4-(4-dimethylamino-phenyl)-2H-phthalazin-1-one | 75884-69-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4-(4-dimethylamino-phenyl)-2H-phthalazin-1-one
• 英文别名: 4-(4-Dimethylamino-phenyl)-2H-phthalazin-1-on；4-[4-(dimethylamino)phenyl]-2H-phthalazin-1-one
• CAS: 75884-69-4
• 化学式: C₁₆H₁₅N₃O
• 分子量: 265.315
• InChiKey: XIDJIOMKKHURHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  44.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(4-dimethylamino-phenyl)-2H-phthalazin-1-one 在 三氯氧磷 作用下， 生成 1-chloro-4-(p-dimethylaminophenyl)-phthalazine
  参考文献：
  名称：

  酞嗪和哒嗪系列的肼衍生物

  摘要：

  描述了酞嗪和哒嗪的肼基衍生物，其药理学兴趣已在其他地方报道。基本类型的化学修饰涉及杂环或芳香环上的取代，吡啶环取代芳香核，最后改变肼残基。

  DOI：

  10.1002/hlca.19510340122
• 作为产物：
  描述：

  2-[4-(二甲基氨基)苯甲酰基]苯甲酸 在 乙醇 、 一水合肼 作用下， 生成 4-(4-dimethylamino-phenyl)-2H-phthalazin-1-one
  参考文献：
  名称：

  酞嗪和哒嗪系列的肼衍生物

  摘要：

  描述了酞嗪和哒嗪的肼基衍生物，其药理学兴趣已在其他地方报道。基本类型的化学修饰涉及杂环或芳香环上的取代，吡啶环取代芳香核，最后改变肼残基。

  DOI：

  10.1002/hlca.19510340122

文献信息

• 4-Arylphthalazin-1(2H)-one derivatives as potent antagonists of the melanin concentrating hormone receptor 1 (MCH-R1)
  作者：Chae Jo Lim、Soo Hee Kim、Byung Ho Lee、Kwang-Seok Oh、Kyu Yang Yi

  DOI：10.1016/j.bmcl.2011.10.111

  日期：2012.1

  A novel series of 4-arylphthalazin-1(2H)-one linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of an extensive SAR study probing the effects of substituents on the 4-arylphthalazin-1(2H)-one C-4 aryl group led to the identification of the 4-(3,4-difluorophenyl) derivative as a highly potent MCH-R1 inhibitor with an IC50 = 1 nM. However, further investigations showed that this substance has unacceptable pharmacokinetic properties including a high clearance and volume of distribution. (C) 2011 Elsevier Ltd. All rights reserved.
• SMALL MOLECULE MODULATORS OF CYTOKINE ACTIVITY
  申请人：Zembower David E.

  公开号：US20100137285A1

  公开（公告）日：2010-06-03

  The present invention provides compounds having formula (I) or (II): and pharmaceutically acceptable derivatives thereof, wherein m, p, R 1 , R 2 , R 3 and R 4 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of diseases, disorders or conditions associated with HGF/SF or other cytokine activity.
• HEPATOCYTE GROWTH FACTOR PATHWAY ACTIVATORS IN FIBROTIC CONNECTIVE TISSUE DISEASES
  申请人：Paka Latha

  公开号：US20100256117A1

  公开（公告）日：2010-10-07

  Methods are provided for treating fibrotic connective tissue diseases such as scleroderma and conditions such as surgically-induced adhesions using compounds that activate the signaling pathways of hepatocyte growth factor.
• ENHANCEMENT OF CELLULAR TRANSPLANTATION USING SMALL MOLEUCLE MODULATORS OF HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY
  申请人：Oehlen Lambertus J.W.M.

  公开号：US20120190668A1

  公开（公告）日：2012-07-26

  The present invention provides methods for enhancing cellular transplantation by exposing cells in vitro or ex vivo, or a recipient of cells, to a small molecule hepatocyte growth factor/scatter factor mimetic. Exemplary compounds are described.
• ENHANCEMENT OF CELLULAR TRANSPLANTATION USING SMALL MOLECULE MODULATORS HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY
  申请人：ANGION BIOMEDICA CORP

  公开号：US20140171419A1

  公开（公告）日：2014-06-19

  The present invention provides methods for enhancing cellular transplantation by exposing cells in vitro or ex vivo, or a recipient of cells, to a small molecule hepatocyte growth factor/scatter factor mimetic. Exemplary compounds are described.