Methyl 4-[2-[5-(4-bromophenyl)-1,2-oxazol-3-yl]-2-(4-tert-butylphenyl)ethyl]benzoate

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: Methyl 4-[2-[5-(4-bromophenyl)-1,2-oxazol-3-yl]-2-(4-tert-butylphenyl)ethyl]benzoate
• 英文别名: methyl 4-[2-[5-(4-bromophenyl)-1,2-oxazol-3-yl]-2-(4-tert-butylphenyl)ethyl]benzoate
• 化学式: C₂₉H₂₈BrNO₃
• 分子量: 518.4
• InChiKey: FQWMKRNCLAAACV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8
• 重原子数：
  34
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  52.3
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Novel Antagonists of the Glucagon Receptor
  申请人：Gomez-Galeno Jorge E.

  公开号：US20120214769A1

  公开（公告）日：2012-08-23

  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.

  本发明提供了式（I）的新化合物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该化合物的制药组合物，以及治疗、预防、延迟发病时间或降低一种或多种需要胰高血糖素受体拮抗剂的疾病或症状的发展或进展的方法，包括1型和2型糖尿病、胰岛素抵抗和高血糖。本发明还提供了制备式I的化合物，包括其盐和共晶体的方法，以及包含该化合物的制药组合物。
• 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。
• Antagonists of the glucagon receptor
  申请人：Metabasis Therapeutics, Inc.

  公开号：EP2786985A2

  公开（公告）日：2014-10-08

  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 their use in 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 resistence and hyperglycemia.

  本发明提供了具有胰高血糖素受体拮抗剂或反向激动剂活性的新型式 I 化合物及其药学上可接受的盐和共晶体。本发明进一步提供了包含这些化合物的药物组合物，以及它们在治疗、预防、推迟发病时间或降低疾病或病情发展或恶化风险的方法中的用途，这些疾病或病情适用于一种或多种胰高血糖素受体拮抗剂，包括 I 型和 II 型糖尿病、胰岛素抵抗和高血糖症。
• US9169201B2
  申请人：——

  公开号：US9169201B2

  公开（公告）日：2015-10-27
• US9701626B2
  申请人：——

  公开号：US9701626B2

  公开（公告）日：2017-07-11