(R)-N-(6-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)-4-(methylsulfonamido)benzamide | 1218934-92-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (R)-N-(6-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)-4-(methylsulfonamido)benzamide
• 英文别名: Imidazo[1,2-b]pyridazine derivative 7；N-[6-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]-4-(methanesulfonamido)benzamide
• CAS: 1218934-92-9
• 化学式: C₂₄H₂₂F₂N₆O₃S
• 分子量: 512.54
• InChiKey: CDMQMPKUGUVGIR-HXUWFJFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  36
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  117
• 氢给体数：
  2
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  (R)-6-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-amine 、 4-甲磺酰氨基苯甲酸 在 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.17h， 以27%的产率得到(R)-N-(6-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazin-3-yl)-4-(methylsulfonamido)benzamide
  参考文献：
  名称：

  [EN] SUBSTITUTED IMIDAZO[1,2B]PYRIDAZINE COMPOUNDS AS TRK KINASE INHIBITORS
  [FR] COMPOSÉS IMIDAZO[1,2B]PYRIDAZINE SUBSTITUÉS COMME INHIBITEURS DE KINASES TRK

  摘要：

  式（I）化合物：其中R1、R2、R3、R4、X、Y和n的含义如规范中所述，是Trk激酶的抑制剂，并且在治疗可以使用Trk激酶抑制剂治疗的疾病中是有用的。

  公开号：

  WO2010033941A1

文献信息

• SUBSTITUTED IMIDAZO[1,2b]PYRIDAZINE COMPOUNDS AS TRK KINASE INHIBITORS
  申请人：Andrews Steven W.

  公开号：US20110166122A1

  公开（公告）日：2011-07-07

  Compounds of Formula (I): in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

  式(I)的化合物：其中R1、R2、R3、R4、X、Y和n具有规范中给出的含义，是Trk激酶的抑制剂，可用于治疗可用Trk激酶抑制剂治疗的疾病。
• METHOD OF TREATMENT USING SUBSTITUTED IMIDAZO[1,2B]PYRIDAZINE COMPOUNDS
  申请人：Andrews Steven W.

  公开号：US20130217662A1

  公开（公告）日：2013-08-22

  Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification.

  治疗哺乳动物中的疾病或紊乱的方法，包括疼痛、癌症、炎症、神经退行性疾病、克鲁兹锥虫感染和骨溶解病，其包括向该哺乳动物投与公式I中R1、R2、R3、R4、X、Y和n在说明书中所给定的含义下的化合物的治疗有效量。
• Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
  申请人：Andrews Steven D.

  公开号：US08450322B2

  公开（公告）日：2013-05-28

  Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

  式(I)的化合物：其中R1、R2、R3、R4、X、Y和n具有规范中给出的含义，是Trk激酶的抑制剂，并且可用于治疗可以用Trk激酶抑制剂治疗的疾病。
• Method of Treatment Using Substituted Imidazo[1,2b]Pyridazine Compounds
  申请人：Array BioPharma, Inc.

  公开号：US20160251357A1

  公开（公告）日：2016-09-01

  Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification.

  治疗哺乳动物中的疾病或障碍的方法，包括疼痛、癌症、炎症、神经退行性疾病、克鲁茨菌感染和骨溶解疾病，其中包括向该哺乳动物投与有效治疗剂量的I型化合物，其中R1，R2，R3，R4，X，Y和n的含义在规范中给出。
• Method of treatment using substituted imidazo[1,2B]pyridazine compounds
  申请人：Andrews Steven W.

  公开号：US09227975B2

  公开（公告）日：2016-01-05

  Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.

  本发明提供了一种治疗哺乳动物中所选疾病或障碍（包括疼痛、癌症、炎症、神经退行性疾病、克鲁兹锥虫感染和溶骨性疾病）的方法，其包括向该哺乳动物施用化合物I的治疗有效量，其中化合物I的R1、R2、R3、R4、X、Y和n的含义如规范中所示。