非布维林 | 7077-33-0

• 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: 非布维林
• 中文别名: 哌乙双苯丁酸酯
• 英文名称: 1.4-Bis-<2-(2-phenyl-butyryl-oxy)-ethyl>-piperazin
• 英文别名: Febuverine；2-[4-[2-(2-phenylbutanoyloxy)ethyl]piperazin-1-yl]ethyl 2-phenylbutanoate
• CAS: 7077-33-0
• 化学式: C₂₈H₃₈N₂O₄
• 分子量: 466.621
• InChiKey: XYCYZUNVTJSIML-UHFFFAOYSA-N

物化性质

• 熔点：
  210 °C
• 沸点：
  561.7±50.0 °C(Predicted)
• 密度：
  1.096±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  34
• 可旋转键数：
  14
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  59.1
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-苯基丁酰氯 在 乙醇 、 碳酸氢钠 作用下， 生成 非布维林
  参考文献：
  名称：

  N，N'-二酰氧基醇基-哌嗪合成肽，具有抗痉挛性

  摘要：

  描述了α-苯基-α-烷基乙酸与N，N′-二-（2-羟基-乙基）-和N，N′-二-（1-羟基丙-2-y1）-哌嗪的酯的合成。这些物质表现出类似罂粟碱的解痉性质。

  DOI：

  10.1002/hlca.19590420406

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。
• Diamine derivatives and their use in oncology
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP0443569A2

  公开（公告）日：1991-08-28

  Compounds of formula wherein R and R3, which may be the same or different, each represents a hydrogen atom, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, substituents being selected from halogen atoms, alkoxy and alkyl groups containing 1 to 5 carbon atoms, said alkyl groups in turn being optionally halo-substituted; R1 and R2, which may be the same or different, each represents a hydrogen atom, an alkyl group containing 1 to 5 carbon atoms, or an optionally substituted aryl or aralkyl group, substituents being as indicated above, or R1 and R2 together represent an alkylene group containing 2 or 3 carbon atoms; m and p, which may be the same or different each represents a number from 0 to 3; n represents the number 2 or 3; and X represents a group of formula R4x -CO-, R4x -COO-, R4x -CONH-, R4x -NHCO-, or R4x -O- and Y represents a group of formula R -CO-, R -COO-, R4y -CONH-, R4y -NHCO-, or R4y -0- in which groups R4y and R4x, which may be the same or different, each represents an optionally substituted aryl, aralkyl or aryloxyalkyl group, substituents being as indicated above, and the alkyl moiety in the aralkyl and aryloxyalkyl groups containing 1 to 5 carbon atoms and being optionally substituted by a cycloalkyl group containing 3 to 8 carbon atoms; and physiologically acceptable acid addition salts thereof have been found to be active in restoring drug-sensitivity to cancer cells that have become multidrug-resistant. They can, therefore, be used as adjuvants in oncology, and they can be administered simultaneously, separately or at intervals in combination with one or more conventional anti-cancer agents for treating malignant tumours and corresponding metastases. Some of these compounds and salts which have not been previously described as well as their manufacture and pharmaceutical compositions containing them are also disclosed.

  式化合物 其中 R 和 R3（可以相同或不同）各自代表一个氢原子、一个含 1 至 5 个碳原子的烷基或一个任选取代的芳基或芳烷基，取代基可选自卤素原子、烷氧基和含 1 至 5 个碳原子的烷基，所述烷基又可任选被卤代；R1 和 R2 可以相同或不同，各自代表一个氢原子、一个含 1 至 5 个碳原子的烷基或一个任选取代的芳基或芳烷基，取代基如上所示，或 R1 和 R2 共同代表一个含 2 或 3 个碳原子的亚烷基； m 和 p 可以相同或不同，各自代表一个 0 至 3 的数字；n 代表数字 2 或 3；X 代表式 R4x -CO-、R4x -COO-、R4x -CONH-、R4x -NHCO- 或 R4x -O- 的基团，Y 代表式 R -CO-、R -COO-、R4y -CONH-、R4y -NHCO- 或 R4y -0- 的基团，其中基团 R4y 和 R4x 可以相同或不同，各自代表任选取代的芳基、芳烷基和芳氧基烷基中的烷基含有 1 至 5 个碳原子，并可选择被含有 3 至 8 个碳原子的环烷基取代；及其生理学上可接受的酸加成盐，已被发现在恢复对多种药物产生抗药性的癌细胞的药物敏感性方面具有活性。因此，它们可用作肿瘤学中的辅助剂，并可与一种或多种常规抗癌剂同时、单独或间隔联合使用，以治疗恶性肿瘤和相应的转移瘤。 此外，还公开了一些以前未曾描述过的化合物和盐类，以及它们的制造方法和含有它们的药物组合物。
• 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。
• Di Paco; Tauro, Farmaco, Edizione Scientifica, 1957, vol. 12, p. 347,351
  作者：Di Paco、Tauro

  DOI：——

  日期：——
• LYOPHILIZATION PROCESS AND PRODUCTS OBTAINED THEREBY
  申请人：Scidose, Llc

  公开号：EP1954244A1

  公开（公告）日：2008-08-13