4-(alpha-Hydroxy-5-(1-imidazolyl)-2-methylbenzyl)-3,5-dimethylbenzoic acid | 104363-98-6

• 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: 4-(alpha-Hydroxy-5-(1-imidazolyl)-2-methylbenzyl)-3,5-dimethylbenzoic acid
• 英文别名: sodium;4-[hydroxy-(5-imidazol-1-yl-2-methylphenyl)methyl]-3,5-dimethylbenzoate
• CAS: 104363-98-6
• 化学式: C20H19N2NaO3
• 分子量: 358.4
• InChiKey: HRUWEADDSLYBSH-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  -0.75
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  78.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-(alpha-Hydroxy-5-(1-imidazolyl)-2-methylbenzyl)-3,5-dimethylbenzoic acid 、 溴乙烷 生成 α-(2,6-dimethyl-4-ethoxycarbonylphenyl)-2-methyl-5-(1-imidazolyl)benzenemethanol
  参考文献：
  名称：

  TSURUDA, MINEO;SHIOTSUKI, TAKAKO;MATSUMOTO, TAKASHI;OE, TAKANORI, YAKUGAKU DZASSI, 109,(1989) N, S. 26-32

  摘要：

  DOI：
• 作为产物：
  描述：

  4-[5-(imidazol-1-yl)-2-methylbenzoyl]-3,5-dimethylbenzoic acid 生成 4-(alpha-Hydroxy-5-(1-imidazolyl)-2-methylbenzyl)-3,5-dimethylbenzoic acid
  参考文献：
  名称：

  Drugs Fut 1988, 13, 970

  摘要：

  DOI：

文献信息

• PHARMACEUTICAL COMPOSITION HAVING IMPROVED RELEASABILITY
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：EP0379579A1

  公开（公告）日：1990-08-01

  pharmaceutical composition comprising sodium 4-(a-hydroxy-5-(1-imidazolyl)-2-methylbenzyl)-3, 5-dimethylbenzoate or its optical isomer or hydrates thereof having improved releasability which further contains D-mannitol and/or sodium hydrogencarbonate and a water-soluble high-molecular compound. This composition can release the above- described compound irrespective of the pH value in digestive tracts including stomach.

  由 4-(a-羟基-5-(1-咪唑基)-2-甲基苄基)-3, 5-二甲基苯甲酸钠或其光学异构体或其水合物组成的药物组合物，具有更好的释放性，其中还含有 D-甘露糖醇和/或碳酸氢钠以及水溶性高分子化合物。这种组合物可以释放上述化合物，而不受消化道（包括胃）pH 值的影响。
• AGENT FOR PREVENTION AND DEPRESSION OF DRY COUGHING CAUSED BY ANGIOTENSIN CONVERTING ENZYME INHIBITORS
  申请人：KISSEI PHARMACEUTICAL CO., LTD.

  公开号：EP0875254A1

  公开（公告）日：1998-11-04

  The present invention is to provide an agent for the prevention and depression of dry coughing caused by angiotensin converting enzyme inhibitors which comprises a thromboxane synthetase inhibitor or thromboxane receptor antagonist as the active ingredient. Administering the drug is effective in preventing and depressing dry coughing caused by angiotensin converting enzyme inhibitors. For example, the use of the drug in combination with ozagrel hydrochloride was found to be effective in significantly dry coughing in hypertonic patients suffering from dry coughing attributable to the administration of captopril.

  本发明旨在提供一种预防和抑制由血管紧张素转换酶抑制剂引起的干咳的药物，其活性成分包括血栓素合成酶抑制剂或血栓素受体拮抗剂。服用该药物可有效预防和抑制血管紧张素转换酶抑制剂引起的干咳。例如，对于因服用卡托普利而引起干咳的高渗患者，将该药物与盐酸奥扎格雷联合使用可有效明显缓解干咳。
• Method for prophylaxis and treatment of diabetic complications with 4[alpha-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid and derivatives
  申请人：——

  公开号：US20030130332A1

  公开（公告）日：2003-07-10

  The present invention relates to an agent for the prophylaxis and treatment of diabetic complications comprising, as an active ingredient, 4-[&agr;-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof. The present invention further relates to a method for the prophylaxis and treatment of diabetic complications comprising administering an effective amount of this compound. The medicament of the present invention is useful for the prophylaxis and treatment of diabetic complications, namely, diabetic neuropathy, nephropathy, ophthalmopathy, arteriosclerosis and the like. The action of the drug is long-lasting for very small doses and a single administration a day is sufficient.

  本发明涉及一种预防和治疗糖尿病并发症的制剂，其活性成分包括4-[&agr;-羟基-2-甲基-5-(1-咪唑基)苄基]-3,5-二甲基苯甲酸、其光学活性化合物或其药学上可接受的盐。本发明还涉及一种预防和治疗糖尿病并发症的方法，该方法包括施用有效量的该化合物。本发明的药物可用于预防和治疗糖尿病并发症，即糖尿病神经病变、肾病、眼病、动脉硬化等。只需很小的剂量，药物的作用就能持久，每天只需服用一次即可。
• Method for prophylaxis and treatment of diabetic complications with 4{alpha-hydroxy-2-methyl-5-(1-imidazolyl)benzyl}-3,5-dimethylbenzoic acid and derivatives
  申请人：Hayashi Yoshiharu

  公开号：US20050239856A1

  公开（公告）日：2005-10-27

  The present invention relates to an agent for the prophylaxis and treatment of diabetic complications comprising, as an active ingredient, 4-[α-hydroxy-2-methyl-5(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof. The present invention further relates to a method for the prophylaxis and treatment of diabetic complications comprising administering an effective amount of this compound. The medicament of the present invention is useful for the prophylaxis and treatment of diabetic complications, namely, diabetic neuropathy, nephropathy, ophthalmopathy, arteriosclerosis and the like. The action of the drug is long-lasting for very small doses and a single administration a day is sufficient.

  本发明涉及一种预防和治疗糖尿病并发症的制剂，其活性成分包括4-[α-羟基-2-甲基-5(1-咪唑基)苄基]-3,5-二甲基苯甲酸、其光学活性化合物或其药学上可接受的盐。本发明还涉及一种预防和治疗糖尿病并发症的方法，包括施用有效量的本化合物。本发明的药物可用于预防和治疗糖尿病并发症，即糖尿病神经病变、肾病、眼病、动脉硬化等。只需很小的剂量，药物的作用就能持久，每天只需服用一次即可。
• JPH02704A
  申请人：——

  公开号：JPH02704A

  公开（公告）日：1990-01-05