butanedioic acid;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate | 1006709-49-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: butanedioic acid;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
• CAS: 1006709-49-4
• 化学式: C24H31ClN2O9
• 分子量: 527.0
• InChiKey: BKAMSNMJKPNJCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  36
• 可旋转键数：
  13
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  175
• 氢给体数：
  4
• 氢受体数：
  11

文献信息

• A process for the preparation of s (-) amlodipine salts
  申请人：Council of Scientific and Industrial Research

  公开号：EP1407773A1

  公开（公告）日：2004-04-14

  Described herein is a process for the preparation of S(-)Amlodipine salts which comprises reaction of S(-)Amlodipine base with a solution of pharmaceutically acceptable acid such as benzene sulfonic acid, oxalic acid, maleic acid, succinic acid and p-toluene sulfonic acid. The reaction is carried out in the presence of an organic solvent at room temperature. The organic solvents include alcohols like ethanol, methanol, 2-propanol, hydrocarbons like toluene and polar solvents like dimethyl sulfoxide. The salt is obtained by addition of water and isolation of the salt formed by filtration. The unique feature of the invention is production of S(-) Amlodipine besylate in good chemical yield, high enantiomeric purity and with the quality required for preparation of pharmaceutical composition i.e. tablet formulation.

  本文描述了一种制备S(-)氨氯地平盐的过程，包括将S(-)氨氯地平碱与苯磺酸、草酸、马来酸、琥珀酸和对甲苯磺酸等药用可接受的酸溶液反应。该反应在有机溶剂存在下在室温下进行。有机溶剂包括乙醇、甲醇、2-丙醇等醇类、甲苯等烃类和二甲基亚砜等极性溶剂。通过加水并通过过滤分离形成的盐来获得盐。该发明的独特特点是以良好的化学产率、高对映纯度和制备制药组合物（如片剂配方）所需的质量生产S(-)氨氯地平苯甲酸盐。
• AMLODIPINE FORMULATIONS
  申请人：Silvergate Pharmaceuticals, Inc.

  公开号：US20190314279A1

  公开（公告）日：2019-10-17

  Provided herein are stable amlodipine liquid formulations. Also provided herein are methods of using amlodipine liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).

  在此提供了稳定的氨氯地平液体制剂。同时还提供了使用氨氯地平液体制剂治疗某些疾病（包括高血压和冠状动脉疾病）的方法。
• Therapeutic compositions comprising excess enantiomer
  申请人：——

  公开号：US20020045648A1

  公开（公告）日：2002-04-18

  The present invention is concerned with pharmaceutical compositions comprising a mixture of amlodipine enantiomers, which compositions have both anti-hypertensive and additional cardiovascular properties derived respectively from their calcium channel-blocking activity and their ability to release vascular nitric oxide (NO).

  本发明涉及制药组合物，其中包含氨氯地平对映体的混合物，这些组合物既具有降压作用，又具有额外的心血管特性，分别源于它们的钙通道阻滞活性和释放血管内皮源性一氧化氮（NO）的能力。
• Therapeutic compositions comprising excess enantiomer of amlodipine
  申请人：Pfizer Limited

  公开号：EP1181932A2

  公开（公告）日：2002-02-27

  The present invention is concerned with pharmaceutical compositions comprising a mixture of amlodipine enantiomers, which compositions have both anti-hypertensive and additional cardiovascular properties derived respectively from their calcium channel-blocking activity and their ability to release vascular nitric oxide (NO).

  本发明涉及由氨氯地平对映体混合物组成的药物组合物，该组合物具有抗高血压和额外的心血管特性，这些特性分别来自其钙通道阻断活性和释放血管一氧化氮（NO）的能力。
• Amlodipine formulations
  申请人：Silvergate Pharmaceuticals, Inc.

  公开号：US10695329B2

  公开（公告）日：2020-06-30

  Provided herein are stable amlodipine oral liquid formulations. Also provided herein are methods of using amlodipine oral liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).

  本文提供了稳定的氨氯地平口服液制剂。本文还提供了使用氨氯地平口服液制剂治疗某些疾病（包括高血压和冠心病）的方法。