苯拉利嗪 | 52395-99-0

• 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: 苯拉利嗪
• 中文别名: 百乐利辛；4-二苯甲基-1-(4-羟基苄基)哌嗪
• 英文名称: 4-(4-benzhydryl-piperazin-1-ylmethyl)-phenol
• 英文别名: Belarizine；4-[(4-benzhydrylpiperazin-1-yl)methyl]phenol
• CAS: 52395-99-0
• 化学式: C₂₄H₂₆N₂O
• 分子量: 358.483
• InChiKey: KBSZKZDILXBWMX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  26.7
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933599090

上下游信息

• 上游原料

  中文名称	英文名称	CAS号	化学式	分子量
  二苯甲基哌嗪	diphenylmethylpiperazine	841-77-0	C17H20N2	252.359

反应信息

• 作为反应物：
  描述：

  对胍基苯甲酸 、 苯拉利嗪 在 吡啶 、 N,N'-二环己基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 72.0h， 生成
  参考文献：
  名称：

  New serine protease inhibitors with leukotriene B4 (LTB4) receptor binding affinity

  摘要：

  A series of new trypsin-like serine protease inhibitors, 1, 2 and 7-23, containing amidinobenzene moiety was found to show potent LTB4-receptor affinity. Among them, compounds 1 and 2 were found to be LTB4 receptor antagonists based on an inhibition assay of human polymorphonuclear neutrophil (PMN) intracellular calcium mobilization induced by LTB4. Compounds 1 and 2, which satisfy the reported structural requirements for good oral activity, are expected to show a balanced dual mode of action, i.e., protease inhibitory activity and LTB4 receptor antagonist activity, in vivo. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00036-9
• 作为产物：
  描述：

  4-乙酰氧基苯甲醛 、 二苯甲基哌嗪 在 sodium cyanoborohydride 作用下， 以 甲醇 为溶剂， 反应 1.0h， 以39%的产率得到苯拉利嗪
  参考文献：
  名称：

  New serine protease inhibitors with leukotriene B4 (LTB4) receptor binding affinity

  摘要：

  A series of new trypsin-like serine protease inhibitors, 1, 2 and 7-23, containing amidinobenzene moiety was found to show potent LTB4-receptor affinity. Among them, compounds 1 and 2 were found to be LTB4 receptor antagonists based on an inhibition assay of human polymorphonuclear neutrophil (PMN) intracellular calcium mobilization induced by LTB4. Compounds 1 and 2, which satisfy the reported structural requirements for good oral activity, are expected to show a balanced dual mode of action, i.e., protease inhibitory activity and LTB4 receptor antagonist activity, in vivo. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00036-9

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• OHTAKA, HIROSHI;KANAZAWA, TOSHIRO;ITO, KEIZO;TSUKAMOTO, GORO, CHEM. AND PHARM. BULL., 35,(1987) N 8, 3270-3275
  作者：OHTAKA, HIROSHI、KANAZAWA, TOSHIRO、ITO, KEIZO、TSUKAMOTO, GORO

  DOI：——

  日期：——
• COMPOUNDS HAVING BOTH POTENT CALCIUM ANTAGONIST AND ANTIOXIDANT ACTIVITY AND USE THEREOF AS CYTOPROTECTIVE AGENTS
  申请人：ALCON LABORATORIES, INC.

  公开号：EP0682664B1

  公开（公告）日：2001-03-14
• LYOPHILIZATION PROCESS AND PRODUCTS OBTAINED THEREBY
  申请人：Scidose, Llc

  公开号：EP1954244A1

  公开（公告）日：2008-08-13