(R)-N-[5-[2-[2-(dibenzothiophen-3-yloxy)ethylamino]-1-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide | 268728-18-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻吩类
• 英文名称: (R)-N-[5-[2-[2-(dibenzothiophen-3-yloxy)ethylamino]-1-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide
• 英文别名: N-[5-[(1R)-2-(2-dibenzothiophen-3-yloxyethylamino)-1-hydroxyethyl]-2-hydroxyphenyl]methanesulfonamide
• CAS: 268728-18-3
• 化学式: C₂₃H₂₄N₂O₅S₂
• 分子量: 472.586
• InChiKey: UQTXHXKAPQCRJO-NRFANRHFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  32
• 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：
  145
• 氢给体数：
  4
• 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。
• NOVEL REMEDIES WITH THE USE OF BETA3 AGONIST
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1258253A1

  公开（公告）日：2002-11-20

  Provided is a therapeutic agent comprising at least a compound having a β3 agonist activity and one member selected from the group consisting of an anticholinergic agent, a monoamine reuptake inhibitor, a lipase inhibitor, a selective serotonin reuptake inhibitor, insulin, an insulin secretagogue, biguanide, an α-glucosidase inhibitor, an insulin sensitizer, a HMG-CoA reductase inhibitor, an anion exchange resin, a fibric acid derivative and a nicotinic acid derivative. The β3-agonist has an activity of inhibiting urinary incontinence. Further, when used together with a remedy for urinary incontinence such as propiverine, oxybutynin hydrochloride or tolterodine, it exerts an enhanced anti-urinary incontinence effect. When used together with an antiobestic agent such as sibutramine or orlistat, it exerts an enhanced antiobestic effect. When used together with an antidiabetic agent such as insulin, glibenclamide, acarbose or rosiglitazone, it exerts an enhanced antidiabetic effect. When used together with an antilipemic agent such as bezafibrate or pravastatin, it exerts an enhanced antilipemic effect.

  选择性 5-羟色胺再摄取抑制剂、胰岛素、胰岛素促泌剂、双胍类、α-葡萄糖苷酶抑制剂、胰岛素增敏剂、HMG-CoA 还原酶抑制剂、阴离子交换树脂、纤维酸衍生物和烟酸衍生物。β3-激动剂具有抑制尿失禁的活性。此外，当与治疗尿失禁的药物，如丙哌瑞林、盐酸奥昔布宁或托特罗定一起使用时，其抗尿失禁的效果会增强。与西布曲明或奥利司他等抗呕吐剂一起使用时，可增强抗呕吐效果。与胰岛素、格列本脲、阿卡波糖或罗格列酮等抗糖尿病药同时使用时，可增强抗糖尿病效果。与贝扎贝特或普伐他汀等抗血脂药同时使用时，可增强抗血脂作用。
• 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。