2-amino-5-morpholinophenol | 25912-15-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 2-amino-5-morpholinophenol
• 英文别名: 2-amino-5-morpholin-4-ylphenol
• CAS: 25912-15-6
• 化学式: C₁₀H₁₄N₂O₂
• 分子量: 194.233
• InChiKey: SFXKFYFQUSRBID-UHFFFAOYSA-N

物化性质

• 沸点：
  422.5±45.0 °C(Predicted)
• 密度：
  1.265±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  58.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-amino-5-morpholinophenol 在 4-二甲氨基吡啶 作用下， 以 乙腈 为溶剂， 反应 4.0h， 生成 6-morpholino-2-oxo-N-(4-phenylbutyl)-1,3-benzoxazole-3-carboxamide
  参考文献：
  名称：

  Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors

  摘要：

  Sphingolipids (SphLs) are a diverse class of molecules that are regulated by a complex network of enzymatic pathways. A disturbance in these pathways leads to lipid accumulation and initiation of several SphL-related disorders. Acid ceramidase is one of the key enzymes that regulate the metabolism of ceramides and glycosphingolipids, which are important members of the SphL family. Herein, we describe the lead optimization studies of benzoxazolone carboxamides resulting in piperidine 22m, where we demonstrated target engagement in two animal models of neuropathic lysosomal storage diseases (LSDs), Gaucher's and Krabbe's diseases. After daily intraperitoneal administration at 90 mg kg(-1), 22m significantly reduced the brain levels of the toxic lipids glucosylsphingosine (GluSph) in 4L;C* mice and galactosylsphingosine (GalSph) in Twitcher mice. We believe that 22m is a lead molecule that can be further developed for the correction of severe neurological LSDs where GluSph or GalSph play a significant role in disease pathogenesis.

  DOI：

  10.1021/acs.jmedchem.9b02004
• 作为产物：
  描述：

  5-氟-2-硝基苯酚 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 、 乙醇 、 乙腈 为溶剂， 20.0~60.0 ℃ 、413.7 kPa 条件下， 反应 5.0h， 生成 2-amino-5-morpholinophenol
  参考文献：
  名称：

  HMOX1 inducers

  摘要：

  本发明涉及结构（I）的化合物作为血红素氧合酶1（HMOX 1）诱导剂。本发明还涉及一种控制哺乳动物体内血红素氧合酶1的活性或数量，或活性和数量的方法。这里提供了变量的定义。

  公开号：

  US10766888B1

文献信息

• Therapeutic heterocyclic compounds
  申请人：——

  公开号：US20030013708A1

  公开（公告）日：2003-01-16

  Provided herein is a compound having the formula (I): 1 Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT 1B and 5HT 1D antagonists.

  本文提供的化合物具有以下式（I）： 其中所述化合物可用于治疗精神障碍，包括但不限于抑郁症、广泛性焦虑、进食障碍、痴呆症、恐慌障碍和睡眠障碍。这些化合物还可能用于治疗胃肠道障碍、心血管调节、运动障碍、内分泌障碍、血管痉挛和性功能障碍。这些化合物是5HT 1B和5HT 1D拮抗剂。
• Therapeutic chromone compounds
  申请人：——

  公开号：US20040087575A1

  公开（公告）日：2004-05-06

  Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT 1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.

  本文提供的是一种化合物，其化学式为（I），其中该化合物可用于治疗包括但不限于抑郁症、广泛性焦虑、进食障碍、痴呆症、恐慌障碍和睡眠障碍在内的精神疾病。这些化合物也可能对治疗胃肠道疾病、心血管调节、运动障碍、内分泌失调、血管痉挛和性功能障碍有用。这些化合物是5HT 1B 拮抗剂。本文还提供了制备化合物（I）和中间体化合物的方法。
• Therapeutic chroman compounds
  申请人：——

  公开号：US20040110745A1

  公开（公告）日：2004-06-10

  Provided herein is a compound represented by the Formula (I) wherein said compounds are useful for the treatment of migraine. Also provided are processes for the preparation of compounds of Formula (I) and intermediates.

  本文提供的是一种化合物，其化学式表示为（I），其中这些化合物对治疗偏头痛有用。还提供了制备化合物（I）和中间体的方法。
• [EN] ANTIBIOTIC COMPOUNDS<br/>[FR] COMPOSÉS ANTIBIOTIQUES
  申请人：DISCUVA LTD

  公开号：WO2018037223A1

  公开（公告）日：2018-03-01

  The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.

  本发明涉及公式（I）的抗生素化合物，含有这些化合物的组合物，以及使用这些化合物治疗细菌性疾病和感染的方法。这些化合物在治疗革兰氏阳性和/或革兰氏阴性细菌引起的感染和疾病方面具有应用，特别是在治疗由淋病奈瑟菌引起的感染和疾病方面。
• [EN] THERAPEUTIC QUINOLINE COMPOUNDS WITH 5-HT-ANTAGONISTIC PROPERTIES<br/>[FR] COMPOSES THERAPEUTIQUES A BASE DE QUINOLINE, ANTAGONISTES DES 5-HT
  申请人：ASTRAZENECA AB

  公开号：WO2003037872A1

  公开（公告）日：2003-05-08

  Provided herein is a compound having the formula (I), (R2 is typically a tertiary nitrogen atom, being either alkyl-substituted or member of a heterocyclic ring; R7 is typically a monocyclic or bicyclic aromatic ring or a heterocyclic ring) wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.

  本文提供的化合物具有式(I)，其中(R2通常是三级氮原子，可以是烷基取代或杂环环中的成员；R7通常是单环或双环芳香环或杂环环)，其中所述化合物可用于治疗精神障碍，包括但不限于抑郁症、广泛性焦虑症、进食障碍、痴呆症、惊恐障碍和睡眠障碍。该化合物也可能用于治疗胃肠疾病、心血管调节、运动障碍、内分泌障碍、血管痉挛和性功能障碍。该化合物是5HT1B和5HT1D拮抗剂。