2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)-2-methylpropanoic acid | 871588-89-5

• 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: 2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)-2-methylpropanoic acid
• 英文别名: 2-(4-Bromo-3,5-dimethyl-1H-pyrazol-1-yl)-2-methylpropanoic acid；2-(4-bromo-3,5-dimethylpyrazol-1-yl)-2-methylpropanoic acid
• CAS: 871588-89-5
• 化学式: C₉H₁₃BrN₂O₂
• 分子量: 261.118
• InChiKey: ADLCKRGWAFXIOM-UHFFFAOYSA-N

物化性质

• 沸点：
  364.8±42.0 °C(Predicted)
• 密度：
  1.50±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  55.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-氨基金刚烷-1-羧酸甲酯 、 2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)-2-methylpropanoic acid 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， 生成 methyl (E)-4-{[2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)-2-methylpropanoyl]amino}adamantane-1-carboxylate
  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
• 作为产物：
  描述：

  3,5-二甲基-4-溴吡唑 、 三氯叔丁醇 在 sodium hydroxide 、 盐酸 作用下， 以 丙酮 、 水 为溶剂， 生成 2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)-2-methylpropanoic acid
  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

• 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。
• Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
  申请人：Pliushchev Marina A.

  公开号：US08372841B2

  公开（公告）日：2013-02-12

  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11-β-羟基类固醇脱氢酶1型酶的抑制剂化合物。本发明还涉及使用11-β-羟基类固醇脱氢酶1型酶的抑制剂用于治疗非胰岛素依赖型2型糖尿病、胰岛素抵抗、肥胖症、脂质代谢紊乱、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病情。
• Methods of use of inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
  申请人：Bitner R. Scott

  公开号：US08415354B2

  公开（公告）日：2013-04-09

  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型酶的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有关的疾病和病症中的应用。
• 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。