N-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-pyrimidin-5-yl)-phthalimide | 59007-55-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: N-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-pyrimidin-5-yl)-phthalimide
• 英文别名: 2-(6-methyl-2,4-dioxo-1H-pyrimidin-5-yl)isoindole-1,3-dione
• CAS: 59007-55-5
• 化学式: C₁₃H₉N₃O₄
• 分子量: 271.232
• InChiKey: KJMSFNVGJRXQRH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  95.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  5-氨基-2,4-二羟基-6-甲基嘧啶 、 苯酐 以20%的产率得到
  参考文献：
  名称：

  CINGOLANI G. M.; GIARDINA D.; CAROTTI A.; CASINI G.; FERAPPI M., FARMACO. ED. SCI. , 1976, 31, NO 2, 133-139

  摘要：

  DOI：

文献信息

• TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
  申请人：Arvinas, Inc.

  公开号：US20180155322A1

  公开（公告）日：2018-06-07

  The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, 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 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，这些化合物可用作雌激素受体（目标蛋白）的调节剂。特别是，本公开涉及包含在一段至少有一种Von Hippel-Lindau配体、一种cereblon配体、凋亡抑制蛋白配体、小鼠双分钟同源2配体或其组合的双功能化合物，这些配体与相应的E3泛素连接酶结合，在另一端有一个与目标蛋白结合的部分，使得目标蛋白被置于泛素连接酶附近，以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白降解/抑制相关的广泛药理活性。可以通过本公开的化合物和组合物治疗或预防由目标蛋白聚集或积累引起的疾病或障碍。
• Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
  申请人：Arvinas, Inc.

  公开号：US10647698B2

  公开（公告）日：2020-05-12

  The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, 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 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，它们可用作雌激素受体（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 Von Hippel-Lindau 配体、cereblon 配体、凋亡蛋白抑制剂配体、小鼠双敏同源物 2 配体或其组合中的至少一种、其一端与相应的 E3 泛素连接酶结合，另一端与靶蛋白结合，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。
• [EN] SOS1 PROTEOLYSIS MODULATOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF<br/>[FR] MODULATEUR DE PROTÉOLYSE SOS1, SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION<br/>[ZH] SOS1蛋白水解调节剂及其制备方法和应用
  申请人：[en]SUZHOU ZELGEN BIOPHARMACEUTICALS CO., LTD.;[zh]苏州泽璟生物制药股份有限公司

  公开号：WO2022188819A1

  公开（公告）日：2022-09-15

  本发明涉及SOS1蛋白水解调节剂及其制备方法和应用。具体地，本发明化合物具有式(I)所示结构，本发明还公开了所述化合物的制备方法及其作为SOS1蛋白水解调节剂的用途，本发明化合物对SOS1水解具有很好的选择性调节作用。
• CINGOLANI G. M.; GIARDINA D.; CAROTTI A.; CASINI G.; FERAPPI M., FARMACO. ED. SCI. <FSTE-AI>, 1976, 31, NO 2, 133-139
  作者：CINGOLANI G. M.、 GIARDINA D.、 CAROTTI A.、 CASINI G.、 FERAPPI M.

  DOI：——

  日期：——