(E)-4-[2-(3,3-difluoro-piperidin-1-yl)-2-methyl-propionylamino]-adamantane-1-carboxylic acid

• 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: (E)-4-[2-(3,3-difluoro-piperidin-1-yl)-2-methyl-propionylamino]-adamantane-1-carboxylic acid
• 英文别名: 4-[[2-(3,3-Difluoropiperidin-1-yl)-2-methylpropanoyl]amino]adamantane-1-carboxylic acid
• 化学式: C₂₀H₃₀F₂N₂O₃
• 分子量: 384.467
• InChiKey: ZBDAZWQMWJFHRD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  69.6
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (E)-4-[2-(3,3-difluoro-piperidin-1-yl)-2-methyl-propionylamino]-adamantane-1-carboxylic acid 、 4-(2-氨基乙基)-苯甲酸甲酯 在 O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate 、 N,N-二异丙基乙胺 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 12.0h， 生成
  参考文献：
  名称：

  Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme

  摘要：

  本发明涉及抑制11-β-羟基类固醇脱氢酶1型酶的化合物。本发明还涉及利用11-β-羟基类固醇脱氢酶1型酶的抑制剂治疗非胰岛素依赖型2型糖尿病、胰岛素抵抗、肥胖、脂质紊乱、代谢综合征以及其他由过度糖皮质激素作用介导的疾病和症状。

  公开号：

  US20050277647A1

文献信息

• TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
  申请人：Bitner R. Scott

  公开号：US20090054426A1

  公开（公告）日：2009-02-26

  A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.

  一种治疗患有与糖尿病相关的中枢神经系统紊乱和缺陷的患者的方法，包括与衰老和神经退行性疾病相关的注意力缺陷障碍，注意力缺陷多动障碍（ADHD），阿尔茨海默病（AD），轻度认知障碍，老年性痴呆症，艾滋病痴呆，神经退行性疾病，抑郁症和精神分裂症，包括向需要此类治疗的患者施用11-β-羟基类固醇脱氢酶1型酶活性的选择性抑制剂的有效量。
• INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
  申请人：Pliushchev Marina A.

  公开号：US20100222316A1

  公开（公告）日：2010-09-02

  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.

  本发明涉及一种抑制11-beta-羟基类固醇脱氢酶1型酶的化合物。本发明还涉及使用11-beta-羟基类固醇脱氢酶1型酶的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病况。
• METHODS OF USE OF INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
  申请人：AbbVie Inc.

  公开号：US20130338169A1

  公开（公告）日：2013-12-19

  The present invention relates to inhibitors of 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型酶抑制剂及其在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、中枢神经系统疾病以及与过度糖皮质激素相关的疾病和病症中的应用。
• Adamantyl- acetamide derivatives as inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
  申请人：Abbott Laboratories

  公开号：EP2345640A1

  公开（公告）日：2011-07-20

  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.

  本发明涉及作为 11-beta- 羟类固醇脱氢酶 1 型酶抑制剂的化合物。本发明进一步涉及 11-beta- 羟类固醇脱氢酶 1 型酶抑制剂用于治疗非胰岛素依赖型 2 型糖尿病、胰岛素抵抗、肥胖、血脂紊乱、代谢综合征以及其他由糖皮质激素作用过度介导的疾病和病症。
• ADAMANTYL-ACETAMIDE DERIVATIVES AS INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
  申请人：ABBOTT LABORATORIES

  公开号：EP1751108A1

  公开（公告）日：2007-02-14