(2R)-1-ethoxy-3-piperazin-1-ylpropan-2-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (2R)-1-ethoxy-3-piperazin-1-ylpropan-2-ol
• 化学式: C₉H₂₀N₂O₂
• 分子量: 188.27
• InChiKey: FKRHIKHPLLIOLR-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  13
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  44.7
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DE PROTÉINES CONTENANT UN BROMODOMAINE
  申请人：ARVINAS INC

  公开号：WO2017030814A1

  公开（公告）日：2017-02-23

  The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

  本发明涉及双功能化合物，其作为靶向泛素化的调节剂具有实用性，特别是根据本发明抑制各种多肽和其他蛋白质的化合物。具体而言，本发明涉及一端含有结合泛素连接酶的VHL配体，另一端含有结合靶蛋白的基团的化合物，使得靶蛋白靠近泛素连接酶以促使该蛋白的降解（和抑制）。根据本发明的化合物表现出与靶向多肽的降解/抑制一致的广泛的药理活性。
• [EN] MODULATORS OF ESTROGEN RECEPTOR PROTEOLYSIS AND ASSOCIATED METHODS OF USE<br/>[FR] MODULATEURS DU RÉCEPTEUR DES ŒSTROGÈNES DE PROTÉOLYSE ET PROCÉDÉS D'UTILISATION ASSOCIÉS
  申请人：ARVINAS INC

  公开号：WO2018140809A1

  公开（公告）日：2018-08-02

  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 a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, 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，其作为雌激素受体（靶蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端为 cereblon、Von Hippel-Lindau 配体结合基团、凋亡抑制蛋白或鼠双分子同源物 2 配体的双功能化合物，该化合物与相应的 E3 泛素连接酶结合，并且另一端含有结合靶蛋白的基团，使得靶蛋白与泛素连接酶靠近，以实现对靶蛋白的降解（和抑制）。本公开展示了与靶蛋白的降解/抑制相关的广泛药理活性范围。本公开的化合物和组合物用于治疗或预防由靶蛋白聚集或积累导致的疾病或紊乱。
• [EN] BIFUNCTIONAL SUBSTITUED PYRIMIDINES AS MODULATORS OF FAK PROTEOLYSE<br/>[FR] PYRIMIDINES SUBSTITUÉES BIFONCTIONNELLES EN TANT QUE MODULATEURS DU PROTÉOLYSE DE FAK
  申请人：UNIV YALE

  公开号：WO2020023851A1

  公开（公告）日：2020-01-30

  The present disclosure relates to bifunctional compounds, which find utility as modulators of focal adhesion kinase (FAK) or protein tyrosine kinase 2 (PTK2). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand 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，其作为调节焦粘附激酶（FAK）或蛋白酪氨酸激酶2（PTK2）的调节剂。具体而言，本公开涉及包含一端为Von Hippel-Lindau、cereblon、凋亡抑制蛋白或鼠双分子同源物2配体的双功能化合物，该配体结合到相应的E3泛素连接酶，另一端为结合目标蛋白的基团，使目标蛋白靠近泛素连接酶以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性范围。本公开的化合物和组合物用于治疗或预防由目标蛋白聚集或积累导致的疾病或紊乱。
• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
  申请人：Arvinas Operations, Inc.

  公开号：EP3660004A1

  公开（公告）日：2020-06-03

  The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

  本公开涉及双功能化合物，它们可用于降解和（抑制）雄激素受体。特别是，本公开涉及的化合物一端含有与 E3 泛素连接酶结合的脑龙配体，另一端含有与雄激素受体结合的分子，这样雄激素受体就被置于泛素连接酶附近，从而实现对雄激素受体的降解（和抑制）。本公开的化合物具有广泛的药理活性，与雄激素受体的降解/抑制作用相一致。
• Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine
  申请人：Nektar Therapeutics

  公开号：US10189859B2

  公开（公告）日：2019-01-29

  The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

  本公开涉及 6-(2,3-二氯苯基)-1,2,4-三嗪-5-胺衍生物的化合物。与本领域已知的其他苯基三嗪相比，所提供的化合物具有独特的效果和差异。