1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine;hydron;dichloride

• 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: 1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine;hydron;dichloride
• 化学式: C27H32Cl2F2N2O3
• 分子量: 541.5
• InChiKey: LOGVKVSFYBBUAJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.74
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  34.2
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine;hydron;dichloride 、 、 sodium hydroxide 在 乙酸乙酯 、 magnesium sulfate 作用下， 以to give 11.1 g of 1-(2,3,4-trimethoxybenzyl)-4-[bis(4-fluorophenyl)methyl]piperazine as an oil的产率得到洛美利嗪
  参考文献：
  名称：

  1-(2,3,4-tri-methoxybenzyl)-4[bis(4-fluorophenyl)methyl] piperazines are

  摘要：

  以下是翻译结果： 一种由以下一般式（I）表示的1-苄基-4-苄基二苯基哌嗪衍生物 ##STR1## 其中R1代表氢原子或甲氧基，R2代表氢原子或氟原子，或其药学上可接受的酸加成盐。该1-苄基-4-苄基二苯基哌嗪衍生物或其酸加成盐可以通过还原缩合苯甲醛衍生物和氟苄基二苯基哌嗪，或在酸受体的存在下缩合苄基卤代物和氟苄基二苯基哌嗪，或缩合苄基哌嗪和氟苄基卤代物，并可选择将产物转化为其酸加成盐来制备。该1-苄基-4-苄基二苯基哌嗪衍生物可用于改善脑血管疾病。

  公开号：

  US04663325A1
• 作为产物：
  描述：

  2,3,4-三甲氧基苯甲醛 、 4,4'-二氟苯甲哌嗪 、 甲酸 以40%的产率得到
  参考文献：
  名称：

  OHTAKA, HIROSHI;KANAZAWA, TOSHIRO;ITO, KEIZO;TSUKAMOTO, GORO, CHEM. AND PHARM. BULL., 35,(1987) N 8, 3270-3275

  摘要：

  DOI：

文献信息

• METHODS FOR TREATING CHRONIC FATIGUE SYNDROME AND MYALGIC ENCEPHALOMYELITIS
  申请人：GRIFFITH UNIVERSITY

  公开号：US20210069180A1

  公开（公告）日：2021-03-11

  In one aspect the invention relates to a method of treatment selected from the group consisting of: (a) treating a symptom such as pain in a subject identified or diagnosed as having Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS); (b) treating a symptom such as pain in a subject having dysfunctional TRPM3 ion channel activity; (c) restoring NK cell function in a subject having dysfunctional TRPM3 ion channel activity; and (d) restoring calcium homeostasis in a subject having dysfunctional TRPM3 ion channel activity. The method comprises the step of administering to the subject a therapeutically effective amount of at least one therapeutic compound selected from the group consisting of: (i) an opioid receptor antagonist; (ii) an opioid antagonist; and (iii) a therapeutic compound that restores TRPM3 ion channel activity. In some embodiments the therapeutic compound is naltrexone hydrochloride.

  在一个方面，该发明涉及一种治疗方法，所述方法选自以下组合：(a)治疗被识别或诊断为患有肌无力性脑脊髓炎/慢性疲劳综合征（ME/CFS）的受试者的症状，例如疼痛；(b)治疗具有TRPM3离子通道活性异常的受试者的症状，例如疼痛；(c)恢复具有TRPM3离子通道活性异常的受试者的NK细胞功能；以及(d)恢复具有TRPM3离子通道活性异常的受试者的钙稳态。该方法包括向受试者施用来自以下组合的至少一种治疗化合物的治疗有效量的步骤：(i)阿片受体拮抗剂；(ii)阿片拮抗剂；以及(iii)恢复TRPM3离子通道活性的治疗化合物。在某些实施例中，治疗化合物是盐酸纳曲酮。
• Novel piperazine derivatives, processes for production thereof, and pharmaceutical compositions comprising said compounds as active ingredient
  申请人：KANEBO, LTD.

  公开号：EP0159566A1

  公开（公告）日：1985-10-30

  A 1-benzyl-4-benzhydrylpiperazine derivative represented by the following general formula (I) wherein R1 represents a hydrogen atom or a methoxy group, and R2 represents a hydrogen or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof. The 1-benzyl-4-benzhydrylpiperazine derivative or an acid addition salt thereof is prepared by reductively condensing a benzaldehyde derivative with a fluorobenzhydrylpiperazine, or condensing a benzyl halide derivative with a fluorobenzhydrylpiperazine optionally in the presence of an acid acceptor, or condensing a benzylpiperazine with a fluorobenzhydryl halide derivative and, optionally converting the product to its acid addition salt. The 1-benzyl-4-benzhydrylpiperazine derivative is useful for improving a cerebrovascular disease.

  由以下通式（I）代表的 1-苄基-4-二氢哌嗪衍生物 其中 R1 代表氢原子或甲氧基，R2 代表氢原子或氟原子，或其药学上可接受的酸加成盐。 1-苄基-4-苯二甲酰基哌嗪衍生物或其酸加成盐的制备方法为：将苯甲醛衍生物与氟苯二甲酰基哌嗪还原缩合，或将苄基卤化物衍生物与氟苯二甲酰基哌嗪缩合（可选择在有酸接受体存在的情况下），或将苄基哌嗪与氟苯二甲酰基卤化物衍生物缩合，并可选择将产物转化为其酸加成盐。 1-苄基-4-二苯甲基哌嗪衍生物可用于改善脑血管疾病。
• Controlled release dosage form
  申请人：TRIASTEK, INC.

  公开号：US10143626B2

  公开（公告）日：2018-12-04

  The present invention generally relates to a pharmaceutical dosage form and controlled release of biologically active agents, diagnostic agents, reagents, cosmetic agents, and agricultural/insecticide agents. In one embodiment, the dosage form has a substrate that forms a compartment, wherein the substrate includes at least a first piece and a second piece, wherein the first piece operably links to the second piece. The dosage form contains a drug content that is loaded into the compartment. The dosage form also has a releaser operably linked to the substrate which upon contact with water or body fluid is capable of separating the first and second piece to open the compartment and release the drug content.

  本发明一般涉及一种药物剂型和生物活性制剂、诊断制剂、试剂、化妆品制剂和农用/杀虫剂制剂的控制释放。在一个实施方案中，该剂型具有形成隔室的基质，其中基质至少包括第一片和第二片，其中第一片与第二片可操作地连接。剂型含有装入隔室的药物成分。该剂型还具有与基质可操作连接的释放器，该释放器在与水或体液接触时能够分离第一和第二片，从而打开隔室并释放药物成分。
• Oral drug dosage forms having desired drug release profiles and uses thereof
  申请人：Triastek, Inc.

  公开号：US10258575B2

  公开（公告）日：2019-04-16

  The present disclosure provides a stable solid pharmaceutical dosage form for oral administration. The dosage form includes a substrate that forms at least one compartment and a drug content loaded into the compartment. The dosage form is so designed that the active pharmaceutical ingredient of the drug content is released in a controlled manner.

  本公开提供了一种用于口服的稳定固体药物剂型。该剂型包括至少形成一个小室的基质和装入小室的药物成分。该剂型的设计使药物内容物中的活性药物成分以可控方式释放。
• Compartmented pharmaceutical dosage forms
  申请人：Triastek, Inc.

  公开号：US10363220B2

  公开（公告）日：2019-07-30

  The present disclosure provides a stable solid pharmaceutical dosage form for oral administration. The dosage form includes a substrate that forms at least one compartment and a drug content loaded into the compartment. The dosage form is so designed that the active pharmaceutical ingredient of the drug content is released in a controlled manner.

  本公开提供了一种用于口服的稳定固体药物剂型。该剂型包括至少形成一个小室的基质和装入小室的药物成分。该剂型的设计使药物内容物中的活性药物成分以可控方式释放。