloromethyl, C 1 -C 6 alkyl, or C 1 -C 6 alkoxy; and    R 3 , R 4 , and R 5 are independently selected from the group consisting of hydrogen, halo, trifluoromethyl, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, cyano, hydroxy, amino, -NHCONH 2 , nitro, -CONH 2 , C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkenyl, C 3 -C 8 cycloalkoxy, C 1 -C 10 alkylthio, C 1 -C 10 alkylamino, C 2 -C 6 alkanoyl, and C 2 -C 6 alkanoyloxy; or a pharmaceutically acceptable salt or solvate thereof.