| 377731-46-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• CAS: 377731-46-9
• 化学式: C₂₀H₂₅NO₅
• 分子量: 359.422
• InChiKey: CKMOMMWDPGJJAW-SGNKCFNYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.83
• 重原子数：
  26.0
• 可旋转键数：
  7.0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  81.79
• 氢给体数：
  1.0
• 氢受体数：
  5.0

反应信息

• 作为产物：
  描述：

  在 sodium hydroxide 作用下， 以 甲醇 为溶剂， 生成
  参考文献：
  名称：

  Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor α (PPARα) agonists

  摘要：

  A new series of 1,3-dioxane-2-carboxylic acid derivatives was synthesized and evaluated for agonist activity at human peroxisome proliferator-activated receptor ( PPAR) subtypes. Structure-activity relationship studies led to the identification of 2-methyl-c-5-[4-(5-methyl-2-phenyl-1,3-oxazol-4-yl) butyl]-1,3-dioxane-r-2-carboxylic acid 4b as a potent PPAR alpha agonist with high subtype selectivity at human receptor subtypes. This compound exhibited a substantial hypolipidemic effect in type 2 diabetic KK-A(y) mice. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.01.086

文献信息

• Heterocyclic compounds
  申请人：——

  公开号：US20040162325A1

  公开（公告）日：2004-08-19

  The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: R 1 -Het-D-E  [1] wherein: R 1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.

  本发明提供了一种预防或治疗高脂血症的药物，其包含以下式子的杂环化合物或其药学上可接受的盐作为活性成分：R1-Het-D-E [1]其中：R1是可选取的取代芳基或芳香族杂环基，Het是双价芳香族杂环基，D是烷基，烯基，炔基或类似物，E是羧基或类似物。本发明中的杂环化合物具有降低血甘油三酯、降低低密度脂蛋白胆固醇、降低血糖和胰岛素的作用，或者提高高密度脂蛋白胆固醇或降低动脉粥样硬化指数的作用，因此在预防或治疗高脂血症、动脉粥样硬化、糖尿病、高血压、肥胖症等方面具有用途。
• HETEROCYCLIC COMPOUNDS
  申请人：Nippon Shinyaku Co., Ltd.

  公开号：EP1295875A1

  公开（公告）日：2003-03-26

  The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1] or a pharmaceutically acceptable salt thereof:         R1―Het―D―E     [1] wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.

  本发明提供了一种预防或治疗高脂血症的药物，其活性成分包括式 [1] 的杂环化合物或其药学上可接受的盐： R1-Het-D-E [1] 其中 R1为任选取代的芳基或芳香杂环基团，Het为二价芳香杂环基团，D为亚烷基、亚烯基、亚炔基或类似基团，E为羧基或类似基团，上述式[1]杂环化合物中的新型化合物，具有降血甘油三酯作用、低密度脂蛋白胆固醇（LDL-C）降低效果、血糖降低效果和血胰岛素降低效果，或高密度脂蛋白胆固醇（HDL-C）增加效果或动脉粥样硬化指数降低效果，因此可用于预防或治疗高脂血症、动脉硬化、糖尿病、高血压、肥胖症等。
• US6998412B2
  申请人：——

  公开号：US6998412B2

  公开（公告）日：2006-02-14
• US7022723B2
  申请人：——

  公开号：US7022723B2

  公开（公告）日：2006-04-04
• US7030143B2
  申请人：——

  公开号：US7030143B2

  公开（公告）日：2006-04-18