2-环丁基-吗啉 | 1219844-05-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 中文名称: 2-环丁基-吗啉
• 英文名称: 2-Cyclobutylmorpholine
• CAS: 1219844-05-9
• 化学式: C₈H₁₅NO
• 分子量: 141.213
• InChiKey: YTPPDLPMYCHVGL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-chloro-6-(3-fluoropyridin-4-yl)-3-methylpyrimidin-4(3H)-one 、 2-环丁基-吗啉 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 生成 2-(2-Cyclobutylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-3-methylpyrimidin-4-one
  参考文献：
  名称：

  Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3β inhibitors for Alzheimer’s disease

  摘要：

  We herein describe the results of further evolution of GSK-3 beta inhibitors for Alzheimer's disease from our promising compounds with in vivo tau phosphorylation inhibitory activity by oral administration. Introduction of a low alkyl group instead of the phenyl group at the 3-position of the morpholine moiety aiming to improve pharmacokinetic profiles resulted in potent low molecular weight GSK-3 beta inhibitors with good in vitro pharmacokinetic profiles, which also showed in vivo tau phosphorylation inhibitory activity by oral administration. Effect of the stereochemistry of the alkyl moiety is also discussed using docking models. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2015.01.005

文献信息

• [EN] INHIBITORS OF CBL-B AND METHODS OF USE THEREOF<br/>[FR] INHIBITEURS DE CBL-B ET LEURS PROCÉDÉS D'UTILISATION
  申请人：NURIX THERAPEUTICS INC

  公开号：WO2019148005A1

  公开（公告）日：2019-08-01

  Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.

  揭示了用于抑制泛素蛋白酶体途径中的E3酶Cbl-b的化合物、组合物和使用方法。这些化合物、组合物和方法可用于调节免疫系统，治疗适合免疫系统调节的疾病，并用于体内、体外或体外细胞的治疗。
• [EN] SMALL MOLECULE FATTY ACID SYNTHASE INHIBITORS<br/>[FR] INHIBITEURS DE SYNTHASE D'ACIDES GRAS À PETITES MOLÉCULES
  申请人：SANFORD BURNHAM MED RES INST

  公开号：WO2015134790A1

  公开（公告）日：2015-09-11

  Provided herein are small molecule Fatty Acid Synthase Inhibitors, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

  本文提供了小分子脂肪酸合成酶抑制剂，包括这些化合物的组合物，以及使用这些化合物和包括这些化合物的组合物的方法。
• Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP0236140A2

  公开（公告）日：1987-09-09

  Carbostyril derivatives or salt thereof, including novel compounds, having activities for curing and/or improving arrhythmia. Some carbostyril devitavies having similar chemical structural formula to those of carbostyril derivatives of the present invention are known in the prior art references, however, above-mentioned parmacological activities have not been known yet.

  具有治疗和/或改善心律失常活性的羧基吡啶衍生物或其盐，包括新型化合物。 一些与本发明羧基吡啶衍生物具有相似化学结构式的羧基吡啶衍生物在现有技术参考文献中是已知的，但是，上述心律失常活性尚未为人所知。
• CYCLIC AMIDE DERIVATIVES FOR PROTECTING AGAINST ULTRAVIOLET RAYS
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP0719258A1

  公开（公告）日：1996-07-03
• INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
  申请人：Nurix Therapeutics, Inc.

  公开号：EP3743063A1

  公开（公告）日：2020-12-02