N'-[3-(2,4-dichlorophenyl)-2-methyl-5-propan-2-ylpyrazolo[1,5-a]pyrimidin-7-yl]-N-(1-pyrimidin-2-ylpiperidin-4-yl)ethane-1,2-diamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N'-[3-(2,4-dichlorophenyl)-2-methyl-5-propan-2-ylpyrazolo[1,5-a]pyrimidin-7-yl]-N-(1-pyrimidin-2-ylpiperidin-4-yl)ethane-1,2-diamine
• 化学式: C₂₇H₃₂Cl₂N₈
• 分子量: 539.5
• InChiKey: JALAEEPTZZHSFR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  37
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  83.3
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Certain alkylene diamine-substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo [1,5-a]-1,3,5-triazines
  申请人：Neurogen Corporation

  公开号：US20030069246A1

  公开（公告）日：2003-04-10

  Disclosed are compounds of the formula: 1 where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

  本发明揭示了以下化合物的公式：1其中R1、R2、R3、R4、R5、R6和X在此定义。这些化合物是NPY1受体的选择性调节剂。这些化合物在治疗许多中枢神经系统疾病、代谢性疾病和外周疾病，特别是进食障碍和高血压方面非常有用。本发明还提供了治疗这些疾病的方法以及包装的制药组合物。本发明的化合物还可用作NPY1受体定位的探针，以及在NPY1受体结合测定中的标准。给出了在受体定位研究中使用这些化合物的方法。
• PYY and agonists thereof for modification of feeding behaviour
  申请人：Imperial Innovations Limited

  公开号：EP2050460A1

  公开（公告）日：2009-04-22

  Methods are disclosed for decreasing calorie intake, food intake, and appetite in a subject. The methods include peripherally administering a therapeutically effective amount of PYY or an agonist thereof to the subject, thereby decreasing the calorie intake of the subject.

  本发明公开了减少受试者卡路里摄入量、食物摄入量和食欲的方法。 这些方法包括向受试者外周施用治疗有效量的PYY或其激动剂，从而减少受试者的卡路里摄入量。
• Modification of feeding behavior
  申请人：Cowley Michael

  公开号：US20050176630A1

  公开（公告）日：2005-08-11

  Methods are disclosed for decreasing calorie intake, food intake, and appetite in a subject. The methods include peripherally administering a therapeutically effective amount of PYY or an agonist thereof to the subject, thereby decreasing the calorie intake of the subject.
• ASSESSMENT OF NEURONS IN THE ARCUATE NUCLEUS TO SCREEN FOR AGENTS THAT MODIFY FEEDING BEHAVIOR
  申请人：Cowley Michael

  公开号：US20080213803A1

  公开（公告）日：2008-09-04

  Screening methods of use in identifying agents that affect caloric intake, food intake, appetite, and energy expenditure are disclosed herein. These methods are used to identify agents of use in treating obesity, or that can be used to decrease the weight of a subject. These methods can also be used to identify agents of use in treating anorexia or cachexia and can be used to increase appetite and to increase the weight and lean body mass of a subject.
• MODIFICATION OF FEEDING BEHAVIOR
  申请人：Cowley Michael

  公开号：US20090209461A1

  公开（公告）日：2009-08-20

  Methods are disclosed for decreasing calorie intake, food intake, and appetite in a subject. The methods include peripherally administering a therapeutically effective amount of PYY or an agonist thereof to the subject, thereby decreasing the calorie intake of the subject.