(5-methyl-2-oxo-1,3-dioxolan-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (5-methyl-2-oxo-1,3-dioxolan-4-yl)methyl 5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylate
• 化学式: C₂₉H₃₂N₆O₆
• 分子量: 560.6
• InChiKey: AUXHDCDOTWZWLN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  41
• 可旋转键数：
  11
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  154
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• Process for Preparing Trityl Olmesartan Medoxomil and Olmesartan Medoxomil
  申请人：Pathi Srinivas Laxminarayan

  公开号：US20100160643A1

  公开（公告）日：2010-06-24

  A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula V, b) deesterifying the compound of formula (V) with a base; and c) reacting the product of step (b) with 4-halomethyl-5-methyl-2-oxo-1,3-dioxolene of formula (IV), wherein X is halogen selected from F or Cl or Br or I, to obtain trityl olmesartan medoxomil of formula. The trityl olmesartan medoxomil may be deprotected to produce olmesartan medoxomil.

  制备三苯甲酰奥美沙坦的过程包括：（a）在极性无水溶剂和碱金属碳酸盐、碱金属氢氧化物、碱金属烷氧基和三级胺所组成的碱中的一种存在下，将4-（1-羟基-1-甲基乙基）-2-丙基咪唑-5-羧酸烷基酯与三苯甲酰联苯溴化物缩合，以获得化合物V的化合物；（b）用碱脱酯化式（V）的化合物；和（c）将步骤（b）的产物与式（IV）的4-卤甲基-5-甲基-2-氧代-1,3-二氧杂环戊烷中的卤素（X）选择自F、Cl、Br或I）反应，以获得三苯甲酰奥美沙坦甲氧苯酰基的化合物。三苯甲酰奥美沙坦甲氧苯酰基可以去保护制得奥美沙坦甲氧苯酰基。
• IMPROVEMENT OF DISSOLVABILITY OF PREPARATION CONTAINING OLMESARTAN MEDOXOMIL
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2253318A1

  公开（公告）日：2010-11-24

  Disclosed is a pharmaceutical composition containing olmesartan medoxomil and amlodipine, which has improved dissolvability. The pharmaceutical composition contains (A) olmesartan medoxomil, (B) amlodipine and (C) a calcium-containing additive.

  本发明公开了一种含有奥美沙坦酯甲珂米和氨氯地平的药物组合物，它具有更好的溶解性。 该药物组合物含有 (A) 奥美沙坦酯、(B) 氨氯地平和 (C) 含钙添加剂。
• MEDICINE FOR PREVENTING OR TREATING HYPERTENSION
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3025711A1

  公开（公告）日：2016-06-01

  Present invention provides a pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by administering (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (A) to (C) simultaneously or separately at a time interval: (A) an angiotensin II receptor antagonist, (B) a calcium antagonist, and (C) a diuretic.

  本发明提供了一种预防或治疗高血压或高血压衍生疾病的药物。该药物的特点是在一定时间间隔内同时或分别给药(i)特异性矿物皮质激素受体拮抗剂和(ii)选自以下成分(A)至(C)的一种或多种成分：(A)血管紧张素 II 受体拮抗剂、(B)钙拮抗剂和(C)利尿剂。
• Pharmaceutical for prophylaxis or treatment of hypertension
  申请人：Daiichi Sankyo Company, Limited

  公开号：US10111858B2

  公开（公告）日：2018-10-30

  A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by comprising (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (A) to (C), for administration simultaneously or separately at a time interval: (A) an angiotensin II receptor antagonist, (B) a calcium antagonist, and (C) a diuretic.

  一种用于预防或治疗高血压或由高血压引起的疾病的药物。该药物的特点是由以下成分组成：(i) 特异性矿物皮质激素受体拮抗剂；(ii) 选自以下成分(A)至(C)的一种或多种成分，在一定时间间隔内同时或分别给药：(A) 血管紧张素 II 受体拮抗剂；(B) 钙拮抗剂；(C) 利尿剂。
• DISSOLUTION PROPERTIES OF DRUG PRODUCTS CONTAINING OLMESARTAN MEDOXOMIL
  申请人：Yada Shuichi

  公开号：US20110038898A1

  公开（公告）日：2011-02-17

  A pharmaceutical composition containing olmesartan medoxomil and amlodipine, which has improved dissolvability. Said composition contains (A) olmesartan medoxomil and (B) amlodipine as active ingredients and (C) a calcium-containing additive. A method of improving the dissolution properties of a pharmaceutical composition containing olmesartan medoxomil and amlodipine by using said composition is also provided.