3-(1,3-benzothiazol-2-yl)-1-(5-hydroxy-2-azatricyclo[3.3.1.1^3,7]dec-2-yl)propan-1-one | 1448696-62-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: 3-(1,3-benzothiazol-2-yl)-1-(5-hydroxy-2-azatricyclo[3.3.1.1^3,7]dec-2-yl)propan-1-one
• 英文别名: 3-(1,3-Benzothiazol-2-yl)-1-(5-hydroxy-2-azatricyclo[3.3.1.13,7]decan-2-yl)propan-1-one；3-(1,3-benzothiazol-2-yl)-1-(5-hydroxy-2-azatricyclo[3.3.1.13,7]decan-2-yl)propan-1-one
• CAS: 1448696-62-5
• 化学式: C₁₉H₂₂N₂O₂S
• 分子量: 342.462
• InChiKey: OCLCJPVKVKLQCK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  81.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-氟磺酰基二氟乙酸 、 3-(1,3-benzothiazol-2-yl)-1-(5-hydroxy-2-azatricyclo[3.3.1.1^3,7]dec-2-yl)propan-1-one 在 copper(l) iodide 作用下， 以 乙腈 为溶剂， 反应 0.5h， 以40 mg的产率得到3-(1,3-benzothiazol-2-yl)-1-[5-(difluoromethoxy)-2-azatricyclo[3.3.1.1^3,7]dec-2-yl]propan-1-one
  参考文献：
  名称：

  [EN] DERIVATIVES OF AZA ADAMANTANE AND USES THEREOF
  [FR] DÉRIVÉS D'AZA-ADAMANTANE ET LEURS UTILISATIONS

  摘要：

  本发明涉及某些酰胺衍生物，具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可以通过抑制该酶而预防或治疗的某些疾病方面具有用处。此外，本发明涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、脂质紊乱如血脂异常、高血压以及其他疾病和病症的治疗中发挥作用。

  公开号：

  WO2013111150A1

文献信息

• DERIVATIVES OF AZA ADAMANTANE AND USES THEREOF
  申请人：CONNEXIOS LIFE SCIENCES PVT. LTD.

  公开号：US20150141650A1

  公开（公告）日：2015-05-21

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可以通过抑制该酶而预防或治疗的某些疾病方面具有用处。此外，本发明涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、脂质紊乱如血脂异常、高血压以及其他疾病和病症的治疗中发挥作用。
• DERIVATIVES OF AZA ADAMANTANES AND USES THEREOF
  申请人：Connexios Life Sciences Pvt. Ltd.

  公开号：EP3266783A1

  公开（公告）日：2018-01-10

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，这些衍生物具有抑制11-beta-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此可用于治疗某些可通过抑制该酶来预防或治疗的疾病。此外，本发明还涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将应用于治疗非胰岛素依赖型 2 型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、血脂紊乱（如血脂异常）、高血压以及其他疾病和病症。
• US9303016B2
  申请人：——

  公开号：US9303016B2

  公开（公告）日：2016-04-05
• [EN] METHOD OF WOUND HEALING<br/>[FR] PROCÉDÉ DE CICATRISATION
  申请人：CONNEXIOS LIFE SCIENCES PVT LTD

  公开号：WO2017025989A1

  公开（公告）日：2017-02-16

  The present invention relates to a method of treating a wound, comprising administering to a subject in need thereof a therapeutically effective amount of an aza adamantane compound, or a pharmaceutically acceptable salt, thereof.
• [EN] DERIVATIVES OF AZA ADAMANTANE AND USES THEREOF<br/>[FR] DÉRIVÉS D'AZA-ADAMANTANE ET LEURS UTILISATIONS
  申请人：CONNEXIOS LIFE SCIENCES PVT LTD

  公开号：WO2013111150A1

  公开（公告）日：2013-08-01

  The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.

  本发明涉及某些酰胺衍生物，具有抑制11-β-羟基类固醇脱氢酶1型（11β-HSD-1）的能力，因此在预防或治疗可以通过抑制该酶而预防或治疗的某些疾病方面具有用处。此外，本发明涉及这些化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗某些疾病中的用途。预计本发明的化合物将在治疗非胰岛素依赖型2型糖尿病（NIDDM）、胰岛素抵抗、肥胖、空腹血糖受损、糖耐量受损、脂质紊乱如血脂异常、高血压以及其他疾病和病症的治疗中发挥作用。