THERAPEUTISCHE CHINUCLIDINDERIVATE.

摘要

PCT No. PCT/US89/05338 Sec. 371 Date Jul. 20, 1990 Sec. 102(e) Date Jul. 20, 1990 PCT Filed Nov. 20, 1989 PCT Pub. No. WO90/05729 PCT Pub. Date May 31, 1990.A series of cis-3-[(cyclic)methylamino]-2-[( alpha -substituted)arylmethyl]quinuclidines, 3-[(cyclic)methylimino]-2-[( alpha -substituted)-arylmethyl]quinuclidines and cis-3-[(cyclic)-methyleneamino]-2-[( alpha -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-benzhydrylquinuclidine and cis-[(2-methoxyphenyl)methylamino]-2-benzhydrylquinuclidine. Methods for preparing these compounds from known starting materials are provided.