1-[2-(4-morpholinyl)ethyl]-4-Piperidinamine | 1019119-64-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-[2-(4-morpholinyl)ethyl]-4-Piperidinamine
• 英文别名: 1-(2-morpholin-4-ylethyl)piperidin-4-amine
• CAS: 1019119-64-2
• 化学式: C₁₁H₂₃N₃O
• mdl: MFCD11131132
• 分子量: 213.323
• InChiKey: PDULOMYBMMGZIL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  41.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(3-t-butyl-5-(3-(naphthalen-1-yl)ureido)-1H-pyrazol-1-yl)benzoic acid 、 1-[2-(4-morpholinyl)ethyl]-4-Piperidinamine 在 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 作用下， 生成 3-(3-(tert-butyl)-5-(3-(naphthalen-1-yl)ureido)-1H-pyrazol-1-yl)-N-(1-(2-morpholinoethyl)piperidin-4-yl)benzamide
  参考文献：
  名称：

  Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α

  摘要：

  Herein we describe the identification and characterization of a class of molecules that are believed to extend into a region of p38 known as the 'switch pocket'. Although these molecules lack a canonical hinge binding motif, they show K(i) values as low as 100 nM against p38. We show that molecules that interact with this region of the protein demonstrate different binding kinetics than a canonical ATP mimetic, as well as a wide range of kinome profiles. Thus, the switch pocket presents new opportunities for kinome selectivity which could result in unique biochemical responses and offer new opportunities in the field of kinase drug discovery. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.04.097

文献信息

• 6,9-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines
  申请人：——

  公开号：US20030105098A1

  公开（公告）日：2003-06-05

  The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

  本发明涉及6-9-二取代的2- [转-（4-氨基环己基）]氨基嘌呤，其在抑制细胞周期依赖性激酶，特别是cdk-2方面具有用途。本发明还提供了一种预防神经细胞凋亡和抑制肿瘤发展的方法。
• IGF-1R INHIBITOR
  申请人：Kanda Yutaka

  公开号：US20090054508A1

  公开（公告）日：2009-02-26

  The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): wherein R 1 represents —NR 4 R 5 [wherein R 4 represents a hydrogen atom or the like, R 5 represents substituted or unsubstituted lower alkyl, —C(═O)R 6 (wherein R 6 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or the like], or the like, and R 2 and R 3 may be the same or different and each represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, or the like} or a pharmaceutically acceptable salt thereof, and the like.

  本发明提供了一种I型胰岛素样生长因子受体（IGF-1R）抑制剂，其包含下式（I）所表示的吲唑衍生物作为活性成分：其中，R1表示—NR4R5[其中，R4表示氢原子或类似物，R5表示取代或未取代的低碳基，—C（═O）R6（其中，R6表示取代或未取代的低碳基，取代或未取代的芳基或类似物），或类似物]，或类似物，R2和R3可以相同也可以不同，分别表示氢原子，羟基，取代或未取代的低烷氧基，或类似物}或其药学上可接受的盐等。
• 6,9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
  申请人：Aventis Pharmaceuticals Inc.

  公开号：US06642231B2

  公开（公告）日：2003-11-04

  The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

  本发明涉及6-9-二取代的2-[trans-(4-氨基环己基)氨基]嘌呤，其对抑制细胞周期依赖性激酶，特别是cdk-2具有用处。本发明还提供了一种预防神经细胞凋亡和抑制肿瘤发展的方法。
• 6,9-DISUBSTITUTED 2- TRANS-(4- AMINOCYCLOHEXYL) AMINO]PURINES
  申请人：Aventis Pharmaceuticals Inc.

  公开号：EP1056744B1

  公开（公告）日：2003-10-22
• US6479487B1
  申请人：——

  公开号：US6479487B1

  公开（公告）日：2002-11-12