2-amino-N-[(2S)-2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide | 133267-39-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-amino-N-[(2S)-2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide
• CAS: 133267-39-7
• 化学式: C₁₂H₁₈N₂O₄
• 分子量: 254.28
• InChiKey: PTKSEFOSCHHMPD-SNVBAGLBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  93.8
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Controlled release pharmaceutical composition for oral use containing midodrine and/or active metabolite, desglymidodrine
  申请人：——

  公开号：US20020034544A1

  公开（公告）日：2002-03-21

  Novel controlled release pharmaceutical compositions for oral use containing midodrine and/or its active metabolite desglymidodrine. The novel compositions are designed to release midodrine and/or desglymidodrine after oral intake in a manner which enables absorption to take place in the gastrointestinal tract so that a relatively fast peak plasma concentration of the active metabolite desglymidodrine is obtained followed by a prolonged and relatively constant plasma concentration of desglymidodrine. The novel compositions may be designed for administration once or twice daily, i.e. a therapeutically effective concentration of desglymidodrine is maintained for a period of at least 10-16 hours followed by a wash out period of about 8-12 hours in order to avoid the well-known midodrine related side effect with respect to supine hypertension. The therapeutically effective concentration of desglymidodrine is regarded as a plasma concentration of desglymidodrine of at least about 3 ng/ml. A composition is designed to release midodrine and/or desglymidodrine in at least the following consecutive steps: i) an initial relatively fast release of midodrine and/or desglymidodrine (in order to obtain a relatively fast onset of action), ii) a steady release or a slower release than in step 1 of midodrine and/or desglymidodrine (in order to maintain a plasma concentration of desglymidodrine which is prolonged and relatively constant), iii) a second rise in release of midodrine and/or desglymidodrine (in order to take advantage of absorption from the colon, i.e. such a second rise release is designed to take place when the composition (or the disintegrated parts of the composition) reaches the colon; normally this is regarded to take about 8 hours after oral intake, and iv) a decline in release rate corresponding to that essentially all midodrine and/or desglymidodrine have been released from the composition. Also disclosed is a method for treating orthostatic hypotension and/or urinary incontinence, the method comprising administration to a patient in need thereof of an effective amount of midodrine and/or desglymidodrine in a composition according to the invention.

  含有米多君和/或其活性代谢物去甘米多君的新型口服控释药物组合物。这些新型组合物的设计目的是在口服后释放米多君和/或去甲斑蝥素，其释放方式可使胃肠道吸收，从而使活性代谢物去甲斑蝥素的血浆浓度相对较快达到峰值，随后去甲斑蝥素的血浆浓度长时间保持相对稳定。 新型组合物可设计为每天给药一次或两次，即去氨加米多君的治疗有效浓度至少维持 10-16 小时，然后经过约 8-12 小时的冲淡期，以避免众所周知的与米多君有关的仰卧位高血压副作用。去氨加米多君的治疗有效浓度是指去氨加米多君的血浆浓度至少约为 3 纳克/毫升。一种组合物可至少按以下连续步骤释放米多君和/或去甘米多君：i) 最初相对快速地释放米多君和/或去氨加米多君（以获得相对快速的起效时间），ii) 稳定释放米多君和/或去氨加米多君或比步骤 1 更慢地释放米多君和/或去氨加米多君（以维持去氨加米多君血浆浓度的长期和相对稳定），iii) 米多君和/或去氨加米多君的第二次上升释放（以利用从结肠吸收的优势，即这种第二次上升释放是通过结肠吸收），iii) 米多君和/或去氨加米多君的第二次上升释放（以利用从结肠吸收的优势，即这种第二次上升释放是通过结肠吸收）。例如，当组合物（或组合物的崩解部分）到达结肠时，第二次释放上升就会发生；通常这被认为是在口服后 8 小时左右；以及 iv) 释放率下降，这与基本上所有米多君和/或去甲米多君都从组合物中释放出来相对应。 本发明还公开了一种治疗直立性低血压和/或尿失禁的方法，该方法包括向有需要的患者施用有效量的米多君和/或去氨加米多君组合物。
• Pharmaceutical compositions comprising desglymidodrine as an active drug substance
  申请人：——

  公开号：US20020147232A1

  公开（公告）日：2002-10-10

  Novel pharmaceutical compositions comprising desglymidodrine or a pharmaceutically acceptable salt thereof as an active drug substance. Desglymidodrine is the active metabolite of the prodrug midodrine. The pharmaceutical composition may be presented in a suitable dosage form for oral, parenteral, mucosal, nasal, sublingual, buccal, topical, vaginal, rectalor ocular etc. administration. A pharmaceutical composition of the invention may be in the form of an immediate and/or modified release composition or it may be designed to release the active drug substance, desglymidodrine, in a relatively fast manner in order to enable a relatively fast onset of the therapeutic effect. The compositions have a suitable shelf-life, i.e. the desglymidodrine contained in the composition is not subject to a significant degradation under storage conditions normally acceptable for pharmaceuticals. Also disclosed is a method for treating animals such as, e.g. mammals and humans with a novel pharmaceutical composition comprising desglymidodrine. Furthermore, is disclosed a novel use of desglymidodrine in the treatment of septic shock and to a method for treating mammals (e.g. humans) suffering from septic shock with a sufficient amount of desglymidodrine

  由去甘米多君或其药学上可接受的盐作为活性药物物质组成的新型药物组合物。去甘米多君是原药米多君的活性代谢产物。本发明的药物组合物可以口服、肠外、粘膜、鼻腔、舌下、口腔、局部、阴道、直肠或眼部等给药的合适剂型呈现。本发明的药物组合物可以是速释和/或改良释放组合物的形式，也可以设计成以相对较快的方式释放活性药物物质去甲斑蝥素，以实现相对较快的治疗效果。组合物具有合适的保质期，即组合物中所含的去氨加米多君在药品通常可接受的储存条件下不会发生明显降解。 还公开了一种用包含去苷腺嘌呤的新型药物组合物治疗动物（如哺乳动物和人类）的方法。 此外，还公开了去氨加米多君在治疗脓毒性休克中的新用途，以及用足量的去氨加米多君治疗患有脓毒性休克的哺乳动物（如人类）的方法。
• US6761904B2
  申请人：——

  公开号：US6761904B2

  公开（公告）日：2004-07-13
• US7070803B2
  申请人：——

  公开号：US7070803B2

  公开（公告）日：2006-07-04