阿克海林 | 67696-82-6

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 中文名称: 阿克海林
• 英文名称: acrihellin
• 英文别名: [(3S,5S,8R,9S,10S,13R,14S,17R)-10-formyl-5,14-dihydroxy-13-methyl-17-(6-oxopyran-3-yl)-2,3,4,6,7,8,9,11,12,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl] 3-methylbut-2-enoate
• CAS: 67696-82-6
• 化学式: C₂₉H₃₈O₇
• 分子量: 498.617
• InChiKey: RIOSSPWEPWYRLD-SBQWKNPYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  36
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.69
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  阿克海林 在 lithium tri-t-butoxyaluminum hydride 作用下， 以 四氢呋喃 为溶剂， 反应 1.0h， 以50%的产率得到D 14279
  参考文献：
  名称：

  Engel; Isaac; Posselt, Arzneimittel-Forschung/Drug Research, 1983, vol. 33, # 9, p. 1215 - 1218

  摘要：

  DOI：
• 作为产物：
  描述：

  3-甲基巴豆酰氯 、 蟾蜍它里定 以 二氯甲烷 为溶剂， 反应 1.5h， 以62.6%的产率得到阿克海林
  参考文献：
  名称：

  Engel; Isaac; Posselt, Arzneimittel-Forschung/Drug Research, 1983, vol. 33, # 9, p. 1215 - 1218

  摘要：

  DOI：

文献信息

• 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。
• 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。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Steroid kit and foamable composition and uses thereof
  申请人：Friedman Doron

  公开号：US20060018937A1

  公开（公告）日：2006-01-26

  A composition and therapeutic kit including an aerosol packaging assembly including a container accommodating a pressurized product and an outlet capable of releasing a foamable composition, including a steroid as a foam. The pressurized product includes a foamable composition including: a container accommodating a pressurized product; and an outlet capable of releasing the pressurized product as a foam; wherein the pressurized product comprises a foamable composition including: i. a steroid; ii. at least one organic carrier selected from the group consisting of a hydrophobic organic carrier, a polar solvent, an emollient and mixtures thereof, at a concentration of about 2% to about 50% by weight; iii. a surface-active agent; iv. about 0.01% to about 5% by weight of at least one polymeric additive selected from the group consisting of a bioadhesive agent, a gelling agent, a film forming agent and a phase change agent; v. water; and vi. liquefied or compressed gas propellant at a concentration of about 3% to about 25% by weight of the total composition. The composition further may include a therapeutically active foam adjuvant, selected from the group consisting of a fatty alcohol, a fatty acid, a hydroxyl fatty acid; and mixtures thereof.

  一种组合物和治疗包，包括一个气雾剂包装组件，其中包括一个容纳加压产品的容器和一个能够以泡沫形式释放可发泡组合物（包括类固醇）的出口。加压产品包括可发泡组合物，其中可发泡组合物包括：容纳加压产品的容器；以及能够将加压产品作为泡沫释放的出口；其中加压产品包括可发泡组合物，其中可发泡组合物包括： i. 类固醇； ii. 至少一种有机载体，选自由疏水性有机载体、极性溶剂、润肤剂及其混合物组成的组，浓度为约 2%至约 50%（按重量计）； iii.约 0.01%至约 5%（按重量计）的至少一种聚合物添加剂，该聚合物添加剂选 自生物粘合剂、胶凝剂、成膜剂和相变剂组成的组； v. 水；以及 vi. 液化或压缩气体推进剂，其浓度约为总组合物的 3%至约 25%（按重量计）。该组合物还可包括一种治疗活性泡沫佐剂，选自脂肪醇、脂肪酸、羟基脂肪酸及其混合物组成的组。
• PHARMACEUTICAL PREPARATION COMPRISING AN ACTIVE DISPERSED ON A MATRIX
  申请人：ALTANA Pharma AG

  公开号：EP1341527A1

  公开（公告）日：2003-09-10