9-Amino-1,4-ethano-1,2,3,4-tetrahydroacridine and related compounds, intermediates and a process for the preparation thereof and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0278499A2
公开(公告)日:1988-08-17
There are disclosed compounds having the formula
wherein R is hydrogen, loweralkyl or loweralkylcarbonyl; R₁ is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; R₂ and R₃ are independently H or CH₃; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, -SH, loweralkylthio, -NHCOR₄ or -NR₅R₆ where R₄ is hydrogen or loweralkyl, and R₅ and R₆ are independently hydrogen, loweralkyl or cycloalkyl; Y and Z are independently a direct bond, CR₇R₈ or CR₇R₈-CR₉R₁₀; and P and Q are independently CR₇ʹR₈ʹ, CR₇ʹR₈ʹ-CR₉ʹR₁₀ʹ or CR₇ʹR₈ʹ-CR₉ʹR₁₀ʹ-CR₁₁R₁₂, where each of R₇ through R₁₂ and R₇ʹ through R₁₀ʹ is independently H or CH₃; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.
所公开的化合物具有以下式子
其中 R 是氢、低级烷基或低级烷基羰基;R₁ 是氢、低级烷基、低级烷基羰基、芳基、稀释烷基
氨基低级烷基、芳基低级烷基、二芳基低级烷基、氧桥接芳基低级烷基或氧桥接二芳基低级烷基;R₂ 和 R₃ 独立地是 H 或 CH₃;X 是氢、低级烷基、环烷基、低级烷氧基、卤素、羟基、硝基、三
氟甲基、甲酰基、低级烷基羰基、芳基羰基、-SH、低级烷
硫基、-NHCOR₄或 -NR₅R₆,其中 R₄ 是氢或低级烷基,R₅ 和 R₆ 独立地是氢、低级烷基或环烷基;Y 和 Z 独立地为直接键、CR₇R₈ 或 CR₇R₈-CR𠢙R₁₀ ;P和Q独立地为CR₇ʹR₈ʹ,CR₇ʹR₈ʹ-CR₉ʹR₁₀ʹ或CR₇ʹR₈ʹ-CR₉ʹR₁₀ʹ-CR₁₁R₁₂,其中R₇至R₁₂和R₇ʹ至R₁₀ʹ各自独立地为H或CH₃;立体异构体、光学异构体和几何异构体及其药学上可接受的酸加成盐,可用于增强记忆力。