3-(4-chlorophenyl)-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)-cyclobutanon | 633317-47-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 英文名称: 3-(4-chlorophenyl)-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)-cyclobutanon
• 英文别名: 3-(4-Chlorophenyl)-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclobutanone；3-(4-chlorophenyl)-3-(5,6,7,8,9,10-hexahydro-[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclobutan-1-one
• CAS: 633317-47-2
• 化学式: C₁₈H₂₀ClN₃O
• 分子量: 329.829
• InChiKey: NCFYDTGZCZTHCE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  47.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(4-chlorophenyl)-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)-cyclobutanon 在 二乙胺基三氟化硫 作用下， 以 二氯甲烷 为溶剂， 反应 24.0h， 生成 3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo [4,3-a]azocine
  参考文献：
  名称：

  [EN] 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA
  [FR] INHIBITEURS DE LA 11-BETA-HYDROXYSTEROIDE DESHYDROGENASE 1 UTILISABLES POUR LE TRAITEMENT DU DIABETE, DE L'OBESITE ET DE LA DYSLIPIDEMIE

  摘要：

  公开号：

  WO2003104207A3
• 作为产物：
  描述：

  3-(4-chlorophenyl)-cis-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)-cyclobutan-r-ol 、 3-(4-chlorophenyl)-cis-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)-cyclobutan-r-ol 在 四丙基高钌酸铵 N-甲基吗啉氧化物 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 生成 3-(4-chlorophenyl)-3-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)-cyclobutanon
  参考文献：
  名称：

  [EN] 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA
  [FR] INHIBITEURS DE LA 11-BETA-HYDROXYSTEROIDE DESHYDROGENASE 1 UTILISABLES POUR LE TRAITEMENT DU DIABETE, DE L'OBESITE ET DE LA DYSLIPIDEMIE

  摘要：

  公开号：

  WO2003104207A3

文献信息

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

  公开号：US20040106664A1

  公开（公告）日：2004-06-03

  Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: 1 are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

  具有I式的化合物，包括药物可接受的盐、水合物和溶剂化合物：1是11&bgr;-HSD1酶的选择性抑制剂。这些化合物可用于治疗糖尿病，如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综合征以及与NIDDM相关的其他症状。
• 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA
  申请人：——

  公开号：US20040048912A1

  公开（公告）日：2004-03-11

  Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: 1 are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

  式I的化合物，包括药学上可接受的盐、水合物和溶剂化物：1是11β-HSD1酶的选择性抑制剂。这些化合物可用于治疗糖尿病，如非胰岛素依赖性糖尿病（NIDDM）、高血糖、肥胖症、胰岛素抵抗、脂质代谢紊乱、高脂血症、高血压、X综合症以及与NIDDM相关的其他症状。
• 11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
  申请人：Merck & Co., Inc.

  公开号：US07179802B2

  公开（公告）日：2007-02-20

  Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

  具有I式的化合物，包括其药学上可接受的盐、水合物和溶剂化物：是11β-HSD1酶的选择性抑制剂。这些化合物可用于治疗糖尿病，如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综合症以及与NIDDM相关的其他症状。
• 11-&bgr;-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia
  申请人：Merck & Co., Inc.

  公开号：US06730690B2

  公开（公告）日：2004-05-04

  Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

  具有I式的化合物，包括其药学上可接受的盐、水合物和溶剂化合物：是11β-HSD1酶的选择性抑制剂。这些化合物对于治疗糖尿病，如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、高血脂症、高血压、X综合症以及与NIDDM相关的其他症状非常有用。
• Method for Transitioning Between Incompatible Olefin Polymerization Catalyst Systems
  申请人：Meier Gerhardus

  公开号：US20110294957A1

  公开（公告）日：2011-12-01

  A method for transitioning from a Ziegler-Natta to a Phillips catalyst system for the olefin polymerization reaction in one reactor, preferably a gas phase reactor, is described. The method comprises the steps of a) discontinuing a first olefin polymerization reaction performed in the presence of the Ziegler-Natta catalyst system; b) performing a second olefin polymerization reaction in the presence of a further catalyst system comprising catalyst components (A) and (B) producing, respectively, a first and a second polyolefin fraction, wherein the M w of the first polyolefin fraction is less than the M w of the second polyolefin fraction and the initial activity of catalyst component (A) exceeds the initial activity of catalyst component (B); and c) performing a third olefin polymerization reaction the presence of the Phillips catalyst system. Thanks to this method, there is no need to empty the reactor after each olefin polymerization reaction, and the transitioning time needed to attain the desired quality of the polyolefin obtained in each olefin polymerization reaction subsequent to the first one is sufficiently short to permit a quick and reliable change of production.