R-2-乙基吗啉 | 1313176-45-2

• 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: R-2-乙基吗啉
• 英文名称: (R)-2-ethylmorpholine
• 英文别名: (2R)-2-ethylmorpholine
• CAS: 1313176-45-2
• 化学式: C₆H₁₃NO
• 分子量: 115.175
• InChiKey: RGNFMQJLAOONTP-ZCFIWIBFSA-N

物化性质

• 沸点：
  160.6±15.0 °C(Predicted)
• 密度：
  0.878±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  8
• 可旋转键数：
  1
• 环数：
  1.0
• 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：

  R-2-乙基吗啉 在 lithium aluminium tetrahydride 、 potassium carbonate 、 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 18.5h， 生成 (R)-N-(2-(2-ethylmorpholino)ethyl)-6-methyl-5-((1-methyl-6-((1-methyl-1H-pyrazol-4-yl)amino)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)amino)nicotinamide
  参考文献：
  名称：

  [EN] PYRAZOLOPYRIMIDINES AND THEIR USES AS PDGFR INHIBITORS
  [FR] PYRAZOLOPYRIMIDINES ET LEURS UTILISATIONS EN TANT QU'INHIBITEURS DE PDGFR

  摘要：

  The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

  公开号：

  WO2023007009A1

文献信息

• SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
  申请人：GLAXOSMITHKLINE LLC

  公开号：US20150152108A1

  公开（公告）日：2015-06-04

  The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

  本发明涉及新型取代桥式脲化合物，相应的相关类似物，药物组合物以及其使用方法。本发明的抑制素调节化合物可用于延长细胞寿命，并治疗和/或预防各种疾病和疾病，包括但不限于与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块疾病、炎症、癌症和/或潮红有关的疾病或疾病，以及那些会受益于增加线粒体活性的疾病或疾病。本发明还涉及包含抑制素调节化合物与另一治疗剂组合的组合物。
• [EN] SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS<br/>[FR] ANALOGUES D'URÉE PONTÉS SUBSTITUÉS EN TANT QUE MODULATEURS DE SIRTUINE
  申请人：GLAXOSMITHKLINE IP NO 2 LTD

  公开号：WO2016079709A1

  公开（公告）日：2016-05-26

  The present invention relates to novel substituted bridged urea analog compounds of Formula (I) or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, processes for making and use of such compounds, alone or in combination with other therapeutic agents, as Sirtuin Modulators useful for increasing lifespan of a cell, and for use in treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.

  本发明涉及一种新型的取代桥式脲类似物化合物，其化学式为（I）或其药学上可接受的盐，相应的药物组合物，制备这种化合物的方法以及单独使用或与其他治疗剂联合使用的这些化合物作为Sirtuin调节剂，可用于增加细胞寿命，并用于治疗和/或预防各种疾病和紊乱，包括但不限于与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块紊乱、炎症、癌症和/或潮红有关的疾病或紊乱，以及那些会受益于增加线粒体活性的疾病或紊乱。
• [EN] ARYL HETEROBICYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ARYLÉS EN TANT QUE BLOQUEURS DU CANAL POTASSIQUE SHAKER KV1.3
  申请人：DE SHAW RES LLC

  公开号：WO2021071832A1

  公开（公告）日：2021-04-15

  A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, where the substituents are as defined herein. Pharmaceutical compositions including the same and method of using the same are also described.

  描述了化合物式(I)或其药用可接受的盐，其中取代基如本文所定义。还描述了包括该化合物的药物组合物以及使用该化合物的方法。
• [EN] PYRIDO[3,4-B]PYRAZINE DERIVATIVES AS SYK INHIBITORS<br/>[FR] DÉRIVÉS PYRIDO[3,4-B]PYRAZINE EN TANT QU'INHIBITEURS DE SYK
  申请人：GLAXO GROUP LTD

  公开号：WO2012123312A1

  公开（公告）日：2012-09-20

  A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.

  化合物的化学式（I）或其盐；它是脾酪氨酸激酶（Syk）的抑制剂，因此可能用于治疗由于肥大细胞、巨噬细胞和B细胞不适当激活而导致的疾病，例如炎症性疾病和/或过敏性疾病，以及癌症治疗，特别是血液恶性肿瘤和自身免疫疾病。
• TETRAHYDROOXEPINOPYRIDINE COMPOUND
  申请人：ASTELLAS PHARMA INC.

  公开号：US20170050973A1

  公开（公告）日：2017-02-23

  [Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an α7 nicotinic acetylcholine receptor (α7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an α7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an α7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an α7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.

  提供的是一种对α7尼古丁乙酰胆碱受体（α7 nACh受体）具有正向别构调节活性（PAM活性）的化合物。解决方法是，本发明者研究了α7 nACh受体上的PAM活性，并发现一种四氢氧杂环吡啶化合物在α7 nACh受体上具有PAM活性，从而完成了本发明。本发明的四氢氧杂环吡啶化合物在α7 nACh受体上具有PAM活性，并可望作为预防或治疗痴呆、认知障碍、精神分裂症、阿尔茨海默病、CIAS、精神分裂症的消极症状、炎症性疾病或疼痛的药剂。