N-[5-(5-methylthiophen-2-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide | 1142937-06-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并吡啶类
• 英文名称: N-[5-(5-methylthiophen-2-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
• CAS: 1142937-06-1
• 化学式: C₁₅H₁₄N₄OS
• 分子量: 298.368
• InChiKey: KKVFPRYVGBLQHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  87.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] [1,2,4]TRIAZOLO[1,5-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS [1,2,4]TRIAZOLO[1,5-A]PYRIDINE ET [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE ET LEUR UTILISATION
  申请人：CANCER REC TECH LTD

  公开号：WO2009047514A1

  公开（公告）日：2009-04-16

  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.

  本发明一般涉及治疗化合物领域，更具体地涉及某些三唑化合物（以下简称为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，这些化合物等等，可以抑制AXL受体酪氨酸激酶功能。本发明还涉及包括这些化合物的药物组合物，以及使用这些化合物和组合物，无论是体外还是体内，来抑制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况，通过抑制AXL受体酪氨酸激酶功能得到缓解的疾病和病况等，包括增生性疾病如癌症等。
• [1,2,4]Triazolo[1,5-a]Pyridine and [1,2,4]Triazolo[1,5-c]Pyrimidine Compounds and Their Use
  申请人：Cancer Research Technology Limited

  公开号：US20140155594A1

  公开（公告）日：2014-06-05

  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的化合物。本发明还涉及包括这些化合物的制药组合物，以及使用这些化合物和组合物在体内外抑制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症，通过抑制AXL受体酪氨酸激酶功能得到缓解的疾病和病症，包括增生性疾病如癌症等。
• JAK KINASE INHIBITOR AND USE THEREOF
  申请人：Jiangsu Carephar Pharmaceutical Co., Ltd

  公开号：EP4011880A1

  公开（公告）日：2022-06-15

  The present invention discloses a JAK kinase inhibitor and use thereof. The JAK kinase inhibitor is a compound represented by formula (I) or a stereoisomer or tautomer thereof or a pharmaceutically acceptable salt thereof or a solvate or prodrug thereof. The present invention further provides the use of the compound of formula I of the present invention in preparation of drugs for preventing or treating JAK kinase-related diseases, especially in preparation of drugs for preventing and/or treating diseases involving cartilage degradation and bone and/or joint degradation, conditions involving inflammation or immune response, endotoxin-driven disease states, cancer, and organ transplantation rejection.

  本发明公开了一种JAK激酶抑制剂及其用途。JAK激酶抑制剂是由式（I）代表的化合物或其立体异构体或同系物或其药学上可接受的盐或其溶解物或原药。本发明进一步提供了本发明式I化合物在制备预防或治疗JAK激酶相关疾病的药物中的用途，特别是在制备预防和/或治疗涉及软骨退化和骨和/或关节退化的疾病、涉及炎症或免疫反应的病症、内毒素驱动的疾病状态、癌症和器官移植排斥反应的药物中的用途。
• [1,2,4]TRIAZOLO[1,5-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE COMPOUNDS AND THEIR USE
  申请人：Cancer Research Technology Limited

  公开号：EP2217578B9

  公开（公告）日：2014-09-10
• US8431596B2
  申请人：——

  公开号：US8431596B2

  公开（公告）日：2013-04-30