didodecyl 2-amino-pentanedioate | 62765-52-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: didodecyl 2-amino-pentanedioate
• 英文别名: dodecyl glutamate；Lauryl glutamate；Didodecyl glutamate hydrochloride；didodecyl 2-aminopentanedioate
• CAS: 62765-52-0
• 化学式: C₂₉H₅₇NO₄
• 分子量: 483.776
• InChiKey: DMTALGRGUIQVPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  10.6
• 重原子数：
  34
• 可旋转键数：
  28
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  78.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  didodecyl 2-amino-pentanedioate 、 alkaline earth salt of/the/ methylsulfuric acid 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 24.0h， 以62%的产率得到
  参考文献：
  名称：

  一种利用小分子营养物质介导的口服纳米递药系统

  摘要：

  一种利用小分子营养物质介导的口服纳米递药系统。本发明公开了一种基于小分子营养物质介导的，主动靶向肠上皮细胞的口服纳米载体及其制备方法，该纳米粒由核壳两部分组成，其中，内核由生物相容性载体材料与活性成分所组成，外壳为共价连接小分子营养物质配体的亲水材料。本发明提高了口服纳米载体的递药效率，在医药领域具有良好的研究和开发应用前景。

  公开号：

  CN112755005B
• 作为产物：
  描述：

  十二烷醇 在 4-二甲氨基吡啶 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 生成 didodecyl 2-amino-pentanedioate
  参考文献：
  名称：

  一种利用小分子营养物质介导的口服纳米递药系统

  摘要：

  一种利用小分子营养物质介导的口服纳米递药系统。本发明公开了一种基于小分子营养物质介导的，主动靶向肠上皮细胞的口服纳米载体及其制备方法，该纳米粒由核壳两部分组成，其中，内核由生物相容性载体材料与活性成分所组成，外壳为共价连接小分子营养物质配体的亲水材料。本发明提高了口服纳米载体的递药效率，在医药领域具有良好的研究和开发应用前景。

  公开号：

  CN112755005B

文献信息

• Polyamino acids functionalized by hydrophobic grafts bearing an anionic charge and applications thereof, such as therapeutic applications
  申请人：Breyne Olivier

  公开号：US20100098656A1

  公开（公告）日：2010-04-22

  The present invention relates to novel materials based on biodegradable polyamino acids that are useful especially for the vectorization of active principle(s) (AP). The invention further relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on these polyamino acids. The object of the invention is to provide a novel polymer starting material that is capable of being used for the vectorization of AP and makes it possible on the one hand to achieve high polymer/AP ratios, and on the other hand optimally to satisfy all the specifications required in the case in point: biocompatibility, biodegradability, ability to associate easily with numerous active principles or to solubilize them, and ability to release these active principles in vivo. This object is achieved by the present invention, which relates first and foremost to linear polyamino acids comprising aspartic units or glutamic units and having hydrophobic grafts comprising hydrophobic groups containing from 8 to 30 carbon atoms, at least one of these hydrophobic grafts having at least one anionic charge and/or one or more mutually identical or different ionizable groups each capable of giving rise to at least one anionic charge. These polymers are amphiphilic and anionic and are capable of being converted easily and economically to particles for the vectorization of active principles, these particles themselves being capable of forming stable aqueous colloidal suspensions.

  本发明涉及基于可生物降解的聚氨基酸的新材料，特别适用于活性成分的载体化。该发明还涉及基于这些聚氨基酸的新型药用、化妆品、饮食或植物保健组合物。本发明的目的是提供一种新型聚合物起始材料，能够用于活性成分的载体化，一方面实现高聚合物/活性成分比，另一方面能够最佳地满足所需的所有规格要求：生物相容性、可生物降解性、能够轻松与许多活性成分结合或溶解它们的能力，以及在体内释放这些活性成分的能力。本发明通过首先涉及含有天冬氨酸单元或谷氨酸单元并具有含有8至30个碳原子的疏水侧链的线性聚氨基酸来实现这一目的，其中至少一个这些疏水侧链具有至少一个阴离子电荷和/或一个或多个能够产生至少一个阴离子电荷的相互相同或不同的离子化基团。这些聚合物是两性和带负电荷的，能够轻松且经济地转化为用于活性成分载体化的颗粒，这些颗粒本身能够形成稳定的水胶体悬浮液。
• MEDICINAL PREPARATION
  申请人：TORAY INDUSTRIES, INC.

  公开号：EP1787661A1

  公开（公告）日：2007-05-23

  A pharmaceutical preparation has a ligand structure specifically recognizing a target site and an amphiphilic compound having a hydrophobic or amphiphilic group. The pharmaceutical preparation employs an amphiphilic compound of specific structure obtained by introducing a chained hydrophilic group with an appropriate flexibility, and thus becomes a fine particle suited for drug targeting. The pharmaceutical preparation is expected to give a prolonged pharmacological effect. A particulate preparation exhibiting a remarkable site targeting property can be formed. Further, according to the selection of matrix forming material, the drug releasing property can be controlled.

  一种药物制剂具有特异性识别靶位点的配体结构和具有疏水或两性亲和性基团的两性化合物。该药物制剂采用通过引入具有适当柔韧性的链状亲水基团获得的特定结构的两性化合物，因此成为适用于药物靶向的细颗粒。 预计该药物制剂将产生持久的药理效应。可以形成具有显著靶向性能的颗粒制剂。此外，根据基质形成材料的选择，可以控制药物释放性能。
• Polyglutamic Acids Functionalised by Histidine Derivatives and Hydrophobic Groups and the Uses Thereof, in Particular for Therapeutic Purposes
  申请人：Soula Olivier

  公开号：US20100034886A1

  公开（公告）日：2010-02-11

  The invention relates to novel biodegradable materials based on modified polyamino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids. The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained to 30 carbon atoms. Said polyglutamates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorization particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7.4), and thereby have to be precipitated on an injection site in the case of a subcutaneous injection.

  该发明涉及基于改性聚氨基酸的新型可生物降解材料，特别适用于载荷活性物质（AS）。该发明还涉及基于这些聚氨基酸的新型药用、化妆品、膳食或植物保护组合物。 该发明的目的是提供一种新型聚合物原料，可用于载荷AS，并能够最佳地满足该领域的所有规范要求：生物相容性、生物降解性、能够轻松与许多活性物质结合或溶解它们，并在体内释放所述活性物质。该目的在30个碳原子处实现。 通过组氨酸衍生物改性的聚谷氨酸在pH低于5时可溶解，并且可以经济地转化为能够形成稳定水性胶体悬浮液的活性物质载体颗粒。相反，这些改性聚谷氨酸在生理pH值（7.4）下不溶于水，因此在皮下注射时必须在注射部位沉淀。
• COPOLYHYDROXYALKYLGLUTAMINES FUNCTIONALISED WITH HYDROPHOBIC GROUPS, AND USES THEREOF, ESPECIALLY IN THERAPEUTICS
  申请人：Soula Rémi

  公开号：US20110044930A1

  公开（公告）日：2011-02-24

  The invention relates to novel biodegradable materials which are based on modified polyamino acids and which can be used for the vectorisation of active principle(s) (AP). The invention also relates to novel pharmaceutical, cosmetic, dietary or phytosanitary compositions based on said polyamino acids. The aim of the invention is to provide a novel polymer raw material which can be used for the vectorisation of active principles and which can optimally fulfil all required specifications in said area, namely: biocompatibility, biodegradability and the ability to become easily associated with many active principles or to solubilise said principles and to release same in vivo. Said aim is achieved with novel copolyhydroxyalkylglutamines comprising glutamine units and optionally glutamate units and bearing hydrophobic groups containing between 8 and 30 carbon atoms. Said copolyhydroxyalkylglutamines are amphiphilic and can be easily and economically transformed into particles for the vectorisation of active principles, whereby said particles can form stable aqueous colloidal suspensions.

  该发明涉及基于改性聚氨基酸的新型可生物降解材料，可用于活性成分的载体化。该发明还涉及基于这些聚氨基酸的新型药用、化妆品、膳食或植物保护组合物。该发明的目的是提供一种新型聚合物原料，可用于活性成分的载体化，并能够最佳地满足该领域中所有所需规格，即生物相容性、生物降解性以及能够轻松与许多活性成分结合或溶解这些成分并在体内释放的能力。通过包含谷氨酰胺单元和可选的谷氨酸单元以及带有含有8至30个碳原子的疏水基团的新型共聚羟基烷基谷氨酰胺，实现了该目的。这些共聚羟基烷基谷氨酰胺是两性的，可以轻松且经济地转化为用于活性成分载体化的颗粒，这些颗粒可以形成稳定的水胶体悬浮液。
• Telechelic Homopolyamino Acids Functionalized with Hydrophobic Groups, and Their Applications, Especially Therapeutic Applications
  申请人：Soula Rémi

  公开号：US20070265192A1

  公开（公告）日：2007-11-15

  The invention relates to novel materials based on biodegradable homopolyamino acids and which can be used for the vectorization of (an) active ingredient(s) (AI). The invention also relates to novel pharmaceutical, cosmetic, dietetic or phytosanitary compositions based on said homopolyamino acids. The aim of the invention is to produce a novel polymer raw material which can be used for the vectorization of AI and which meets all specifications in an optimum manner: biocompatibility, biodegradability, the ability to become easily associated with a large number of active ingredients or to solubilize them and to release said ingredients in vivo. According to the present invention, which primarily relates to linear homopolyamino acids having aspartic or glutamic units and whose extremities include hydrophobic groups having 8-30 carbon atoms. Said homopolymers are amphiphilic and anionic and can easily be transformed at low cost into particles for the vectorization of active ingredients. Said particles can form stable aqueous colloidal suspensions.

  该发明涉及基于可生物降解的同聚氨基酸的新材料，可用于（一种）活性成分（AI）的载体化。该发明还涉及基于这些同聚氨基酸的新型药用、化妆品、饮食或植物保护组合物。该发明的目的是生产一种新型聚合物原料，可用于AI的载体化，并以最佳方式满足所有规格要求：生物相容性、生物降解性，易与大量活性成分结合或溶解，并在体内释放这些成分。根据本发明，主要涉及具有天冬氨酸或谷氨酸单元的线性同聚氨基酸，其末端包括具有8-30个碳原子的疏水基团。这些同聚物是两性和阴离子的，可以低成本地转化为用于活性成分载体化的颗粒。这些颗粒可以形成稳定的水性胶体悬浮液。