1-(2-Methyl-2-aza-bicyclo[2.2.1]hept-5-en-3-yl)-ethanone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-(2-Methyl-2-aza-bicyclo[2.2.1]hept-5-en-3-yl)-ethanone
• 英文别名: 1-(2-Methyl-2-azabicyclo[2.2.1]hept-5-en-3-yl)ethanone
• 化学式: C₉H₁₃NO
• 分子量: 151.208
• InChiKey: CMTCVILLDWKYDT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  盐酸甲胺 、 环戊二烯 、 丙酮醛 以 水 为溶剂， 反应 20.0h， 以67%的产率得到1-(2-Methyl-2-aza-bicyclo[2.2.1]hept-5-en-3-yl)-ethanone
  参考文献：
  名称：

  Aza Diels-Alder reactions in water: Cyclocondensation of C-acyl iminium ions with cyclopentadiene

  摘要：

  DOI：

  10.1016/s0040-4039(00)84425-1

文献信息

• Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
  申请人：Cottrell M. Kevin

  公开号：US20070161789A1

  公开（公告）日：2007-07-12

  The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

  本发明涉及式I的化合物：或其药学上可接受的盐或混合物，其抑制丝氨酸蛋白酶活性，特别是丝氨酸蛋白酶NS3-NS4A的活性。因此，它们通过干扰丙型肝炎病毒的生命周期而起作用，并且也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，无论是用于外体使用还是用于治疗患有HCV感染的患者的给药，以及制备这些化合物的过程。本发明还涉及通过给予本发明的化合物组成物来治疗患者的HCV感染的方法。本发明还涉及制备这些化合物的过程。
• Inhibitors of serine proteases, particular HCV NS3-NS4A protease
  申请人：Pitlik Janos

  公开号：US20070292933A1

  公开（公告）日：2007-12-20

  The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

  本发明涉及抑制丝氨酸蛋白酶活性的化合物，特别是乙型肝炎病毒NS3-NS4A蛋白酶的活性。因此，它们通过干扰乙型肝炎病毒的生命周期而起作用，并且也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，无论是用于体外使用还是用于治疗患有HCV感染的患者的给药。本发明还涉及通过给予含有本发明化合物的组合物来治疗患有HCV感染的患者的方法。本发明还涉及制备这些化合物的过程。
• INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE
  申请人：Pitlik Janos

  公开号：US20100173851A1

  公开（公告）日：2010-07-08

  The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

  本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒NS3-NS4A蛋白酶活性的化合物。因此，它们通过干扰丙型肝炎病毒的生命周期发挥作用，并且也可用作抗病毒剂。本发明还涉及包含这些化合物的组合物，无论是用于体外使用还是用于治疗HCV感染的患者的给药。本发明还涉及通过给予含有本发明化合物的组合物来治疗患者的HCV感染的方法。本发明还涉及制备这些化合物的方法。
• Inhibitors of Serine Proteases
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20130177531A1

  公开（公告）日：2013-07-11

  This invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof wherein C* represents a diastereomeric carbon comprising a mixture of R and S isomers wherein the R isomer is greater than 50% of the mixture.
• INHIBITORS OF SERINE PROTEASES
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20140056847A1

  公开（公告）日：2014-02-27

  This invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof wherein C* represents a diastereomeric carbon comprising a mixture of R and S isomers wherein the R isomer is greater than 50% of the mixture.