donepezil pamoate | 1417425-02-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: donepezil pamoate
• 英文别名: donepezil monopamoate；2-[(1-Benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid；2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;4-[(3-carboxy-2-hydroxynaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylic acid
• CAS: 1417425-02-5
• 化学式: C₂₃H₁₆O₆*C₂₄H₂₉NO₃
• 分子量: 767.876
• InChiKey: JBJMZLLPMSIQQQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.75
• 重原子数：
  57
• 可旋转键数：
  10
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  154
• 氢给体数：
  4
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  disodium pamoate 、 盐酸多奈哌齐 以 水 为溶剂， 生成 donepezil pamoate
  参考文献：
  名称：

  [EN] DONEPEZIL PAMOATE, PREPARATION METHODE AND ITS USE
  [FR] PAMOATE DE DONÉPEZILE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION

  摘要：

  揭示了含有多奈哌齐的帕莫酸盐的组合物、其制备方法和用途。

  公开号：

  WO2013079007A1

文献信息

• [EN] DONEPEZIL PAMOATE AND METHODS OF MAKING AND USING THE SAME<br/>[FR] PAMOATE DE DONEPEZIL ET SES PROCÉDÉS DE FABRICATION ET D'UTILISATION
  申请人：GU ZIQIANG

  公开号：WO2013078608A1

  公开（公告）日：2013-06-06

  The present invention relates to the discovery that pamoate salts of donepezil provide a long acting and/or extended release profile of donepezil. Thus, in one aspect of the invention, the invention includes pamoate salt of donepezil. Preferably, the pamoate salt is characterized by a ratio of donepezil to pamoate of 1:1 or 2:1. The pamoate salt can be crystalline including anhydrous, hydrate or solvate forms, or their polymorphs, or amorphous. The invention further relates to methods of preparing pamoate salts. The invention further relates to methods of treating an individual in need thereof comprising administering a pharmaceutical composition comprising a pamoate salt of donepezil.

  本发明涉及到发现，帕莫酸盐多奈哌齐提供了多奈哌齐的长效和/或延缓释放特性。因此，在本发明的一个方面，本发明包括帕莫酸盐多奈哌齐。优选，帕莫酸盐的多奈哌齐特征是多奈哌齐与帕莫酸的比例为1:1或2:1。帕莫酸盐可以是结晶的，包括无水物、水合物或溶剂物形式，或它们的多晶形式，或无定形的。本发明还涉及制备帕莫酸盐的方法。本发明还涉及治疗有需要的个体的方法，包括给予含有帕莫酸盐多奈哌齐的药物组合物。
• DONEPEZIL PAMOATE, METHOD OF PREPARATION AND USE THEREOF
  申请人：Gu Ziqiang

  公开号：US20140315952A1

  公开（公告）日：2014-10-23

  The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.

  揭示了含有多奈哌齐的帕莫酸盐的组合物，其制备方法和用途。
• Acid Addition Salt of Donepezil and Pharmaceutical Composition Thereof
  申请人：Nadkarni Sunil Sadanand

  公开号：US20140243278A1

  公开（公告）日：2014-08-28

  Disclosed is an acid addition salt of donepezil, wherein acid counterion is selected from the group consisting of pamoic acid, cypionic acid, camphor sulfonic acid, enanthic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, valeric acid, Dibenzoyl-D-Tartaric acid and terephthalic acid. Disclosed is a process for the preparation and pharmaceutical composition comprising the same. More specifically, disclosed is concerned with the pamoate acid addition salts of donepezil. Disclosed also is long acting formulation comprising the acid addition salt of donepezil and process for the preparation thereof.

  本发明涉及一种多奈哌齐的酸盐加合物，其中酸对离子选自以下组合：泊酸、环戊酸、樟脑磺酸、庚酸、咐西酸、葡萄糖酸、葡萄糖醛酸、乳糖酸、月桂酸、戊酸、苯甲酸-D-酒石酸和对苯二甲酸。本发明还涉及制备该酸盐加合物的方法和包含该酸盐加合物的制药组合物。更具体地，本发明涉及泊酸盐酸盐加合物的多奈哌齐。本发明还涉及包含多奈哌齐酸盐加合物的长效制剂及其制备方法。
• PHARMACEUTICAL COMPOSITION FOR PARENTERAL ADMINISTRATION, CONTAINING DONEPEZIL
  申请人：Dongkook Pharmaceutical Co., Ltd.

  公开号：EP2982367A1

  公开（公告）日：2016-02-10

  The present invention relates to a composition for parenteral administration, containing donepezil as an active ingredient, and a preparation method therefor. Donepezil, which has been conventionally used for oral or transdermal administration, is prepared as microparticles comprising a biodegradable and biocompatible polymer and a release controller so as to be provided as a pharmaceutical composition for sustained release parenteral administration, thereby enabling in vivo sustained release continuously for 2-12 weeks or more. Therefore, it is possible to reduce the frequency of administration to a patient and maintain an effective concentration in the blood for a long time.

  本发明涉及一种含有多奈哌齐作为活性成分的肠外给药组合物及其制备方法。多奈哌齐通常用于口服或透皮给药，本发明将其制备成微颗粒，其中包含一种可生物降解且生物相容的聚合物和一种释放控制器，从而将其作为一种药物组合物提供给患者，用于肠外持续释放给药，从而实现在体内持续释放 2-12 周或更长时间。因此，可以减少对患者的给药频率，并长期保持血液中的有效浓度。
• NEW METHOD FOR PREPARING DONEPEZIL PAMOATE
  申请人：Zhejiang Huahai Pharmaceutical Co., Ltd.

  公开号：EP3620450A1

  公开（公告）日：2020-03-11

  Disclosed is a new method for preparing a donepezil pamoate (1-benzyl-4-[(5,6-dimethoxyindan-2-one)methyl]piperidine pamoate). The donepezil pamoate prepared by using the method has a high purity and a good flowability.

  本发明公开了一种制备帕莫酸多奈哌齐酯（1-苄基-4-[(5,6-二甲氧基茚满-2-酮)甲基]哌啶帕莫酸酯）的新方法。使用该方法制备的帕莫酸多奈哌齐具有高纯度和良好的流动性。