卡布比妥 | 960-05-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 卡布比妥
• 中文别名: 丁酰胺比妥
• 英文名称: 5-Butyl-5-<2-carbamoyloxy-ethyl>-barbitursaeure
• 英文别名: 5-n-Butyl-5-<2-carbamoyloxy-ethyl>-barbitursaeure；5-butyl-5-(2-carbamoyloxy-ethyl)-pyrimidine-2,4,6-trione；Carbubarb；2-(5-butyl-2,4,6-trioxo-1,3-diazinan-5-yl)ethyl carbamate
• CAS: 960-05-4
• 化学式: C₁₁H₁₇N₃O₅
• 分子量: 271.273
• InChiKey: ZWGPHQZXAPWKOV-UHFFFAOYSA-N

物化性质

• 熔点：
  192-194°

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  19
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  128
• 氢给体数：
  3
• 氢受体数：
  5

安全信息

• 海关编码：
  2933540000

文献信息

• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Compositions and methods to effect the release profile in the transdermal administration of active agents
  申请人：——

  公开号：US20020004065A1

  公开（公告）日：2002-01-10

  Compositions and methods for the transdermal delivery of active agents up to a period of seven days or more at substantially a zero-order release rate comprising a pharmaceutically acceptable adhesive matrix and a polymeric plastic material that provides a release rate regulating effect on the active agents.

  本发明涉及一种用于经皮递送活性药剂的组合物和方法，该组合物和方法能够在持续时间为七天或更长时间内以几乎零阶释放速率递送活性药剂，包括一种药学上可接受的粘合基质和一种聚合物塑料材料，该聚合物塑料材料对活性药剂具有释放速率调节作用。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Novel prodrugs of N-H bond-containing compounds and methods of making thereof
  申请人：The University of Kansas

  公开号：US20030119814A1

  公开（公告）日：2003-06-26

  The present invention relates to novel prodrugs of pharmaceutical compounds containing one or more N—H bonds. More specifically, the present embodiment of the invention relates to prodrugs wherein sulfur-containing promoieties are attached to pharmaceutical compounds which contain one or more N—H bonds to produce prodrugs containing at least one N—S bond. These N—S bond-containing prodrugs could have optimized stability, solubility, cell membrane permeability, pharmacokinetic properties and other pharmaceutical properties over the pharmaceutical compounds from which they are formed, depending upon the nature of the promoiety. Reversion of the prodrug to the parent pharmaceutical compound occurs by the reaction of the prodrugs with thiol molecules such as cysteine, glutathione or any other thiol containing molecule. Further, the present invention relates to methods of making N—S bond-containing prodrugs of pharmaceutical compounds containing one or more N—H bonds whereby sulfur-containing promoieties are attached to the parent compounds to create at least one N—S bond.

  本发明涉及一种新型药物化合物的前药，其中包含一个或多个N-H键。更具体地，本发明实施例涉及将含有一个或多个N-H键的药物化合物与含有硫的前体连接起来，以产生至少一个N-S键的前药。这些含N-S键的前药可能具有优化的稳定性、溶解度、细胞膜通透性、药代动力学性质和其他药物性质，这取决于前体的性质。前药向父药物化合物的还原通过前药与半胱氨酸、谷胱甘肽或任何其他含有巯基的分子反应而发生。此外，本发明还涉及一种制备含有一个或多个N-H键的药物化合物的N-S键前药的方法，其中将硫含量的前体连接到父化合物上，以创建至少一个N-S键。