[(2R,3R,4R,5R)-5-乙酰氨基-4,6-二羟基-2-(羟基甲基)四氢吡喃-3-基]硫酸氢酯 | 45233-43-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: [(2R,3R,4R,5R)-5-乙酰氨基-4,6-二羟基-2-(羟基甲基)四氢吡喃-3-基]硫酸氢酯
• 英文名称: N-Acetyl-D-galactosamine 4-sulfate
• 英文别名: [(2R,3R,4R,5R)-5-acetamido-1,2,4-trihydroxy-6-oxohexan-3-yl] hydrogen sulfate
• CAS: 45233-43-0
• 化学式: C₈H₁₅NO₉S
• 分子量: 301.27
• InChiKey: RKFMAQNDSSSRTH-OSMVPFSASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.8
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  179
• 氢给体数：
  5
• 氢受体数：
  9

文献信息

• Oligosaccharide biomarkers for mucopolysaccharidoses and other related disorders
  申请人：Meikle John Peter

  公开号：US20060286034A1

  公开（公告）日：2006-12-21

  The present invention is related to methods for diagnosing mucopolysaccharidoses (“MPS”) and related diseases. This invention pertains to methods for identifying and quantitating biochemical markers (“biomarkers”) that are present in biological fluids or tissues of a patient having a MPS or related disorder. One aspect of the method comprises determining a target quantity of a target MPS biomarker oligosaccharide from a target biological sample taken from the target animal, and then comparing the target quantity to a reference quantity of a reference MPS biomarker oligosaccharide for the diagnosis, characterization, monitoring, and clinical management of MPS and related disease. This invention also describes a kit comprising a oligosaccharide derivatization solution; an acid solution; an internal standard; a solid phase extraction column; a solid phase extraction column wash solution; an oligosaccharide elution solution; and a set of instructions for using the kit to diagnose a MPS or related disease.

  本发明涉及诊断粘多糖病（“MPS”）及相关疾病的方法。本发明涉及一种用于识别和定量生物标志物（“生物标记物”）的方法，这些生物标记物存在于患有MPS或相关疾病的患者的生物体液或组织中。该方法的一个方面包括确定来自目标生物样本的目标动物的目标MPS生物标记物寡糖的目标量，然后将目标量与用于诊断、表征、监测和临床管理MPS和相关疾病的参考MPS生物标记物寡糖的参考量进行比较。本发明还描述了一种工具包，包括寡糖衍生物溶液；酸溶液；内部标准；固相萃取柱；固相萃取柱洗涤溶液；寡糖洗脱溶液；以及一套用于使用该工具包诊断MPS或相关疾病的说明书。
• [EN] POLYMERIC CONJUGATES AND USES THEREOF<br/>[FR] CONJUGUÉS POLYMÈRES ET LEURS UTILISATIONS
  申请人：FUNDACION DE LA COMUNIDAD VALENCIANA CENTRO DE INVESTIG PRINCIPE FELIPE

  公开号：WO2020193802A1

  公开（公告）日：2020-10-01

  The present invention relates to novel chemical entities comprising a polymeric carrier incorporating covalently linked drug(s) as well as their pharmaceutical compositions containing the said polymer-drug conjugates as pharmaceutical agents and their uses thereof in therapy and, more particularly, but not exclusively, to novel conjugates having attached thereto a targeting moiety, an imaging agent and one or more therapeutic agents to promote axonal growth and for the treatment of neurodegenerative and inflammatory diseases, central nervous system traumatic injuries and cancer.

  本发明涉及一种新型化学实体，包括将药物共价连接到聚合载体中的药物，以及包含所述聚合物-药物共轭物作为药物代理的药物组合物，以及它们在治疗中的用途，更具体地说，但不限于，涉及附有靶向基团、成像剂和一个或多个治疗剂的新型共轭物，用于促进轴突生长和治疗神经退行性和炎症性疾病、中枢神经系统创伤性损伤和癌症。
• Immunomodulating compositions for treatment of immune system disorders
  申请人：——

  公开号：US20010009680A1

  公开（公告）日：2001-07-26

  The present invention relates to a composition for use as an immunomodulator comprising small molecular weight components of less than 3000 daltons, and having the following properties: a) is extractable from bile of animals; b) is capable of stimulating monocytes and macrophages in vitro and in vivo; c) is capable of modulating tumor necrosis factor production; d) contains no measurable IL-1&agr;, IL-1&bgr;, TNF, IL-6, IL-8, IL-4, GM-CSF or IFN-&ggr;; e) has an anti-proliferative effect in a malignant mouse hybridoma cell line; f) shows no cytotoxicity to human peripheral blood mononuclear cells or lymphocytes; and g) is not an endotoxin. The invention also relates to a method of preparing the composition, its use as an immunomodulator, and its use in the treatment of diseases and conditions having an immunological component.

  本发明涉及一种用作免疫调节剂的组合物，包括小分子量成分，分子量小于3000道尔顿，并具有以下特性：a）可从动物的胆汁中提取；b）能够在体外和体内刺激单核细胞和巨噬细胞；c）能够调节肿瘤坏死因子的产生；d）不含可测量的IL-1α、IL-1β、TNF、IL-6、IL-8、IL-4、GM-CSF或IFN-γ；e）对恶性小鼠杂交瘤细胞系具有抗增殖作用；f）对人类外周血单核细胞或淋巴细胞没有细胞毒性；g）不是内毒素。该发明还涉及一种制备该组合物的方法，其用作免疫调节剂，并在治疗具有免疫成分的疾病和病况中的应用。
• INTRACELLULAR ORGANELLE PEPTIDE TARGETED ENZYME SUBSTRATES
  申请人：Marker Gene Technologies, Inc.

  公开号：US20150219654A1

  公开（公告）日：2015-08-06

  This invention relates to substrates and methods for the visualization of intracellular organelles, such as the lysosome, peroxiosome, nucleus, Endoplasmic Reticulum and Golgi Apparatus, based upon organelle enzyme activity. Such compounds represent a novel combination of chemically distinct enzyme substrates with targeting and detection substrates which are activated by enzyme activity inside target organelles to produce a detectable signal. The organelle targeted enzyme substrates of this invention are designed to provide high fluorescence at lower pH values found in some organelles and can be used for monitoring enzyme activity inside cells at very low concentrations.

  该发明涉及基于细胞器酶活性的底物和方法，用于可视化细胞内细胞器，如溶酶体、过氧化物酶体、细胞核、内质网和高尔基体。这些化合物代表了具有化学上不同的酶底物与靶向和检测底物的新型组合，这些底物受到靶细胞器内的酶活性的激活而产生可检测信号。该发明的细胞器靶向酶底物旨在在一些细胞器中发现的较低pH值下提供高荧光，并可用于监测细胞内酶活性的非常低浓度。
• ANTITHROMBOTIC
  申请人：SEIKAGAKU KOGYO KABUSHIKI KAISHA

  公开号：EP0671414A1

  公开（公告）日：1995-09-13

  An antithrombotic containing dermatan sulfate or a pharmacologically acceptable salt thereof (DS) as the active ingredient. The use of a DS derived from a crest or a disaccharide component thereof having a Δ Di-OS value of at least 3 % or a molecular weight of at least 25 thousand serves to maintain an effective blood level for long and conduct efficiently thrombus dilation or prevention. When used together with a tissue plasminogen activator (t-PA), DS can accelerate remarkably thrombolysis and reduce the amount of t-PA used. This drug is useful for treating and preventing various types of thrombosis such as myocardial infarct and disseminated intravascular coagulation syndrome. Further it can inhibit blood coagulation in extracorporeal circulation such as renal dialysis.

  一种抗血栓药，含有硫酸皮质素或其药理上可接受的盐（DS）作为活性成分。硫酸皮质酯来源于嵴或其双糖成分，其ΔDi-OS 值至少为 3%或分子量至少为 25000，可长期保持有效血药浓度，有效扩张或预防血栓形成。当与组织纤溶酶原激活剂（t-PA）一起使用时，DS 能显著加速血栓溶解并减少 t-PA 的用量。这种药物可用于治疗和预防各种血栓形成，如心肌梗塞和弥散性血管内凝血综合征。此外，它还能抑制体外循环（如肾透析）中的血液凝固。