Cambridge id 5156892

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Cambridge id 5156892
• 英文别名: 3,5,7-trimethyladamantane-1-carbohydrazide
• 化学式: C₁₄H₂₄N₂O
• 分子量: 236.357
• InChiKey: WQISOVSDRNHPJG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  Cambridge id 5156892 、 1-氮杂-2-甲氧基-1-环庚烯 以 甲苯 为溶剂， 生成 3-(3,5,7-trimethyl-1-adamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
  参考文献：
  名称：

  Adamantyl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1

  摘要：

  Adamantyl triazoles were identified as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). They are active both in in vitro and in in vivo pharmacodynamic models. The synthesis and structure-activity relationships of these inhibitors are presented. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.06.040

文献信息

• 11-Beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
  申请人：Balkovec M. James

  公开号：US20050070720A1

  公开（公告）日：2005-03-31

  Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body.

  化合物公式为（I）的化合物，包括其药学上可接受的盐和前药：是11β-HSD1酶的选择性抑制剂。它们抑制11β-HSD1介导的可的松和其他11-酮基-糖皮质激素转化为皮质醇和其他11β-羟基-糖皮质激素的过程。因此，11β-HSD1抑制剂减少了目标组织中皮质醇的含量，从而调节了皮质醇的效应。调节皮质醇可能对控制非胰岛素依赖性糖尿病（NIDDM）、高血糖、肥胖症、胰岛素抵抗、血脂异常、高脂血症、高血压、X综合征和与体内过多皮质醇有关的其他症状有效。
• EP1474139A4
  申请人：——

  公开号：EP1474139A4

  公开（公告）日：2005-06-29
• 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA
  申请人：Merck & Co., Inc.

  公开号：EP1474139A2

  公开（公告）日：2004-11-10
• US7329683B2
  申请人：——

  公开号：US7329683B2

  公开（公告）日：2008-02-12
• [EN] 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA<br/>[FR] INHIBITEURS DE LA 11-BETA-HYDROXYSTEROIDE DESHYDROGENASE 1 UTILES POUR LE TRAITEMENT DU DIABETE, DE L'OBESITE ET DE LA DYSLIPIDEMIE
  申请人：MERCK & CO INC

  公开号：WO2003065983A2

  公开（公告）日：2003-08-14

  Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body.