吡咯利芬 | 15686-97-2

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 中文名称: 吡咯利芬
• 英文名称: 2-acetoxy-3-methyl-1,2-diphenyl-4-pyrrolidino-butane
• 英文别名: 2-Acetoxy-3-methyl-1,2-diphenyl-4-pyrrolidino-butan；propiverine；Pyrrolifene；(3-methyl-1,2-diphenyl-4-pyrrolidin-1-ylbutan-2-yl) acetate
• CAS: 15686-97-2
• 化学式: C₂₃H₂₉NO₂
• 分子量: 351.489
• InChiKey: XPSOFSIDLMRECY-UHFFFAOYSA-N

物化性质

• 沸点：
  476.7±45.0 °C(Predicted)
• 密度：
  1.078±0.06 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜
• 保留指数：
  2396

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

制备方法与用途

生物活性方面，Pyrrolifene 是一种镇痛药，并且具有消炎作用。

反应信息

• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 生成 吡咯利芬
  参考文献：
  名称：

  Esters of substituted aminobutanes

  摘要：

  公开号：

  US02728779A1

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。
• Soluble glycosaminoglycanases and methods of preparing and using soluble glycosaminoglycanases
  申请人：Halozyme, Inc.

  公开号：US10016491B2

  公开（公告）日：2018-07-10

  The invention relates to the discovery of novel soluble neutral active Hyaluronidase Glycoproteins (sHASEGPs), methods of manufacture, and their use to facilitate administration of other molecules or to alleviate glycosaminoglycan associated pathologies. Minimally active polypeptide domains of the soluble, neutral active sHASEGP domains are described that include asparagine-linked sugar moieties required for a functional neutral active hyaluronidase domain. Included are modified amino-terminal leader peptides that enhance secretion of sHASEGP. The invention further comprises sialated and pegylated form of a recombinant sHASEGP to enhance stability and serum pharmacokinetics over naturally occurring slaughterhouse enzymes. Further described are suitable formulations of a substantially purified recombinant sHASEGP glycoprotein derived from a eukaryotic cell that generate the proper glycosylation required for its optimal activity.

  本发明涉及新型可溶性中性活性透明质酸酶糖蛋白（sHASEGPs）的发现、制造方法及其用于促进其他分子的给药或缓解糖胺聚糖相关病症的用途。本文描述了可溶性中性活性 sHASEGP 结构域的最小活性多肽结构域，其中包括功能性中性活性透明质酸酶结构域所需的天冬酰胺连接糖分子。本发明还包括可增强 sHASEGP 分泌的修饰氨基末端领导肽。本发明还包括重组 sHASEGP 的苷元化和聚乙二醇化形式，与天然存在的屠宰场酶相比，可提高稳定性和血清药代动力学。本发明还描述了从真核细胞中提取的基本纯化的重组 sHASEGP 糖蛋白的合适制剂，该制剂可产生其最佳活性所需的适当糖基化。
• 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。
• HATOBA, L.;DZHABUR, S.;ZHELYAZKOV, L., GOD. VISSH. XIM.-TEXNOL. IN-T. SOFIYA, 1983, 29, N 2, 28-31
  作者：HATOBA, L.、DZHABUR, S.、ZHELYAZKOV, L.

  DOI：——

  日期：——

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