5-Amino-2-(2-furyl)-7-(4-(3-hydroxy-3-methylbutyl)piperazinyl)[1,2,4]triazolo[1,5-c]pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 5-Amino-2-(2-furyl)-7-(4-(3-hydroxy-3-methylbutyl)piperazinyl)[1,2,4]triazolo[1,5-c]pyrimidine
• 英文别名: 4-[4-[5-Amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]pyrimidin-7-yl]piperazin-1-yl]-2-methylbutan-2-ol
• 化学式: C₁₈H₂₅N₇O₂
• 分子量: 371.442
• InChiKey: OWXDAQGBLGQRBA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  109
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• THERAPEUTIC AGENT FOR MIGRAINE
  申请人：Ikeda Junichi

  公开号：US20110183992A1

  公开（公告）日：2011-07-28

  Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A 2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A 2A receptor antagonistic activity, which has an affinity for the adenosine A 2A receptor 10 times or higher than that for the adenosine A 1 receptor, or a pharmaceutically acceptable salt thereof; and the like.

  提供了治疗和/或预防偏头痛的药物，其作为活性成分包含具有选择性腺苷A2A受体拮抗活性的化合物或其药学上可接受的盐；作为活性成分包含具有选择性腺苷A2A受体拮抗活性的化合物的治疗和/或预防偏头痛药物，其与腺苷A1受体相比具有10倍或更高的亲和力，或其药学上可接受的盐；等等。
• [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP1116722A1

  公开（公告）日：2001-07-18

  [1,2,4]Triazolo[1,5-c]pyrimidine derivatives represented by the general formula (I) or pharmacologically acceptable salts thereof which show adenosine A2A receptor antogonism, wherein R1 represents heteroaryl, etc.; R2 represents hydrogen, etc.; na and nb represent each an integer of 0 to 4; Q represents hydrogen, etc.; R4 and R5 represent each lower alkyl or aryl, or R4 form together with the adjacent carbon atom a saturated carbon ring when R3 is any of (i) to (iii); or R4 represent each hydrogen, lower alkyl or aryl, or R4 and R5 form together with the adjacent carbon atom a saturated carbon ring when R3 is (iv).

  通式（I）代表的[1,2,4]三唑并[1,5-c]嘧啶衍生物 或其药理上可接受的盐类，具有腺苷 A2A 受体拮抗作用，其中 R1 代表杂芳基等；R2 代表氢等；na 和 nb 分别代表 0 至 4 的整数；Q 代表氢等。当 R3 为(i)至(iii)中的任一项时，R4 和 R5 各自代表低级烷基或芳基，或 R4 与相邻碳原子一起形成饱和碳环；或当 R3 为(iv)时，R4 各自代表氢、低级烷基或芳基，或 R4 和 R5 与相邻碳原子一起形成饱和碳环。
• PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR MOTOR DISORDER
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP1902716A1

  公开（公告）日：2008-03-26

  For example, an agent for preventing and/or treating movement disorder comprising, as an active ingredient, a triazolopyrimidine derivative having an adenosine A2A receptor antagonistic action, which is represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, R2 represents a hydrogen atom, or the like, R3 represents -WR4, or the like, and Q1 represents a hydrogen atom or 3,4-dimethoxybenzyl), or a pharmaceutically acceptable salt thereof, and the like are provided.

  例如，一种用于预防和/或治疗运动障碍的制剂，其活性成分包括具有腺苷 A2A 受体拮抗作用的三唑并嘧啶衍生物，该衍生物由下式（I）表示： (其中R1代表取代或未取代的芳基或取代或未取代的杂环基团，R2代表氢原子或类似物，R3代表-WR4或类似物，Q1代表氢原子或3,4-二甲氧基苄基），或其药学上可接受的盐等。
• A2A antagonists for use in the treatment of motor disorders
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP2258372A1

  公开（公告）日：2010-12-08

  For example, an agent for preventing and/or treating movement disorder comprising, as an active ingredient, a triazolopyrimidine derivative having an adenosine A2A receptor antagonistic action, which is represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, R2 represents a hydrogen atom, or the like, R3 represents -WR4, or the like, and Q1 represents a hydrogen atom or 3,4-dimethoxybenzyl), or a pharmaceutically acceptable salt thereof, and the like are provided.

  例如，一种用于预防和/或治疗运动障碍的制剂，其活性成分包括具有腺苷 A2A 受体拮抗作用的三唑并嘧啶衍生物，该衍生物由下式（I）表示： (其中R1代表取代或未取代的芳基或取代或未取代的杂环基团，R2代表氢原子或类似物，R3代表-WR4或类似物，Q1代表氢原子或3,4-二甲氧基苄基），或其药学上可接受的盐等。
• A METHOD OF TREATING AN ANXIETY DISORDER
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP1631294B1

  公开（公告）日：2010-09-15