tert-butyl 3-((3-hydroxypropyl)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-((3-hydroxypropyl)amino)azetidine-1-carboxylate
• 英文别名: Tert-butyl 3-(3-hydroxypropylamino)azetidine-1-carboxylate
• 化学式: C₁₁H₂₂N₂O₃
• 分子量: 230.307
• InChiKey: NIHMUXLXURHRQC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  16
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.91
• 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-((3-hydroxypropyl)amino)azetidine-1-carboxylate 在 硝酸 、 乙酸酐 、 potassium carbonate 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 反应 34.0h， 生成 3-((1-((4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl)sulfonyl)azetidin-3-yl)amino)propyl nitrate
  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 、 3-氨基-1-丙醇 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89.2%的产率得到tert-butyl 3-((3-hydroxypropyl)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

• Quinolone derivatives as fibroblast growth factor receptor inhibitors
  申请人：Principia Biopharma, Inc.

  公开号：US11078199B2

  公开（公告）日：2021-08-03

  Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本发明公开了成纤维细胞生长因子抑制剂（FGFR），因此可用于治疗可通过抑制 FGFR 治疗的疾病的化合物。还公开了含有此类化合物的药物组合物和制备此类化合物的工艺。
• [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
• QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR RECEPTOR INHIBITORS
  申请人：Principia Biopharma, Inc.

  公开号：US20190233418A1

  公开（公告）日：2019-08-01

  Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
• 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.