6,7-dichloro-2-methylsulfonyl-3-(N-tert-butylamino)quinoxaline | 281209-71-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6,7-dichloro-2-methylsulfonyl-3-(N-tert-butylamino)quinoxaline
• 英文别名: 6,7-dichloro-2-methylsulfonyl-3-tertbutylaminoquinoxaline；N-[6,7-Dichloro-3-(methylsulfonyl)-2-quinoxalinyl]N-tert-butylamine；N-(tert-Butyl)-6,7-dichloro-3-(methylsulfonyl)quinoxalin-2-amine；N-tert-butyl-6,7-dichloro-3-methylsulfonylquinoxalin-2-amine
• CAS: 281209-71-0
• 化学式: C₁₃H₁₅Cl₂N₃O₂S
• 分子量: 348.253
• InChiKey: GNZCSGYHILBXLL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  80.3
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-(N-叔丁基氨基)-3,6,7-三氯喹喔啉 、 sodium methansulfinate 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 6,7-dichloro-2-methylsulfonyl-3-(N-tert-butylamino)quinoxaline
  参考文献：
  名称：

  Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor

  摘要：

  Following our previous publication describing the biological profiles, we herein describe the structure-activity relationships of a core set of quinoxalines as the hGLP-1 receptor agonists. The most potent and efficacious compounds are 6,7-dichloroquinoxalines bearing an alkyl sulfonyl group at the C-2 position and a secondary alkyl amino group at the C-3 position. These findings serve as a valuable starting point for the discovery of more drug-like small molecule agonists for the hGLP-1 receptor. (C) Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.06.086

文献信息

• Treatment of hyperinsulinemic hypoglycemia with GLP-1 antagonist exendin(9-39)
  申请人：The Board of Trustees of The Leland Stanford Junio

  公开号：US10660937B2

  公开（公告）日：2020-05-26

  Treatment of hyperinsulinemic hypoglycemia comprises administration of an effective amount of glucagon-like peptide-1 receptor antagonist (GLP1RA) exendin(9-39). Patients suffering from hyperinsulinemic hypoglycemia after bariatric surgery or gastrointestinal surgery experience particular benefit, as there is no current method effective for their treatment. Prevention or reduction of acute adverse effects of postprandial hypoglycemia, such as palpitations, tremor, weakness, sweating, confusion, fatigue, blurred vision, seizures, or loss of consciousness, and prevention of chronic adverse effects of hyperinsulinemic hypoglycemia, such as cognitive impairment, can be achieved by treatment with GLP1RA exendin(9-39).

  治疗高胰岛素血症性低血糖症的方法包括服用有效剂量的胰高血糖素样肽-1受体拮抗剂（GLP1RA）exendin(9-39)。减肥手术或胃肠道手术后出现高胰岛素血症低血糖的患者尤其受益，因为目前还没有有效的治疗方法。使用 GLP1RA exendin(9-39) 可以预防或减轻餐后低血糖的急性不良反应，如心悸、震颤、虚弱、出汗、精神错乱、疲劳、视力模糊、癫痫发作或意识丧失，还可以预防高胰岛素血症低血糖的慢性不良反应，如认知障碍。
• Treatment of post-bariatric hypoglycemia with GLP-1 antagonists
  申请人：The BOT of The Leland Stanford Junior University

  公开号：US10993992B2

  公开（公告）日：2021-05-04

  Treatment of hyperinsulinemic hypoglycemia comprises administration of an effective amount of a glucagon-like peptide-1 receptor antagonist (GLP1RA) alone or in combination with an amylinomimetic agent or any anti-gastric emptying agent. Patients suffering from hyperinsulinemic hypoglycemia after bariatric surgery experience particular benefit, as there is no current method effective for their treatment. Prevention or reduction of acute adverse effects of postprandial hypoglycemia, such as palpitations, tremor, weakness, sweating, confusion, fatigue, blurred vision, seizures, or loss of consciousness, and prevention of chronic adverse effects of hyperinsulinemic hypoglycemia, such as cognitive impairment, can be achieved by treatment with GLP1RA.

  治疗高胰岛素血症性低血糖症的方法包括单独或联合使用有效量的胰高血糖素样肽-1 受体拮抗剂 (GLP1RA)、拟淀粉药剂或任何抗胃排空药剂。减肥手术后出现高胰岛素血症低血糖的患者尤其受益，因为目前还没有有效的治疗方法。使用 GLP1RA 可以预防或减轻餐后低血糖的急性不良反应，如心悸、震颤、虚弱、出汗、精神错乱、疲劳、视力模糊、癫痫发作或意识丧失，还可以预防高胰岛素血症低血糖的慢性不良反应，如认知障碍。
• METHODS FOR TREATING DISORDERS OF THE GASTROINTESTINAL TRACT USING A GLP-1 AGONIST
  申请人：Sinai Health System

  公开号：EP2555791B1

  公开（公告）日：2017-11-01
• TREATMENT OF POST-BARIATRIC HYPOGLYCEMIA WITH GLP-1 ANTAGONISTS
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：EP3297653A1

  公开（公告）日：2018-03-28
• Methods for Treating Disorders of the Gastrointestinal Tract Using a GLP-1 Agonist
  申请人：Drucker Daniel J.

  公开号：US20130053316A1

  公开（公告）日：2013-02-28

  The invention provides a method of treating a subject having, or at risk of developing, a condition in which functioning of the small or large intestine is impaired, enhancing functioning or preventing damage to the small or large intestine in a subject, or ameliorating inflammation of the small or large intestine in a subject, comprising administering to the subject a GLP-1 receptor agonist. A GLP-1 receptor agonist may also be provided in a pharmaceutically acceptable form in an amount effective to treat or prevent conditions of the small or large intestine. Further, pharmaceutical compositions are provided for the treatment or prevention of conditions of the small or large intestine comprising a GLP-1 receptor agonist, together with a pharmaceutically acceptable carrier, excipient or vehicle.