[1,2,4]Triazolo[4,3-b]pyridazine | 274-83-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并哒嗪类
• 英文名称: [1,2,4]Triazolo[4,3-b]pyridazine
• 英文别名: s-Triazolo<4,3-b>pyridazin；s-triazolo<4,3-b>pyridazine；1,2,4-Triazolo[4,3-b]pyridazine
• CAS: 274-83-9
• 化学式: C₅H₄N₄
• 分子量: 120.114
• InChiKey: YRACHDVMKITFAZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  43.1
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  [1,2,4]Triazolo[4,3-b]pyridazine 在 氢溴酸 作用下， 以 溶剂黄146 为溶剂， 反应 27.0h， 生成 3-Morpholino-<1,2,4>triazolo<4,3-b>pyridazin
  参考文献：
  名称：

  Kosary, Judit; Gabanyi, Zoltan, Chemische Berichte, 1983, vol. 116, # 10, p. 3513 - 3515

  摘要：

  DOI：
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 phosphate buffer 、 immobilized α-chymotrypsin 作用下， 反应 72.0h， 以39%的产率得到[1,2,4]三唑并[4,3-b]哒嗪-3-羧酸
  参考文献：
  名称：

  Kosary, Judit, ACH - Models in Chemistry, 2000, vol. 137, # 4, p. 451 - 454

  摘要：

  DOI：

文献信息

• Metal free [4+1] and [5+1] annulation reactions to prepare heterocycles using DMF and its derivatives as one-carbon source
  作者：Yiwen Xu、Bei Shen、Lingfeng Liu、Chunhua Qiao

  DOI：10.1016/j.tetlet.2020.151844

  日期：2020.5

  in a variety of pharmaceutical and agrochemical agents. Herein, we report a highly efficient and practical method using DMF and its derivative for the [4+1] and [5+1] annulation reactions to prepare these heterocycles. This metal free reaction takes advantages of shelf stable DMF as solvent and carbon donor, imidazole chloride as catalyst, the mild reaction condition tolerates a broad substrate range

  1,2,4-三唑并[3,4- a ]吡啶和相关的杂环以及取代的三嗪是在各种药物和农用化学试剂中普遍发现的支架。在这里，我们报告了一种高效且实用的方法，该方法使用DMF及其衍生物进行[4 + 1]和[5 + 1]环化反应，以制备这些杂环。这种无金属的反应利用了贮存稳定的DMF作为溶剂和碳供体，使用咪唑氯化物作为催化剂的优势，温和的反应条件可耐受广泛的底物范围并替代。制备的3-未取代的1,2,4-三唑并[3,4- a ]吡啶和衍生物允许在3-位进一步引入各种官能团。
• Protein Kinase Inhibitors (Variants), Use Thereof in Treating Oncological Diseases and a Pharmaceutical Composition Based Thereon
  申请人：Obshchestvo s ogranichennoy otvetstvennostyou "Fusion Pharma"

  公开号：US20140213592A1

  公开（公告）日：2014-07-31

  The present invention relates to the treatment of oncological, chronic inflammatory and similar diseases with the aid of new families of chemical compounds having improved efficiency with regard to the inhibition of Abl kinase and mutant forms thereof, as well as other therapeutically significant kinases. It describes protein kinase inhibitors in the form of compounds of general formula (I) and compounds of general formula (II), or a tautomer, an individual isomer, a mixture of isomers, a pharmaceutically acceptable salt, a solvate or a hydrate thereof.

  本发明涉及使用新的化学化合物家族辅助治疗肿瘤、慢性炎症和类似疾病，这些化合物家族在抑制Abl激酶及其突变形式以及其他具有治疗意义的激酶方面具有提高的效率。本发明描述了蛋白激酶抑制剂，其形式为通式(I)和通式(II)的化合物，或其互变异构体、单个异构体、异构体混合物、药学上可接受的盐、溶剂或其水合物。
• 6-triazolopyridazine sulfanyl benzothiazole derivatives as MET inhibitors
  申请人：Albert Eva

  公开号：US08546393B2

  公开（公告）日：2013-10-01

  The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.

  本公开涉及式(I)的化合物：其中，A，W，X和Ra如本公开所定义，以及其盐，以及包含该化合物的制药组合物，制备它们的过程以及它们作为药物的用途，特别是作为MET抑制剂。
• NOVEL 6-TRIAZOLOPYRIDAZINESULFANYL BENZOTHIAZOLE AND BENZIMIDAZOLE DERIVATIVES, METHOD FOR PRODUCTION THEREOF AND APPLICATION AS MEDICAMENTS AND PHARMNACEUTICAL COMPOSITIONS AND NOVEL USE AS MET INHIBITORS
  申请人：ALBERT Eva

  公开号：US20100298315A1

  公开（公告）日：2010-11-25

  The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.

  本公开涉及式(I)的化合物：其中，A、W、X和Ra如本公开所定义，以及其盐，以及包含所述化合物的制药组合物，制备它们的过程以及它们作为药物的用途，特别是作为MET抑制剂。
• PROTEIN KINASE INHIBITORS (VARIANTS), USE THEREOF IN TREATING ONCOLOGICAL DISEASES AND A PHARMACEUTICAL COMPOSITION BASED THEREON
  申请人：Obshchestvo S Ogranichennoy Otvetstvennostyou "Fusion Pharma"

  公开号：EP2743266B8

  公开（公告）日：2016-09-28

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