3-Bromo-5-thiophen-2-yl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 3-Bromo-5-thiophen-2-yl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxylic acid
• 化学式: C₁₂H₅BrF₃N₃O₂S
• 分子量: 392.15
• InChiKey: GIUQAIBXNDGIHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  95.7
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• Pharmaceutical use of substituted pyrazolo[1,5-a]pyrimidines
  申请人：Andersen Sune Henrik

  公开号：US20070270408A1

  公开（公告）日：2007-11-22

  The use of substituted pyrazolo[1,5-a]pyrimidines for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions are described. Also a novel class of substituted pyrazolo[1,5-a]pyrimidines their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

  本文描述了使用取代的吡唑并[1,5-a]嘧啶类化合物来调节11β-羟类固醇脱氢酶1型（11βHSD1）活性的方法，并将这些化合物用作制药组合物。同时，本文还描述了一类新型的取代吡唑并[1,5-a]嘧啶类化合物及其在治疗中的应用，包括含有这些化合物的制药组合物以及这些化合物在制药中的应用。这些化合物是11βHSD1活性的调节剂，更具体地说是抑制剂，可以在需要降低细胞内活性糖皮质激素浓度的一系列医学疾病的治疗、预防和/或预防中发挥作用。
• Cell migration inhibiting compositions and methods and compositions for treating cancer
  申请人：Edwards L. David

  公开号：US20060128742A1

  公开（公告）日：2006-06-15

  Methods for treating an individual having cancer are provided. The method may include administering a cell migration inhibitor and a chemotherapeutic agent to the individual to inhibit migration of cancer cell. Inhibiting cell migration may increase cell division. In this manner, the cell migration inhibitor and the chemotherapeutic agent in combination may have increased efficacy compared to the chemotherapeutic agent alone due to the increased cell division. The cell migration inhibitor may include any of the inhibitors described herein. For example, the cell migration inhibitor may be an organic molecule having a molecular weight of less than about 700, a monoclonal antibody, or a natural product.

  本文提供了治疗癌症患者的方法。该方法可包括向患者施用细胞迁移抑制剂和化疗药物，以抑制癌细胞的迁移。抑制细胞迁移可增加细胞分裂。这样，由于细胞分裂增加，细胞迁移抑制剂和化疗剂联合使用的疗效可能比单独使用化疗剂的疗效更好。细胞迁移抑制剂可包括本文所述的任何抑制剂。例如，细胞迁移抑制剂可以是分子量小于约 700 的有机分子、单克隆抗体或天然产物。
• PYRAZOLOPYRIMIDINES AS SODIUM CHANNEL INHIBITORS
  申请人：Icagen, Inc.

  公开号：EP1506196B1

  公开（公告）日：2012-01-18
• CELL MIGRATION INHIBITING COMPOSITIONS AND METHODS AND COMPOSITIONS FOR TREATING CANCER
  申请人：Avolix Pharmaceuticals

  公开号：EP1576110A2

  公开（公告）日：2005-09-21
• EP1576110A4
  申请人：——

  公开号：EP1576110A4

  公开（公告）日：2007-11-07