Amide derivatives as selective serotonin re-uptake inhibitors

   
   

The present invention relates to compounds of formula (I), 1 wherein R.sup.1 is selected from: (a) (C.sub.1-C.sub.6)alkyl, optionally substituted by 1-3 substituents, each independently selected from: (i) CF.sub.3, OH, (C.sub.1-C.sub.6)alkyl, (C.sub.3-C.sub.6)cycloalkyl, (C.sub.1-C.sub.6)alkoxy and halo. (ii) Phenyl, optionally fused with phenyl or cyclohexyl, said phenyl or fused phenyl optionally substituted with 1-3 groups selected from (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkyl ester, OH and halo; and (b) (C.sub.3-C.sub.6)cycloalkyl, optionally fused with (C.sub.5-C.sub.7)cycloalkyl, said cycloalkyl or fused cycloalkyl optionally substituted by OH, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy and halo. R.sup.2 is Phenyl, optionally fused to (C.sub.4-C.sub.6)cycloalkyl, phenyl or pyridyl, said phenyl or fused phenyl moiety optionally substituted with 1-3 groups each independently selected from (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy, halo and OH; n is 1 to 2; and pharmaceutically acceptable salts, solvates or polymorphs thereof; With the proviso that when n is 2 and R.sup.1 is 2-(3,4-dimethoxylphenyl)-- 1-ethyl, 3,3-diphenyl-1-propyl or 2,4-difluorophenyl, then R.sup.2 cannot be 4-trifluoromethoxyphenyl, 2,4,6-trimethoxyphenyl, 4-acetoxyphenyl or 2,4-difluorophenyl; which are a class of selective serotonin re-uptake inhibitors (SSRIs).

Присытствыющий вымысел относит к смесям формулы (i), 1 при котором R.sup.1 выбрано от: (a) (C.sub.1-C.sub.6)alkyl, опционно замененное 1-3 заместителями, каждым независимо выбранным от: (i) CF.sub.3, oh, (C.sub.1-C.sub.6)alkyl, (C.sub.3-C.sub.6)cycloalkyl, (C.sub.1-C.sub.6)alkoxy и венчик. (ii) Фенил, опционно сплавленный с фениловым или циклогексилом, сказанным фениловым или сплавленным фенилом опционно заменил при 1-3 групп выбранных от (C.sub.1-C.sub.6)alkyl, (эстер C.sub.1-C.sub.6)alkyl, oh и венчик; и (b) (C.sub.3-C.sub.6)cycloalkyl, опционно сплавленное с (C.sub.5-C.sub.7)cycloalkyl, сказанное cycloalkyl или сплавленное cycloalkyl опционно замененное oh, (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy и венчик. R.sup.2 фенилово, опционно после того как я сплавлено (C.sub.4-C.sub.6)cycloalkyl, фенил или pyridyl, сказанный фениловый или сплавленный фениловый moiety опционно заменили с 1-3 группами каждым независимо выбранным от (C.sub.1-C.sub.6)alkyl, (C.sub.1-C.sub.6)alkoxy, венчик и oh; н от 1 до 2; и фармацевтически приемлемо соли, solvates или полиморфы thereof; With the proviso that когда н 2 и R.sup.1 2-(3,4-dimethoxylphenyl) -- 1-ethyl, 3,3-diphenyl-1-propyl или 2,4-difluorophenyl, после этого R.sup.2 не могут быть 4-trifluoromethoxyphenyl, 2,4,6-trimethoxyphenyl, 4-acetoxyphenyl или 2,4-difluorophenyl; будут тип селективных иов АБС битор ре-ponimani4 серотонина (SSRIs).

 
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