普拉莫瑞林二盐酸盐 | 158827-34-0

• 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: 普拉莫瑞林二盐酸盐
• 英文名称: Pralmorelin dihydrochloride
• 英文别名: (2S)-6-amino-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-aminopropanoyl]amino]-3-naphthalen-2-ylpropanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]hexanamide;dihydrochloride
• CAS: 158827-34-0
• 化学式: C45H57Cl2N9O6
• 分子量: 890.9
• InChiKey: ILOHMCCDCAUTQF-JESKXYQHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  62
• 可旋转键数：
  21
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  256
• 氢给体数：
  11
• 氢受体数：
  8

文献信息

• POWDERY INHALATIONAL PREPARATIONS AND PROCESS FOR PRODUCING THE SAME
  申请人：Kaken Pharmaceutical Co., Ltd.

  公开号：EP1238661A1

  公开（公告）日：2002-09-11

  The present invention is aimed at providing a dry powder inhalation with minimal adhesive-agglomerative property during storage and with a good inhalation behavior for a pharmaceutically active ingredient, and is adry powder inhalation wherein at least an active ingredient is adhered to the surface of a carrier particle comprised of erythritol and/or trehalose. It is also a dry powder inhalation wherein at least S-36496 and/or Pralmorelin dihydrochloride is adhered to the surface of the carrier particle. It is further a dry powder inhalation wherein at least an active ingredient and a surface modifier are adhered to the surface of the carrier particle. It is also a preparation method of these. Said dry powder inhalation may be applied to the capsules for use in an inhaler device. In addition to the achievement of above objectives, the present invention provides a dry powder inhalation with improved taste in inhalation or with reduced discomfort in the oral cavity and the throat, and a preparation method for enabling an easy preparation thereof without complicated processes.

  本发明旨在提供一种干粉吸入剂，该干粉吸入剂在贮存过程中具有最小的粘附结块特性，并且对药物活性成分具有良好的吸入性能，它是一种干粉吸入剂，其中至少有一种活性成分被粘附在由赤藓糖醇和/或曲卤糖组成的载体颗粒表面。它也是一种干粉吸入剂，其中至少有 S-36496 和/或盐酸普拉莫林附着在载体颗粒表面。这也是一种干粉吸入剂，其中至少有一种活性成分和一种表面改性剂附着在载体颗粒的表面。这也是其中的一种制备方法。所述干粉吸入剂可应用于胶囊，以便在吸入器装置中使用。除了实现上述目标之外，本发明还提供了一种干粉吸入剂，其吸入口感有所改善，或减少了口腔和咽喉的不适感，还提供了一种制备方法，使其无需复杂工序即可轻松制备。
• NERVE PROTECTIVE DRUGS
  申请人：Kaken Pharmaceutical Co., Ltd.

  公开号：EP1258250A1

  公开（公告）日：2002-11-20

  An agent for prevention or treatment of diseases involving degeneration or death of nerve cells, characterized by containing a growth hormone secretion promoting substance as an active ingredient, is provided.

  提供了一种预防或治疗涉及神经细胞变性或死亡的疾病的制剂，其特征是含有一种促进生长激素分泌的物质作为活性成分。
• PRALMORELIN-CONTAINING NASAL DROP PREPARATIONS
  申请人：Kaken Pharmaceutical Co., Ltd.

  公开号：EP1297838A1

  公开（公告）日：2003-04-02

  The preparation for intranasal administration comprising D-alanyl-3-(naphthalen-2-yl)-D-alanyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide (pralmorelin) and/or an acid addition salt thereof as an active ingredient and water permits a marked increase in the in vivo absorption of pralmorelin and hence provides adequate efficacy even if it is administered in a small dose at a time. The preparation also allows pralmorelin to be dissolved in an increased amount, so it can be formulated pharmaceutically with great ease. It also high stability over time.

  由 D-丙氨酰-3-(萘-2-基)-D-丙氨酰-L-丙氨酰-L-色氨酰-D-苯丙氨酰-L-赖氨酰胺（普拉莫林）和/或其酸性加成盐作为活性成分和水组成的鼻内给药制剂可显著增加普拉莫林的体内吸收，因此即使每次给药剂量较小，也能提供足够的疗效。这种制剂还能使普拉莫林的溶解量增加，因此可以非常容易地进行药物配制。此外，它还具有较高的长期稳定性。
• PREVENTIVES OR REMEDIES FOR HEART FAILURE
  申请人：Kaken Pharmaceutical Co., Ltd.

  公开号：EP1297839A1

  公开（公告）日：2003-04-02

  Preparations for preventing or treating acute heart failure, chronic heart failure at a phase of acute exacerbation or heart failure at a phase of transition to chronic heart failure, which contain D-alanyl-3-(naphthalen-2-yl)-D-alanyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide and/or salts thereof as an active ingredient.

  用于预防或治疗急性心力衰竭、处于急性加重期的慢性心力衰竭或处于向慢性心力衰竭过渡阶段的心力衰竭的制剂，其活性成分含有D-丙氨酰-3-(萘-2-基)-D-丙氨酰-L-丙氨酰-L-色氨酰-D-苯丙氨酰-L-赖氨酰胺和/或其盐。
• CELL MIGRATION INHIBITOR
  申请人：Kaken Pharmaceutical Co., Ltd.

  公开号：EP1464339A1

  公开（公告）日：2004-10-06

  An agent for prevention or treatment of vascular disease and renal dysfunction that are accompanied by the migration of vascular smooth muscle cells and mesangial cells comprises as an active ingredient a growth-hormone secretion promoting substance receptor agonist that have a strong inhibitory action on the migration of vascular smooth muscle cells and mesangial cells. Using such an agent for prevention or treatment, one can suppress arteriosclerosis, recurrence of intimal thickening after angioplasty, and even glomerulosclerosis.

  一种用于预防或治疗伴有血管平滑肌细胞和间质细胞迁移的血管疾病和肾功能障碍的制剂，其有效成分包括对血管平滑肌细胞和间质细胞迁移具有强烈抑制作用的生长激素分泌促进物质受体激动剂。使用这种制剂进行预防或治疗，可以抑制动脉硬化、血管成形术后内膜增厚复发，甚至肾小球硬化。