1-Alkoxy-naphthalene-2-carboxamide derivatives with high affinity for the serotonin 5-HT1A receptor
申请人:LILLY INDUSTRIES LIMITED
公开号:EP0585116A1
公开(公告)日:1994-03-02
Pharmaceutical compounds of the formula:
in which each R¹ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R² is hydrogen, C₁₋₄ alkyl or C₂₋₄ alkenyl, R³ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ alkylthio, halogen, nitro or -NR'R'' where R' and R'' are each hydrogen or C₁₋₄ alkyl, R⁴ and R⁵ are each hydrogen, C₁₋₄ alkyl, optionally substituted phenyl or C₆₋₉ cycloalkyl optionally substituted by 1 to 4 C₁₋₄ alkyl groups, R⁶ is optionally substituted phenyl,tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C₆₋₁₀ cycloalkyl optionally substituted with 1 to 4 C₁₋₄ alkyl groups or a phenyl group, or C₄₋₉ heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.
式中的药物化合物:
其中每个 R¹ 是氢、C₁₋₄ 烷基、C₁₋₄ 烷氧基、卤素或硝基,且 n 是 0、1、2 或 3;R² 是氢、C₁₋₄ 烷基或 C₂₋₄ 烯基;R³ 是氢、C₁₋₄ 烷基、C₁₋₄ 烷氧基、C₁₋₄ 硫代烷基、卤素、硝基或 -NR'R'' 其中 R' 和 R'' 分别为氢或 C₁₋₄ 烷基,R⁴ 和 R⁵ 分别为氢或 C₁₋₄ 烷基、R⁴ 和 R⁵ 各为氢、C 烷基、任选取代的苯基或任选被 1 至 4 个 C₁₋₄ 烷基取代的 C₆₋₉ 环烷基,R⁶ 为任选取代的苯基、四氢萘基、邻苯二甲酰亚胺基、糖精基、戊二酰亚胺基、C₆₋₁₀环烷基,可选被 1 至 4 个 C₁₋₄烷基或苯基取代,或 C₄₋₉杂代环烷基,可选被 1-4 个烷基取代,x 为 1、2 或 3,y 为 0 或 1,z 为 0、1、2 或 3;及其盐类。