6-bromo-4-cyclopropyl-8-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide | 1204574-49-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 英文名称: 6-bromo-4-cyclopropyl-8-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide
• 英文别名: 6-Bromo-4-cyclopropyl-8-fluoro-2,3-dihydro-1lambda6,2,4-benzothiadiazine 1,1-dioxide；6-bromo-4-cyclopropyl-8-fluoro-2,3-dihydro-1λ6,2,4-benzothiadiazine 1,1-dioxide
• CAS: 1204574-49-1
• 化学式: C₁₀H₁₀BrFN₂O₂S
• 分子量: 321.17
• InChiKey: QULAAMGNURGZHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  57.8
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Cycloalkylated benzothiadiazines, a process for their preparation and pharmaceutical compostions containing them
  申请人：FRANCOTTE Pierre

  公开号：US20100009974A1

  公开（公告）日：2010-01-14

  Compounds of formula (I): wherein: R Cy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.

  式（I）的化合物：其中：RCy表示未取代或取代的环烷基或环烷基烷基，R1、R2、R3和R4，可以相同也可以不同，每个代表氢或卤素原子或硝基团；氰基；羟基；烷氧基；烷基；未取代或取代的氨基团；羧基；烷氧羰基；芳基氧羰基；未取代或取代的氨基羰基。含有这些化合物的药物产品，可用于治疗或预防通过AMPA受体调节剂可治疗的疾病。
• Nanoparticles for targeted delivery of active agents to the lung
  申请人：Fraunhofer-Gesellschaft zur Förderung der Angewandten Forschung e.V.

  公开号：EP2106806A1

  公开（公告）日：2009-10-07

  The advantages of coupling NPs containing lipophilic cytotoxic drugs with MAbs followed by local delivery to the lungs include: direct delivery to lungs, prolonged residence time in the target tissue; continuous release of significant potent drug doses at tumor sites and better cytotoxic drug internalization in tumors allowing improved efficacy. The present invention concerns a delivery system administered to the lung by inhalation comprising a polymer-based nanoparticle; and a linker comprising a first portion non-covalently anchored to said nanoparticle, wherein at least part of said first portion comprises a hydrophobic/lipophilic segment embedded in said nanoparticle; and a second portion comprising a maleimide compound exposed at the outer surface of said nanoparticle. In accordance with one embodiment, the delivery system comprises one or more targeting agents, each covalently bound to said maleimide compound. In accordance with yet another embodiment, the delivery system comprises a drug. A specific example for a linker in accordance with the invention is octadecyl-4-(maleimideomethyl)cyclohexane-carboxylic amide (OMCCA).

  将含有亲脂性细胞毒性药物的 NPs 与 MAbs 联用，然后局部输送到肺部的优点包括：直接输送到肺部，延长在靶组织中的停留时间；在肿瘤部位持续释放大量强效药物，以及细胞毒性药物在肿瘤中更好的内化，从而提高疗效。本发明涉及一种通过吸入给药到肺部的给药系统，该系统包括聚合物基纳米粒子；以及连接剂，该连接剂包括非共价锚定到所述纳米粒子上的第一部分，其中所述第一部分的至少一部分包括嵌入所述纳米粒子的疏水/亲油段；以及第二部分，该第二部分包括暴露在所述纳米粒子外表面的马来酰亚胺化合物。根据一个实施方案，所述递送系统包括一种或多种靶向剂，每种靶向剂都与所述马来酰亚胺化合物共价结合。根据另一个实施方案，所述递送系统包括药物。根据本发明，连接剂的一个具体例子是十八烷基-4-（马来酰亚胺甲基）环己烷羧酰胺（OMCCA）。
• NANOPARTICLES FOR TARGETED DELIVERY OF ACTIVE AGENTS
  申请人：YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM

  公开号：EP1996234A2

  公开（公告）日：2008-12-03
• Nouveaux dérivés de benzothiadiazines cycloalkylées, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
  申请人：Les Laboratoires Servier

  公开号：EP2147915B1

  公开（公告）日：2010-09-15
• NANOPARTICLES FOR TARGETED DELIVERY OF ACTIVE AGENTS TO THE LUNG
  申请人：Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V.

  公开号：EP2257312A2

  公开（公告）日：2010-12-08