racem.-1-Propionyloxy-2-dimethylaminomethyl-1-benzyl-1,2,3,4-tetrahydro-naphthalin | 95437-05-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: racem.-1-Propionyloxy-2-dimethylaminomethyl-1-benzyl-1,2,3,4-tetrahydro-naphthalin
• 英文别名: 1-Propionyloxy-2-dimethylaminomethyl-1-benzyl-tetralin；rac.-1-Propionyloxy-2-dimethylaminomethyl-1-benzyl-1,2,3,4-tetrahydro-naphthalin；[1-benzyl-2-[(dimethylamino)methyl]-3,4-dihydro-2H-naphthalen-1-yl] propanoate
• CAS: 95437-05-1
• 化学式: C₂₃H₂₉NO₂
• 分子量: 351.489
• InChiKey: ONCSOGCUZXTJCV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  26
• 可旋转键数：
  7
• 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

文献信息

• Verfahren zur Herstellung von pharmazeutischen Zusammensetzungen enthaltend unilamellare Liposomen
  申请人：CIBA-GEIGY AG

  公开号：EP0152379A2

  公开（公告）日：1985-08-21

  Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von pharmazeutischen Zusammensetzungen in Form einer wässrigen wässrigen Dispersion enthaltend unilamellare Liposomen bestehend aus (1) einer amphipatischen Verbindung mit biologischer Wirkung und (II) einem Phospholipid oder einem analogen Lipid und gegebenenfalls einem zusätzlichen Lipid. Die Liposomendispersion wird durch Herstellung einer homogenen Mischung der Komponenten und Dispersion der homogenen Mischung in wässriger Phase erhalten. Die uRilamellaren Liposomen können als Träger von amphipatischen Wirkstoffen unterschiedlichster Art therapeutisch verwendet werden.

  本发明涉及一种制备水分散液形式的药物组合物的工艺，该水分散液由单拉米脂质体组成，单拉米脂质体由(1)具有生物活性的两性化合物和(II)磷脂或类似脂质以及可选的附加脂质组成。 脂质体分散液是通过制备各组分的均匀混合物并将该均匀混合物分散在水相中获得的。 单拉米脂质体可作为各种两性活性成分的载体用于治疗。
• 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。
• 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。
• 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：EP1551370A1

  公开（公告）日：2005-07-13
• [EN] 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<br/>[FR] AGREGAT A CAPACITE DE DEFORMATION ACCRUE, COMPRENANT AU MOINS TROIS COMPOSANTS AMPHIPATHIQUES PERMETTANT UN TRANSPORT AMELIORE A TRAVERS DES BARRIERES SEMI-PERMEABLES, ET POUR ADMINISTRATION NON EFFRACTIVE DE MEDICAMENTS IN VIVO, EN PARTICULIER PAR VOIE TRANSCUTANEE
  申请人：IDEA AG

  公开号：WO2004032900A1

  公开（公告）日：2004-04-22

  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.