米氟嗪 | 79467-23-5

• 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: 米氟嗪
• 中文别名: 苗扶来精
• 英文名称: Mioflazine
• 英文别名: 1-[4,4-bis(4-fluorophenyl)butyl]-4-[2-(2,6-dichloroanilino)-2-oxoethyl]piperazine-2-carboxamide
• CAS: 79467-23-5
• 化学式: C₂₉H₃₀Cl₂F₂N₄O₂
• 分子量: 575.5
• InChiKey: VWXFUOAKGNJSBI-UHFFFAOYSA-N

物化性质

• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  39
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  78.7
• 氢给体数：
  2
• 氢受体数：
  6

制备方法与用途

生物活性方面，Mioflazine 是一种具有口服活性的核苷转运抑制剂，并且有望用于治疗睡眠障碍。它能够抑制核苷的摄取。

文献信息

• THERAPEUTIC AGENTS FOR IRRITABLE BOWEL SYNDROME
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP2077122A1

  公开（公告）日：2009-07-08

  The present invention provides a therapeutic agent for irritable bowel syndrome which comprises, as an active ingredient, a compound having an adenosine uptake inhibitory activity, a therapeutic agent for irritable bowel syndrome which comprises, as an active ingredient, a tricyclic compound represented by formula (I) [wherein L represents -NHC(=O)- or the like, R1 represents a hydrogen atom, halogen, or the like, X1-X2-X3 represents S-CR7=CR8 (wherein R7 and R8 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like), or the like, Y represents -CH2SO2-, -SO2CH2- or the like, R2 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, or the like] or a pharmaceutically acceptable salt thereof, and the like.

  本发明提供了一种治疗肠易激综合征的药物，其包括作为活性成分的具有腺苷摄取抑制活性的化合物，一种治疗肠易激综合征的药物，其包括作为活性成分的由式(I)表示的三环化合物[其中L代表-NHC(=O)-或类似物，R1代表氢原子、卤素或类似物，X1-X2-X3代表S-CR7=CR8（其中R7和R8可以相同也可以不同，每个代表氢原子、卤素、取代或未取代的较低烷基等），或类似物，Y代表-CH2SO2-、-SO2CH2-或类似物，R2代表取代或未取代的较低烷基、取代或未取代的较低烷氧基、取代或未取代的芳基或类似物]或其药学上可接受的盐等。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Composite materials for controlled release of water soluble products
  申请人：Ying Y. Jackie

  公开号：US20060024377A1

  公开（公告）日：2006-02-02

  Composite materials comprising a water-soluble compound adsorbed onto a basic inorganic material and a bio-degradable polymer which yields acidic degradation products, methods of producing same, and methods of use thereof are described, wherein the composite materials are designed so as to provide controlled release of the water soluble molecule.

  本发明涉及一种复合材料，包括吸附在碱性无机材料上的水溶性化合物和可生物降解聚合物，其产生酸性降解产物，描述了其制备方法和使用方法，其中复合材料的设计旨在提供水溶性分子的控制释放。
• Cell permeable nanoconjugates of shell-crosslinked knedel (SCK) and peptide nucleic acids ("PNAs") with uniquely expressed or over-expressed mRNA targeting sequences for early diagnosis and therapy of cancer
  申请人：Becker L. Matthew

  公开号：US20060159619A1

  公开（公告）日：2006-07-20

  A functional biologically active particle conjugate useful for diagnosis and treating cancer as a bioportal comprises a nanoscale particle having associated therewith an intracellular targeting ligand comprising a PNA, or another nuclease resistant oligonucleotide analog such as MOE-mRNA (2′-methoxyethyl mRNA) or LNA (locked nucleic acid), having a sequence that binds selectively to an uniquely expressed or overexpressed mRNA specific to the cancer or disease state in a living mammal. In one aspect the uniquely overexpressed target specific to the cancer or disease state is the unr mRNA which can be targeted by the antisense sequence PNA50.

  一种功能性生物活性颗粒共轭物，用于诊断和治疗癌症，作为生物门户，包括与之相关联的细胞内靶向配体，包括PNA或其他核酸酶抵抗性寡核苷酸类似物，如MOE-mRNA（2'-甲氧基乙基mRNA）或LNA（锁定核酸），具有选择性结合于哺乳动物体内癌症或疾病状态特异性表达或过表达的mRNA序列。在一个方面，特异性过表达的靶点是unr mRNA，可以通过反义序列PNA50进行靶向。
• FOCUSTED ULTRASOUND HYPERTHERMIA
  申请人：KING'S COLLEGE LONDON

  公开号：US20180178043A1

  公开（公告）日：2018-06-28

  The invention relates to a hyperthermia (focused ultrasound—FUS) method where an energy source is applied, repeatedly, to a desired part of the body to induce hyperthermia, e.g. using image guidance. Hyperthermia is applied after a drug or biopharmaceutical (API) and/or their labelled equivalents (theranostics) and/or their drug delivery systems has been administered to the live subject to cause the enhanced tissue distribution and/or controlled release of the drug, previously encapsulated in thermo-sensitive (lipid nano)particles, to a desired site of the body. Hyperthermia (Ultrasound) is then halted, and the site of interest. Hyperthermia is then applied again using image guidance to monitor drug's accumulation in the tissue. The drug and or the drug delivery system are also labelled (for imaging) to allow real time monitoring and modulation of the API in the human body which can be used to direct and guide the FUS at the site of interest.

  本发明涉及一种高温疗法（聚焦超声波-FUS）方法，在该方法中，能量源被反复应用于身体的所需部位，以诱导高温疗法，例如使用图像引导。在给活体主体注射药物或生物制品（API）和/或它们的标记等价物（治疗诊断）和/或它们的药物递送系统后，应用高温疗法，以导致药物之前包封在热敏（脂质纳米）颗粒中的增强组织分布和/或控制释放到身体的所需部位。然后停止高温疗法（超声波），并选择感兴趣的部位。然后再次使用图像引导应用高温疗法，以监测药物在组织中的积累。药物和/或药物递送系统也被标记（用于成像），以允许实时监测和调节人体中的API，可用于引导和指导在感兴趣的部位使用FUS。