Carnitinamide | 16630-38-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: Carnitinamide
• 英文别名: (4-amino-2-hydroxy-4-oxobutyl)-trimethylazanium
• CAS: 16630-38-9
• 化学式: C7H17N2O2+
• 分子量: 161.22
• InChiKey: KWIXGIMKELMNGH-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  -1.5
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  63.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  Carnitinamide 、 磷酸肌酸 、 白碳黑 在 Carnitinamide 作用下， 以to obtain 30 ml of a cell-free extract的产率得到左旋肉碱
  参考文献：
  名称：

  Method for producing carnitine, L-carnitinamide hydrolase and method for

  摘要：

  本发明涉及一种生产肉碱的方法，包括将肉碱酰胺与（A）能够水解肉碱酰胺形成肉碱的酰胺酶或（B）含有该酰胺酶、肉碱酰胺水解酶的微生物在反应介质中接触，以及生产该酰胺酶和肉碱酰胺水解酶的方法。

  公开号：

  US04918012A1
• 作为试剂：
  描述：

  Carnitinamide 、 磷酸肌酸 、 白碳黑 在 Carnitinamide 作用下， 以to obtain 30 ml of a cell-free extract的产率得到左旋肉碱
  参考文献：
  名称：

  Method for producing carnitine, L-carnitinamide hydrolase and method for

  摘要：

  本发明涉及一种生产肉碱的方法，包括将肉碱酰胺与（A）能够水解肉碱酰胺形成肉碱的酰胺酶或（B）含有该酰胺酶、肉碱酰胺水解酶的微生物在反应介质中接触，以及生产该酰胺酶和肉碱酰胺水解酶的方法。

  公开号：

  US04918012A1

文献信息

• Formulation of an erodible, gastric retentive oral dosage form using in vitro disintegration test data
  申请人：——

  公开号：US20030133985A1

  公开（公告）日：2003-07-17

  Erodible, gastric-retentive dosage forms are provided that are formulated using the in vitro drug release profile obtained with USP Disintegration test equipment rather the USP Dissolution Apparatus. The invention is premised on the discovery that the USP Disintegration Test and modified versions thereof are far more predictive of the in vivo release profile for a controlled release dosage form than is the standard USP Dissolution Test, particularly controlled release dosage forms of the swellable, erodible type. The dosage forms generally comprise particles of a biocompatible, hydrophilic polymer having the active agent incorporated therein, wherein the particles are optionally but preferably compacted into a tablet or loaded into a capsule. The dosage forms can be used to deliver water-insoluble or sparingly soluble drugs as well as water-soluble drugs, providing that the latter are coated with a protective coating or contained in a protective vesicle.

  提供可侵蚀的、胃滞留的剂型，其配方使用USP分散测试设备获得的体外药物释放剖面，而不是USP溶解器。该发明是基于发现，USP分散测试及其修改版本比标准的USP溶解测试更能预测可控释放剂型的体内释放剖面，特别是膨胀、侵蚀型的可控释放剂型。该剂型通常包括生物相容性、亲水性聚合物的颗粒，其中活性成分被纳入其中，颗粒可以选择但最好是压缩成片剂或装入胶囊。该剂型可用于输送水不溶性或难溶性药物，以及水溶性药物，前提是后者被涂上保护涂层或包含在保护小囊中。
• Formulation of an erodible, gastric retentive oral diuretic
  申请人：——

  公开号：US20030152622A1

  公开（公告）日：2003-08-14

  An erodible, gastric-retentive oral diuretic is provided that is formulated using the in vitro drug release profile obtained with USP Disintegration test equipment rather the USP Dissolution Apparatus. The invention is premised on the discovery that the USP Disintegration Test and modified versions thereof are far more predictive of the in vivo release profile for a controlled release dosage form than is the standard USP Dissolution Test, particularly controlled release dosage forms of the swellable, erodible type. The dosage forms generally comprise particles of a biocompatible, hydrophilic polymer having the active agent incorporated therein, wherein the particles are optionally but preferably compacted into a tablet or loaded into a capsule. The dosage forms can be used to deliver water-insoluble or sparingly soluble drugs as well as water-soluble drugs, providing that the latter are coated with a protective coating or contained in a protective vesicle. Using the controlled release dosage form, adverse side effects associated with peak diuresis are diminished or eliminated, while the overall diuretic effect of the drug is maintained.

  提供了一种可侵蚀、胃内停留的口服利尿剂，其配方使用了通过美国药典溶解试验设备获得的体外药物释放特性，而不是使用美国药典溶出仪。该发明基于发现，美国药典溶解试验及其修改版本远比标准的美国药典溶出试验更具预测性，特别是对于可膨胀、可侵蚀类型的控释剂型的体内释放特性。这些剂型通常包括含有活性成分的生物相容性、亲水性聚合物颗粒，其中这些颗粒可以选择性地但最好是被压制成片剂或装入胶囊中。这些剂型可用于输送水不溶性或难溶性药物以及水溶性药物，只要后者被覆盖有保护层或包含在保护泡囊中。使用控释剂型，可以减轻或消除与高峰利尿相关的不良副作用，同时保持药物的整体利尿效果。
• N,N-dinitramide salts as solubilizing agents for biologically active agents
  申请人：——

  公开号：US20030026850A1

  公开（公告）日：2003-02-06

  A method is provided for enhancing the solubility of an ionizable compound in a lipophilic medium by admixing the compound with an effective solubility-enhancing amount of an N,N-dinitramide salt. The ionizable compound, upon ionization, gives rise to a biologically active cationic species that ionically associates with the N,N-dinitramide anion N(NO 2 ) 2 − following admixture with the N,N-dinitramide salt. The biologically active cationic species may be a pharmacologically active cation, in which case the method is useful for enhancing the penetration of the blood-brain barrier by the pharmacologically active cation. In other embodiments, the ionizable compounds are medical imaging or diagnostic agents, or agricultural agents such as pesticides. Salts of biologically active cations and N,N-dinitramide ion are also provided as novel compositions of matter.

  本发明提供了一种通过将离子化合物与有效的增溶剂量的N，N-二硝酰胺盐混合来增强离子化合物在亲脂性介质中的溶解度的方法。离子化合物在离子化后会产生一种生物活性阳离子物种，该物种在与N，N-二硝酰胺盐混合后会离子地与N(NO2)2-结合。如果生物活性阳离子物种是一种药理学活性阳离子，则该方法对于增强药理学活性阳离子的穿越血脑屏障是有用的。在其他实施例中，离子化合物是医学成像或诊断剂或农业剂，例如杀虫剂。还提供了生物活性阳离子和N，N-二硝酰胺离子的盐作为新的物质组成。
• PPAR-DELTA LIGANDS AND METHODS OF THEIR USE
  申请人：Murphy Brian J.

  公开号：US20090163481A1

  公开（公告）日：2009-06-25

  The disclosure provides compounds, compositions, and methods for modulating PPARδ receptor. In one embodiment, the compounds of the disclosure comprise a tri-substituted thiazole group. The substituent at the 2-position of the thiazole group provides steric bulk to the compounds. The compounds, compositions, and methods may be useful, for example, in the treatment of cancer.

  本披露提供了用于调节PPARδ受体的化合物，组合物和方法。在一种实施例中，披露的化合物包括三取代噻唑基团。噻唑基团的2位取代基为化合物提供了立体体积。这些化合物，组合物和方法可能在癌症治疗中有用。
• PROCESS FOR PRODUCTION OF BETAINE
  申请人：Oishi Kosuke

  公开号：US20090325246A1

  公开（公告）日：2009-12-31

  According to the present invention, by using 4-halogeno-3-hydroxybutanamide as a substrate in quaternary amination reaction with trialkylamine which is an important step in betaine (such as carnitine) preparation processes, it becomes possible to reduce the production of crotonic acid derivatives (the major by-product) greatly compared to conventional processes. Consequently, it becomes possible to prepare a betaine, such as carnitine, at a high yield. The present invention also relates to a process for preparing a betaine represented by formula (1) below, comprising a step of quaternary aminating an amide represented by formula (2) below: wherein A 1 , A 2 and A 3 individually represent a C 1 -C 20 hydrocarbon group which may have a substituent(s); and X 1 is a halogen atom.

  根据本发明，在甜菜碱（如肉碱）制备过程中，使用4-卤代-3-羟基丁酰胺作为底物与三烷基胺进行季铵化反应，可以大大减少与传统工艺相比产生的巴豆酸衍生物（主要副产物）。因此，可以高产得到甜菜碱（如肉碱）。本发明还涉及一种制备下式（1）所表示的甜菜碱的方法，包括季铵化下式（2）所表示的酰胺的步骤：其中A1、A2和A3分别表示可以具有取代基的C1-C20烃基；X1为卤素原子。