富马酸尼唑苯酮 | 54533-86-7

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 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: 富马酸尼唑苯酮
• 中文别名: 尼唑苯酮富马酸盐；2'-氯-2-(2-二乙胺甲基-1-咪唑基)-5-硝基二苯酮富马酸盐
• 英文名称: Nizofenone fumarate
• 英文别名: (E)-but-2-enedioic acid;(2-chlorophenyl)-[2-[2-(diethylaminomethyl)imidazol-1-yl]-5-nitrophenyl]methanone
• CAS: 54533-86-7
• 化学式: C25H25ClN4O7
• 分子量: 528.9
• InChiKey: JDQAUUIBFFFOOV-WLHGVMLRSA-N

物化性质

• 熔点：
  157-158℃

计算性质

• 辛醇/水分配系数(LogP)：
  4.22
• 重原子数：
  37
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  159
• 氢给体数：
  2
• 氢受体数：
  9

制备方法与用途

制备方法

本品是一种新型咪唑类药物，主要用于改善缺血性脑血管疾病。它能够提高脑功能，抑制脑梗死的发生；同时还能改善脑缺血后的脑电波异常，并恢复锥体束的功能。研究表明，在动物实验中，该药物可以显著延长在缺血或缺氧条件下脑细胞的存活时间，从而缓解因缺氧引起的多种症状。

此药物适用于治疗由缺血导致的脑功能障碍，特别是在蛛网膜下腔出血急性期及其它类型的脑出血所引发的急性脑缺血情况。

文献信息

• CRYSTALLINE CONDITION DISLOCATING METHOD
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0665009A1

  公开（公告）日：1995-08-02

  An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition (△ is dislocated to another crystalline condition (○), i.e., when the dislocation of crystalline condition (△->○) is carried out.

  本发明的目的是提供一种简单、快速和均匀地将结晶药物的结晶状态变位的方法，而且是一次性大量变位。本发明针对的是一种使用挤压机将某种结晶状态（△）的结晶药物变位到另一种结晶状态（○）的方法，即结晶状态（△->○）变位的方法。
• IONTOPHORESIS DEVICE
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP0705619A1

  公开（公告）日：1996-04-10

  To avoid a reduction of the conductivity in iontophoresis due to the electrical decomposition and the changes in chemical properties of the electrodes themselves, covering by an electrical insulator, and to prevent a drop in the transport rate due to ions freed from the electrode. Provision is made of an electrode structure provided integrally with a reversible electrode and an auxiliary electrode for regeneration of the same and a regeneration current conducting means for conducting a current for regeneration of the reversible electrode when the therapeutic current is off, or the invention is comprised of a reversible electrode and an ion exchange membrane difficult for ions freed from that electrode to penetrate.

  为了避免在离子透入疗法中由于电极本身的电分解和化学性质的变化而导致电导率下降，需要用电绝缘体覆盖，并防止由于离子从电极中释放出来而导致传输速率下降。本发明提供了一种电极结构，该电极结构中集成有一个可逆电极和一个用于再生的辅助电极，以及一个再生电流传导装置，用于在治疗电流关闭时传导电流，使可逆电极再生，或者本发明由一个可逆电极和一个离子交换膜组成，从该电极释放的离子难以渗透。
• Iontoporesis device
  申请人：HISAMITSU PHARMACEUTICAL CO., INC.

  公开号：EP1195175A2

  公开（公告）日：2002-04-10

  To avoid a reduction of the conductivity in iontophoresis due to the electrical decomposition and the changes in chemical properties of the electrodes themselves, covering by an electrical insulator, and to prevent a drop in the transport rate due to ions freed from the electrode. Provision is made of an electrode structure provided integrally with a reversible electrode and an auxiliary electrode for regeneration of the same and a regeneration current conducting means for conducting a current for regeneration of the reversible electrode when the therapeutic current is off, or the invention is comprised of a reversible electrode and an ion exchange membrane difficult for ions freed from that electrode to penetrate.

  为了避免在离子透入疗法中由于电极本身的电分解和化学性质的变化而导致电导率下降，需要用电绝缘体覆盖，并防止由于离子从电极中释放出来而导致传输速率下降。本发明提供了一种电极结构，该电极结构中集成有一个可逆电极和一个用于再生的辅助电极，以及一个再生电流传导装置，用于在治疗电流关闭时传导电流，使可逆电极再生，或者本发明由一个可逆电极和一个离子交换膜组成，从该电极释放的离子难以渗透。
• NOVEL AGENTS FOR AMELIORATING MOTOR DISORDER
  申请人：Juridical Foundation, The Chemo-Sero-Therapeutic Research Institute

  公开号：EP1374887A1

  公开（公告）日：2004-01-02

  A novel medicament for treating neurodegenerative diseases, especially for ameliorating dyskinesia, comprising as an active ingredient selenoprotein P and/or a peptide fragment or a series of peptide fragments derived from said protein is provided. The novel medicament for treating neurodegenerative diseases, especially for ameliorating dyskinesia, according to the present invention is suitably applicable to diseases with decrease in motor function.

  本发明提供了一种用于治疗神经退行性疾病，特别是用于改善运动障碍的新型药物，其有效成分包括硒蛋白 P 和/或肽片段或由所述蛋白衍生的一系列肽片段。根据本发明，用于治疗神经退行性疾病，特别是用于改善运动障碍的新型药物适用于运动功能下降的疾病。
• THROMBUS/THROMBOGENESIS INHIBITORS
  申请人：Mitsubishi Pharma Corporation

  公开号：EP1430890A1

  公开（公告）日：2004-06-23

  The inhibitors of thrombus/thrombogenesis comprising as the active ingredient aminoalkoxybibenzyls represented by the following formula (I), pharmaceutically acceptable salts thereof or solvates thereof. wherein R1, R2 and R3 represent each hydrogen, etc.; R4 represents -N(R5)(R6); and m is an integer of from 0 to 5. The above drugs are particularly efficacious for inhibiting thrombus/thrombogenesis in ischemic cerebrovascular failures selected from transient cerebral ischemic attack and cerebral infaction.

  血栓/血栓形成抑制剂，其活性成分包括下式(I)代表的氨基烷氧基联苄、其药学上可接受的盐或其溶液。 其中 R1、R2 和 R3 分别代表氢等；R4 代表-N(R5)(R6)；m 为 0 至 5 的整数。上述药物对抑制选自短暂性脑缺血发作和脑梗塞的缺血性脑血管衰竭中的血栓/血栓形成特别有效。