匹可卓那净 | 17692-43-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 匹可卓那净
• 中文别名: 1-肼基-4-(吡啶-4-甲基)二氮杂萘；吡考屈嗪
• 英文名称: 1-hydrazino-4-pyridin-4-ylmethyl-phthalazine
• 英文别名: Picodralazine；[4-(pyridin-4-ylmethyl)phthalazin-1-yl]hydrazine
• CAS: 17692-43-2
• 化学式: C₁₄H₁₃N₅
• 分子量: 251.291
• InChiKey: KCASCYQNVLPVDP-UHFFFAOYSA-N

物化性质

• 沸点：
  495.6±47.0 °C(Predicted)
• 密度：
  1.33±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  76.7
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 海关编码：
  2933990090

文献信息

• 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 uses for drugs targeting glutamine synthetase
  申请人：NewThera

  公开号：EP1752143A1

  公开（公告）日：2007-02-14

  The present invention relates to novel therapeutic uses of tianeptine, salts, isomers, prodrugs, metabolites and structural analogs thereof. Furthermore, the present invention relates to the use of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof, in obtaining methods of screening and of developing drugs. Finally, the present invention relates to the novel therapeutic use of other glutamine synthetase (GS) ligands and to the use of these ligands in obtaining methods for screening and developing drugs.

  本发明涉及噻奈普汀、其盐类、异构体、原药、代谢物和结构类似物的新型治疗用途。此外，本发明还涉及噻奈普汀、其盐类、异构体、原药、代谢物和结构类似物在获得药物筛选和开发方法中的用途。最后，本发明涉及其他谷氨酰胺合成酶（GS）配体的新型治疗用途，以及使用这些配体获得筛选和开发药物的方法。
• Aggregate with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin
  申请人：IDEA AG

  公开号：EP1815846A2

  公开（公告）日：2007-08-08

  The application describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components, which differ at least 2-times to 10-times in solubility, ensures said aggregates to have extended, unusually adaptable surfaces. This is probably due to simultaneous action on said aggregates of at least two more soluble substances amongst said three system components, at least one of which is an active ingredient and preferably a drug; the third component, alternatively, can take the role of a drug. The application further deals with the use of said combinations in pharmaceutical preparations capable of transporting drugs into the body of warm blood creatures. This is made possible by the drug loading capability of said aggregates with the highly flexible and deformable coating, which renders the resulting drug carriers highly adaptable. The application finally reveals suitable methods and favourable conditions for carrier manufacturing and application. The application also describes novel formulations of nonsteroidal anti-inflammatory drugs (NSAIDs) based on complex aggregates with at least three amphipatic components suspended in a suitable, e.g. pharmaceutically acceptable, polar liquid medium.

  该申请描述了在极性液体中形成聚集悬浮液的至少三种两性物质的组合。对溶解度至少相差 2 倍到 10 倍的体系成分的明智选择，确保了所述聚集体具有扩展的、异常适应的表面。这可能是由于在上述三种系统成分中，至少有两种可溶性物质同时作用于上述聚集体，其中至少有一种是活性成分，最好是药物；第三种成分也可以起到药物的作用。本申请还涉及上述组合物在药物制剂中的应用，这些药物制剂能够将药物输送到温血动物体内。这得益于具有高柔韧性和可变形涂层的聚合体的药物装载能力，从而使所制成的药物载体具有很强的适应性。该申请最终揭示了载体制造和应用的合适方法和有利条件。本申请还介绍了非甾体抗炎药（NSAIDs）的新型制剂，该制剂基于悬浮在适当的（如药学上可接受的）极性液体介质中的至少含有三种两性成分的复合聚集体。
• 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。
• Aggregates with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin
  申请人：——

  公开号：US20040105881A1

  公开（公告）日：2004-06-03

  The invention describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components, which differ at least 2-times to 10-times in solubility, ensures said aggregates to have extended, unusually adaptable surfaces. This is probably due to simultaneous action on said aggregates of at least two more soluble substances amongst said three system components, at least one of which is an active ingredient and preferably a drug; the third component, alternatively, can take the role of a drug. The patent further deals with the use of said combinations in pharmaceutical preparations capable of transporting drugs into the body of warm blood creatures. This is made possible by the drug loading capability of said aggregates with the highly flexible and deformable coating, which renders the resulting drug carriers highly adaptable. The patent finally reveals suitable methods and favourable conditions for carrier manufacturing and application.

  本发明描述了在极性液体中形成聚集悬浮液的至少三种两性物质的组合。对溶解度至少相差 2 倍到 10 倍的体系成分的明智选择，确保了所述聚集体具有扩展的、异常适应的表面。这可能是因为在上述三种系统成分中，至少有两种可溶性物质同时作用于上述聚集体，其中至少有一种是活性成分，最好是药物；第三种成分也可以起到药物的作用。该专利还涉及在能够将药物输送到温血动物体内的药物制剂中使用上述组合物。这得益于上述聚合体的药物装载能力以及高度柔韧和可变形的涂层，这使得所制成的药物载体具有很强的适应性。该专利最终揭示了载体制造和应用的合适方法和有利条件。