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PHARMACEUTICAL COMPOSITIONS CONTAINING ARYL-SUBSTITUTED OLEFINIC AMINE COMPOUNDS

机译:包含芳基取代的烯烃胺化合物的药物组合物

摘要

Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound of Formula (I): wherein X is C-R', C-OR', C-CH2-OR' wherein R' is selected from the group consisting of H, C1-C5 alkyl, an aromatic group containing species and alkyl-, halo-, or amino-substituted aromatic group containing species; E' is hydrogen or C1-C5 alkyl or halo substituted C1-C5 alkyl; E'' is C1-C5 alkyl or halo substituted C1-C5 alkyl; Z' and Z'' are each individually selected from the group consisting of hydrogen, C1-C5 alkyl, aryl rings, and can form a ring structure (a), A, A' and A'' are each individually selected from the group consisting of hydrogen, C1-C7 alkyl, and halo; m is 0 or 1; p is 0 or 1 with the proviso that when m or p is 0 then that E'' is hydrogen; and the wavy line in the structure represents a cis (Z) or trans (E) form of the compound. Exemplary compounds include (E)-N-methyl-4-[3-(benzyloxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-phenoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-phenylpyridin)yl]-3-buten-1-amine.
机译:易感或患有中枢神经系统疾病(例如阿尔茨海默氏病,帕金森氏病,图雷特氏综合症,注意力缺陷障碍或精神分裂症)的患者,可通过服用有效量的式(I)的芳基取代的烯烃胺化合物来治疗是C-R′,C-OR′,C-CH2-OR′,其中R′选自H,C1-C5烷基,含芳香族基团和被烷基,卤素或氨基取代的基团含芳族物质; E′为氢或C1-C5烷基或卤素取代的C1-C5烷基; E''为C1-C5烷基或卤素取代的C1-C5烷基; Z′和Z″各自独立地选自氢,C 1 -C 5烷基,芳基环,并且可以形成环结构(a),A,A′和A″各自独立地选自组由氢,C1-C7烷基和卤素组成; m为0或1; p为0或1,条件是当m或p为0时,E''为氢;结构中的波浪线表示化合物的顺式(Z)或反式(E)形式。示例性的化合物包括(E)-N-甲基-4- [3-(苄氧基吡啶)基] -3-丁烯-1-胺,(E)-N-甲基-4- [3-(5-苯氧基吡啶)基] -3-丁烯-1-胺,(E)-N-甲基-4- [3-(5-异丙氧基吡啶))]-3-丁烯-1-胺,(E)-N-甲基-4- [3 -(5-甲氧基甲基吡啶基)基] -3-丁烯-1-胺和(E)-N-甲基-4- [3-(5-苯基吡啶基)基] -3-丁烯-1-胺。

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