9-amino-2-[2-(1-benzylpiperidin-4-yl)ethyl]-3H-pyrrolo[3,4-b]quinolin-1-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 9-amino-2-[2-(1-benzylpiperidin-4-yl)ethyl]-3H-pyrrolo[3,4-b]quinolin-1-one
• 化学式: C₂₅H₂₈N₄O
• 分子量: 400.5
• InChiKey: BIKSGVGPKWCRCQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  62.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Agents and crystals for improving excretory potency of urinary bladder
  申请人：——

  公开号：US20020177593A1

  公开（公告）日：2002-11-28

  Agents for improving potentcy of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholine esterase and an action to improve the excretory potency of urinary bladder. As an example, crystals of of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.

  改善膀胱功能的药剂，包括一种非卡巴酯类胺化合物，具有乙酰胆碱酯酶抑制作用。特别地，提供了一种三环、紧凑、杂环衍生物的晶体，具有优异的抑制乙酰胆碱酯酶作用和改善膀胱排泄功能的作用。例如，揭示了8-[3-[1-[(3-氟苯基)-甲基]-4-哌啶基]-1-氧代丙基]-1,2,5,6-四氢-4H-吡咯烷[3,2,1-ij]-喹啉-4-酮或其盐和含有它们的药物组合物。
• Agents for improving excretory potency of urinary bladder
  申请人：——

  公开号：US20040116457A1

  公开（公告）日：2004-06-17

  Agents for improving excretory potency of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action.

  改善排泄能力的尿道代理，包括一种非卡巴酯型胺类化合物，具有乙酰胆碱酯酶抑制作用。
• DRUGS FOR IMPROVING VESICAL EXCRETORY STRENGTH
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1118322A1

  公开（公告）日：2001-07-25

  Agents for improving excretory potency of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action.

  改善膀胱排泄能力的制剂，其中包括一种具有乙酰胆碱酯酶抑制作用的非氨基甲酸酯类胺类化合物。
• Acetylcholinesterase inhibitors for improving excretory potency of urinary bladder
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1604653A1

  公开（公告）日：2005-12-14

  Agents for improving excretory potency of the urinary bladder which comprises an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action.

  改善膀胱排泄能力的制剂，其中包括一种具有乙酰胆碱酯酶抑制作用的非氨基甲酸酯类胺类化合物。
• PREVENTIVE/REMEDY FOR URINARY DISTURBANCE
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1640021A1

  公开（公告）日：2006-03-29

  It is intended to provide a preventive/remedy for urinary disturbance containing a compound, which shows an acetylcholine esterase inhibitory activity but substantially has no butyrylcholine esterase inhibitory activity, showing no side effect and being safe and efficacious without inhibiting the urine collection function; a preventive/remedy for dry mouth induced by the administration of a remedy for urinary disturbance and a preventive or remedy for hyperactive bladder not accompanied by dry mouth; and a method of screening a substance preventing/treating urinary disturbance without inhibiting the urine collection function characterized by comprising measuring and comparing the acetylcholine esterase inhibitory activity and the butyrylcholine esterase inhibitory activity of a test compound.

  本发明旨在提供一种预防/治疗排尿障碍的药物，其中含有一种化合物，该化合物具有乙酰胆碱酯酶抑制活性，但基本上不具有丁酰胆碱酯酶抑制活性，且无副作用，安全有效，不会抑制尿液收集功能；一种预防/治疗因服用治疗排尿障碍的药物而引起的口干的药物，以及一种预防或治疗不伴有口干的膀胱过度活动症的药物；以及一种筛选预防/治疗排尿障碍而不抑制尿液收集功能的物质的方法，其特征在于包括测量和比较试验化合物的乙酰胆碱酯酶抑制活性和丁酰胆碱酯酶抑制活性。