依利沙坦 | 149968-26-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 依利沙坦
• 英文名称: Elisartan
• 英文别名: 2-butyl-4-chloro-1((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-1H-imidazole-5-carboxylic acid,-1-(ethoxycarbonyloxy)ethylester；HN-65021；1-ethoxycarbonyloxyethyl 2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
• CAS: 149968-26-3
• 化学式: C₂₇H₂₉ClN₆O₅
• 分子量: 553.017
• InChiKey: IDAWWPOAHPVPMY-UHFFFAOYSA-N

物化性质

• 沸点：
  745.0±70.0 °C(Predicted)
• 密度：
  1.35±0.1 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  6.5
• 重原子数：
  39
• 可旋转键数：
  14
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  134
• 氢给体数：
  1
• 氢受体数：
  9

安全信息

• 储存条件：
  2-8℃

制备方法与用途

生物活性方面，Elisartan 是一种可口服的非肽类 angiotensin II AT1 受体拮抗剂，其作为 HN-12206 的前体药物，具备显著的降压作用。

文献信息

• [EN] DUAL-ACTING ANTIHYPERTENSIVE AGENTS<br/>[FR] AGENTS ANTIHYPERTENSIFS À DOUBLE ACTION
  申请人：THERAVANCE INC

  公开号：WO2009035543A1

  公开（公告）日：2009-03-19

  The invention relates to compounds having the formula: (I) wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

  本发明涉及具有以下公式的化合物：(I) 其中：Ar、r、R3、Z、X和R5-7按说明书定义，或其药用可接受盐。这些化合物具有AT1受体拮抗活性和中性内肽酶抑制活性。本发明还涉及包含这些化合物的药物组合物；使用这些化合物的方法；以及制备这些化合物的过程和中间体。
• NEPRILYSIN INHIBITORS
  申请人：Hughes Adam D.

  公开号：US20130330366A1

  公开（公告）日：2013-12-12

  In one aspect, the invention relates to compounds having the formula XII: where R a , R b , R 2 , R 7 , and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

  在一方面，本发明涉及具有公式XII的化合物： 其中R a ，R b ，R 2 ，R 7 和X如说明书中所定义，或其药用可接受的盐。所述的化合物是具有中性粒细胞弹性蛋白酶抑制活性的化合物的前药。在另一方面，本发明涉及包含这些化合物的药物组合物；使用这些化合物的方法；以及制备这些化合物的过程和中间体。
• [EN] NEPRILYSIN INHIBITORS<br/>[FR] INHIBITEURS DE LA NÉPRILYSINE
  申请人：THERAVANCE BIOPHARMA R & D IP LLC

  公开号：WO2015116786A1

  公开（公告）日：2015-08-06

  In one aspect, the invention relates to compounds having the formula (I): where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

  在一方面，本发明涉及具有公式（I）的化合物：其中R1-R6定义如说明书中所述，或其药用可接受的盐。这些化合物具有中性粒细胞弹性蛋白酶抑制活性。在另一方面，本发明涉及包含这些化合物的药物组合物；使用这些化合物的方法；以及制备这些化合物的过程和中间体。
• [EN] NOVEL BIPHENYL SARTANS<br/>[FR] NOUVEAUX BIPHÉNYLSARTANS
  申请人：UNIV MELBOURNE

  公开号：WO2011134019A1

  公开（公告）日：2011-11-03

  The present invention relates to compounds and compositions useful in modulating the renin-angiotensin system (RAS) in cells, and in particular to compounds which, inter alia, act as angiotensin II antagonists by binding to angiotensin II receptors. The invention also relates to the use of these compounds and compositions in the treatment of conditions responsive to angiotensin II antagonists such as hypertension, edema, renal failure, benign prostatic hypertrophy glaucoma, atherosclerosis, diabetes, Alzheimer's disease and congestive heart failure.

  本发明涉及在细胞中调节肾素-血管紧张素系统（RAS）的化合物和组合物，特别是涉及一些作为血管紧张素II拮抗剂的化合物，通过结合血管紧张素II受体发挥作用。该发明还涉及在治疗对血管紧张素II拮抗剂敏感的疾病中使用这些化合物和组合物，如高血压、水肿、肾功能衰竭、良性前列腺增生、青光眼、动脉粥样硬化、糖尿病、阿尔茨海默病和充血性心力衰竭。
• NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS
  申请人：Mammen Mathai

  公开号：US20130323271A1

  公开（公告）日：2013-12-05

  In one aspect, the invention relates to compounds having the formula: where R 1 , R 2 , R 3 , R 7 , R 8 , Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

  在一方面，本发明涉及具有以下公式的化合物：其中R1、R2、R3、R7、R8、Z、X、b和c按说明书定义，或其药用可接受的盐。这些化合物是氧化氮供体并具有中性内肽酶抑制活性。在另一方面，本发明涉及包含此类化合物的药物组合物；使用此类化合物的方法；以及制备此类化合物的过程和中间体。