[9-(Bromomethyl)-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] 3-hydroxy-2-phenylpropanoate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羟基酸及其衍生物
• 英文名称: [9-(Bromomethyl)-3-oxa-9-azatricyclo[3.3.1.02,4]nonan-7-yl] 3-hydroxy-2-phenylpropanoate
• 化学式: C₁₇H₂₀BrNO₄
• 分子量: 382.2
• InChiKey: WRLNTYOXEQJCFT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  62.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] METHODS OF TREATING EPILEPSY USING THE SAME<br/>[FR] PROCÉDÉS DE TRAITEMENT DE L'ÉPILEPSIE À L'AIDE DE CEUX-CI
  申请人：TREVENA INC

  公开号：WO2021046183A1

  公开（公告）日：2021-03-11

  The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of S1P1 receptor and methods of using the same for the treatment of seizures, epilepsy related conditions, epilepsy-related syndrome, and the like as described herein.

  本实施例部分涉及化合物，或其药用盐，或用于调节S1P1受体活性的药物组合物，以及使用这些化合物治疗癫痫、癫痫相关疾病、癫痫相关综合征等的方法。
• BENZODIAZEPINE PRODUCT WITH ACTIVITY ON THE CENTRAL NERVOUS AND VASCULAR SYSTEMS
  申请人：UNIVERSIDAD DE LA HABANA

  公开号：US20190270738A1

  公开（公告）日：2019-09-05

  Formula III compound, its products and pharmaceutical compositions containing them for the treatment of central nervous and vascular system diseases, particularly neurodegenerative disorders with cognitive deterioration, diseases associated with oxidative stress, diseases taking in mitochondrial dysfunction, Parkinson's disease and neuropathic pain, as well as the pathological processes associated with aging.

  Formula III 化合物，其产物和含有它们的药物组合物，用于治疗中枢神经系统和血管系统疾病，特别是伴有认知恶化的神经退行性疾病，与氧化应激有关的疾病，涉及线粒体功能障碍的疾病，帕金森病和神经病性疼痛，以及与衰老有关的病理过程。
• 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。
• [EN] NANOPARTICLES<br/>[FR] NANOPARTICULES
  申请人：KING'S COLLEGE LONDON

  公开号：WO2016198862A1

  公开（公告）日：2016-12-15

  The invention provides a (drug-containing) lipid nanoparticle with: (i) at least one phospholipid; (ii) at least one lysolipid; and (iii) at least one phospholipid comprising a hydrophilic polymer;and (iv) at least one structural lipid of formula (I) which has the following general structure: (I) wherein R and R' are long hydrocarbyl hydrophobic chains, Y is a linker element, and PHG is a polar head group described as large according to its van der Waals radius, and which is different from the phospholipid (i). The lipid nanoparticle can release a drug (or API) from within the lipid nanoparticleas a result of focussed ultrasound (FUS) applied continuously, at least twice, to a desired part of the body to induce hyperthermia (an increase in temperature). FUS is applied after the lipid nanoparticle containing the drug has been administered to the live subject, and causes controlled release of the drug at the desired site of the body. Ultrasound is then halted, and the site of interest allowed to cool. Ultrasound is then applied again. Lipidnanoparticles can be labelled (for MRI, NIRF imaging),enablin greal time monitoring of the drug in the human body. Imaging information can be used to direct and guide the nature of the FUS applied to the site of interest.

  本发明提供了一种（含药物的）脂质纳米粒子，其包含：（i）至少一种磷脂；（ii）至少一种溶血磷脂；（iii）至少一种包含亲水性聚合物的磷脂；以及（iv）至少一种结构脂质，其具有以下一般结构式（I）：（I）其中R和R'是长的烃基疏水链，Y是连接元素，PHG是极性头基，根据其范德华半径描述为大，且不同于磷脂（i）。脂质纳米粒子可以通过聚焦超声（FUS）在体内所需部位连续施加至少两次，诱导体温升高（发热），从而释放药物（或API）从脂质纳米粒子内部释放。在给活体主体注入含药物的脂质纳米粒子后，施加FUS会导致药物在体内所需部位的受控释放。然后停止超声，让感兴趣的部位冷却。然后再次施加超声。脂质纳米粒子可以被标记（用于MRI、NIRF成像），从而实现对人体内药物的实时监测。成像信息可以用于指导和引导施加于感兴趣部位的FUS的性质。