2-[(2-methoxy-phenoxy)-phenyl-methyl]-morpholine | 742010-90-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-[(2-methoxy-phenoxy)-phenyl-methyl]-morpholine
• 英文别名: 2-[α-(2-methoxy-phenoxy)-benzyl]-morpholine；2-[alpha-(2-methoxy-phenoxy)-benzyl]-morpholine；2-[(2-methoxyphenoxy)-phenylmethyl]morpholine
• CAS: 742010-90-8
• 化学式: C₁₈H₂₁NO₃
• 分子量: 299.37
• InChiKey: MZGJHBJKODTIQM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  39.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-benzyl-2-[α-(2-methoxy-phenoxy)-benzyl]-morpholine 在 钯 silica gel 、 氯仿 、 甲醇 、 ammonium hydroxide 作用下， 以 乙醇 、 盐酸 为溶剂， 反应 4.0h， 以to obtain 2-[α-(2-methoxy-phenoxy)-benzyl]-morpholine (2.1 g; yield 54.7%) as a transparent oil的产率得到2-[(2-methoxy-phenoxy)-phenyl-methyl]-morpholine
  参考文献：
  名称：

  Substituted morpholine derivatives and pharmaceutical compositions

  摘要：

  本文揭示了替代吗啡啶衍生物，例如化合物2-[α-(3,4-甲氧基苯氧基)-苄基]-吗啡啶。所述化合物对中枢神经系统活性，并可用作抗抑郁剂。

  公开号：

  US04271160A1

文献信息

• Substituted morpholine derivatives and compositions
  申请人：Farmitalia Carlo Erba, S.p.A.

  公开号：US04229449A1

  公开（公告）日：1980-10-21

  Substituted morpholine derivatives, such as, for instance, the compound 2-[.alpha.-(2-methoxy-phenoxy)-benzyl]-morpholine are disclosed. The claimed compounds are active on the central nervous system, and may be used as antidepressant agents.

  替代吗啉衍生物，例如化合物2-[α-(2-甲氧基苯氧基)-苄基]-吗啉已被披露。所述化合物对中枢神经系统活性，并可用作抗抑郁药物。
• [EN] ORGANIC COMPOUNDS<br/>[FR] COMPOSÉS ORGANIQUES
  申请人：INTRA-CELLULAR THERAPIES INC

  公开号：WO2016154027A1

  公开（公告）日：2016-09-29

  The present invention relates to novel pyridinoxy phenylpropanamines, their pharmaceutical compositions and methods of use. In addition, the present invention relates to therapeutic methods that penetrate the blood-brain barrier and regulate the norepinephrine and serotonin transporters ("NET/SERT").

  本发明涉及新型吡啶氧基苯基丙胺、其药物组合物和使用方法。此外，本发明涉及能穿透血脑屏障并调节去甲肾上腺素和5-羟色胺转运体（"NET/SERT"）的治疗方法。
• Method for treatment of depression and anxiety disorders by combination therapy
  申请人：Arneric P. Stephen

  公开号：US20050059654A1

  公开（公告）日：2005-03-17

  A method is provided of treating depression in mammals, including a human, as well as depression and a concomitant disease, disorder or condition exemplified by, but not limited to, anxiety, sleep disorder and post-traumatic stress disorder. The method comprises administering to the mammal in effective amount a combination of active ingredients comprising a) an alpha-2delta (A2D) ligand or a prodrug thereof, or a pharmaceutically acceptable salt of said A2D ligand or said prodrug and, active agents selected from; (b) a selective serotonin re-uptake inhibitor (SSRI) or a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug, (c) a selective noradrenaline re-uptake inhibitor (SNRI) or a prodrug thereof or a pharmaceutically acceptable salt of said SNRI or said prodrug and mixtures of (b) and (c). A pharmaceutical composition comprising a therapeutically effective amount (a) an A2D ligand or a prodrug thereof, or a pharmaceutically acceptable salt of said A2D ligand or said prodrug and active agents selected from; (b) an SSRI or a prodrug thereof or a pharmaceutically acceptable salt of said SSRI or said prodrug, (c) an SNRI or a prodrug thereof or a pharmaceutically acceptable salt of said SNRI or said prodrug and mixtures of (b) and (c) is also provided. Preferred active ingredients for the treatment and the pharmaceutical composition include pregabalin, gabapentin, sertraline and reboxetine.

  本发明提供了一种治疗哺乳动物（包括人类）抑郁症的方法，以及抑郁症和伴随疾病、障碍或状况的方法，例如但不限于焦虑症、睡眠障碍和创伤后应激障碍。该方法包括向哺乳动物施用有效量的活性成分组合，其中包括 a) α-2δ（A2D）配体或其原药，或所述 A2D 配体或所述原药的药学上可接受的盐，以及选自以下各项的活性剂；(b) 选择性血清素再摄取抑制剂（SSRI）或其原药或所述 SSRI 或所述原药的药学上可接受的盐， (c) 选择性去甲肾上腺素再摄取抑制剂（SNRI）或其原药或所述 SNRI 或所述原药的药学上可接受的盐，以及 (b) 和 (c) 的混合物。还提供了一种药物组合物，该组合物包含治疗有效量的(a) A2D 配体或其原药，或所述 A2D 配体或所述原药的药学上可接受的盐和选自以下的活性剂；(b) SSRI 或其原药或所述 SSRI 或所述原药的药学上可接受的盐；(c) SNRI 或其原药或所述 SNRI 或所述原药的药学上可接受的盐以及(b)和(c)的混合物。用于治疗和药物组合物的优选活性成分包括普瑞巴林、加巴喷丁、舍曲林和雷贝西汀。
• COMBINATION COMPRISING AN ALPHA-2-DELTA LIGAND AND AN SSRI AND/OR SNRI FOR TREATMENT OF DEPRESSION AND ANXIETY DISORDERS
  申请人：Warner-Lambert Company LLC

  公开号：EP1675582A1

  公开（公告）日：2006-07-05
• Pyridine derivatives as NET/SERT modulators
  申请人：Intra-Cellular Therapies, Inc.

  公开号：EP2161998B1

  公开（公告）日：2015-09-02