首页> 外国专利> Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4dimethylpiperidin-2,6-diones (1) and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine2,6-dione pamoate.

Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4dimethylpiperidin-2,6-diones (1) and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine2,6-dione pamoate.

机译:某些3-苯基-3-二甲基氨基烷基-4,4-二甲基哌啶-2,6-二酮(1)的新型pamoate盐及其药理学上可接受的溶剂化物避免了大鼠的体重减轻和肝细胞变化,将其限制在允许的极限有效水平上相应盐酸盐的临床剂量,用于治疗或预防与压力有关的情感障碍,例如焦虑,抑郁,偏头痛和睡眠呼吸暂停。优选的pamoate盐是3(3,5-二甲氧基苯基)-3-(3-二甲基氨基丙基)-4,4-二甲基哌啶-2,6-二酮pamoate,尤其是3(3-甲氧基苯基)-3-(3-二甲基氨基丙基) -4,4-二甲基哌啶2,6-二酮pamoate。

摘要

Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4dimethylpiperidin-2,6-diones (1) and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine2,6-dione pamoate.
机译:某些3-苯基-3-二甲基氨基烷基-4,4-二甲基哌啶-2,6-二酮(1)的新型pamoate盐及其药理学上可接受的溶剂化物避免了大鼠的体重减轻和肝细胞变化,将其限制在允许的极限有效水平上相应盐酸盐的临床剂量,用于治疗或预防与压力有关的情感障碍,例如焦虑,抑郁,偏头痛和睡眠呼吸暂停。优选的pamoate盐是3(3,5-二甲氧基苯基)-3-(3-二甲基氨基丙基)-4,4-二甲基哌啶-2,6-二酮pamoate,尤其是3(3-甲氧基苯基)-3-(3-二甲基氨基丙基) -4,4-二甲基哌啶2,6-二酮pamoate。

著录项

  • 公开/公告号EA007900B1

    专利类型

  • 公开/公告日2007-02-27

    原文格式PDF

  • 申请/专利权人 PRESTWICKPHARMACEUTICALS;INC.;

    申请/专利号EA20050000242

  • 发明设计人 WERMUTHCAMILLEGEORGE;

    申请日2003-08-18

  • 分类号A61K31/451;A61P25;C07D211/88;

  • 国家 EA

  • 入库时间 2022-08-21 20:59:00

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