N1-[4-([4,6-di(ethylamino)-1,3,5-triazin-2-yl]aminomethyl)cyclohexyl]methyl-2-thiophenesulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三嗪类
• 英文名称: N1-[4-([4,6-di(ethylamino)-1,3,5-triazin-2-yl]aminomethyl)cyclohexyl]methyl-2-thiophenesulfonamide
• 英文别名: N-[[4-[[[4,6-bis(ethylamino)-1,3,5-triazin-2-yl]amino]methyl]cyclohexyl]methyl]thiophene-2-sulfonamide
• 化学式: C₁₉H₃₁N₇O₂S₂
• 分子量: 453.633
• InChiKey: HPOJWMMWCXRHQX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  30
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.63
• 拓扑面积：
  158
• 氢给体数：
  4
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  、 2-噻吩磺酰氯 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 以93%的产率得到N1-[4-([4,6-di(ethylamino)-1,3,5-triazin-2-yl]aminomethyl)cyclohexyl]methyl-2-thiophenesulfonamide
  参考文献：
  名称：

  Selective NPY (Y5) antagonists (triazines)

  摘要：

  这项发明涉及选择性拮抗剂，用于NPY（Y5）受体的三嗪衍生物。该发明提供了一种包含本发明化合物的治疗有效量和药用可接受载体的药物组合物。该发明提供了一种由本发明化合物的治疗有效量和药用可接受载体组合而成的药物组合物。此外，该发明还提供了一种制备药物组合物的方法，包括将本发明化合物的治疗有效量与药用可接受载体组合。

  公开号：

  US06340683B1

文献信息

• Selective NPY (Y5) antagonists
  申请人：Marzabadi R. Mohammad

  公开号：US20050176709A1

  公开（公告）日：2005-08-11

  This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

  本发明涉及三嗪衍生物、双环化合物和三环化合物，它们是选择性 Y5 受体拮抗剂。该发明提供一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供一种药物组合物，由本发明化合物的治疗有效量和药学上可接受的载体组成。本发明提供一种制备药物组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体混合。本发明还提供一种使用本发明化合物制备药物组合物的方法，用于治疗异常情况，其中通过降低人类 Y5 受体的活性来缓解异常情况。
• TRIAZINE DERIVATIVES FOR USE AS SELECTIVE NPY (Y5) ANTAGONISTS
  申请人：H. LUNDBECK A/S

  公开号：EP1816127A1

  公开（公告）日：2007-08-08

  This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

  本发明涉及三嗪衍生物、双环化合物和三环化合物，它们是 NPY（Y5）受体的选择性拮抗剂。本发明提供了一种药物组合物，其中包含治疗有效量的本发明化合物和药学上可接受的载体。本发明提供了一种由治疗有效量的本发明化合物和药学上可接受的载体组合而成的药物组合物。本发明提供了一种制备药物组合物的工艺，该工艺包括将治疗有效量的本发明化合物与药学上可接受的载体相结合。本发明进一步提供了本发明化合物用于制备治疗异常的药物组合物的用途，其中通过降低人Y5受体的活性来缓解异常。
• 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。
• Assessment of neurons in the arcuate nucleus to screen for agents that modify feeding behavior
  申请人：Cowley Michael

  公开号：US20050015820A1

  公开（公告）日：2005-01-20

  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.

  本文公开了用于鉴定影响热量摄入、食物摄入、食欲和能量消耗的制剂的筛选方法。这些方法可用于鉴定治疗肥胖症或可用于减轻受试者体重的药物。这些方法还可用于确定治疗厌食症或恶病质的药物，并可用于增加食欲和增加受试者的体重和瘦体重。
• EP1499277A4
  申请人：——

  公开号：EP1499277A4

  公开（公告）日：2005-08-31