Ethyl 2-[4-[[amino-[(1-methylindol-3-yl)methyl]amino]methyl]piperidin-1-yl]pyrimidine-5-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Ethyl 2-[4-[[amino-[(1-methylindol-3-yl)methyl]amino]methyl]piperidin-1-yl]pyrimidine-5-carboxylate
• 英文别名: ethyl 2-[4-[[amino-[(1-methylindol-3-yl)methyl]amino]methyl]piperidin-1-yl]pyrimidine-5-carboxylate
• 化学式: C₂₃H₃₀N₆O₂
• 分子量: 422.5
• InChiKey: CCSCESOFJDZYSG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  89.5
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• NOVEL ANTAGONISTS OF THE GLUCAGON RECEPTOR
  申请人：Metabasis Therapeutics, Inc.

  公开号：US20140135400A1

  公开（公告）日：2014-05-15

  The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

  本发明提供了一种新型化合物Formula (I)及其药学上可接受的盐和共晶体，具有胰高血糖素受体拮抗剂或反向激动剂活性。本发明还提供了包含这些化合物的药物组合物，以及用于治疗、预防、延迟发病时间或降低一种或多种胰高血糖素受体拮抗剂适用的疾病或病症的风险，包括I型和II型糖尿病、胰岛素抵抗和高血糖的方法。本发明还提供了制备Formula (I)化合物，包括其盐和共晶体，以及包含它们的药物组合物的方法。
• US8759519B2
  申请人：——

  公开号：US8759519B2

  公开（公告）日：2014-06-24