(3E)-3-[2-[(1R,8aS)-6-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidene-3,4,4a,6,7,8-hexahydro-1H-naphthalen-1-yl]ethylidene]-4-hydroxyoxolan-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酯类
• 英文名称: (3E)-3-[2-[(1R,8aS)-6-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidene-3,4,4a,6,7,8-hexahydro-1H-naphthalen-1-yl]ethylidene]-4-hydroxyoxolan-2-one
• 化学式: C₂₀H₃₀O₅
• 分子量: 350.4
• InChiKey: BOJKULTULYSRAS-ZJFCSBQFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  87
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Compounds and Combinations Thereof for Inhibiting Beta-Amyloid Production and Methods of Use Thereof
  申请人：Paris Daniel

  公开号：US20080058330A1

  公开（公告）日：2008-03-06

  Provided are compounds which can be used in combination for treating diseases associated with a condition associated with cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which in combination can decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of the compounds.

  提供了一些化合物，可以组合使用来治疗与阿尔茨海默病淀粉样蛋白相关的疾病，如阿尔茨海默病。还提供了一种方法，通过给予治疗有效量的化合物组合来减少β-淀粉样蛋白的产生和细胞中的电容性钙离子进入，从而治疗或降低发生β-淀粉样蛋白产生、β-淀粉样蛋白沉积、β-淀粉样蛋白神经毒性（包括tau异常过度磷酸化）和与阿尔茨海默病淀粉样蛋白相关的微胶质病变。此外，还提供了一种方法，通过给予诊断有效量的化合物来诊断动物或人类中与阿尔茨海默病淀粉样蛋白相关的疾病。
• Compounds for inhibiting beta-amyloid production and methods of identifying the compounds
  申请人：Mullan J. Michael

  公开号：US20070037855A1

  公开（公告）日：2007-02-15

  Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells.

  提供的化合物可用于治疗与阿尔茨海默淀粉样蛋白在大脑中积累有关的疾病，例如阿尔茨海默病。还提供了筛选此类化合物的方法，通过测量细胞中的电容性钙离子进入，其中细胞可以选择性地过度表达APP或其片段。还提供了通过给予治疗有效量的化合物来治疗或降低β-淀粉样蛋白产生、β-淀粉样蛋白沉积、β-淀粉样蛋白神经毒性（包括tau的异常高磷酸化）和与阿尔茨海默淀粉样蛋白在大脑中积累有关的微胶质细胞增生的方法。此外，还提供了通过给动物或人类施用诊断有效量的抑制电容性钙离子进入细胞的化合物来诊断与阿尔茨海默淀粉样蛋白在大脑中积累有关的疾病的方法。
• Compounds for Inhibiting Beta-Amyloid Production and Methods of Identifying the Compounds
  申请人：Mullan Michael J.

  公开号：US20100215735A1

  公开（公告）日：2010-08-26

  Provided are compounds useful for treating diseases associated with a cerebral accumulation of Alzheimer's amyloid, such as Alzheimer's disease. Also provided are methods for screening for such compounds, by measuring capacitative calcium entry in cells which optionally overexpress APP or a fragment thereof. Also provided are methods of treating or reducing the risk of developing β-amyloid production, β-amyloid deposition, β-amyloid neurotoxicity (including abnormal hyperphosphorylation of tau) and microgliosis associated with cerebral accumulation of Alzheimer's amyloid by administering therapeutically effective amounts of compounds which decrease β-amyloid production and capacitative calcium entry in cells. Further provided are methods for diagnosing diseases associated with cerebral accumulation of Alzheimer's amyloid in animals or humans by administering diagnostically effective amounts of compounds which inhibit capacitative calcium entry in cells.

  提供了一些化合物，可用于治疗与阿尔茨海默氏淀粉样物质在大脑中积累有关的疾病，如阿尔茨海默病。还提供了筛选这些化合物的方法，通过测量在细胞中的电容性钙离子进入，这些细胞可以选择性地过表达APP或其片段。还提供了通过给予治疗有效量的化合物来治疗或降低发生β-淀粉样物质产生、β-淀粉样物质沉积、β-淀粉样物质神经毒性（包括tau异常过磷酸化）和与阿尔茨海默氏淀粉样物质在大脑中积累有关的小胶质细胞增生的风险的方法，这些化合物可以减少β-淀粉样物质产生和细胞中的电容性钙离子进入。此外，还提供了通过给动物或人体内给予诊断有效量的化合物来诊断与阿尔茨海默氏淀粉样物质在大脑中积累有关的疾病的方法，这些化合物可以抑制细胞中的电容性钙离子进入。
• VERWENDUNG EINES TRP-MODULATORS ZUR PROPHYLAXE UND/ODER LINDERUNG VON WEIDETETANIE UND/ODER GEBÄRPARESE BEI WIEDERKÄUERN ODER SCHWIELENSOHLERN
  申请人：Freie Universität Berlin

  公开号：EP3195857A1

  公开（公告）日：2017-07-26

  Die Erfindung betrifft die neuartige Verwendung eines Futtermittelzusatzes in der Prophylaxe und/oder Linderung von Weidetetanie und/oder Gebärparese in einem Tier aus der Unterordnung der Wiederkäuer (Ruminantia) oder der (wiederkäuenden) Schwielensohler (Tylopoda). Der Futtermittelzusatz enthält mindestens einen TRP-Modulator. Die Erfindung betrifft ferner die neuartige Verwendung eines TRP-Modulators als Arzneimittel in der Behandlung von Weidetetanie und/oder Gebärparese in einem Tier aus der Unterordnung der Wiederkäuer (Ruminantia) oder der (wiederkäuenden) Schwielensohler (Tylopoda).

  本发明涉及一种饲料添加剂在预防和/或缓解反刍动物亚目（Ruminantia）或（反刍动物）胼胝体目（Tylopoda）动物的牧场四肢抽搐症和/或产后瘫痪中的新用途。饲料添加剂中至少含有一种 TRP 调节剂。本发明还涉及一种 TRP 调节剂作为药物治疗反刍动物亚目（Ruminantia）或（反刍动物）胼胝体目（Tylopoda）动物放牧性四肢抽搐和/或产后麻痹的新用途。
• COMPOSITION FOR PREVENTING AND TREATING ACUTE AND CHRONIC WOUNDS
  申请人：Foodar Advanced Research S.r.l.

  公开号：EP3861991A1

  公开（公告）日：2021-08-11

  A composition combining andrographolide and hydroxytyrosol is provided for the prevention and/or treatment of acute and/or chronic wounds; an injury or lesion of the skin; ulcers or ulceration; or for accelerating the physiological process of wound healing. The composition induces the collagen synthesis in human skin fibroblast and accelerate the physiological process of wound healing. The composition may be in a form suitable for oral administration or topical application.

  本发明提供了一种结合穿心莲内酯和羟基酪醇的组合物，用于预防和/或治疗急性和/或慢性伤口；皮肤损伤或病变；溃疡或溃烂；或加速伤口愈合的生理过程。该组合物能诱导人体皮肤成纤维细胞合成胶原蛋白，加速伤口愈合的生理过程。组合物可以是适合口服或局部应用的形式。