(R)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)n(2-hydroxyethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | 1260843-60-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: (R)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)n(2-hydroxyethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
• 英文别名: (R)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)-N-(2-hydroxyethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide；5-[(2R)-2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl]-N-(2-hydroxyethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
• CAS: 1260843-60-4
• 化学式: C₁₉H₂₁FN₆O₃
• 分子量: 400.413
• InChiKey: YLAKIDRGVDYWAA-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  105
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  (R)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)n(2-hydroxyethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide 、 盐酸 反应 16.0h， 生成 (R)-N-(2-chloroethyl)-5-(2-(5-fluoro-2-oxo-1,2-dihydropyridin-3-yl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
  参考文献：
  名称：

  MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS

  摘要：

  公式I的化合物和药物可接受的盐，其中环A、环B、W、m、D、R2、R2a、R3、R3a和Z的定义如此处所述，是Trk激酶的抑制剂，并且在治疗疼痛、癌症、炎症、神经退行性疾病和某些传染病方面很有用。

  公开号：

  US20130203776A1
• 作为产物：
  描述：

  (R)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxylic acid 、 O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 、 C.I.酸性橙108 在 acetonitrile-water 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 以to yield the product as white solid (95 mg, 85% yield)的产率得到(R)-5-(2-(5-fluoro-2-methoxypyridin-3-yl)pyrrolidin-1-yl)n(2-hydroxyethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
  参考文献：
  名称：

  MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS

  摘要：

  公式I的化合物和药物可接受的盐，其中环A、环B、W、m、D、R2、R2a、R3、R3a和Z的定义如此处所述，是Trk激酶的抑制剂，并且在治疗疼痛、癌症、炎症、神经退行性疾病和某些传染病方面很有用。

  公开号：

  US20130203776A1

文献信息

• [EN] SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS<br/>[FR] COMPOSÉS PYRAZOLO[1,5-A]PYRIMIDINES SUBSTITUÉES EN TANT QU'INHIBITEURS DES TRK KINASES
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2011006074A1

  公开（公告）日：2011-01-13

  Compounds of Formula (I) and salts thereof 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 such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

  式（I）的化合物及其盐，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，并且在治疗可以用Trk激酶抑制剂治疗的疾病中具有用处，如疼痛、癌症、炎症、神经退行性疾病和某些传染病。
• [EN] MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS<br/>[FR] COMPOSÉS MACROCYCLIQUES EN TANT QU'INHIBITEURS DE KINASE TRK
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2011146336A1

  公开（公告）日：2011-11-24

  Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

  式I的化合物及其药用可接受盐，其中环A、环B、W、m、D、R2、R2a、R3、R3a和Z按照定义，是Trk激酶的抑制剂，可用于治疗疼痛、癌症、炎症、神经退行性疾病和某些传染病。
• SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS
  申请人：Allen Shelley

  公开号：US20120108568A1

  公开（公告）日：2012-05-03

  Compounds of Formula (I) and salts thereof 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 such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

  式(I)的化合物及其盐，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，可用于治疗可以用Trk激酶抑制剂治疗的疾病，例如疼痛、癌症、炎症、神经退行性疾病和某些传染病。
• Substituted Pyrazolo [1,5-A] Pyrimidine Compounds as TRK Kinase Inhibitors
  申请人：Array BioPharma Inc.

  公开号：US20150031667A1

  公开（公告）日：2015-01-29

  Compounds of Formula I: and salts thereof 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 such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

  公式I的化合物及其盐，其中R1、R2、R3、R4、X、Y和n的含义如说明书所述，是Trk激酶的抑制剂，并可用于治疗可以用Trk激酶抑制剂治疗的疾病，如疼痛、癌症、炎症、神经退行性疾病和某些传染性疾病。
• Macrocyclic compounds as Trk kinase inhibitors
  申请人：Andrews Steven Wade

  公开号：US08933084B2

  公开（公告）日：2015-01-13

  Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

  化合物I的公式及其药物可接受的盐，其中环A、环B、W、m、D、R2、R2a、R3、R3a和Z的定义如本文所述，是Trk激酶的抑制剂，并可用于治疗疼痛、癌症、炎症、神经退行性疾病和某些传染病。