2-methyl-6-(piperidin-4-yloxy)pyridine | 724700-04-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-methyl-6-(piperidin-4-yloxy)pyridine
• 英文别名: 4-(6-methylpyridin-2-yl-oxy)piperidine；methyl-6-(piperidin-4-yloxy)pyridin；2-methyl-6-piperidin-4-yloxypyridine
• CAS: 724700-04-3
• 化学式: C₁₁H₁₆N₂O
• mdl: MFCD16713765
• 分子量: 192.261
• InChiKey: JPZKICXEFHFVGE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.545
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-methyl-6-(piperidin-4-yloxy)pyridine 、 (2R,3S)-2-propyl-1-(4-(trifluoromethyl)nicotinoyl)-3-(4-(trifluoromethyl)phenoxy)piperidine-3-carboxylic acid 在 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 C₃₄H₃₆F₆N₄O₄
  参考文献：
  名称：

  Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors

  摘要：

  Led by the structural information of the screening hit with mDM2 protein, a structure modification of Leu26 moiety of the novel p53-hDM2 inhibitors was conducted. A structure-activity relationship study of 4-substituted piperidines revealed compound 20t with good potencies and excellent CYP450 profiles. (C) 2016 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2016.03.078

文献信息

• UDP GLYCOSYLTRANSFERASE INHIBITORS AND METHODS OF USE
  申请人：GENZYME CORPORATION

  公开号：US20200102324A1

  公开（公告）日：2020-04-02

  Described herein is a compound of Formula (I), and pharmaceutically acceptable salts thereof. Also described herein are compositions and the use of such compositions in methods of treating a variety of diseases and conditions, in particular Krabbe's Disease (KD) and Metachromatic leukodystrophy (MLD).

  本文描述了一种化合物，其化学式为（I），以及其药用盐。本文还描述了这些组合物以及在治疗各种疾病和症状的方法中使用这些组合物，特别是克拉贝氏病（KD）和间染色质白质脑病（MLD）。
• [EN] OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2019243530A1

  公开（公告）日：2019-12-26

  The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein RB is an aromatic heterobicyclic radical selected from the group consisting of (b-1) to (b-6).

  本发明涉及具有式(I)所示结构的O-GIcNAc水解酶（OGA）抑制剂。该发明还涉及包含这种化合物的药物组合物、制备这种化合物和组合物的方法，以及利用这种化合物和组合物预防和治疗抑制OGA有益的疾病，如tau病变，特别是阿尔茨海默病或进行性上核性麻痹；以及伴有tau病理的神经退行性疾病，特别是由C90RF72突变引起的肌萎缩侧索硬化或额颞叶痴呆症。其中RB是从（b-1）到（b-6）组成的芳香杂双环基团。
• SULFAMIDE-METALLOPROTEASE INHIBITORS
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP0958287B1

  公开（公告）日：2002-09-11
• THIENO[3,2-B]PYRIDINE DERIVATIVES AS UDP GLYCOSYLTRANSFERASE INHIBITORS AND METHODS OF USE
  申请人：Genzyme Corporation

  公开号：EP3861000A1

  公开（公告）日：2021-08-11
• OGA INHIBITOR COMPOUNDS
  申请人：Janssen Pharmaceutica NV

  公开号：US20210122763A1

  公开（公告）日：2021-04-29

  The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.