赛利拉敏 | 47128-12-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 赛利拉敏
• 英文名称: 2-[(4-chloro-phenyl)-(1-methyl-piperidin-4-ylidene)-methyl]-pyridine
• 英文别名: cycliramine；2-[(4-chlorophenyl)-(1-methylpiperidin-4-ylidene)methyl]pyridine
• CAS: 47128-12-1
• 化学式: C₁₈H₁₉ClN₂
• 分子量: 298.815
• InChiKey: HZNVLDCWAVIXRK-UHFFFAOYSA-N

物化性质

• 沸点：
  441.1±35.0 °C(Predicted)
• 密度：
  1.163±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  16.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  赛利拉敏 在 氢氧化钾 、 三乙胺 作用下， 以 甲苯 为溶剂， 生成 2-[(4-Chlorophenyl)-piperidin-4-ylidenemethyl]pyridine
  参考文献：
  名称：

  血小板活化因子和组胺的双重拮抗剂。鉴定N-酰基-4-（5,6-二氢-11H-苯并[5,6]环庚-[1,2-b]吡啶-11-亚吡啶）哌啶的双重活性的结构要求。

  摘要：

  DOI：

  10.1021/jm00105a069

文献信息

• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• 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。
• 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。
• Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
  申请人：——

  公开号：US20030180352A1

  公开（公告）日：2003-09-25

  The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides, and solubilizers. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides, and solubilizers. The compositions of the present invention can be used for improved delivery of active ingredients.

  本发明提供了固体药物组合物，用于改进其中所含或单独给药的各种活性成分的给药。在一个实施方案中，固体药物组合物包括固体载体，固体载体包括基质和基质上的封装层。封装层可包括活性成分、亲水性表面活性剂、亲油性表面活性剂和甘油三酯以及增溶剂的不同组合。在另一个实施方案中，固体药物组合物包括固体载体，固体载体由活性成分、亲水表面活性剂、亲油表面活性剂和甘油三酯以及增溶剂的不同组合构成。本发明的组合物可用于改善活性成分的给药。