奥沙巴唑 | 35578-20-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: 奥沙巴唑
• 英文名称: 9-Benzoyl-6-methoxy-1,2,3,4-tetrahydro-carbazol-3-carbonsaeure
• 英文别名: 9-Benzoyl-6-methoxy-1,2,3,4-tetrahydrocarbazole-3-carboxylic acid；oxarbazole
• CAS: 35578-20-2
• 化学式: C₂₁H₁₉NO₄
• 分子量: 349.386
• InChiKey: ZNHCPKKNDKCPDG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  68.5
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为产物：
  描述：

  Benzaldehyd-1-benzoyl-1-(4-methoxy-phenyl)-hydrazon 、 4-羰基环己羧酸 、 盐酸 、 以 溶剂黄146 为溶剂， 反应 3.0h， 以to give 47.4 g的产率得到奥沙巴唑
  参考文献：
  名称：

  9-Acyl-1,2,3,4-tetrahydrocarbazole-3 and 4-carboxylic acids

  摘要：

  本文描述了具有3或4位羧基取代的新型9-芳酰基-1,2,3,4-四氢咔唑衍生物及其相应的酯类，具有抗炎活性，还介绍了其制备方法和新型中间体。

  公开号：

  US03948939A1

文献信息

• [EN] CARBONATE PRODRUGS AND METHODS OF USING THE SAME<br/>[FR] PROMÉDICAMENTS CARBONATÉS ET LEURS MÉTHODES D'UTILISATION
  申请人：NEUROGESX INC

  公开号：WO2009143297A1

  公开（公告）日：2009-11-26

  The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

  本发明提供了碳酸盐前药，其包括连接到母药基团的羟基或羧基上的碳酸磷酸酐前药基团。这些前药可能比母药具有改进的物理化学性质。还提供了使用碳酸盐前药治疗对母药具有响应的疾病或症状的方法，以及配套工具和单剂量。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• [EN] DUAL FUNCTIONING IONIC LIQUIDS AND SALTS THEREOF<br/>[FR] LIQUIDES IONIQUES À DOUBLE FONCTION ET SELS DE CEUX-CI
  申请人：UNIV ALABAMA

  公开号：WO2010078300A1

  公开（公告）日：2010-07-08

  Disclosed herein are ionic liquid compositions comprising active pharmaceutical, biological, and nutritional compounds, and methods of use. Further disclosed are compositions of matter including liquid ion pairs alone or in solution and their use; compositions of ionic liquids that are 'solvated,' for example, 'hydrated' and their uses.

  本文揭示了包括活性药物、生物学和营养化合物的离子液体组合物，以及其使用方法。进一步揭示了包括液态离子对的物质组合物，单独或溶解后使用；以及离子液体的“溶剂化”组合物，例如“水合”的组合物及其用途。
• Microparticles With Modified Release of At Least One Active Principle and Oral Pharmaceutical Form Comprising Same
  申请人：Dargelas Frederic

  公开号：US20090220611A1

  公开（公告）日：2009-09-03

  The invention concerns microparticulate systems with modified release of oral active principle(s). The invention aims at providing a novel pharmaceutical with time-dependent and pH-dependent release mechanism, enabling: a) the latent period preceding the release of the active principle in the stomach; b) the pH triggering the release of the active principle in the intestine; c) the release speed of the active principle. This is achieved through the use of coated microparticles made from particles of active principle each coated with two coating films A and B. A comprises: film-forming (co)polymer (A1) insoluble in fluids of the gastrointestinal tract; ethylcellulose (co)polymer (A2) soluble in fluids of the gastrointestinal tract; plasticizing polyvinylpyrrolidone (A3); castor oil/optionally a surfactant and/or magnesium stearate lubricant (A4). B comprises a hydrophilic polymer (B1) bearing ionized groups with neutral pH (EUDRAGIT® L100-55) and a hydrophobic compound (B2) (LUBRITAB®). The invention also concerns medicines based on said microparticles.

  该发明涉及具有口服活性原理改性释放的微粒系统。该发明旨在提供一种具有时间依赖性和pH依赖性释放机制的新型药物，实现：a）在胃中释放活性原理之前的潜伏期；b）在肠道中触发释放活性原理的pH值；c）活性原理的释放速度。这是通过使用由活性原理颗粒制成的被包覆的微粒来实现的，每个微粒都涂有两层涂膜A和B。A包括：在胃肠道液体中不溶解的成膜（共）聚合物（A1）；在胃肠道液体中可溶解的乙基纤维素（共）聚合物（A2）；增塑剂聚乙烯吡咯烷酮（A3）；蓖麻油/可选的表面活性剂和/或硬脂酸镁润滑剂（A4）。B包括具有中性pH的离子化基团的亲水性聚合物（B1）（EUDRAGIT® L100-55）和疏水化合物（B2）（LUBRITAB®）。该发明还涉及基于这些微粒的药物。
• 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。