3,5-bis(3,4 dihydroxyphenyl)pyrazole | 1147315-28-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3,5-bis(3,4 dihydroxyphenyl)pyrazole
• 英文别名: 4-[3-(3,4-dihydroxyphenyl)-1H-pyrazol-5-yl]benzene-1,2-diol
• CAS: 1147315-28-3
• 化学式: C₁₅H₁₂N₂O₄
• 分子量: 284.271
• InChiKey: DDQQCEQYIIMLMQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  110
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  3,5-Bis(1,3-benzodioxol-5-yl)-1H-pyrazol 在 三溴化硼 、 甲醇 作用下， 以 二氯甲烷 为溶剂， 反应 27.0h， 以67%的产率得到3,5-bis(3,4 dihydroxyphenyl)pyrazole
  参考文献：
  名称：

  Compounds, Compositions, and Methods for the Treatment of Beta-Amyloid Diseases and Synucleinopathies

  摘要：

  二羟基芳基化合物及其药学上可接受的酯类，其合成方法，含有它们的制药组合物，以及它们在β-淀粉样蛋白病（如阿尔茨海默病中观察到的）和突触核蛋白病（如帕金森病中观察到的）治疗中的用途，以及用于制造这种治疗药物。

  公开号：

  US20100331380A1

文献信息

• Compounds, Compositions and Methods for the Treatment of Islet Amyloid Polypeptide (IAPP) Accumulation in Diabetes
  申请人：Lake Thomas

  公开号：US20090227647A1

  公开（公告）日：2009-09-10

  Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of IAPP or amylin fibril diseases, and the manufacture of medicaments for such treatment.

  二羟基芳基化合物和药用可接受的酯，它们的合成，含有它们的药物组合物，以及它们在治疗IAPP或淀粉样蛋白纤维病中的用途，以及用于制造用于这种治疗的药物。
• Compounds, Compositions and Methods for the Treatment of Beta-Amyloid Diseases and Synucleinopathies
  申请人：Esposito Luke A.

  公开号：US20090111863A1

  公开（公告）日：2009-04-30

  Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of β-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

  二羟基芳基化合物及其药学上可接受的酯，其合成方法，包含它们的药物组合物，以及它们在β-淀粉样蛋白疾病（如阿尔茨海默病中所观察到的）和突触核蛋白病（如帕金森病中所观察到的）的治疗中的使用，以及用于制造这种治疗药物。
• COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF BETA-AMYLOID DISEASES AND SYNUCLEINOPATHIES
  申请人：Esposito Luke A.

  公开号：US20120252858A1

  公开（公告）日：2012-10-04

  Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of β-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

  二羟基芳基化合物及其药学上可接受的酯类，其合成，含有它们的制药组合物，以及它们在治疗β-淀粉样病变，如阿尔茨海默病中观察到的和突触核蛋白病，如帕金森病中观察到的使用，以及用于制造此类治疗药物。
• NEW DRUG FOR INHIBITING AGGREGATION OF PROTEINS INVOLVED IN DISEASES LINKED TO PROTEIN AGGREGATION AND/OR NEURODEGENERATIVE DISEASES
  申请人：Giese Armin

  公开号：US20110293520A1

  公开（公告）日：2011-12-01

  The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R 1 )(R 2 )—, —C(R 3 )═, —N(R 4 )—, —N═, —N + (R 5 )═, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).

  本发明涉及一种由公式（E）表示的化合物。本发明还涉及一种由公式（E）表示的化合物，用于治疗或预防与蛋白质聚集和/或神经退行性疾病相关的疾病。此外，本发明涉及包含本发明化合物的制药和诊断组合物，以及一种试剂盒。此外，本发明还涉及一种成像聚集蛋白沉积物的方法。还公开了一种用于制备可检测标记的本发明化合物的试剂盒。公式（E）中，X、Y和L分别独立地从—C（R1）（R2）—、—C（R3）═、—N（R4）—、—N═、—N+（R5）═、—O—和—S—中非定向选择；M和Z分别独立地从公式（I）和公式（II）中非定向选择。
• DRUG FOR INHIBITING AGGREGATION OF PROTEINS INVOLVED IN DISEASES LINKED TO PROTEIN AGGREGATION AND/OR NEURODEGENERATIVE DISEASES
  申请人：Ludwig-Maximilians-Universität München

  公开号：US20160185730A1

  公开（公告）日：2016-06-30

  The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed.

  本发明涉及一种由式(E)所表示的化合物。本发明还涉及一种由式(E)所表示的化合物，用于治疗或预防与蛋白质聚集和/或神经退行性疾病有关的疾病。此外，本发明还涉及包含本发明化合物的制药和诊断组合物，以及一种试剂盒。此外，本发明还涉及一种成像聚集蛋白沉积物的方法。还公开了一种用于制备本发明化合物的可检测标记试剂盒。