3-[3,5-dimethyl-4-(3-oxo-3-piperazin-1-ylpropyl)-1H-pyrrol-2-ylmethylene]-1,3-dihydroindol-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-[3,5-dimethyl-4-(3-oxo-3-piperazin-1-ylpropyl)-1H-pyrrol-2-ylmethylene]-1,3-dihydroindol-2-one
• 英文别名: THRX-165724；(3Z)-3-[[3,5-dimethyl-4-(3-oxo-3-piperazin-1-ylpropyl)-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one
• 化学式: C₂₂H₂₆N₄O₂
• 分子量: 378.474
• InChiKey: KVIAIJLTPHXNEB-AQTBWJFISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  77.2
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Indolinone derivatives
  申请人：——

  公开号：US20040198804A1

  公开（公告）日：2004-10-07

  Compounds of formula (I) 1 in which R 1 , R 2 , R 3 and R 4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of proliferative disorders, such as cancer.

  式(I)1的化合物中，其中R1、R2、R3和R4具有规范中给出的含义，是用于治疗增殖性疾病，例如癌症的受体酪氨酸激酶抑制剂。
• Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
  申请人：Arvinas Operations, Inc.

  公开号：US10806737B2

  公开（公告）日：2020-10-20

  The present disclosure relates to bifunctional compounds, which find utility as modulators of FLT3 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein FLT3, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of the target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，它们可用作 FLT3（靶蛋白）的调节剂。特别是，本公开涉及双功能化合物，其一端含有与 E3 泛素连接酶结合的 Von Hppel-Lindau（脑龙）配体，另一端含有与靶蛋白 FLT3 结合的分子，从而将靶蛋白置于泛素连接酶附近，以实现对靶蛋白的降解（和抑制）。本公开物具有与降解/抑制靶蛋白相关的广泛药理活性。本公开的化合物和组合物可以治疗或预防因目标蛋白聚集或积聚而导致的疾病或失调。
• INDOLINONE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
  申请人：Theravance, Inc.

  公开号：EP1458713A1

  公开（公告）日：2004-09-22
• FLT3 INHIBITORS FOR IMMUNE SUPPRESSION
  申请人：THE JOHNS-HOPKINS UNIVERSITY

  公开号：EP1778224B1

  公开（公告）日：2014-03-26
• Oncokinase fusion polypeptides associated with hyperproliferative and related disorders, nucleic acids encoding the same and methods for detecting and identifying the same
  申请人：Briesewitz Roger

  公开号：US20080102472A1

  公开（公告）日：2008-05-01

  Oncokinase fusion polypeptides associated with hyperproliferative disorders and the polynucleotides encoding for such fusion polypeptides are provided. The fusion polypeptides have a C-terminal tyrosine kinase domain fused to an N-terminal domain that is not normally fused to the C-terminal tyrosine kinase domain and they possess constitutively activated tyrosine kinase activity. Also provided are methods for detecting and identifying the fusion polypeptides and polynucleotides and methods of diagnosing disease conditions associated with the fusion polypeptides and polynucleotides. In addition, screening assays for identifying agents useful for treating disease conditions associated with such fusion polypeptides and polynucleotides are provided. Furthermore, methods of treating disease conditions associated with the presence of the fusion polypeptides are provided.