N-[5-[2-[2-(3-hydroxy-9H-carbazol-2-yloxy)ethylamino]-1-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide

• 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: N-[5-[2-[2-(3-hydroxy-9H-carbazol-2-yloxy)ethylamino]-1-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide
• 英文别名: N-[5-[2-[2-(3-hydroxy-9H-carbazole-2-yloxy)ethylamino]-1-hydroxyethyl]-2-hydroxyphenyl]methansulfonamide；N-[2-hydroxy-5-[1-hydroxy-2-[2-[(3-hydroxy-9H-carbazol-2-yl)oxy]ethylamino]ethyl]phenyl]methanesulfonamide
• 化学式: C₂₃H₂₅N₃O₆S
• 分子量: 471.534
• InChiKey: VBXJNUVUFQZVBR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  33
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  152
• 氢给体数：
  6
• 氢受体数：
  8

文献信息

• Novel tricyclic compounds and drug compositions containing same
  申请人：ASAHI KASEI KOGYO KABUSHIKI KAISHA

  公开号：US20030139475A1

  公开（公告）日：2003-07-24

  Compounds having a &bgr;-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R 1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R 2 represents hydrogen, hydroxymethyl, NHR 3 , SO 2 NR 4 R 4′ , or nitro; R 6 represents hydrogen or lower alkyl; and X represents nitrogen, R 9 represents hydrogen, one of R 7 and R 8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.

  具有&bgr;-3肾上腺素受体激动剂的化合物，可用于治疗和预防糖尿病、肥胖症、高脂血症等疾病，其通式表示为(I)，并且包括其盐，以及制备这些化合物和其中间体的方法。其中，R代表氢或甲基；R1代表氢、卤素、羟基、苄氧基、氨基或羟甲基；R2代表氢、羟甲基、NHR3、SO2NR4R4′或硝基；R6代表氢或低碳基；X代表氮；R9代表氢；R7和R8中的一个代表氢，而另一个代表氢、氨基、乙酰氨基或羟基。
• NOVEL TRICYCLIC COMPOUNDS AND DRUG COMPOSITIONS CONTAINING THE SAME
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0882707A1

  公开（公告）日：1998-12-09

  Compounds represented by general formula (I) or salts thereof, a process for producing the same, and intermediates therefor, wherein R represents hydrogen or methyl; R1 represents hydrogen, hologeno, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4, or nitro; R6 represents hydrogen or lower alkyl; and X represents nitrogen, oxygen, sulfur, or methylene, provided that when X represents nitrogen, oxygen, or sulfur, then R9 represents hydrogen, one of R7 an R8 represents hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy, and when X represents methylene, then R7 and R8 each represents hydrogen and R9 represents hydrogen, amino, etc. They have a β-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc.

  通式(I)所代表的化合物或其盐类，以及生产该化合物或其盐类的工艺和中间体，其中R代表氢或甲基；R1代表氢、囟素、羟基、苄氧基、氨基或羟甲基；R2代表氢、羟甲基、NHR3、SO2NR4R4或硝基；R6代表氢或低级烷基；X代表氮、氧、硫或亚甲基，但当X代表氮、氧或硫时，R9代表氢，R7和R8中的一个代表氢，另一个代表氢、氨基、乙酰氨基或羟基；当X代表亚甲基时，R7和R8各自代表氢，R9代表氢、氨基等。它们具有β-3肾上腺素受体激动剂的作用，可作为治疗和预防糖尿病、肥胖症、高脂血症等的药物。
• Combinations comprising a beta-agonist and a further antidiabetic agent
  申请人：SmithKline Beecham p.l.c.

  公开号：US20030073644A1

  公开（公告）日：2003-04-17

  A method for the treatment of diabetes mellitus and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a beta agonist and another antidiabetic agent, to a mammal in need thereof.

  一种治疗哺乳动物（如人类）糖尿病及糖尿病相关病症的方法，该方法包括向有需要的哺乳动物施用有效、无毒且药学上可接受量的β受体激动剂和另一种抗糖尿病剂。
• Compositions and methods for the amelioration of leptin resistance
  申请人：——

  公开号：US20040242485A1

  公开（公告）日：2004-12-02

  It is an objective of the present invention to provide a novel method of ameliorating leptin resistance. In order to achieve the above objective, the present invention provides a method of ameliorating leptin resistance in a patient, which comprises a process of administering a &bgr; 3 adrenergic receptor agonist to the patient with leptin resistance.

  本发明的目的是提供一种改善瘦素抵抗的新方法。为了实现上述目标，本发明提供了一种改善患者瘦素抗性的方法，该方法包括给患者注射一种&bgr； 3 肾上腺素能受体激动剂。
• US6037362A
  申请人：——

  公开号：US6037362A

  公开（公告）日：2000-03-14