(-)-4-((αS)-α-((2R,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethyl-benzamide | 200407-08-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (-)-4-((αS)-α-((2R,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethyl-benzamide
• 英文别名: (-)-4-((αS)-α-((2R,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethylbenzamide；(-)-4-((alphaS)-alpha-((2R,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethylbenzamide；4-[(S)-[(2R,5R)-2,5-dimethyl-4-prop-2-enylpiperazin-1-yl]-(3-hydroxyphenyl)methyl]-N,N-diethylbenzamide
• CAS: 200407-08-5
• 化学式: C₂₇H₃₇N₃O₂
• 分子量: 435.61
• InChiKey: LBLDMHBSVIVJPM-YPCDYVTLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  47
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  咪唑 、 (-)-4-((αS)-α-((2R,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N,N-diethyl-benzamide 、 叔丁基二甲基氯硅烷 以 乙醇 、 二氯甲烷 、 水 、 甲苯 、 乙腈 为溶剂， 生成 4-((αS)-α-((2R,5R)-2,5-dimethyl-4-propyl-1-piperazinyl)-3-(tert-butyldimethylsilyloxy)benzyl)-N,N-diethylbenzamide
  参考文献：
  名称：

  Compositions and methods for reducing respiratory depression

  摘要：

  本发明涉及一种用于减少、治疗或预防动物呼吸抑制的方法和组合物，使用的化合物的结构如下：##STR1##其中：Ar、G、Z、R.sup.2、R.sup.3、R.sup.4、R.sup.5、R.sup.6和R.sup.7如规范中所定义，或其药学上可接受的酯或盐。

  公开号：

  US05807858A1

文献信息

• Method of treating sexual dysfunctions with delta opioid receptor agonist compounds
  申请人：——

  公开号：US20030186872A1

  公开（公告）日：2003-10-02

  Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.

  通过向受试者施用含有δ阿片受体激动剂的药物组合物，以延迟受试者在性刺激过程中射精的发生，用于治疗性功能障碍的组合物和治疗方法。
• Compositions and Methods for Reducing Respiratory Depression and Attendant SIde Effects of Mu Opioid Compounds
  申请人：Ardent Pharmaceuticals, Inc.

  公开号：US20020111359A1

  公开（公告）日：2002-08-15

  Abstract of Disclosure A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound. Preferred examples of such delta receptor agonist compound include diarylmethyl piperazine compounds and diarylmethyl piperidine compounds, and pharmaceutical compositions thereof, having utility in medical therapy for reducing respiratory depression associated with certain analgesics, such as mu opiates.

  披露摘要：一种减少、治疗或预防动物中药物介导的呼吸抑制、肌肉僵硬或恶心/呕吐的方法，涉及向接受混合δ/μ阿片受体激动剂或呼吸抑制药物的动物施用有效量的δ受体激动剂化合物。此类δ受体激动剂化合物的优选示例包括二苯甲基哌嗪化合物和二苯甲基哌啶化合物，以及具有医疗疗效的药物组合物，可用于减少与某些镇痛药物（如μ阿片类药物）相关的呼吸抑制。
• Compositions and methods for reducing respiratory depression and
  申请人：Delta Pharmaceuticals

  公开号：US05985880A1

  公开（公告）日：1999-11-16

  A method of reducing, treating or preventing drug-mediated respiratory depression in an animal, incident to the administration to said animal of a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a .delta. receptor agonist compound.

  在动物中减少、治疗或预防药物介导的呼吸抑制的方法，涉及向接受呼吸抑制药物的动物投予有效量的δ受体激动剂化合物。
• [EN] METHOD OF TREATING SEXAUAL DYSFUNCTIONS WITH DELTA OPIOID RECEPTOR AGONIST COMPOUNDS<br/>[FR] METHODE DE TRAITEMENT DE DYSFONCTIONS SEXUELLES AU MOYEN DE COMPOSES D'AGONISTE DU RECEPTEUR DELTA OPIOIDE
  申请人：ARDENT PHARMACEUTICALS INC

  公开号：WO2003057223A1

  公开（公告）日：2003-07-17

  Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.

  本发明涉及一种通过给予患者含有δ-阿片受体激动剂的药物组合物来治疗性功能障碍的方法。在性刺激期间，该药物组合物的有效剂量可以延迟患者射精的开始。
• Compositions and methods for reducing respiratory depression and attendant side effects of mu opioid compounds
  申请人：Chang Kwen-Jen

  公开号：US20050255151A1

  公开（公告）日：2005-11-17

  A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound. Preferred examples of such delta receptor agonist compound include diarylmethyl piperazine compounds and diarylmethyl piperidine compounds, and pharmaceutical compositions thereof, having utility in medical therapy for reducing respiratory depression associated with certain analgesics, such as mu opiates.

  本发明涉及一种减少、治疗或预防动物在接受混合的delta/mu阿片类激动剂或呼吸抑制介导药物时出现的呼吸抑制、肌肉僵硬或恶心/呕吐的方法，包括向接受该药物的动物投与有效剂量的delta受体激动剂化合物。这种delta受体激动剂化合物的优选例子包括二芳基甲基哌嗪化合物和二芳基甲基哌啶化合物，以及其制药组合物，在医疗治疗中用于减轻与某些镇痛药物（如mu阿片类药物）相关的呼吸抑制。