3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)butoxy]-4-fluorobenzoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)butoxy]-4-fluorobenzoic acid
• 化学式: C₁₆H₁₉FN₂O₃
• 分子量: 306.33
• InChiKey: JIBCFQWUVLWUMR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  75.2
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] CONJUGATION OF PHARMACEUTICALLY ACTIVE AGENTS WITH TRANSTHYRETIN LIGANDS THROUGH ADJUSTABLE LINKERS TO INCREASE SERUM HALF-LIFE<br/>[FR] CONJUGAISON D'AGENTS PHARMACEUTIQUEMENT ACTIFS AVEC DES LIGANDS DE TRANSTHYRÉTINE PAR DES LIANTS RÉGLABLES POUR AUGMENTER LA DEMI-VIE DE SÉRUM
  申请人：ALHAMADSHEH MAMOUN M

  公开号：WO2016025129A1

  公开（公告）日：2016-02-18

  A delivery system for active agents, and methods of making and using the systems, are provided. The delivery systems have (i) a ligand that is selective for an endogeneous plasma protein in the serum of a subject; and, (ii) a linker configured for operatively attaching the ligand covalently to an active agent to increase the half-life of the active agent in the serum.

  提供了一种用于活性成分的递送系统，以及制造和使用这些系统的方法。这些递送系统具有：(i) 一种选择性地与受试者血清中的内源性血浆蛋白结合的配体；以及 (ii) 一个连接物，配置为以共价键的方式将配体操作地附着到活性成分上，以增加活性成分在血清中的半衰期。
• [EN] TRANSTHYRETIN STABILIZERS AND THEIR USE FOR INHIBITING TRANSTHYRETIN AMYLOIDOSIS AND PROTEIN-PROTEIN INTERACTIONS<br/>[FR] STABILISANTS DE TRANSTHYRÉTINE ET LEUR UTILISATION POUR INHIBER L'AMYLOSE DE LA TRANSTHYRÉTINE ET LES INTERACTIONS PROTÉINE-PROTÉINE
  申请人：UNIV LELAND STANFORD JUNIOR

  公开号：WO2014100227A1

  公开（公告）日：2014-06-26

  Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.

  本文公开了一些化合物及其组合物，可用于增加蛋白质的稳定性，特别是那些容易错折和形成聚集体的蛋白质。本文还提供了使用这些化合物和组合物来增加蛋白质稳定性并因此减少这些蛋白质聚集体形成的方法。本文还公开了异二功能化合物，其中包括通过连接剂连接到靶向基团的TTR结合化合物，用于破坏目标蛋白质的PPI。
• CONJUGATION OF PHARMACEUTICALLY ACTIVE AGENTS WITH TRANSTHYRETIN LIGANDS THROUGH ADJUSTABLE LINKERS TO INCREASE SERUM HALF-LIFE
  申请人：ALHAMADSHEH MAMOUN M.

  公开号：US20160045609A1

  公开（公告）日：2016-02-18

  A delivery system for active agents, and methods of making and using the systems, are provided. The delivery systems have (i) a ligand that is selective for an endogeneous plasma protein in the serum of a subject; and, (ii) a linker configured for operatively attaching the ligand covalently to an active agent to increase the half-life of the active agent in the serum.

  提供了一种活性成分的传递系统以及制备和使用该系统的方法。传递系统具有（i）一种选择性为受试者血清中内源性血浆蛋白的配体；和（ii）一个连接物，配置为共价地将配体操作性地附加到活性成分上，以增加活性成分在血清中的半衰期。
• Systems for stabilizing and delivering active agents
  申请人：Alhamadsheh Mamoun M

  公开号：US10172959B2

  公开（公告）日：2019-01-08

  A delivery system for active agents, and methods of making and using the systems, are provided. The delivery systems have (i) a ligand that is selective for an endogeneous plasma protein in the serum of a subject; and, (ii) a linker configured for operatively attaching the ligand covalently to an active agent to increase the half-life of the active agent in the serum.

  本文提供了一种用于活性剂的递送系统，以及制造和使用该系统的方法。这些给药系统具有：(i) 对受试者血清中的内源性血浆蛋白具有选择性的配体；(ii) 用于将配体共价连接到活性剂上以延长活性剂在血清中的半衰期的连接体。
• Enhanced active agents
  申请人：Alhamadsheh Mamoun M

  公开号：US10363318B2

  公开（公告）日：2019-07-30

  The teachings provide active agents that are conjugated with delivery systems that increase the half-life, and reduce the immunogenicity, of the active agents. Methods of making and using the systems are also provided. The delivery systems have (i) a ligand that is selective for an endogeneous plasma protein in the serum of a subject; and, (ii) a linker configured for operatively attaching the ligand covalently to an active agent to increase the half-life of the active agent in the serum.

  本教导提供了与递送系统共轭的活性制剂，可延长活性制剂的半衰期并降低其免疫原性。还提供了制造和使用这些系统的方法。这些递送系统具有：(i) 对受试者血清中的内源性血浆蛋白具有选择性的配体；(ii) 连接体，用于将配体共价连接到活性剂上，以延长活性剂在血清中的半衰期。