N-[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl-L-proline ethyl ester (9CI) | 87420-38-0

• 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
• 英文名称: N-[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl-L-proline ethyl ester (9CI)
• 英文别名: ethyl (2S)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]pyrrolidine-2-carboxylate
• CAS: 87420-38-0
• 化学式: C₂₂H₃₂N₂O₅
• 分子量: 404.5
• InChiKey: NNTZCVNBFRUGPA-WDSOQIARSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  29
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  84.9
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Process for preparation of carboxyalkyldipeptide derivatives
  申请人：Merck & Co., Inc.

  公开号：EP0079521A1

  公开（公告）日：1983-05-25

  A process for the preparation of carboxyalkyldipeptide compounds of the Formula is described wherein R6 is hydroxy, loweralkoxy, or amino; R, R2 and R7 are hydrogen or loweralkyl; R3 is, e.g., hydrogen, or loweralkyl, R' is, e.g., hydrogen, or alkyl of from 1 to 20 carbon atoms, R4 is hydrogen or loweralkyl, R5 is, e.g., hydrogen, or loweralkyl, and, R4 and R5 may be connected together to form an alyklene bridge of from 2 to 4 carbon atoms. The process comprises reacting a compound of the Formula with a dipeptide (or protected dipeptide) of the Formula and an alkali metal cyanide or a trimethylsilycyanide, to form an amino nitrile compound of the Formula followed by hydrolysis. These compounds are useful as converting enzyme inhibitors and as antihypertensive agents.

  描述了一种制备Formula的羧基烷基二肽化合物的过程，其中R6为羟基、低烷氧基或氨基；R、R2和R7为氢或低烷基；R3为氢、低烷基等；R'为氢、1-20碳原子的烷基等；R4为氢或低烷基；R5为氢、低烷基等，R4和R5可以连接在一起形成2-4个碳原子的烷基桥。该过程包括将Formula的化合物与Formula的二肽（或保护的二肽）和碱金属氰化物或三甲基硅氰化物反应，形成Formula的氨基腈化合物，然后进行水解。这些化合物可用作转化酶抑制剂和降压剂。
• Prodrugs of (1S,9S)-9-[[(1S)-1-carboxy-3-phenylpropyl]amino]octahydro-10-oxo-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid and their use in transdermal therapeutic systems
  申请人：Hexal AG

  公开号：EP2537534A1

  公开（公告）日：2012-12-26

  The present invention relates to diester prodrugs of cilazaprilate which undergo enzymatic cleavage to release the active metabolite cilazaprilate that is used for the treatment of hypertension and congestive heart failure. Furthermore the diester prodrugs of cilazaprilate possess all the properties necessary to be topically administered, preferably via transdermal therapeutic systems.

  本发明涉及西拉普利酸二酯原药，该原药经过酶裂解后释放出活性代谢物西拉普利酸，用于治疗高血压和充血性心力衰竭。此外，西拉普利酸二酯原药具有局部给药所需的所有特性，最好是通过透皮治疗系统给药。
• Transdermal administration of ACE inhibitors
  申请人：——

  公开号：US20030064933A1

  公开（公告）日：2003-04-03

  Disclosed is a dermal composition comprising enalapril ethyl ester or another prodrug corresponding to a pharmaceutically active form of an ACE inhibitor in an amount corresponding to a therapeutically effective amount of enalaprilat (or other pharmaceutically active form of enalapri) or pharmaceutically active form of the ACE inhibitor in admixture with a pharmaceutically acceptable carrier. In a preferred embodiment, the carrier is a pressure-sensitive adhesive matrix comprising a polymer or polymer blend. The dermal composition is applied in a method of substantially increasing the flux of enalaprilat through the skin of a human or an animal by maintaining the dermal composition in contact with the skin.

  本发明公开了一种皮肤用组合物，该组合物包含依那普利乙酯或与 ACE 抑制剂的药学活性形式相对应的另一种原药，其用量与治疗有效量的依那普利拉（或依那普利的其他药学活性形式）或 ACE 抑制剂的药学活性形式相对应，并与药学上可接受的载体混合。在一个优选的实施方案中，载体是由聚合物或聚合物混合物组成的压敏粘合基质。通过保持皮肤组合物与皮肤的接触，将皮肤组合物应用于大幅增加依那普利拉通过人或动物皮肤的通量的方法中。
• Transdermal administration of ace inhibitors
  申请人：Li Chensheng

  公开号：US20050100589A1

  公开（公告）日：2005-05-12

  Disclosed is a dermal composition comprising enalapril ethyl ester or another prodrug corresponding to a pharmaceutically active form of an ACE inhibitor in an amount corresponding to a therapeutically effective amount of enalaprilat (or other pharmaceutically active form of enalapri) or pharmaceutically active form of the ACE inhibitor in admixture with a pharmaceutically acceptable carrier. In a preferred embodiment, the carrier is a pressure-sensitive adhesive matrix comprising a polymer or polymer blend. The dermal composition is applied in a method of substantially increasing the flux of enalaprilat through the skin of a human or an animal by maintaining the dermal composition in contact with the skin.

  本发明公开了一种皮肤用组合物，该组合物包含依那普利乙酯或与 ACE 抑制剂的药学活性形式相对应的另一种原药，其用量与治疗有效量的依那普利拉（或依那普利的其他药学活性形式）或 ACE 抑制剂的药学活性形式相对应，并与药学上可接受的载体混合。在一个优选的实施方案中，载体是由聚合物或聚合物混合物组成的压敏粘合基质。通过保持皮肤组合物与皮肤的接触，将皮肤组合物应用于大幅增加依那普利拉通过人或动物皮肤的通量的方法中。
• Esters of (1S,9S)-9-[[(1S)-1-carboxy-3-phenylpropyl]amino]octahydro-10-oxo-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid and their therapeutic use.
  申请人：Hexal AG

  公开号：EP2537534B1

  公开（公告）日：2014-12-17