5-piperidin-4-yl-5,7-dihydro-6H-imidazo[4,5-c]pyridazin-6-one | 784155-46-0

• 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: 5-piperidin-4-yl-5,7-dihydro-6H-imidazo[4,5-c]pyridazin-6-one
• 英文别名: 5-piperidin-4-yl-7H-imidazo[4,5-c]pyridazin-6-one
• CAS: 784155-46-0
• 化学式: C₁₀H₁₃N₅O
• 分子量: 219.246
• InChiKey: DBNHKNBCHDGALZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  70.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  benzyl 4-(6-oxo-6,7-dihydro-5H-imidazo[4,5-c]pyridazin-5-yl)piperidine-1-carboxylate 在 钯 乙醇 作用下， 以 乙醇 为溶剂， 反应 16.0h， 以to afford the title compound (26 mg)的产率得到5-piperidin-4-yl-5,7-dihydro-6H-imidazo[4,5-c]pyridazin-6-one
  参考文献：
  名称：

  CGRP receptor antagonists

  摘要：

  本发明涉及以下式子的化合物：式子I和式子II：（其中变量R1，R2，R3，R4，A，B，G，J，Q，T，U，V，W，X和Y的定义如本文所述），这些化合物可用作CGRP受体的拮抗剂，并且可用于治疗或预防CGRP参与的疾病，例如头痛、偏头痛和群头痛。本发明还涉及包含这些化合物的制药组合物以及在预防或治疗CGRP参与的这些疾病中使用这些化合物和组合物的用途。

  公开号：

  US07893052B2

文献信息

• Cgrp Receptor Antagonists
  申请人：Paone V. Daniel

  公开号：US20080090806A1

  公开（公告）日：2008-04-17

  The present invention is directed to compounds of Formula (I) and Formula (II) (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

  本发明涉及式（I）和式（II）化合物（其中变量R1、R2、R3、R4、A、B、G、J、Q、T、U、V、W、X和Y的定义如本文所述），其作为CGRP受体拮抗剂在治疗或预防CGRP参与的疾病，如头痛、偏头痛和集群性头痛中有用。本发明还涉及包含这些化合物的制药组合物以及这些化合物和组合物在预防或治疗CGRP参与的这些疾病中的使用。
• CGRP RECEPTOR ANTAGONISTS
  申请人：Paone Daniel Vincent

  公开号：US20100298303A1

  公开（公告）日：2010-11-25

  The present invention is directed to compounds of Formula I: and Formula II: (where variables R 1 , R 2 , R 3 , R 4 , A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

  本发明涉及式I和式II的化合物：（其中变量R1，R2，R3，R4，A，B，G，J，Q，T，U，V，W，X和Y如本文所定义），其作为CGRP受体拮抗剂在治疗或预防CGRP参与的疾病，如头痛、偏头痛和集群头痛中具有用途。本发明还涉及包含这些化合物的制药组合物以及在预防或治疗CGRP参与的这些疾病中使用这些化合物和组合物的用途。
• [EN] IMIDAZOBENZAZEPINE CGRP RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DE RÉCEPTEURS DE CGRP DE TYPE IMIDAZOBENZAZÉPINE
  申请人：MERCK & CO INC

  公开号：WO2009105348A1

  公开（公告）日：2009-08-27

  Compounds of Formula I: I (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.

  公式I的化合物：I（其中变量R1A、R1B、R2、R3、R4、A和Z的定义如本文所述）可用作CGRP受体的拮抗剂，对于治疗或预防CGRP受体参与的疾病，例如头痛，特别是偏头痛和集群头痛非常有用。本发明还涉及包含这些化合物的制药组合物以及这些化合物和组合物在预防或治疗CGRP受体参与的这些疾病中的使用。
• US6953790B2
  申请人：——

  公开号：US6953790B2

  公开（公告）日：2005-10-11
• US7235545B2
  申请人：——

  公开号：US7235545B2

  公开（公告）日：2007-06-26