Azepan-1-yl-[5-(4-chlorophenyl)-2-methyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]methanone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: Azepan-1-yl-[5-(4-chlorophenyl)-2-methyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]methanone
• 化学式: C₂₁H₂₀ClF₃N₄O
• 分子量: 436.9
• InChiKey: YRCWUMHRRJVNFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  30
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  50.5
• 氢给体数：
  0
• 氢受体数：
  6

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。
• PYRIDYLPHENOL COMPOUND AND USE THEREOF
  申请人：Sasaki Satoshi

  公开号：US20090156646A1

  公开（公告）日：2009-06-18

  The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: or a salt thereof, a prodrug thereof, and a pharmaceutical agent containing the same; wherein Ring A represents a 5- to 8-membered homocyclic or heterocyclic group optionally having a substituent other than formula —X-R 1 wherein X represents a bond or a spacer, and R 1 represents optionally substituted amino or an optionally substituted nitrogen-containing heterocyclic group; Ring B represents an optionally substituted benzene ring; R 2 represents an optionally substituted homocyclic or heterocyclic group; and R 3 and R 4 independently represent a hydrogen atom, cyano, acyl or an optionally substituted hydrocarbon group.

  本发明提供了一种具有转移素受体拮抗活性的化合物，可用于预防和治疗激素依赖性癌症、良性前列腺增生、子宫内膜异位症、早熟、子宫肌瘤等。更具体地，本发明提供了一种化合物，其表示为以下公式：或其盐、前药及含有该化合物的药物制剂；其中环A表示一个5-至8-成员的同环或异环族群，可选地具有除公式—X-R1以外的取代基，其中X表示键或空间组分，而R1表示可选地取代的氨基或可选地取代的含氮杂环族群；环B表示可选地取代的苯环；R2表示可选地取代的同环或异环族群；而R3和R4独立地表示氢原子、氰基、酰基或可选地取代的碳氢基团。
• Pharmaceutical use of substituted pyrazolo [1,5- a]pyrimidines
  申请人：NOVO NORDISK A/S

  公开号：EP1782859A2

  公开（公告）日：2007-05-09

  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.

  描述了取代的吡唑并[1,5-a]嘧啶在调节 11β- 羟类固醇脱氢酶 1 型（11βHSD1）活性方面的用途，以及这些化合物作为药物组合物的用途。此外，还介绍了一类新型的取代吡唑并[1,5-a]嘧啶，它们在治疗中的用途、包含这些化合物的药物组合物以及它们在制造药物中的用途。本化合物是 11βHSD1 活性的调节剂，更具体地说是抑制剂，可用于治疗、预防和/或预防一系列需要降低细胞内活性糖皮质激素浓度的疾病。
• Combinations of an 11-beta-hydroxysteroid dehaydrogenase type 1 inhibitor and a glucocorticoid receptor agonist
  申请人：NOVO NORDISK A/S

  公开号：EP1854487A2

  公开（公告）日：2007-11-14

  Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist for treating some forms of cancer, diseases and disorders having inflammation as a component, and to minimize the side effects associated with glucorticoid receptor agonist therapy.

  由 11β- 羟类固醇脱氢酶 1 型抑制剂和糖皮质激素受体激动剂组成的联合疗法，用于治疗某些形式的癌症、以炎症为组成部分的疾病和失调，并最大限度地减少与糖皮质激素受体激动剂疗法相关的副作用。
• Combination therapy using an 11B-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent for the treatment of metabolic syndrome and related diseases and disorders
  申请人：NOVO NORDISK A/S

  公开号：EP1862181A2

  公开（公告）日：2007-12-05

  Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.

  由 11β- 羟类固醇脱氢酶 1 型抑制剂和降压药组成的联合疗法，可用于治疗、预防和降低胰岛素抵抗、血脂异常、肥胖、高血压及其他相关疾病和紊乱的发病风险。