1-aminosulfonyladamantan-4-one | 898265-69-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-aminosulfonyladamantan-4-one
• 英文别名: 4-oxoadamantane-1-sulfonamide
• CAS: 898265-69-5
• 化学式: C₁₀H₁₅NO₃S
• 分子量: 229.3
• InChiKey: XWEDVXAAKUOPSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  85.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-aminosulfonyladamantan-4-one 在 palladium on activated charcoal 氨 、 氢气 、 O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate 、 N,N-二异丙基乙胺 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 48.0h， 生成
  参考文献：
  名称：

  Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors

  摘要：

  Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.

  DOI：

  10.1016/j.bmcl.2006.10.008
• 作为产物：
  描述：

  5-羟基-2-金刚烷酮 在 盐酸 、 四氧化锇 、 N-甲基吲哚酮 、 lithium amide 、 氢溴酸 、 对甲苯磺酸 、 ferric nitrate 、 锌 作用下， 以 四氢呋喃 、 苯 为溶剂， 反应 111.0h， 生成 1-aminosulfonyladamantan-4-one
  参考文献：
  名称：

  Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors

  摘要：

  Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.

  DOI：

  10.1016/j.bmcl.2006.10.008

文献信息

• Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
  申请人：Patel R. Jyoti

  公开号：US20060281773A1

  公开（公告）日：2006-12-14

  The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

  本发明涉及抑制11-β-羟基类固醇脱氢酶1型酶的化合物。本发明进一步涉及使用11-β-羟基类固醇脱氢酶1型酶抑制剂治疗非胰岛素依赖性2型糖尿病、胰岛素抵抗、肥胖症、脂质代谢紊乱、代谢综合征和其他由过度糖皮质激素作用介导的疾病和状况。
• Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
  申请人：Abbott Laboratories

  公开号：US07855308B2

  公开（公告）日：2010-12-21

  The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

  本发明涉及一类抑制11-β-羟基类固醇脱氢酶1型酶的化合物。本发明进一步涉及使用11-β-羟基类固醇脱氢酶1型酶抑制剂治疗非胰岛素依赖型2型糖尿病、胰岛素抵抗、肥胖症、脂质代谢紊乱、代谢综合征和其他由过度糖皮质激素作用介导的疾病和情况。
• INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
  申请人：Bitner R. Scott

  公开号：US20130045978A1

  公开（公告）日：2013-02-21

  The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

  本发明涉及11-β-羟基类固醇脱氢酶1型酶的抑制剂及其在治疗非胰岛素依赖型2型糖尿病、胰岛素抵抗、肥胖症、脂质代谢紊乱、代谢综合症、中枢神经系统疾病以及与过度糖皮质激素相关的疾病和状况中的应用。
• WO2006/74244
  申请人：——

  公开号：——

  公开（公告）日：——
• ADAMANTYL DERIVATIVES AS INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
  申请人：ABBOTT LABORATORIES

  公开号：EP1846363A2

  公开（公告）日：2007-10-24