摘要:
Novel phenethylamine derivatives are central nervous system antidepressants. The compounds are those having the formula where A is where the dotted line represents optional unsaturation; R 1 and R 7 are, independently, hydrogen or C 1 -C 6 alkyl; R 2 is C 1 -C 6 alkyl; R 4 is hydrogen, C 1 -C 4 alkyl, formyl or C 2 -C 7 alkanoly; R 5 and R 6 are hydrogen or defined substituents and n is 0,1,2,3, or 4 and their pharmaceutically acceptable salts. Novel intermediates for the preparation of these compounds include those of the formulae
wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl; R¹ and R² are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R¹ and R² represent a methylenedioxy grouping; and the pharmacologically acceptable salts thereof are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids. Processes for preparing the compounds and pharmaceutical compositions containing them are also covered.
摘要翻译:式CHEM的化合物,其中R是氢,低级烷基,苄基或新戊酰氧基甲基; R 1和R 2独立地为氢,低级烷基,低级烷氧基,三氟甲基,三氟甲氧基,甲磺酰基氨基,乙酰氨基或卤素,或者当R 1和R 2表示亚甲二氧基时; 其药理学上可接受的盐是可用于治疗和预防由兴奋性氨基酸过度刺激引起的中枢神经系统相关病理状况的NMDA拮抗剂。 还包括制备含有它们的化合物和药物组合物的方法。