1-[N-[(1S)-1-Carboxy-3-phenylpropyl]-L-alanyl]-L-proline 4-hydroxybutyl ester | 674285-98-4

• 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: 1-[N-[(1S)-1-Carboxy-3-phenylpropyl]-L-alanyl]-L-proline 4-hydroxybutyl ester
• 英文别名: (2S)-2-[[(2S)-1-[(2S)-2-(4-hydroxybutoxycarbonyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-4-phenylbutanoic acid
• CAS: 674285-98-4
• 化学式: C₂₂H₃₂N₂O₆
• 分子量: 420.506
• InChiKey: OSBUMQUEZIOTJC-WDSOQIARSA-N

物化性质

• 沸点：
  629.9±55.0 °C(Predicted)
• 密度：
  1.225±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  30
• 可旋转键数：
  13
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  116
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• Proline ester and preparation containing the same for percutaneous administration
  申请人：Furuishi Takayuki

  公开号：US20050288232A1

  公开（公告）日：2005-12-29

  A proline ester represented by the following formula (I): wherein R 1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.

  以下是翻译结果： 一种由以下式子(I)所表示的脯氨酸酯： 其中R1代表羟基-低烷基基团、低烷氧基-低烷基基团或低烷氧基-低烷氧基-低烷基基团，或其药学上可接受的盐。本发明的脯氨酸酯(I)及其药学上可接受的盐可作为依那普利酸的前药，该药物可用于预防或治疗循环系统疾病，如高血压、心脏疾病（如心肌肥大、心力衰竭和心肌梗死）、肾炎和中风。因此，含有该酯或其盐的药物最好从药效和用途的角度来看，制成经皮制剂，特别是贴片。
• PROLINE ESTER AND PREPARATION CONTAINING THE SAME FOR PERCUTANEOUS ADMINISTRATION
  申请人：Toaeiyo Ltd.

  公开号：EP1538158A1

  公开（公告）日：2005-06-08

  A proline ester represented by the following formula (I) : wherein R1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.

  由下式（I）代表的脯氨酸酯： 其中 R1 代表羟基-低级烷基、低级烷氧基-低级烷基或低级烷氧基-低级烷氧基-低级烷基或其药学上可接受的盐。 本发明的脯氨酸酯（I）及其药学上可接受的盐可用作依那普利拉的原药，而依那普利拉是一种可用于预防或治疗循环系统疾病的药物，如高血压、心脏病（如心脏肥大、心力衰竭和心肌梗塞）、肾炎和肾功能衰竭。因此，从药用活性和用途的角度来看，含有酯或其盐的药物最好配制成经皮制剂，特别是贴剂。
• US7323489B2
  申请人：——

  公开号：US7323489B2

  公开（公告）日：2008-01-29