6-[2-(3-Benzoylphenyl)propionylsulfamoyl]hexanoic acid | 848432-28-0

• 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: 6-[2-(3-Benzoylphenyl)propionylsulfamoyl]hexanoic acid
• 英文别名: 6-[2-(3-benzoylphenyl)propanoylsulfamoyl]hexanoic acid
• CAS: 848432-28-0
• 化学式: C₂₂H₂₅NO₆S
• 分子量: 431.5
• InChiKey: VGOKYAPDTMDJHF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  30
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  126
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  酮基布洛芬 、 N-羟基-7-氮杂苯并三氮唑 、 1,2-二氯乙烷 、 ethyl 6-sulfamoylhexanoate 在 盐酸 、 magnesium sulfate 作用下， 以 二氯甲烷 为溶剂， 反应 72.0h， 以yielded 2.0 g (44%) of the title compound的产率得到6-[2-(3-Benzoylphenyl)propionylsulfamoyl]hexanoic acid
  参考文献：
  名称：

  Plasma protein affinity tags

  摘要：

  增加治疗剂在血浆中半衰期的方法和新型多肽衍生物。

  公开号：

  US07897560B2

文献信息

• Novel plasma protein affinity tags
  申请人：Dorwald Zaragoza Florencio

  公开号：US20070105750A1

  公开（公告）日：2007-05-10

  Method for increasing half-life of therapeutic agents in plasma and novel polypeptide derivatives.

  增加治疗药物在血浆中半衰期的方法和新型多肽衍生物。
• Novel Plasma Protein Affinity Tags
  申请人：Dorwald Florencio Zaragoza

  公开号：US20100184641A1

  公开（公告）日：2010-07-22

  Method for increasing half-life of therapeutic agents in plasma and novel polypeptide derivatives.

  增加治疗药物在血浆中半衰期的方法和新的多肽衍生物。
• ALBUMIN-BINDING DERIVATIVES OF THERAPEUTIC PEPTIDES
  申请人：NOVO NORDISK A/S

  公开号：EP1667724A2

  公开（公告）日：2006-06-14
• US7897560B2
  申请人：——

  公开号：US7897560B2

  公开（公告）日：2011-03-01
• [EN] NOVEL PLASMA PROTEIN AFFINITY TAGS<br/>[FR] NOUVELLES ETIQUETTES D'AFFINITE POUR LES PROTEINES PLASMIQUES
  申请人：NOVO NORDISK AS

  公开号：WO2005028516A2

  公开（公告）日：2005-03-31

  The present invention relates to a new drug delivery system, based on novel compounds with high affinity to plasma proteins (= affinity tags). These affinity tags can be linked to therapeutically active compounds and thereby enhance their half-life in plasma by reversible binding to plasma proteins.The present invention intends to provide a versatile delivery system for therapeutic agents, such as proteins, peptides, or small molecule drugs, by covalently binding these therapeutic agents to a plasma-protein ligand, capable of reversible binding to one or several plasma proteins. We have designed a novel linking strategy which enables the covalent binding of known, plasma-protein binding carboxylic acids to a broad variety of therapeutic peptides or proteins, or to any other type of compound, of which a prolonged periferal exposure at well-defined concentrations is required. This strategy consists in converting said plasma-protein binding carboxylic acid into a carboxylic acid mimetic, having a pKa between -5 and +7, in order to be ionized to a significant extent in plasma. Such a carboxylic acid mimetic could be, for instance, an N-acylsulfbnamide, which contains an additional functional group which enables covalent binding of the acid mimetic to a therapeutic agent. This linking strategy should not significantly disturb the structure of the plasma-protein binding acid, if a suitable acid mimetic has been chosen. The present invention álso relates to a compound of the general formula (II), wherein R1, G, Z, X, and Y are defined as described. The present invention also relates to pharmaceutical compositions comprising a compound according to the present invention and the use of compounds according to the present invention for preparing medicaments for treating disease.