N-[4-(4-methyl-1-piperazinyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine | 551919-93-8

• 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: N-[4-(4-methyl-1-piperazinyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine
• 英文别名: N-(4-(4-methylpiperazin-1-yl)phenyl)-4-(pyrazolo[1,5-b]pyridazin-3-yl)pyrimidin-2-amine；N-[4-(4-methylpiperazin-1-yl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine
• CAS: 551919-93-8
• 化学式: C₂₁H₂₂N₈
• 分子量: 386.459
• InChiKey: AUAUBVTWWCYNPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  74.5
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-(Dimethylamino)-1-pyrazolo[1,5-b]pyridazin-3-ylprop-2-en-1-one 、 1-(4-(4-甲基哌嗪-1-基)苯基)胍 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 N-[4-(4-methyl-1-piperazinyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine
  参考文献：
  名称：

  Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors

  摘要：

  A novel series of pyrazolo[1,5-b]pyridazines have been synthesized and identified as cyclin dependant kinase inhibitors potentially useful for the treatment of solid tumors. Modification of the hinge-binding amine or the C(2)- and C(6)-substitutions on the pyrazolopyridazine core provided potent inhibitors of CDK4 and demonstrated enzyme selectivity against VEGFR-2 and GSK3beta.

  DOI：

  10.1016/j.bmcl.2008.09.069

文献信息

• [EN] PYRADAZINE COMPOUNDS AS GSK-3 INHIBITORS<br/>[FR] COMPOSES DE PYRADAZINE UTILES COMME INHIBITEURS DE GSK-3
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2004035588A1

  公开（公告）日：2004-04-29

  The present invention relates generally to inhibitors of the kinases, such as GSK3, and more particularly to fused pyradazine compounds according to formula (I) and methods of their use.

  本发明通常涉及激酶抑制剂，如GSK3，更具体地涉及根据式(I)的融合吡啶并嘧啶化合物及其使用方法。
• [EN] PYRAZOLOPARIDAZINE DERIVATIVES<br/>[FR] DERIVES DE PYRAZOLOPARIDAZINE
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2003051886A1

  公开（公告）日：2003-06-26

  Fused pyradazine derivatives, which are useful as CDK inhibitors are described herein. The described invention also includes methods of making such fused pyradazines derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

  本文描述了作为CDK抑制剂有用的融合吡嗪衍生物。所述发明还包括制备这种融合吡嗪衍生物的方法，以及将其用于治疗增生性疾病的方法。
• Pyradazine compounds as gsk-3 inhibitors
  申请人：Dickerson Howard Scott

  公开号：US20060069097A1

  公开（公告）日：2006-03-30

  The present invention relates generally to inhibitors of the kinases, such as GSK3, and more particularly to fused pyradazine compounds and methods of their use.

  本发明通常涉及抑制激酶的抑制剂，例如GSK3，更具体地涉及融合嘧啶二氮杂环化合物及其使用方法。
• Meloxicam compositions
  申请人：Kanbe Hideyoshi

  公开号：US20050038018A1

  公开（公告）日：2005-02-17

  A pharmaceutical composition comprising: (a) meloxicam or a pharmaceutically acceptable salt thereof; and (b) one or more additional pharmaceutically active compounds selected from antacids, sedatives, and central nervous system stimulants, and the use of such composition of an inflammatory disease, symptoms of an inflammatory disease, including various symptoms thereof, and/or headache, toothache, ache after tooth extraction, sore throat, otalgia, arthralgia, neuralgia, lumbago, myalgia, muscle stiffness of shoulder, pain of contusion, pain of fracture, pain of sprain, menstrual pain, traumatic pain, chill, exothermic reaction and/or cold and various symptoms of cold such as sore throat, chill, pyrexia, headache, arthralgia and muscle pain.

  一种药物组合物，包括(a) 美洛昔康或其药学上可接受的盐；和(b) 一种或多种选自抗酸剂、镇静剂和中枢神经系统兴奋剂的附加药学活性化合物，以及使用这种组合物治疗炎症性疾病、炎症性疾病的症状（包括其各种症状）和/或头痛、牙痛、拔牙后疼痛、咽喉痛、耳痛、关节痛、神经痛、腰痛、肌痛、咽喉痛、耳痛、关节痛、神经痛、腰痛、肌痛、肩部肌肉僵硬、挫伤痛、骨折痛、扭伤痛、痛经、外伤痛、畏寒、放热反应和/或感冒以及感冒的各种症状，如咽喉痛、畏寒、发热、头痛、关节痛和肌肉痛。
• Pyrazolopyridazine derivatves
  申请人：Badiang G Jennifer

  公开号：US20050090507A1

  公开（公告）日：2005-04-28

  Fused pyradazine derivatives, which are useful as CDK inhibitors are described herein. The described invention also includes methods of making such fused pyradazines derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

  本文描述了可用作 CDK 抑制剂的融合哒嗪衍生物。所描述的发明还包括制造这种融合哒嗪衍生物的方法，以及将其用于治疗过度增殖性疾病的方法。