2-(4-(pyridin-4-yl)-1H-pyrazol-3-yl)pyridine | 1333492-57-1

• 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: 2-(4-(pyridin-4-yl)-1H-pyrazol-3-yl)pyridine
• 英文别名: 2-(4-pyridin-4-yl-1H-pyrazol-5-yl)pyridine
• CAS: 1333492-57-1
• 化学式: C₁₃H₁₀N₄
• 分子量: 222.249
• InChiKey: BBCZFQGWUUVLBW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-吡啶甲酸乙酯 在 palladium 10% on activated carbon 、 氢气 、 双(三甲基硅烷基)氨基钾 、 一水合肼 、 溶剂黄146 、 sodium hydroxide 作用下， 以 四氢呋喃 、 水 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 26.08h， 生成 2-(4-(pyridin-4-yl)-1H-pyrazol-3-yl)pyridine
  参考文献：
  名称：

  2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-β1 and activin A signalling

  摘要：

  Novel inhibitors of TGF-beta 1 and activin A signalling based on a 2-aryl-4-(3-(pyridin-2-yl)-1H-pyrazol-4yl) pyridine pharmacophore have been synthesised. Compounds containing phenyl or aromatic nitrogen heterocycle substituents inhibited both types of signalling with HEK-293T cells in culture, with a selectivity preference for TGF-beta 1. Synthetic compounds containing pyridin-3-yl, pyrazol-4-yl, pyrazol-1-yl or 1H-imidazoyl-1-yl substituents exhibited structural and functional attributes suitable for further investigation related to the development of more potent TGF-beta inhibitors. (C) 2011 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2010.12.120

文献信息

• ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES
  申请人：Synthis, LLC

  公开号：US20200147234A1

  公开（公告）日：2020-05-14

  The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.

  本公开涉及包含ALK5抑制剂的抗体药物偶联物及其用途。
• Compounds and methods for selectively targeting tumor-associated mucins
  申请人：Barbeau Donald L.

  公开号：US20120022016A1

  公开（公告）日：2012-01-26

  The present invention relates to pharmaceutical compositions containing tumor-selective targeted inhibitor glycoconjugates. These bioconjugates are ALK5 inhibitors covalently bound to biocompatible carrier molecules which selectively target and specifically bind to Muc4 that is overexpressed on a variety of tumor cell types. The ALK5 inhibitors are conjugated to tumor targetable glycans through a covalent linker. Preferably the acid-labile linker is designed to be stable in plasma and releases pharmacologically active inhibitors through acid-catalyzed hydrolysis in the acidic environment of the target tumor where the inhibitor activity is restored. Because the glycoconjugates are stable at physiological pH and in plasma, they advantageously reduce undesirable systemic ALK5 inhibitor activity; however, the preferable glycoconjugates are acid-labile conjugates that can be hydrolyzed upon reaching the more acid environment of the tumor.
• US8871744B2
  申请人：——

  公开号：US8871744B2

  公开（公告）日：2014-10-28