(E)-N'-((4-oxo-4H-chromen-3-yl)methylene)nicotinohydrazide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: (E)-N'-((4-oxo-4H-chromen-3-yl)methylene)nicotinohydrazide
• 英文别名: STAT5 Inhibitor；N-[(E)-(4-oxochromen-3-yl)methylideneamino]pyridine-3-carboxamide
• 化学式: C₁₆H₁₁N₃O₃
• 分子量: 293.282
• InChiKey: DAVIKTBRCQWOGT-GIJQJNRQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  80.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• USE OF COMPOUND IN PREPARATION OF DRUG FOR TREATING ATHEROSCLEROSIS
  申请人：Generos Biopharma Ltd.

  公开号：EP3960175A1

  公开（公告）日：2022-03-02

  Disclosed is use of a compound in the preparation of a medicament for treating atherosclerosis. The compound is selected from a group consisting of a compound of formula I, Nib2 and a pharmaceutically acceptable salt thereof. Based on the mechanism of atherogenesis, the invention started with the inhibition of inflammatory reaction. The research results showed that the compounds disclosed herein can significantly inhibit the macrophage foaming, reduce the deposition of lipidic necrotic substances, and reduce the formation of plaques, thus to some extent delaying or inhibiting atherosclerosis.

  公开了一种化合物在制备治疗动脉粥样硬化药物中的用途。该化合物选自由式 I、Nib2 及其药学上可接受的盐组成的组。根据动脉粥样硬化的发生机制，本发明从抑制炎症反应入手。研究结果表明，本发明公开的化合物能明显抑制巨噬细胞发泡，减少脂质坏死物质的沉积，减少斑块的形成，从而在一定程度上延缓或抑制动脉粥样硬化的发生。
• COMBINED INHIBITION OF AMINO ACID TRANSPORTERS FOR INHIBITING HUMAN PLASMACYTOID DENDRITIC CELL ACTIVITY DURING AUTOIMMUNITY
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP4008330A1

  公开（公告）日：2022-06-08

  The present invention relates to the treatment of autoimmune diseases through inhibition of human plasmacytoid dendritic cell activity. The treatment is based on a combination of one inhibitor of antiporter system xc-, and at least one inhibitor selected from the group consisting of a JAK2 inhibitor, a SLC7A5:SLC3A2 inhibitor, an inhibitor targeting IL-3 receptor alpha, IL-3 receptor beta, an inhibitor targeting GM-CSF, an inhibitor targeting GM-CSF receptor alpha, and an inhibitor targeting STAT5. The present invention also provided pharmaceutical compositions comprising said combination.

  本发明涉及通过抑制人类浆细胞树突状细胞活性来治疗自身免疫性疾病。该治疗方法基于一种抗转运体系统xc-的抑制剂和至少一种选自JAK2抑制剂、SLC7A5:SLC3A2抑制剂、靶向IL-3受体α的抑制剂、IL-3受体β的抑制剂、靶向GM-CSF的抑制剂、靶向GM-CSF受体α的抑制剂和靶向STAT5的抑制剂组成的组的抑制剂的组合。本发明还提供了包含所述组合物的药物组合物。
• [EN] USE OF COMPOUND IN PREPARATION OF DRUG FOR TREATING ATHEROSCLEROSIS<br/>[FR] UTILISATION DE COMPOSÉ DANS LA PRÉPARATION D'UN MÉDICAMENT POUR TRAITER L'ATHÉROSCLÉROSE<br/>[ZH] 一种化合物在制备治疗动脉粥样硬化药物中的应用
  申请人：GENEROS BIOPHARMA LTD

  公开号：WO2020216335A1

  公开（公告）日：2020-10-29

  一种化合物在制备治疗动脉粥样硬化药物中的应用，其中所述化合物包括如式I所述的化合物、Nib2其在药学上可接受的盐中的一种或多种。根据动脉粥样硬化发生机制，从炎症反应的产生入手，已有研究表明，所述化合物可显著抑制巨噬细胞泡沫化，减少脂性坏死物质沉淀，减少斑块的形成，在一定程度上可以延缓或抑制动脉粥样硬化。
• METHODS FOR TREATING TYROSINE-KINASE-INHIBITOR-RESISTANT MALIGNANCIES IN PATIENTS WITH GENETIC POLYMORPHISMS OR AHI1 DYSREGULATIONS OR MUTATIONS EMPLOYING DIANHYDROGALACTITOL, DIACETYLDIANHYDROGALACTITOL, DIBROMODULCITOL, OR ANALOGS OR DERIVATIVES THEREOF
  申请人：Del Mar Pharmaceuticals

  公开号：EP2872161A2

  公开（公告）日：2015-05-20
• DIANHYDROGALACTITOL FOR USE IN TREATING TYROSINE-KINASE-INHIBITOR-RESISTANT MALIGNANCIES IN PATIENTS WITH GENETIC POLYMORPHISMS OR AHI1 DYSREGULATIONS OR MUTATIONS
  申请人：Del Mar Pharmaceuticals

  公开号：EP2872161B1

  公开（公告）日：2020-12-16