(+/-)-2-<(inden-7-yloxy)methyl>-4-ethylmorpholine | 60929-17-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚和异茚
• 英文名称: (+/-)-2-<(inden-7-yloxy)methyl>-4-ethylmorpholine
• 英文别名: 4-ethyl-2-(3H-inden-4-yloxymethyl)-morpholine；4-ethyl-2-(7-indenyloxymethyl)morpholine；4-ethyl-2-(3H-inden-4-yloxymethyl)morpholine
• CAS: 60929-17-1
• 化学式: C₁₆H₂₁NO₂
• 分子量: 259.348
• InChiKey: NQGZTPHYLCNJRP-UHFFFAOYSA-N

物化性质

• 沸点：
  399.5±42.0 °C(Predicted)
• 密度：
  1.089±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  21.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-amino-3-(3H-inden-4-yloxy)propan-2-ol 在 lithium aluminium tetrahydride 、 sodium methylate 、 potassium carbonate 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 、 二氯甲烷 为溶剂， 生成 (+/-)-2-<(inden-7-yloxy)methyl>-4-ethylmorpholine
  参考文献：
  名称：

  Syntheses of (.+-.)-2-((inden-7-yloxy)methyl)morpholine hydrochloride (YM-08054, indeloxazine hydrochloride) and its derivatives with potential cerebral-activating and antidepressive properties.

  摘要：

  研究了(±)-2-[(茚-7-基氧基)甲基]吗啉盐酸盐（7·HCl，YM-08054，盐酸吲哚嗪）的合成及其光学拆分为左旋和右旋异构体。采用优先结晶法从7·HCl及其互变异构体(±)-2-[(茚-4-基氧基)-甲基]吗啉盐酸盐(6·HCl)的平衡混合物中优先结晶，建立了7·HCl的实用合成方法。 ，在催化量的碱的存在下，在MeOH中。研究发现，7·HCl 及其左旋异构体 ((-)-7·HCl) 不仅具有很强的抗抑郁活性，而且具有强大的脑激活特性。还简要讨论了相关化合物的合成和药理活性。

  DOI：

  10.1248/cpb.33.3766

文献信息

• 2-(Indenyloxymethyl) morpholine derivatives
  申请人：Yamanouchi Pharmaceutical Co., Ltd.

  公开号：US04109088A1

  公开（公告）日：1978-08-22

  2-(Indenyloxymethyl) morpholine derivatives are disclosed. These derivatives are excellent in methamphetamine stereotyped increasing and antireserpine activities which are useful as antidepression agents.

  披露了2-(Indenyloxymethyl) morpholine衍生物。这些衍生物在增加甲基苯丙胺的刻板行为和抗利血平活性方面表现出色，可用作抗抑郁药物。
• Use of combinations comprising a corticosteroid and a pyrimidopyrimidine in the treatment of inflammatory diseases
  申请人：Combinatorx, Incorporated

  公开号：EP2070550A1

  公开（公告）日：2009-06-17

  The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering to the patient a tetra-substituted pyrimidopyrimidine, either alone or in combination with one or more additional agents. The invention also features a composition containing a tetra-substituted pyrimidopyrimidine in combination with one or more additional agents.

  本发明的特点是通过向患者单独或与一种或多种附加制剂联合使用四取代嘧啶嘧啶，治疗被诊断患有或有可能患上免疫炎症性疾病的患者。本发明的另一个特点是含有四取代嘧啶嘧啶的组合物与一种或多种附加制剂的组合物。
• Methods, compositions, and kits for the treatment of ophthalmic disorders
  申请人：CombinatoRx, Inc.

  公开号：EP2218442A1

  公开（公告）日：2010-08-18

  The invention features methods, compositions and kits comprising a corticosteroid and a non-steroidal immunophilin-dependent immunosuppressant for treating an ophthalmic disorder in a patient, wherein at least one of said corticosteroid and said non-steroidal immunophilin-dependent immunosuppressant is present at a low concentration, in particular wherein said corticosteroid is prednisolone acetate and said non-steroidal immunophilin-dependent immunosuppressant is cyclosporine A.

  本发明的特征是包含皮质类固醇和非类固醇免疫嗜血素依赖性免疫抑制剂的方法、组合物和试剂盒，用于治疗患者的眼科疾病、其中，所述皮质类固醇和所述非类固醇免疫嗜血素依赖性免疫抑制剂中至少有一种以低浓度存在，特别是所述皮质类固醇为醋酸泼尼松龙，所述非类固醇免疫嗜血素依赖性免疫抑制剂为环孢素 A。
• Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines
  申请人：——

  公开号：US20040229849A1

  公开（公告）日：2004-11-18

  The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering an SSRI or analog or metabolite thereof and, optionally, a corticosteroid or other compound to the patient. The invention also features a pharmaceutical composition containing an SSRI or analog or metabolite thereof and a corticosteroid or other compound for the treatment or prevention of an immunoinflammatory disorder.

  本发明的特点是通过向患者施用 SSRI 或其类似物或代谢物以及皮质类固醇或其他化合物来治疗被诊断患有或有可能患上免疫炎症性疾病的患者。本发明的另一个特点是含有 SSRI 或其类似物或代谢物和皮质类固醇或其他化合物的药物组合物，用于治疗或预防免疫炎症性疾病。
• Combination therapy for the treatment of immunoinflammatory disorders
  申请人：——

  公开号：US20040224876A1

  公开（公告）日：2004-11-11

  The invention features a method for treating a patient diagnosed with, or at risk of developing, an immunoinflammatory disorder by administering a non-steroidal immunophilin-dependent immunosuppressant (NsIDI) and an NsIDI enhancer (NsIDIE) or analog or metabolite thereof to the patient. The invention also features a pharmaceutical composition containing an NsIDI and NsIDIE or analog or metabolite thereof for the treatment or prevention of an immunoinflammatory disorder.

  本发明的特点是通过向患者施用非甾体类免疫嗜血素依赖性免疫抑制剂（NsIDI）和NsIDI增强剂（NsIDIE）或其类似物或代谢物来治疗被诊断患有或有可能患上免疫炎症性疾病的患者。本发明还具有一种含有 NsIDI 和 NsIDIE 或其类似物或代谢物的药物组合物，用于治疗或预防免疫炎症性疾病。