4-oxo-4-((4-sulfamoylphenethyl)amino)butanoic acid | 401819-70-3

• 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: 4-oxo-4-((4-sulfamoylphenethyl)amino)butanoic acid
• 英文别名: 4-oxo-4-(4-sulfamoylphenethylamino)butanoic acid；4-Oxo-4-{[2-(4-sulfamoylphenyl)ethyl]amino}butanoic acid；4-oxo-4-[2-(4-sulfamoylphenyl)ethylamino]butanoic acid
• CAS: 401819-70-3
• 化学式: C₁₂H₁₆N₂O₅S
• mdl: MFCD01104615
• 分子量: 300.335
• InChiKey: BWHDBKANFPGCIT-UHFFFAOYSA-N

物化性质

• 密度：
  1.379±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  20
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  135
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  丁二酸酐 、 4-(2-氨乙基)苯磺酰胺 在 1,4-二氧六环 作用下， 以 1,4-二氧六环 为溶剂， 反应 16.0h， 以to yield the desired product (1.4 g, 4.6 mol, 92%) as a white solid的产率得到4-oxo-4-((4-sulfamoylphenethyl)amino)butanoic acid
  参考文献：
  名称：

  Inhibitors of carbonic anhydrase IX

  摘要：

  这段话的中文翻译如下：用于诊断成像和治疗表达CA-IX过度的疾病的新型放射性药物包括一种复合物，其中含有能够结合CA-IX活性催化位点的磺酰胺基团，以及适用于放射性成像和/或放射性治疗的放射性核素。

  公开号：

  US08877970B2

文献信息

• [EN] OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF<br/>[FR] COMPOSITIONS D'OLIGONUCLÉOTIDES ET PROCÉDÉS ASSOCIÉS
  申请人：WAVE LIFE SCIENCES LTD

  公开号：WO2019075357A1

  公开（公告）日：2019-04-18

  Among other things, the present disclosure provides technologies for altering splicing, particularly for increasing inclusion of exons in splicing products. In some embodiments, the present disclosure provides SMN2 oligonucleotides, compositions, and methods thereof. In some embodiments, the present disclosure provides chirally controlled SMN2 oligonucleotide compositions. In some embodiments, provided oligonucleotides and compositions can increase level of an exon 7-containing SMN2 splicing product and/or a gene product thereof. In some embodiments, the present disclosure provides methods for treatment of splicing-related conditions, disorders and diseases. In some embodiments, the present disclosure provides methods for treating SMN2-related conditions, disorders and diseases such as SMA (spinal muscular atrophy) and ALS (amyotrophic lateral sclerosis).

  本公开提供了用于改变剪接的技术，特别是用于增加剪接产物中外显子包含量的技术。在某些实施例中，本公开提供了SMN2寡核苷酸、组合物及其方法。在某些实施例中，本公开提供了立体控制的SMN2寡核苷酸组合物。在某些实施例中，所提供的寡核苷酸和组合物可以增加外显子7包含的SMN2剪接产物的水平和/或其基因产物的水平。在某些实施例中，本公开提供了用于治疗剪接相关疾病、疾病和疾病的方法。在某些实施例中，本公开提供了用于治疗SMN2相关疾病、疾病和疾病的方法，如脊髓性肌萎缩症（SMA）和肌萎缩侧索硬化（ALS）。
• [EN] OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF<br/>[FR] COMPOSITIONS OLIGONUCLÉOTIDIQUES ET MÉTHODES ASSOCIÉES
  申请人：WAVE LIFE SCIENCES LTD

  公开号：WO2019032612A1

  公开（公告）日：2019-02-14

  Among other things, the present disclosure provides oligonucleotides, compositions, and methods thereof. Among other things, the present disclosure encompasses the recognition that structural elements of oligonucleotides, such as base sequence, chemical modifications (e.g., modifications of sugar, base, and/or internucleotidic linkages) or patterns thereof, conjugation with additional chemical moieties, and/or stereochemistry [e.g., stereochemistry of backbone chiral centers (chiral internucleotidic linkages)], and/or patterns thereof, can have significant impact on oligonucleotide properties and activities, e.g., knockdown ability, stability, delivery, etc. In some embodiments, the oligonucleotides decrease the expression, activity and/or level of a C9orf72 gene, including but not limited to, one comprising a repeat expansion, or a gene product thereof. In some embodiments, the present disclosure provides methods for treatment of diseases using provided oligonucleotide compositions, for example, in treatment of C9orf72-related disorders.

  本公开提供寡核苷酸、组合物及其方法等内容。本公开涵盖了对寡核苷酸的结构元素（如碱基序列、化学修饰（例如糖、碱基和/或核苷酸间连接的修饰）或其模式、与额外化学基团的结合以及/或立体化学[例如骨架手性中心的立体化学（手性核苷酸间连接）]及/或其模式等）的认识，这些因素可能对寡核苷酸的性质和活性（例如敲低能力、稳定性、传递等）产生重要影响。在某些实施例中，寡核苷酸降低C9orf72基因的表达、活性和/或水平，包括但不限于包含重复扩展或其基因产物的基因。在某些实施例中，本公开提供使用所提供的寡核苷酸组合物治疗疾病的方法，例如治疗C9orf72相关疾病。
• INHIBITORS OF CARBONIC ANHYDRASE IX
  申请人：Zimmerman Craig

  公开号：US20090175794A1

  公开（公告）日：2009-07-09

  Novel radiopharmaceuticals that are useful in diagnostic imaging and therapeutic treatment of disease characterized by over expression of CA-IX comprise a complex that contains a sulfonamide moiety which is capable of binding the active catalytic site of CA-IX, and a radionuclide adapted for radioimaging and/or radiotherapy:

  具有在诊断成像和治疗过度表达CA-IX疾病中有用的新型放射性药物，包括一种含有磺胺基团的复合物，该基团能够结合CA-IX的活性催化位点，以及适用于放射成像和/或放射治疗的放射性核素：
• Tetracyclic Anthraquinone Derivatives
  申请人：Tianjin Hemay Bio-Tech Co., Ltd

  公开号：US20150166595A1

  公开（公告）日：2015-06-18

  Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, n are defined as in the present application.

  公开了一种由式（I）表示的化合物及其药用可接受的盐，其中R1、R2、R3、R4、R5、W、n的定义如本申请中所述。
• Tetracyclic anthraquinone derivatives
  申请人：TIANJIN HEMAY ONCOLOGY PHARMACEUTICAL CO., LTD.

  公开号：US10294260B2

  公开（公告）日：2019-05-21

  Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, W, n are defined as in the present application. Also disclosed is a method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound and a salt thereof according to the present application possess good anticancer and/or antitumor activity, and good water solubility and stability, as well as good tolerance in animal bodies. Also disclosed is a process for preparing a compound represented by formula (I) of the present application.

  公开了一种由式 (I) 代表的化合物及其药学上可接受的盐、 其中 R1、R2、R3、R4、R5、W、n 的定义与本申请相同。还公开了一种治疗癌症的方法，包括向有需要的受试者施用治疗有效量的式 (I) 所代表的化合物或其药学上可接受的盐。根据本申请的化合物及其盐具有良好的抗癌和/或抗肿瘤活性、良好的水溶性和稳定性，以及在动物体内良好的耐受性。本申请还公开了一种制备式（I）所代表的化合物的工艺。