Enalapril maleate and felodipine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Enalapril maleate and felodipine
• 英文别名: (Z)-but-2-enedioic acid;(2S)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]pyrrolidine-2-carboxylic acid;5-O-ethyl 3-O-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
• 化学式: C42H51Cl2N3O13
• 分子量: 876.8
• InChiKey: DPNLWHDRPGNSKB-IKNOHHBKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.28
• 重原子数：
  60
• 可旋转键数：
  18
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  235
• 氢给体数：
  5
• 氢受体数：
  15

文献信息

• COMPOUNDS AND METHODS FOR TREATING INSULIN RESISTANCE SYNDROME
  申请人：Cohen Stephen Michael

  公开号：US20140227289A1

  公开（公告）日：2014-08-14

  The present invention relates to a method of treating or preventing insulin resistance syndrome in an animal body by administering an inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK) gene, or a functional variant thereof, or an inhibitor of PERK protein or a functional variant thereof or a method of reducing activity of transcription factors of the FOXO family (Foxo 1, 3a, 4 and 6) by administering an inhibitor of protein kinase RNA-like endoplasmic reticulum kinase (PERK) gene, or a functional variant thereof, or an inhibitor of PERK protein or a functional variant thereof. The present invention also relates to different compounds and methods for using PERK gene or PERK protein.

  本发明涉及通过给动物体内注射蛋白激酶RNA样内质网激酶（PERK）基因的抑制剂或其功能变体，或PERK蛋白或其功能变体的抑制剂，或通过给动物体内注射蛋白激酶RNA样内质网激酶（PERK）基因的抑制剂或其功能变体，或PERK蛋白或其功能变体的抑制剂来减少FOXO家族转录因子（Foxo 1、3a、4和6）活性的方法，用于治疗或预防动物体内的胰岛素抵抗综合征。本发明还涉及不同的化合物和使用PERK基因或PERK蛋白的方法。
• REDUCING ER STRESS IN THE TREATMENT OF OBESITY AND DIABETES
  申请人：Hotamisligil Gökhan S.

  公开号：US20100075894A1

  公开（公告）日：2010-03-25

  Endoplasmic reticulum stress has been found to be associated with obesity. Therefore, agents that reduce or prevent ER stress may be used to treat diseases associated with obesity including peripheral insulin resistance, hypergylcemia, and type 2 diabetes. Two compounds which have been shown to reduce ER stress and to reduce blood glucose levels include 4-phenyl butyric acid (PBA), tauroursodeoxycholic acid (TUDCA), and trimethylamine N-oxide (TMAO). Other compounds useful in reducing ER stress are chemical chaperones such as trimethylamine N-oxide and glycerol. The present invention provides methods of treating a subject suffering from obesity, hyperglycemia, type 2 diabetes, or insulin resistance using ER stress reducers such as PBA, TUDCA, and TMAO. Methods of screening for ER stress reducers by identifying agents that reduce levels of ER stress markers in ER stressed cells are also provided. These agents may find use in methods and pharmaceutical compositions for treating obesity-associated diseases.

  内质网应激与肥胖有关。因此，减少或防止内质网应激的药物可用于治疗与肥胖相关的疾病，包括外周胰岛素抵抗、高血糖和2型糖尿病。已经显示出减少内质网应激并降低血糖水平的两种化合物包括4-苯基丁酸（PBA）、牛磺胆酸（TUDCA）和三甲胺氧化物（TMAO）。其他有用于减少内质网应激的化合物是化学分子伴侣，例如三甲胺氧化物和甘油。本发明提供了使用内质网应激减轻剂如PBA、TUDCA和TMAO治疗患有肥胖、高血糖、2型糖尿病或胰岛素抵抗的受试者的方法。还提供了通过识别减少内质网应激标志物水平的药物筛选内质网应激减轻剂的方法。这些药物可用于治疗与肥胖相关的疾病的方法和制药组合物。
• Active agent loaded uniform, rigid, spherical, nanoporous calcium phosphate particles and methods of making and using the same
  申请人：Laboratory Skin Care, Inc.

  公开号：US10028903B2

  公开（公告）日：2018-07-24

  Uniform, rigid, spherical nanoporous calcium phosphate particles that define an internal space and an amount of active agent present in the internal space are provided. Also provided are topical delivery compositions that include the active agent loaded particles, as well as methods of making the particles and topical compositions. The particles and compositions thereof find use in a variety of different applications, including active agent delivery applications.

  本发明提供了均匀、坚硬、球形的纳米多孔磷酸钙颗粒，这些颗粒限定了内部空间和内部空间中的活性剂含量。此外，还提供了包括活性剂负载颗粒的局部给药组合物，以及制造颗粒和局部组合物的方法。这些颗粒及其组合物可用于各种不同的应用，包括活性剂递送应用。
• Reducing ER stress in the treatment of obesity and diabetes
  申请人：Hotamisligil S. Gokhan

  公开号：US20060073213A1

  公开（公告）日：2006-04-06

  Endoplasmic reticulum stress has been found to be associated with obesity. Therefore, agents that reduce or prevent ER stress may be used to treat diseases associated with obesity including peripheral insulin resistance, hypergylcemia, and type 2 diabetes. Two compounds which have been shown to reduce ER stress and to reduce blood glucose levels include 4-phenyl butyric acid (PBA), tauroursodeoxycholic acid (TUDCA), and trimethylamine N-oxide (TMAO). Other compounds useful in reducing ER stress are chemical chaperones such as trimethylamine N-oxide and glycerol. The present invention provides methods of treating a subject suffering from obesity, hyperglycemia, type 2 diabetes, or insulin resistance using ER stress reducers such as PBA, TUDCA, and TMAO. Methods of screening for ER stress reducers by identifying agents that reduce levels of ER stress markers in ER stressed cells are also provided. These agents may find use in methods and pharmaceutical compositions for treating obesity-associated diseases.

  研究发现，内质网应激与肥胖有关。因此，减少或预防内质网应激的药物可用于治疗与肥胖有关的疾病，包括外周胰岛素抵抗、高血糖和 2 型糖尿病。有两种化合物已被证明可以减少ER应激和降低血糖水平，其中包括4-苯基丁酸（PBA）、牛磺酸去氧胆酸（TUDCA）和三甲胺N-氧化物（TMAO）。其他有助于降低 ER 应激的化合物还有化学伴侣素，如三甲胺 N-氧化物和甘油。本发明提供了使用ER应激还原剂如PBA、TUDCA和TMAO治疗肥胖、高血糖、2型糖尿病或胰岛素抵抗的方法。此外，还提供了通过识别能降低 ER 应激细胞中 ER 应激标记物水平的制剂来筛选 ER 应激抑制剂的方法。这些制剂可用于治疗肥胖相关疾病的方法和药物组合物中。
• EP1799263A4
  申请人：——

  公开号：EP1799263A4

  公开（公告）日：2009-07-29