4-(3-methyl-3H-imidazol-4-ylmethyl)-3-propyl-dihydro-furan-2-one

• 分子结构分类: 有机化合物 - 生物碱及其衍生物
• 英文名称: 4-(3-methyl-3H-imidazol-4-ylmethyl)-3-propyl-dihydro-furan-2-one
• 英文别名: 4-(3-Methyl-3H-imidazol-4-ylmethyl)-3-propyl-dihydro-furan-2-on；4-((1-Methyl-1H-imidazol-5-yl)methyl)-3-propyldihydrofuran-2(3H)-one；4-[(3-methylimidazol-4-yl)methyl]-3-propyloxolan-2-one
• 化学式: C₁₂H₁₈N₂O₂
• 分子量: 222.287
• InChiKey: HXISNRUOUSNUDX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  44.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  4-(3-methyl-2-thioxo-2,3-dihydro-1H-imidazol-4-ylmethyl)-3-propyl-dihydro-furan-2-one 在 硝酸 作用下， 生成 4-(3-methyl-3H-imidazol-4-ylmethyl)-3-propyl-dihydro-furan-2-one
  参考文献：
  名称：

  Preobrashenskii et al., Doklady Akademii Nauk SSSR, 1951, vol. 81, p. 613,615, 616

  摘要：

  DOI：

文献信息

• Medical use of inhibitors of glutaminyl and glutamate cyclases
  申请人：Probiodrug AG

  公开号：EP1961416A1

  公开（公告）日：2008-08-27

  The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.

  本发明提供了哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物、QC的新效应物、筛选此类效应物的方法、以及使用此类效应物和包含此类效应物的药物组合物来治疗可通过调节QC活性来治疗的病症。优选的组合物还包括DP IV或类似DP IV酶的抑制剂，用于治疗或缓解可通过调节QC和DP IV活性来治疗的病症。
• Use of inhibitors of glutaminyl clyclase
  申请人：Probiodrug AG

  公开号：EP2289498A1

  公开（公告）日：2011-03-02

  The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of diseases that can be treated by modulation of QC-activity, e.g. diseases selected from the group consisting of duodenal cancer with or w/o Heliobacter pylori infections, colorectal cancer, Zolliger-Ellison syndrome, Familial British Dementia and Familial Danish Dementia.

  本发明提供了哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物、QC 的新效应物和这种效应物的用途以及包含这种效应物的药物组合物，用于治疗可通过调节 QC 活性来治疗的疾病，例如：选自幽门螺杆菌感染或未感染幽门螺杆菌的十二指肠癌、结肠直肠癌、佐利格-艾利森综合征、家族性英国痴呆症和家族性痴呆症等疾病。例如：十二指肠癌（伴有或不伴有幽门螺旋杆菌感染）、结肠直肠癌、Zolliger-Ellison 综合征、家族性英国痴呆症和家族性丹麦痴呆症。
• Use of effectors of glutaminyl and glutamate cyclases
  申请人：Demuth Hans-Ulrich

  公开号：US20050058635A1

  公开（公告）日：2005-03-17

  The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.

  本发明提供了哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物、QC的新效应物、筛选此类效应物的方法、以及使用此类效应物和包含此类效应物的药物组合物来治疗可通过调节QC活性来治疗的病症。优选的组合物还包括DP IV或类似DP IV酶的抑制剂，用于治疗或缓解可通过调节QC和DP IV活性来治疗的病症。
• MEDICAL USE OF INHIBITORS OF GLUTAMINYL AND GLUTAMATE CYCLASES FOR TREATING ALZHEIMER'S DISEASE AND DOWN SYNDROME
  申请人：Probiodrug AG

  公开号：EP1620082B1

  公开（公告）日：2010-04-21
• INHIBITORS OF GLUTAMINYL CYCLASE
  申请人：Probiodrug AG

  公开号：EP1620091B1

  公开（公告）日：2010-03-31