N-(pyridin-2-yl)pyrazin-2-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N-(pyridin-2-yl)pyrazin-2-amine
• 英文别名: N-2-pyridinyl-2-pyrazinamine；N-pyridin-2-ylpyrazin-2-amine
• 化学式: C₉H₈N₄
• 分子量: 172.189
• InChiKey: GOYIJZBEFGZUSR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(pyridin-2-yl)pyrazin-2-amine 在 盐酸羟胺 、 sodium hydride 、 potassium hydroxide 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 22.33h， 生成 N-hydroxy-4-((pyrazin-2-yl(pyridin-2-yl)amino)methyl)benzamide
  参考文献：
  名称：

  [EN] NOVEL HISTONE DEACETYLASE INHIBITORS
  [FR] NOUVEAUX INHIBITEURS DE L'HISTONE DÉSACÉTYLASE

  摘要：

  本发明是该化合物的化合物或其药学上可接受的盐。这些化合物可用作HDAC抑制剂。

  公开号：

  WO2014181137A1
• 作为产物：
  描述：

  2-溴吡啶 、 氨基吡嗪 在 tris-(dibenzylideneacetone)dipalladium(0) 、 potassium tert-butylate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 作用下， 以 甲苯 为溶剂， 反应 30.0h， 以83%的产率得到N-(pyridin-2-yl)pyrazin-2-amine
  参考文献：
  名称：

  [EN] NOVEL HISTONE DEACETYLASE INHIBITORS
  [FR] NOUVEAUX INHIBITEURS DE L'HISTONE DÉSACÉTYLASE

  摘要：

  本发明是该化合物的化合物或其药学上可接受的盐。这些化合物可用作HDAC抑制剂。

  公开号：

  WO2014181137A1

文献信息

• [EN] OXADIAZOLYLTHIOPHENE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS<br/>[FR] DÉRIVÉS D'OXADIAZOLYLTHIOPHÈNE À UTILISER EN TANT QU'INHIBITEURS DE L'HISTONE DÉSACÉTYLASE
  申请人：KARUS THERAPEUTICS LTD

  公开号：WO2019166824A1

  公开（公告）日：2019-09-06

  A compound of Formula I : (I) or a pharmaceutically acceptable salt thereof, wherein: each R' is QR1; each Q is independently selected from a bond, -C1-C10 alkylene, -C2-C10 alkenylene, -C(O)-, -C(O)O-, -C(O)N(R1)-, -C(O)N(R1)SO2- -N(R1)C(O)-, - N(R1)-, -N(SO2(R1)), -N(R1)SO2- -C(O)NR4R5-, -N(R4R5)C(O)-, -N(R4R5)- - S-, -SO-, -SO2-, -S(O)O-, -SO2N(R1)- and -O-; each R1 is independently selected from H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C1-C10 haloalkyl, C1-C10 heteroalkyl, aryl, heteroaryl, C3-C10 cycloalkyl, -(C1-C10 alkylene)-C3-C10 cycloalkyl, halogen, cyano, C1-C10 alkylene- aryl, C1-C10 alkylene heteroaryl, C1-C10 heterocycloalkyl and -(C1-C10 alkylene)- C1-C10 heterocycloalkyl. The compounds are inhibitors of HDAC and therefore have potential utility in the therapy of a number of conditions including cancer and inflammation.

  一种Formula I的化合物：(I)或其药学上可接受的盐，其中：每个R'是QR1；每个Q独立地选自键，-C1-C10烷基，-C2-C10烯基，-C(O)-，-C(O)O-，-C(O)N(R1)-，-C(O)N(R1)SO2-，-N(R1)C(O)-，-N(R1)-，-N(SO2(R1))，-N(R1)SO2-，-C(O)NR4R5-，-N(R4R5)C(O)-，-N(R4R5)-，-S-，-SO-，-SO2-，-S(O)O-，-SO2N(R1)-和-O-；每个R1独立地选自H，C1-C10烷基，C2-C10烯基，C2-C10炔基，C1-C10卤代烷基，C1-C10杂原子烷基，芳基，杂芳基，C3-C10环烷基，-(C1-C10烷基)-C3-C10环烷基，卤素，氰基，C1-C10烷基-芳基，C1-C10烷基-杂原子芳基，C1-C10杂环烷基和-(C1-C10烷基)-C1-C10杂环烷基。这些化合物是HDAC的抑制剂，因此在治疗包括癌症和炎症在内的多种疾病中具有潜在用途。
• [EN] BICYCLYLARYL-ARYL-AMINE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS DE TYPE BICYCLYLARYL-ARYL-AMINE ET LEUR UTILISATION
  申请人：CANCER REC TECH LTD

  公开号：WO2009103966A1

  公开（公告）日：2009-08-27

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) 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 CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation: (I).

  本发明一般涉及治疗化合物领域，更具体地涉及以下式（以下简称BCAA化合物）的某些双环芳基芳基胺化合物，该化合物在某些情况下抑制检查点激酶1（CHK1）激酶功能。本发明还涉及包含这种化合物的药物组合物，以及利用这种化合物和组合物在体内外抑制CHK1激酶功能，并用于治疗由CHK1介导的疾病和症状，通过抑制CHK1激酶功能得到缓解等，包括增殖性疾病如癌症等，可选地与另一药剂组合使用，例如，（a）DNA拓扑异构酶I或II抑制剂；（b）DNA损伤剂；（c）抗代谢物或TS抑制剂；（d）微管靶向药物；和（e）电离辐射。
• [EN] PYRAZIN-2-YL-PYRIDIN-2-YL-AMINE AND PYRAZIN-2-YL-PYRIMIDIN-4-YL-AMINE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS PYRAZIN-2-YL-PYRIDIN-2-YL-AMINE ET PYRAZIN-2-YL-PYRIMIDIN-4-YL-AMINE ET LEURS UTILISATIONS
  申请人：CANCER REC TECH LTD

  公开号：WO2009044162A1

  公开（公告）日：2009-04-09

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin- 2 - yl -pyridin- 2 -yl -amine and pyrazine - 2 - yl -pyrimidin- 4 - yl -amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1 ) 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 CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1. that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or Il inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisiπq radiation. wherein: -X= is independently -CRA5= or -N=; and the rest of the substituents are as specified in the claims.

  本发明一般涉及治疗化合物领域，更具体地涉及某些联苯胺化合物（在此称为BAA化合物），特别是某些式（I）的吡啶-2-基-吡啶-2-基-胺和吡嗪-2-基-吡啶-4-基-胺化合物，该化合物等抑制检查点激酶1（CHK1）激酶功能。本发明还涉及包含这种化合物的药物组合物，以及利用这种化合物和组合物在体外和体内抑制CHK1激酶功能，并治疗由CHK1介导的疾病和症状，通过抑制CHK1激酶功能而得到缓解的疾病和症状，包括增生性疾病如癌症等，可选择与另一药剂结合，例如，（a）DNA拓扑异构酶I或II抑制剂；（b）DNA损伤剂；（c）抗代谢物或TS抑制剂；（d）微管靶向剂；和（e）电离辐射。其中：-X=独立为-CRA5=或-N=；其余取代基如索引中所述。
• [EN] COMBINATIONS COMPRISING HISTONE DEACETYLASE INHIBITORS<br/>[FR] ASSOCIATIONS COMPRENANT DES INHIBITEURS D'HISTONE DÉSACÉTYLASE
  申请人：KARUS THERAPEUTICS LTD

  公开号：WO2017208032A1

  公开（公告）日：2017-12-07

  The invention relates to a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and at least one second agent selected from the group consisting of proteasome inhibitors, tumour immunotherapeutics or immunomodulatory agents, signal transduction pathway inhibitors, agents inhibiting the BCL2 family of proteins, agents inhibiting Mcl-1, poly (ADP-ribose) polymerase (PARP) Inhibitors, aromatase inhibitors, conventional cytotoxic agents or a miscellaneous agent selected from abiraterone, ARN-509 and MYC inhibitors.

  该发明涉及公式(I)的化合物或其药用可接受的盐，以及来自蛋白酶体抑制剂、肿瘤免疫治疗剂或免疫调节剂、信号传导途径抑制剂、抑制BCL2蛋白家族的药剂、抑制Mcl-1的药剂、聚(ADP-核糖)聚合酶（PARP）抑制剂、芳香化酶抑制剂、传统细胞毒剂或从阿比特龙、ARN-509和MYC抑制剂中选择的其他药剂中至少一种第二药剂的组合。
• [EN] NOVEL HISTONE DEACETYLASE INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE L'HISTONE DÉSACÉTYLASE
  申请人：KARUS THERAPEUTICS LTD

  公开号：WO2014181137A1

  公开（公告）日：2014-11-13

  The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors.

  本发明是该化合物的化合物或其药学上可接受的盐。这些化合物可用作HDAC抑制剂。