3-(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethyl-piperidine-2,6-dione pamoate | 666175-73-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 3-(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethyl-piperidine-2,6-dione pamoate
• 英文别名: 4-[(3-Carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid;3-[3-(dimethylamino)propyl]-3-(3-methoxyphenyl)-4,4-dimethylpiperidine-2,6-dione
• CAS: 666175-73-1
• 化学式: C₁₉H₂₈N₂O₃*C₂₃H₁₆O₆
• 分子量: 720.819
• InChiKey: BJIMIJQKGIVERL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.74
• 重原子数：
  53
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  174
• 氢给体数：
  5
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  3-(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethyl-piperidine-2,6-dione bisulphate salt 、 pamoic acid 在 ammonium hydroxide 作用下， 以 二氯甲烷 、 水 、 乙醇 为溶剂， 生成 3-(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethyl-piperidine-2,6-dione pamoate
  参考文献：
  名称：

  [EN] PIPERIDIN-2,6-DIONE PAMOATE SALTS AND THEIR USE FOR THE TREATMENT OF STRESS-RELATED AFFECTIVE DISORDERS
  [FR] PAMOATES DE PIPERIDINE-2,6-DIONE ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES AFFECTIFS EN LIAISON AVEC LE STRESS

  摘要：

  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）的帕莫酸盐及其药学上可接受的溶剂化物，在治疗或预防压力相关情感障碍，如焦虑、抑郁、偏头痛和睡眠呼吸暂停中，不会出现大鼠体重减轻和肝细胞变化，这限制了相应盐酸的允许临床剂量的边缘有效水平。首选的帕莫酸盐是3（3,5-二甲氧基苯基）-3-（3-二甲基氨丙基）-4,4-二甲基哌啶-2,6-二酮帕莫酸盐，尤其是3（3-甲氧基苯基）-3-（3-二甲基氨丙基）-4,4-二甲基哌啶-2,6-二酮帕莫酸盐。

  公开号：

  WO2004017970A1

文献信息

• Piperidin-2, 6-dione pamoate salts and their use for the treatment of affective disorders
  申请人：Wermuth Camille Georges

  公开号：US20090182012A1

  公开（公告）日：2009-07-16

  Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones 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(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate.

  某些3-苯基-3-二甲基氨基烷基-4,4-二甲基哌啶-2,6-二酮的帕莫酸盐和药理学上可接受的溶剂化物，与相应的盐酸盐治疗或预防与压力有关的情感障碍，如焦虑、抑郁、偏头痛和睡眠呼吸暂停症，相比之下，不会出现大鼠的体重减轻和肝细胞改变，这些改变限制了相应的盐酸盐在治疗或预防这些疾病时的有效剂量。首选的帕莫酸盐是3（3,5-二甲氧基苯基）-3-（3-二甲基氨丙基）-4,4-二甲基哌啶-2,6-二酮帕莫酸盐，尤其是3（3-甲氧基苯基）-3-（3-二甲基氨丙基）-4,4-二甲基哌啶-2,6-二酮帕莫酸盐。
• Piperidin-2,6-dione pamoate salts and their use for the treatment of stress-related affective disorders
  申请人：Wermuth Georges Camille

  公开号：US20060025443A1

  公开（公告）日：2006-02-02

  Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones 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(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate.

  某些 3-苯基-3-二甲基氨基烷基-4,4-二甲基哌啶-2,6-二酮的新型帕莫阿特盐及其药理上可接受的溶解物不会导致大鼠体重减轻和肝细胞变化，而这些变化将相应盐酸盐的允许临床剂量限制在治疗或预防与压力有关的情感障碍（如焦虑、抑郁、偏头痛和睡眠呼吸暂停）的勉强有效水平。首选的帕莫酸盐是 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-2,6-二酮帕莫酸酯，特别是 3(3-甲氧基苯基)-3-(3-二甲基氨基丙基)-4,4-二甲基哌啶-2,6-二酮帕莫酸酯。
• PIPERIDIN-2,6-DIONE PAMOATE SALTS AND THEIR USE FOR THE TREATMENT OF STRESS-RELATED AFFECTIVE DISORDERS
  申请人：Prestwick Pharmaceuticals, Inc.

  公开号：EP1539160A1

  公开（公告）日：2005-06-15
• US7514454B2
  申请人：——

  公开号：US7514454B2

  公开（公告）日：2009-04-07
• [EN] PIPERIDIN-2,6-DIONE PAMOATE SALTS AND THEIR USE FOR THE TREATMENT OF STRESS-RELATED AFFECTIVE DISORDERS<br/>[FR] PAMOATES DE PIPERIDINE-2,6-DIONE ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES AFFECTIFS EN LIAISON AVEC LE STRESS
  申请人：PRESTWICK PHARMACEUTICALS INC

  公开号：WO2004017970A1

  公开（公告）日：2004-03-04

  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.

  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）的帕莫酸盐及其药学上可接受的溶剂化物，在治疗或预防压力相关情感障碍，如焦虑、抑郁、偏头痛和睡眠呼吸暂停中，不会出现大鼠体重减轻和肝细胞变化，这限制了相应盐酸的允许临床剂量的边缘有效水平。首选的帕莫酸盐是3（3,5-二甲氧基苯基）-3-（3-二甲基氨丙基）-4,4-二甲基哌啶-2,6-二酮帕莫酸盐，尤其是3（3-甲氧基苯基）-3-（3-二甲基氨丙基）-4,4-二甲基哌啶-2,6-二酮帕莫酸盐。