罗加米定

• 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
• 中文名称: 罗加米定
• 中文别名: 罗各米定
• 英文名称: N-diaminomethylene-(trans-2,5-dihydro 2,5-dimethyl-1H-pyrrol-1-yl)acetamide
• 英文别名: N-carbamimidoyl-2-[(2R,5R)-2,5-dimethyl-2,5-dihydropyrrol-1-yl]acetamide
• 化学式: C₉H₁₆N₄O
• 分子量: 196.252
• InChiKey: QHMGFQBUOCYLDT-RNFRBKRXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  84.7
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  罗加米定 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 4.5h， 生成 <2-(trans-2,5-dihydro-2,5-dimethyl-1H-pyrrol-1-yl)ethyl>guanidine
  参考文献：
  名称：

  Synthesis and antidiarrheal activity of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides related to guanfacine

  摘要：

  A series of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides, related to guanfacine, were prepared and tested for antidiarrheal activity in castor oil dosed rats. trans-N-(Aminoiminomethyl)-2,5-dihydro-2,5-dimethyl-1H-pyrrole-1-acetami de (2), in which the dichlorophenyl ring of guanfacine is replaced by 2,5-dimethyl-2,5-dihydropyrrole, showed potent antidiarrheal activity but possessed only minimal cardiovascular activity in rats.

  DOI：

  10.1021/jm00149a013
• 作为产物：
  描述：

  2,5-二甲基-3-吡咯啉 在 sodium methylate 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 37.0h， 生成 罗加米定
  参考文献：
  名称：

  Synthesis and antidiarrheal activity of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides related to guanfacine

  摘要：

  A series of N-(aminoiminomethyl)-1H-pyrrole-1-acetamides, related to guanfacine, were prepared and tested for antidiarrheal activity in castor oil dosed rats. trans-N-(Aminoiminomethyl)-2,5-dihydro-2,5-dimethyl-1H-pyrrole-1-acetami de (2), in which the dichlorophenyl ring of guanfacine is replaced by 2,5-dimethyl-2,5-dihydropyrrole, showed potent antidiarrheal activity but possessed only minimal cardiovascular activity in rats.

  DOI：

  10.1021/jm00149a013

文献信息

• [EN] PRODRUG COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] COMPOSITIONS DE PROMÉDICAMENT ET PROCÉDÉS DE TRAITEMENT
  申请人：AQUESTIVE THERAPEUTICS INC

  公开号：WO2021087359A1

  公开（公告）日：2021-05-06

  Pharmaceutical compositions include a prodrug of epinephrine are described.

  药物组合物包括表述的肾上腺素前药。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• Guanidine derivatives
  申请人：John Wyeth & Brother, Ltd.

  公开号：US04140793A1

  公开（公告）日：1979-02-20

  The invention concerns novel guanidine derivatives of the general formula (I) ##STR1## or pharmaceutically acceptable acid addition salts thereof, where.circle.Nrepresents ##STR2## wherein R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl, trifluoromethyl or halogen and R.sup.11 and R.sup.12 each represent hydrogen, lower alkyl, trifluoromethyl or halogen with the proviso that when one or both R.sup.11 or R.sup.12 groups represent halogen then R.sup.1 and R.sup.2 each represent lower alkyl, trifluoromethyl or halogen, R.sup.9 and R.sup.10 each represent hydrogen, lower alkyl or trifluoromethyl and R.sup.13 and R.sup.14 each represent hydrogen, lower alkyl, trifuoromethyl or halogen with the proviso that when one or both R.sup.13 and R.sup.14 groups represent halogen then R.sup.9 and R.sup.10 each represent lower alkyl or trifluoromethyl and R.sup.7 and R.sup.8 each represent hydrogen or lower alkyl and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each represent hydrogen or lower alkyl or R.sup.4 and R.sup.6 are each hydrogen and R.sup.3 and R.sup.5 together represent dimethylene or trimethylene. The guanidine derivatives lower blood pressure in warm-blooded animals.

  该发明涉及一种通式（I）的新型胍啶衍生物 ##STR1## 或其药学上可接受的酸盐，其中.circle.N代表 ##STR2## 其中R.sup.1和R.sup.2分别代表氢、较低的烷基、三氟甲基或卤素，R.sup.11和R.sup.12分别代表氢、较低的烷基、三氟甲基或卤素，但当R.sup.11或R.sup.12中的一个或两个代表卤素时，则R.sup.1和R.sup.2分别代表较低的烷基、三氟甲基或卤素，R.sup.9和R.sup.10分别代表氢、较低的烷基或三氟甲基，R.sup.13和R.sup.14分别代表氢、较低的烷基、三氟甲基或卤素，但当R.sup.13和R.sup.14中的一个或两个代表卤素时，则R.sup.9和R.sup.10分别代表较低的烷基或三氟甲基，R.sup.7和R.sup.8分别代表氢或较低的烷基，R.sup.3、R.sup.4、R.sup.5和R.sup.6分别代表氢或较低的烷基，或者R.sup.4和R.sup.6分别代表氢，R.sup.3和R.sup.5一起代表二亚甲基或三亚甲基。这些胍啶衍生物能降低温血动物的血压。
• [EN] DUAL FUNCTIONING IONIC LIQUIDS AND SALTS THEREOF<br/>[FR] LIQUIDES IONIQUES À DOUBLE FONCTION ET SELS DE CEUX-CI
  申请人：UNIV ALABAMA

  公开号：WO2010078300A1

  公开（公告）日：2010-07-08

  Disclosed herein are ionic liquid compositions comprising active pharmaceutical, biological, and nutritional compounds, and methods of use. Further disclosed are compositions of matter including liquid ion pairs alone or in solution and their use; compositions of ionic liquids that are 'solvated,' for example, 'hydrated' and their uses.

  本文揭示了包括活性药物、生物学和营养化合物的离子液体组合物，以及其使用方法。进一步揭示了包括液态离子对的物质组合物，单独或溶解后使用；以及离子液体的“溶剂化”组合物，例如“水合”的组合物及其用途。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。