1-[[5-(4-methoxyphenyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]carbonyl]-4-(phenylmethyl)piperidine | 1076205-75-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-[[5-(4-methoxyphenyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]carbonyl]-4-(phenylmethyl)piperidine
• 英文别名: (4-Benzylpiperidin-1-yl)-[5-(4-methoxyphenyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]methanone
• CAS: 1076205-75-8
• 化学式: C₂₇H₂₅F₃N₄O₂
• 分子量: 494.516
• InChiKey: MQNYYNKGYKNHFC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  36
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  59.7
• 氢给体数：
  0
• 氢受体数：
  7

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。
• [EN] ALPHA-UNSUBSTITUTED ARYLMETHYL PIPERAZINE PYRAZOLO[1,5-A] PYRIMIDINE AMIDE DERIVATIVES<br/>[FR] DÉRIVÉS D'AMIDE PYRIMIDINE ARYLMETHYL PIPERAZINE PYRAZOLO[1,5-a] À SUBSTITUTION ALPHA
  申请人：PANACOS PHARMACEUTICALS INC

  公开号：WO2008134035A1

  公开（公告）日：2008-11-06

  [EN] Methods of preventing, treating or delaying the onset of HIV in a subject by administering to the subject novel pharmaceutically active arylmethyl pyrazolo[1,5-a ]pyrimidine amide derivatives, or pharmaceutical compositions containing the same are described. Additionally, compounds of novel pharmaceutically active arylmethyl piperazine pyrazolo[l,5-a]pyrimidine amide derivatives and their use for the manufacture of specific medicaments are described.
  [FR] Cette invention concerne des méthodes permettant de prévenir, de traiter ou de retarder le début du VIH chez un sujet par administration audit sujet de nouveaux dérivés d'amide pyrimide arylmethyl pyrazolo[1,5-a ] présentant une activité pharmaceutique, ou de compositions pharmaceutiques contenant de tels dérivés. En outre, cette invention concerne des composés de dérivés d'amide pyrimide arylmethyl pyrazolo[1,5-a ] présentant une activité pharmaceutique ainsi que l'utilisation de ceux-ci pour la fabrication de médicaments spécifiques.