N-[3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]methanesulfonamide | 1257705-22-8

• 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: N-[3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]methanesulfonamide
• 英文别名: N-[3-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)-phenyl]-methanesulfonamide
• CAS: 1257705-22-8
• 化学式: C₁₃H₁₃N₅O₂S
• 分子量: 303.345
• InChiKey: PQFVZIJDKBFNRR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  111
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  5-溴-[1,2,4]三噻唑[1,5-A]吡啶-2-胺 、 3-甲磺酰氨基苯硼酸 在 N-[3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]methanesulfonamide 、 silica gel 作用下， 以N-[3-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)-phenyl]-methanesulfonamide (461 mg, 18%) was isolated as a beige powder的产率得到N-[3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]methanesulfonamide
  参考文献：
  名称：

  Preparation and Uses of 1,2,4-Triazolo [1,5a] Pyridine Derivatives

  摘要：

  本申请涉及通式I的化合物及其盐，其中X、R1A、R1B、R2、R3、R4和R5的定义如本文所述。该申请还涉及治疗过度增殖性疾病或疾病的组合物和方法。

  公开号：

  US20100311693A1
• 作为试剂：
  描述：

  5-溴-[1,2,4]三噻唑[1,5-A]吡啶-2-胺 、 3-甲磺酰氨基苯硼酸 在 N-[3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]methanesulfonamide 、 silica gel 作用下， 以N-[3-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)-phenyl]-methanesulfonamide (461 mg, 18%) was isolated as a beige powder的产率得到N-[3-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]methanesulfonamide
  参考文献：
  名称：

  Preparation and Uses of 1,2,4-Triazolo [1,5a] Pyridine Derivatives

  摘要：

  该应用程序部分涉及一般式I化合物和/或其盐，其中X、R1A、R1B、R2、R3、R4和R5的定义如本文所述。该应用程序还涉及组合物和方法，用于抑制至少在有需要的患者中的JAK2，以治疗需要抑制至少JAK2的疾病或疾病。

  公开号：

  US20130296312A1

文献信息

• TRIAZOLE DERIVATIVES AS KINASE INHIBITORS
  申请人：Wilson Francis

  公开号：US20100227800A1

  公开（公告）日：2010-09-09

  The invention relates to compounds of formula (I); wherein X and R 1 to R 5 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

  本发明涉及式(I)的化合物；其中X和R1至R5的含义如所述及权利要求中所述。所述化合物可用作蛋白激酶抑制剂，特别是Itk或PI3K的抑制剂，用于治疗或预防免疫、炎症或过敏性疾病。本发明还涉及包括所述化合物的制药组合物，以及制备这些化合物的方法以及作为药物的生产和使用。
• Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
  申请人：Curry Matthew A.

  公开号：US08501936B2

  公开（公告）日：2013-08-06

  This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.

  本申请涉及一般式I的化合物及其盐，其中X、R1A、R1B、R2、R3、R4和R5的定义如本文所述。本申请还涉及治疗过度增殖性疾病或障碍的组合物和方法。
• [1,2,4]Triazolo[1,5-a]Pyridine and [1,2,4]Triazolo[1,5-c]Pyrimidine Compounds and Their Use
  申请人：Pavé Grégoire Alexandre

  公开号：US20100298339A1

  公开（公告）日：2010-11-25

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.

  本发明涉及治疗化合物领域，更具体地涉及某些三唑化合物（在此称为TAZ化合物），特别是某些[1,2,4]三唑并[1,5-a]吡啶和[1,2,4]三唑并[1,5-c]嘧啶化合物，其中包括抑制AXL受体酪氨酸激酶功能。本发明还涉及包含这种化合物的制药组合物，以及使用这种化合物和组合物在体内和体外抑制AXL受体酪氨酸激酶功能，并用于治疗由AXL受体酪氨酸激酶介导的疾病和病情，这些疾病和病情可以通过抑制AXL受体酪氨酸激酶功能得到改善，包括癌症等增殖性疾病。
• Triazole derivatives as kinase inhibitors
  申请人：CELLZOME AG

  公开号：EP1894931A1

  公开（公告）日：2008-03-05

  The invention relates to compounds of formula (I) wherein X and R1 to R5 have the meaning as cited in the description and the claims. Said compounds are useful as Itk protein kinase inhibitors for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

  本发明涉及式 (I) 的化合物 其中 X 和 R1 至 R5 具有在说明书和权利要求书中引用的含义。所述化合物可作为 Itk 蛋白激酶抑制剂用于治疗或预防免疫性、炎症性或过敏性疾病。本发明还涉及包括上述化合物的药物组合物、此类化合物的制备以及作为药物的生产和使用。
• PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a]PYRIDINE DERIVATIVES
  申请人：Cephalon, Inc.

  公开号：EP2438066A2

  公开（公告）日：2012-04-11