tert-butyl 3-((4-hydroxybutyl)amino)azetidine-1-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: tert-butyl 3-((4-hydroxybutyl)amino)azetidine-1-carboxylate
• 英文别名: Tert-butyl 3-(4-hydroxybutylamino)azetidine-1-carboxylate；tert-butyl 3-(4-hydroxybutylamino)azetidine-1-carboxylate
• 化学式: C₁₂H₂₄N₂O₃
• 分子量: 244.334
• InChiKey: MDHFXVOYKIJKKV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  17
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 3-((4-hydroxybutyl)amino)azetidine-1-carboxylate 在 potassium carbonate 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 反应 18.0h， 生成 2-(2-ethoxy-5-((3-((4-hydroxybutyl)amino)azetidin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one
  参考文献：
  名称：

  [EN] NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS
  [FR] COMPOSÉS INHIBITEURS DE PDE-5 ET/OU DE PDE-6 DONNEURS D'OXYDE D'AZOTE

  摘要：

  公开号：

  WO2021094830A3
• 作为产物：
  描述：

  1-Boc-3-氮杂环丁酮 、 4-氨基-1-丁醇 在 三乙酰氧基硼氢化钠 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以80.58%的产率得到tert-butyl 3-((4-hydroxybutyl)amino)azetidine-1-carboxylate
  参考文献：
  名称：

  [EN] NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS
  [FR] COMPOSÉS INHIBITEURS DE PDE-5 ET/OU DE PDE-6 DONNEURS D'OXYDE D'AZOTE

  摘要：

  公开号：

  WO2021094830A3

文献信息

• [EN] NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS DE PDE-5 ET/OU DE PDE-6 DONNEURS D'OXYDE D'AZOTE
  申请人：ILDONG PHARMACEUTICAL CO LTD

  公开号：WO2021094830A3

  公开（公告）日：2021-06-24
• NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS
  申请人：Ildong Pharmaceutical Co., Ltd.

  公开号：EP4058457A2

  公开（公告）日：2022-09-21
• NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS, AND USES THEREOF
  申请人：ILDONG PHARMACEUTICAL CO., LTD.

  公开号：US20220153746A1

  公开（公告）日：2022-05-19

  The present disclosure provides uses of phosphodiesterase 5 (PDE-5) and/or phosphodiesterase 6 (PDE-6) inhibitor compounds and uses of compositions including said compounds. In some embodiments, said compounds are nitrogen oxide (NO) donating PDE-5 and/or -6 inhibitor compounds that include a nitrogen oxide-containing donor substituent attached to a benzenesulfonamide group. The compounds can provide dual functionality for increasing protein kinase G (PKG) activity by inhibiting PDE-5 and PDE-6, and/or stimulating guanylate cyclase via donation of NO from the donor substituent of the compound. The present disclosure also provides methods of using said compounds and compositions for inhibiting PDE-5 and/or -6 and increasing activity of PKG. The compounds and compositions find use in the treatment of a variety of eye diseases. For example, the subject compounds may be used as a therapeutic agent for glaucoma, age-related macular degeneration, diabetic retinopathy, xerophthalmia, dry eye syndrome, cataracts or uveitis.
• [EN] NITROGEN OXIDE-DONATING PDE-5 AND/OR PDE-6 INHIBITOR COMPOUNDS, AND USES THEREOF<br/>[FR] COMPOSÉS INHIBITEURS DE PDE-5 ET/OU DE PDE-6 DONNEURS D'OXYDE D'AZOTE, ET LEURS UTILISATIONS
  申请人：[en]ILDONG PHARMACEUTICAL CO., LTD.

  公开号：WO2022096930A2

  公开（公告）日：2022-05-12

  The present disclosure provides uses of phosphodiesterase 5 (PDE-5) and/or phosphodiesterase 6 (PDE-6) inhibitor compounds and uses of compositions including said compounds. In some embodiments, said compounds are nitrogen oxide (NO) donating PDE-5 and/or -6 inhibitor compounds that include a nitrogen oxide-containing donor substituent attached to a benzenesulfonamide group. The compounds can provide dual functionality for increasing protein kinase G (PKG) activity by inhibiting PDE-5 and PDE-6, and/or stimulating guanylate cyclase via donation of NO from the donor substituent of the compound. The present disclosure also provides methods of using said compounds and compositions for inhibiting PDE-5 and/or -6 and increasing activity of PKG. The compounds and compositions find use in the treatment of a variety of eye diseases. For example, the subject compounds may be used as a therapeutic agent for glaucoma, age-related macular degeneration, diabetic retinopathy, xerophthalmia, dry eye syndrome, cataracts or uveitis.
• WO2022/96930
  申请人：——

  公开号：——

  公开（公告）日：——