6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-(1,3-dimethylpyrazol-4-yl)-3-methyl-1H-benzimidazol-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-(1,3-dimethylpyrazol-4-yl)-3-methyl-1H-benzimidazol-2-one
• 化学式: C₁₈H₁₉N₅O₂
• 分子量: 337.4
• InChiKey: ZVRLVNNYTYCLKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  76.2
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• NOVEL SUBSTITUTED BICYCLIC COMPOUNDS AS BROMODOMAIN INHIBITORS
  申请人：ZENITH EPIGENETICS CORP.

  公开号：US20160145248A1

  公开（公告）日：2016-05-26

  The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.

  该发明涉及替代双环化合物，其通过与溴结构域结合对BET蛋白功能进行抑制，包括这些化合物的药物组合物、以及这些化合物和组合物在治疗中的用途。
• [EN] HETERO-BIFUNCTIONAL DEGRADER COMPOUNDS AND THEIR USE AS MODULATORS OF TARGETED UBIQUINATION (VHL)<br/>[FR] COMPOSÉS DE DÉGRADATION HÉTÉRO-BIFONCTIONNELS ET LEUR UTILISATION EN TANT QUE MODULATEURS DE L'UBIQUINATION CIBLÉE (VHL)
  申请人：GENENTECH INC

  公开号：WO2019183523A1

  公开（公告）日：2019-09-26

  The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds that contain on one end a VHL ligand moiety, which binds to the VHL ubiquitin ligase (E3), and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. The target protein may be EGFR. Also disclosed are VHL ligands.

  本公开涉及双功能化合物，可用作靶向泛素化的调节剂。特别是，本公开是针对包含在一端具有VHL配体基团的化合物，该基团结合到VHL泛素连接酶(E3)，而在另一端具有结合目标蛋白的基团，从而实现目标蛋白/多肽的降解。目标蛋白可以是EGFR。还公开了VHL配体。
• Substituted bicyclic compounds as bromodomain inhibitors
  申请人：ZENITH EPIGENETICS LTD

  公开号：US10226451B2

  公开（公告）日：2019-03-12

  The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.

  本发明涉及取代的双环化合物，这些化合物可通过与溴结构域结合来抑制 BET 蛋白的功能；本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗中的应用。
• (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof
  申请人：Genentech, Inc.

  公开号：US11242344B2

  公开（公告）日：2022-02-08

  The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.

  本公开涉及可用作靶向泛素化调节剂的双功能化合物。特别是，本公开涉及的化合物一端含有与 VHL E3 泛素连接酶结合的 VHL 配体分子，另一端含有与靶蛋白结合的分子，从而实现靶蛋白/多肽的降解。还公开了 VHL 配体。
• (4-HYDROXYPYRROLIDIN-2-YL)-HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Genentech, Inc.

  公开号：US20210309660A1

  公开（公告）日：2021-10-07

  The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.