(R)-N-[3-[2-[2-(7-hydroxy-9H-carbazol-2-yloxy)ethylamino]-1-hydroxyethyl]phenyl]methanesulfonamide | 344780-58-1

• 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: (R)-N-[3-[2-[2-(7-hydroxy-9H-carbazol-2-yloxy)ethylamino]-1-hydroxyethyl]phenyl]methanesulfonamide
• 英文别名: N-[3-[(1R)-1-hydroxy-2-[2-[(7-hydroxy-9H-carbazol-2-yl)oxy]ethylamino]ethyl]phenyl]methanesulfonamide
• CAS: 344780-58-1
• 化学式: C₂₃H₂₅N₃O₅S
• 分子量: 455.535
• InChiKey: OEYXNGHJHLGQRD-QHCPKHFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 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：
  132
• 氢给体数：
  5
• 氢受体数：
  7

文献信息

• Novel substituted tricyclic compounds
  申请人：——

  公开号：US20030040538A1

  公开（公告）日：2003-02-27

  Compounds of the general formula (I) are useful in the treatment and prevention of &bgr;3-related diseases including diabetes, obesity and hyperlipidemia wherein R 1 is hydrogen, halogen, or hydroxyl; R 2 is C 1-4 alkyl or benzyl; R 3 is OR, halogen, trifluoromethyl, C 1-8 alkyl, lower acyl, NR 4 R 4′ , nitro, or cyano; R is hydrogen, C 1-8 alkyl, benzyl group, or optionally substituted lower acyl; R 4 and R 4′ are each independently hydrogen, C 1-4 alkyl, lower acyl, benzyl, or SO 2 R 5 ; R 5 is C 1-4 alkyl or benzyl; W is oxygen, a secondary nitrogen atom (NH), or sulfur; and * represents an asymmetric carbon atom. 1

  通式（I）的化合物在治疗和预防与β3相关的疾病，包括糖尿病、肥胖症和高脂血症方面具有用处，其中R1是氢、卤素或羟基；R2是C1-4烷基或苄基；R3是OR、卤素、三氟甲基、C1-8烷基、较低酰基、NR4R4'、硝基或氰基；R是氢、C1-8烷基、苄基或可选取代的较低酰基；R4和R4'各自独立地为氢、C1-4烷基、较低酰基、苄基或SO2R5；R5是C1-4烷基或苄基；W是氧、次级氮原子（NH）或硫；*代表不对称碳原子。
• NOVEL SUBSTITUTED TRICYCLIC COMPOUNDS
  申请人：Asahi Kasei Kabushiki Kaisha

  公开号：EP1238973A1

  公开（公告）日：2002-09-11

  Compounds of the general formula (I) are useful in the treatment and prevention of β3-related diseases including diabetes, obesity and hyperlipidemia wherein R1 is hydrogen, halogen, or hydroxyl; R2 is lower alkyl or benzyl; R3 is OR, halogen, trifluoromethyl, lower alkyl, lower acyl, NR4R4', nitro, or cyano; R is hydrogen, lower alkyl, benzyl group, or optionally substituted lower acyl; R4 and R4' are each independently hydrogen, lower alkyl, lower acyl, benzyl, or SO2R5; R5 is lower alkyl or benzyl; W is oxygen, a secondary nitrogen atom (NH), or sulfur; and * represents an asymmetric carbon atom.

  通式（I）化合物可用于治疗和预防与β3 有关的疾病，包括糖尿病、肥胖症和高脂血症 其中 R1 是氢、卤素或羟基；R2 是低级烷基或苄基；R3 是 OR、卤素、三氟甲基、低级烷基、低级酰基、NR4R4'、硝基或氰基；R 是氢、低级烷基、苄基或任选取代的低级酰基；R4 和 R4'各自独立地是氢、低级烷基、低级酰基、苄基或 SO2R5；R5 是低级烷基或苄基；W 是氧、仲氮原子 (NH) 或硫；以及 * 代表不对称碳原子。
• 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。