3-(4-bromo-2,6-dimethyl-benzyl)-6-(2-methyl-oxiranylmethyl)-6-phenyl-[1,3]oxazinan-2-one | 1254223-45-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: 3-(4-bromo-2,6-dimethyl-benzyl)-6-(2-methyl-oxiranylmethyl)-6-phenyl-[1,3]oxazinan-2-one
• 英文别名: 3-[(4-Bromo-2,6-dimethylphenyl)methyl]-6-[(2-methyloxiran-2-yl)methyl]-6-phenyl-1,3-oxazinan-2-one
• CAS: 1254223-45-4
• 化学式: C₂₃H₂₆BrNO₃
• 分子量: 444.368
• InChiKey: BXRPUSVCLSPNRC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  42.1
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
  申请人：Renz Martin

  公开号：US20100331320A1

  公开（公告）日：2010-12-30

  This invention relates to novel compounds of the Formula Ik, Im 1 , Im 2 , Im 5 , In 1 , In 2 , In 5 , Io 1 , Io 2 , Io 5 , Ip 1 , Ip 3 , pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

  这项发明涉及到Ik、Im1、Im2、Im5、In1、In2、In5、Io1、Io2、Io5、Ip1、Ip3的新化合物，以及其药学上可接受的盐和药物组合物，这些化合物对于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病是有用的。该发明还涉及这些新化合物的药物组合物和它们在细胞中减少或控制皮质醇的产生或抑制皮质醇酮转化为皮质醇的方法。
• Cyclic Inhibitors of 11Beta-Hydroxysteroid Dehydrogenase 1
  申请人：Himmelsbach Frank

  公开号：US20130096108A1

  公开（公告）日：2013-04-18

  Disclosed is a compound represented by Formula (Im 1 ): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (Im 1 ) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11β-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (Im 1 ), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (Im 1 ) are defined herein.

  本发明揭示了一种由公式（Im1）表示的化合物，或其药学上可接受的盐、单水合物、对映体或二对映异构体。本发明还揭示了包括公式（Im1）化合物或其药学上可接受的盐、单水合物、对映体或二对映异构体的制药组合物，以及抑制11β-HSD1活性的方法，其中包括向需要此类治疗的哺乳动物施用公式（Im1）化合物或其药学上可接受的盐、单水合物、对映体或二对映异构体的有效量。公式（Im1）中变量的值在此定义。
• Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2687525A1

  公开（公告）日：2014-01-22

  This invention relates to novel compounds of the Formula lm1, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals.

  本发明涉及式 lm1 的新型化合物、其药学上可接受的盐及其药物组合物，可用于治疗与哺乳动物体内 11 β-HSD1 的调节或抑制有关的疾病。
• CYCLIC INHIBITORS OF 11 BETA-HYDROXYSTEROID DEHYDROGENASE 1
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2324018A1

  公开（公告）日：2011-05-25
• CYCLIC INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2687525B1

  公开（公告）日：2015-09-23