C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/231, 260/272
C07D 453/02 (2006.01) A61K 31/44 (2006.01)
Patent
CA 2003441
A series of cis-3-[(cyclic)methylamino]-2- [(.alpha.-substituted)arylmethyl]quinuclidines, 3-[(cyclic)methylimino]-2-[(.alpha.-substitituted)- 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-quinuclidinne, 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.
Divulgation d'une série de cis-3-[(cyclic)méthylamino]-2- [(alpha-substitutant)arylméthyl]quinuclidines, 3-[(cyclic)méthylimino]-2-[(alpha-substituant)- arylméthyl]quinuclidines et cis-3-[(cyclo)- méthylèneamino]-2-[(alpha-substituant)arylméthyl]quinuclidines, incluant leurs sels acceptables en pharmacie. Ces composés sont utiles comme antagonistes de la substance P et, par conséquent, efficaces pour le traitement des problèmes gastro-intestinaux, des troubles du système nerveux central, des maladies inflammatoires, de la douleur et des migraines. Parmi les composés privilégiés, on peut citer les suivants : cis-3-[(2- chlorophényl)méthylamino]-2-benzhydrylquinuclidine, cis-3-[(2-trifluorophényl)méthylamino]2-benzhydryl- quinuclidine et cis-[(2-méthoxyphényl)méthylamino]- 2-benzhydrylquinuclidine. On présente les méthodes pour préparer ces composés à partir de matières premières connues.
Limited Pfizer
Smart & Biggar
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