Donepezil chloride

• 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 chloride
• 英文别名: 2-[(1-benzylpiperidin-4-yl)methyl]-2-chloro-5,6-dimethoxy-3H-inden-1-one
• 化学式: C₂₄H₂₈ClNO₃
• 分子量: 413.9
• InChiKey: MIAXWQWTJFPRRI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  38.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Sigma receptor binding agent containing indanone derivative
  申请人：Iimura Yoichi

  公开号：US20090137629A1

  公开（公告）日：2009-05-28

  A method for treatment of a mental disorder containing the step of administering a therapeutically effective amount of a sigma receptor binding agent containing an indanone compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. The variables of formula (I) are recited in the present specification.

  一种治疗精神障碍的方法，包括以下步骤：给予治疗有效量的sigma受体结合剂，该结合剂包含以下式子（I）所表示的indanone化合物，其药理学上可接受的盐或水合物。式子（I）的变量在本说明书中已列出。
• SIGMA RECEPTOR BINDER CONTAINING INDANONE DERIVATIVE
  申请人：Eisai Co., Ltd.

  公开号：EP1468684A1

  公开（公告）日：2004-10-20

  The present invention provides an indanone derivative and an excellent sigma receptor binding agent comprising an indanone derivative. More specifically, it provides a sigma receptor binding agent comprising an indanone derivative represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate of them. In the formula (I), R1, R2, R3 and R4 are the same as or different from each other and each represents hydrogen atom, a halogen atom, hydroxyl group, nitrile group, a C1-6 alkyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a C1-6 alkoxy group which may be substituted, a cycloalkoxy group having three to eight carbon atoms which may be substituted, an acyl group having one to six carbon atoms which may be substituted, a C1-6 alkoxycarbonyl group which may be substituted, a C1-6 alkylaminocarbonyloxy group which may be substituted, a di(C1-6 alkyl)aminocarbonyloxy group which may be substituted, nitro group, an amino group which may be substituted, an amido group which may be substituted, mercapto group or a thio-C1-6 alkoxy group which may be substituted, and further R1 with R2, R2 with R3, or R3 with R4 may together form an aliphatic ring, an aromatic ring, a heterocyclic ring or an alkylenedioxy ring; the partial structure: represents a group represented by >CH-CH2-, >C=CH- or >C(-R7)-CH2-; m represents an integer of 0 or 1 to 5; and R5 represents hydrogen atom, a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C2-6 alkynyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a 2,2-(alkylenedioxy)ethyl group or a group represented by the formula: (wherein the ring C represents benzene ring, an aliphatic ring or a heterocyclic ring; R6s are the same as or different from each other and each represents hydrogen atom, a halogen atom, hydroxyl group, nitrile group, a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C2-6 alkynyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a C1-6 alkoxy group which may be substituted, a C1-6 alkoxyalkoxy group which may be substituted, an aryloxy group which may be substituted or an aralkyloxy group which may be substituted, and further two of R6s may together form an aliphatic ring, an aromatic ring, a heterocyclic ring or an alkylenedioxy ring; R7 represents a halogen atom, hydroxyl group, a C1-6 alkyl group which may be substituted, a C1-6 alkoxy group, nitrile group, a halogeno-C1-6 alkyl group, a hydroxyl-C1-6 alkyl group, a cyano-C1-6 alkyl group, an amino-C1-6 alkyl group, nitro group, azide group, an amino group which may be substituted, a carbamoyl group which may be substituted, a carboxyl group which may be substituted, mercapto group or a thio-C1-6 alkoxy group; and n represents an integer of 1 to 5), provided that 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine, a pharmacologically acceptable salt thereof or a hydrate of them are excluded.

  本发明提供了一种茚满酮衍生物和一种包含茚满酮衍生物的优良σ受体结合剂。更具体地说，本发明提供了一种σ受体结合剂，它由下式所代表的茚酮衍生物、其药理学上可接受的盐或它们的水合物组成。 在式 (I) 中，R1、R2、R3 和 R4 彼此相同或不同，各自代表氢原子、卤素原子、羟基、腈基、可被取代的 C1-6 烷基、具有三至八个碳原子且可被取代的环烷基、可被取代的 C1-6 烷氧基、具有三至八个碳原子且可被取代的环烷氧基、具有一至六个碳原子且可被取代的酰基、可被取代的 C1-6 烷氧基羰基、可被取代的 C1-6 烷基氨基羰氧基、可被取代的二（C1-6 烷基）氨基羰氧基、硝基、可被取代的氨基、可被取代的酰胺基、巯基或可被取代的硫代-C1-6 烷氧基，此外，R1 与 R2、R2 与 R3 或 R3 与 R4 可共同形成脂肪环、芳香环、杂环或烷基二氧基环；部分结构： 代表由 >CH-CH2-、>C=CH- 或 >C(-R7)-CH2-代表的基团；m 代表 0 或 1 至 5 的整数；R5 代表氢原子、可被取代的 C1-6 烷基、可被取代的 C2-6 烯基、可被取代的 C2-6 烷基、可被取代的具有 3 至 8 个碳原子的环烷基、2,2-(烷基二氧基)乙基或由式...代表的基团： (其中环 C 代表苯环、脂肪环或杂环；R6s 彼此相同或不同，各自代表氢原子、卤素原子、羟基、腈基、可被取代的 C1-6 烷基、可被取代的 C2-6 烯基、可被取代的 C2-6 烷基、具有三至八个碳原子的可被取代的环烷基、可被取代的 C1-6 烷氧基、可被取代的 C1-6 烷氧基、可被取代的芳氧基或可被取代的芳烷氧基，另外两个 R6 可共同形成脂肪环、芳香环、杂环或烷二氧基环；R7 代表卤素原子、羟基、可被取代的 C1-6 烷基、C1-6 烷氧基、腈基、卤素-C1-6 烷基、羟基-C1-6 烷基、氰基-C1-6 烷基、氨基-C1-6 烷基、硝基、叠氮基、可被取代的氨基、可被取代的氨基甲酰基、可被取代的羧基、巯基或硫代-C1-6 烷氧基；和 n 代表 1 至 5 的整数），但不包括 1-苄基-4-[(5,6-二甲氧基-1-茚酮)-2-基]甲基哌啶、其药理学上可接受的盐或它们的水合物。
• PERCUTANEOUS ABSORPTION PREPARATION
  申请人：NITTO DENKO CORPORATION

  公开号：EP2098232A1

  公开（公告）日：2009-09-09

  [Object] The present invention provides a percutaneously absorbable preparation for percutaneous absorption of donepezil or its hydrochloride which is stable and resistant to loss of cohesiveness of the pressure-sensitive adhesive layer while attached and resistant to adhesive transfer due to cohesive failure during removal by peeling. [Solution] The percutaneously absorbable preparation comprises 2-[(1-benzyl-4-piperidinyl)methyl]-5,6-dimethoxyindan-1-on and/or its hydrochloride and a metal chloride in a pressure-sensitive adhesive layer which has been crosslinked.

  [目的]本发明提供了一种用于经皮吸收多奈哌齐或其盐酸盐的可经皮吸收制剂，该制剂在附着时稳定且不易失去压敏胶层的内聚力，在剥离去除时不易因内聚力失效而导致胶转移。 [解决方案] 经皮可吸收制剂包括 2-[（1-苄基-4-哌啶基）甲基]-5,6-二甲氧基茚满-1-酮和/或其盐酸盐，以及位于已交联的压敏胶层中的金属氯化物。
• SKIN IRRITATION SUPPRESSANT AND TRANSDERMAL PREPARATION
  申请人：Hisamitsu Pharmaceutical Co., Inc.

  公开号：EP2564873A1

  公开（公告）日：2013-03-06

  Provided is a skin irritation suppressant for transdermal preparations, having a sufficient reduction effect of skin irritation due to a drug. Also provided is a transdermal preparation comprising the skin irritation suppressant. One embodiment of the invention is a skin irritation suppressant for suppressing the skin irritation due to a drug and a pharmaceutical ingredient to be used in a transdermal preparation other than the drug, the skin irritation suppressant comprising a sterol compound selected from the group consisting of cholesterol, cholesterol derivatives and cholesterol analogs, and the drug is one or more basic drugs selected from the group consisting of tolterodine, asenapine, bisoprolol, risperidone, nicotine and citalopram, and their pharmaceutically acceptable salts.

  本发明提供了一种用于透皮制剂的皮肤刺激抑制剂，它能充分减少药物对皮肤的刺激。还提供了一种包含该皮肤刺激抑制剂的透皮制剂。本发明的一个实施方案是一种皮肤刺激抑制剂，用于抑制由药物引起的皮肤刺激，以及用于除药物外的透皮制剂中的药物成分，该皮肤刺激抑制剂包括选自由胆固醇、胆固醇衍生物和胆固醇类似物组成的组中的固醇化合物、药物是一种或多种基本药物，选自由托特罗定、阿塞那平、比索洛尔、利培酮、尼古丁和西酞普兰及其药学上可接受的盐组成的组。
• Rapidly disintegrating oral dissolvable film
  申请人：CURE Pharmaceutical Holding Corp.

  公开号：US11344506B2

  公开（公告）日：2022-05-31

  The present invention provides for an oral dissolvable film that includes a rapidly dissolving binder, a film forming polymer, a moisture deterring polymer, and at least one of a first active ingredient and a second active ingredient. Also provided is a method of forming an oral dissolvable film and kits that include the oral dissolvable film. Also provided is a method of delivering one or more active ingredients to a subject that include orally administering the oral dissolvable film.

  本发明提供了一种口腔可溶解薄膜，它包括快速溶解粘合剂、成膜聚合物、防潮聚合物以及第一种活性成分和第二种活性成分中的至少一种。还提供了一种形成口服可溶膜的方法和包括口服可溶膜的试剂盒。还提供了一种向受试者提供一种或多种活性成分的方法，包括口服该口腔可溶膜。