| abstract |
A series of cis-3-[(cyclic)methylamino]-2-[(α-substituted)arylmethyl]quinuclidines, 3-[(cyclic)methylimino]-2-[(α-substituted)-arylmethyl]quinuclidines and cis-3-[(cyclic)-methyleneamino]-2-[(α-substituted)arylmethyl]-quinuclidines, including their pharmaceutically acceptable salts, are disclosed. These particular compounds are found to be useful as substance P antagonists and therefore, are of value in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases and pain or migraine. Preferred member compounds include cis-3-[(2-chlorophenyl)methylamino]-2-benzhydryl-quinuclidine, cis-3-[(2-trifluorophenyl)methylamino]-2-benzhydryl-quinuclidine and cis-[(2-methoxyphenyl)methylamino]-2-benzhydrylquinuclidine. Methods for preparing these compounds from known starting materials are provided. |