2-{2-[benzyl(methyl)amino]ethoxy}ethan-1-ol | 115972-93-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-{2-[benzyl(methyl)amino]ethoxy}ethan-1-ol
• 英文别名: 2-[2-[Benzyl(methyl)amino]ethoxy]ethanol
• CAS: 115972-93-5
• 化学式: C₁₂H₁₉NO₂
• 分子量: 209.288
• InChiKey: VMCKVGNNQRSYTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-{2-[benzyl(methyl)amino]ethoxy}ethan-1-ol 在 palladium 10% on activated carbon 作用下， 以 甲醇 为溶剂， 生成 2-[2-(甲基氨基)乙氧基]乙醇
  参考文献：
  名称：

  [EN] COMPOUNDS AND METHODS OF TREATING RNA-MEDIATED DISEASES
  [FR] COMPOSÉS ET MÉTHODES DE TRAITEMENT DE MALADIES MÉDIÉES PAR L'ARN

  摘要：

  公开号：

  WO2017136450A3
• 作为产物：
  描述：

  苯甲醛 在 甲醇 、 三乙酰氧基硼氢化钠 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 6.0h， 生成 2-{2-[benzyl(methyl)amino]ethoxy}ethan-1-ol
  参考文献：
  名称：

  COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

  摘要：

  本公开涉及双功能化合物，其用于降解和（抑制）雄激素受体。具体而言，本公开涉及包含一端结合到E3泛素连接酶的谷氨酰腺苷环配体，另一端结合到雄激素受体的部分的化合物，使得雄激素受体与泛素连接酶靠近，以实现雄激素受体的降解（和抑制）。本公开展示了与根据本公开涉及的化合物相关的广泛的药理活性范围，与雄激素受体的降解/抑制一致。

  公开号：

  US20180099940A1

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
  申请人：Arvinas, Inc.

  公开号：US20180099940A1

  公开（公告）日：2018-04-12

  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，其用于降解和（抑制）雄激素受体。具体而言，本公开涉及包含一端结合到E3泛素连接酶的谷氨酰腺苷环配体，另一端结合到雄激素受体的部分的化合物，使得雄激素受体与泛素连接酶靠近，以实现雄激素受体的降解（和抑制）。本公开展示了与根据本公开涉及的化合物相关的广泛的药理活性范围，与雄激素受体的降解/抑制一致。
• INDOLE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS
  申请人：Arvinas, Inc.

  公开号：US20180072711A1

  公开（公告）日：2018-03-15

  The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.

  本公开涉及化合物及其药用盐，含有这些化合物的组合物、配方和药物，以及它们的制备过程。该公开还涉及化合物、组合物、配方和药物的用途，例如作为雌激素受体活性的抑制剂，包括降解雌激素受体，治疗由雌激素受体介导的疾病和症状。
• [EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF THE ANDROGEN RECEPTOR<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DU RÉCEPTEUR DES ANDROGÈNES
  申请人：ARVINAS INC

  公开号：WO2016118666A1

  公开（公告）日：2016-07-28

  The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. 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 Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

  本发明涉及双功能化合物，其可用于降解和（抑制）雄激素受体。具体而言，本发明涉及含有一端与泛素连接酶结合的VHL配体，另一端含有与雄激素受体结合的部分的化合物，使得雄激素受体与泛素连接酶靠近以实现雄激素受体的降解（和抑制）。本发明展示了与根据本发明的化合物相关的广泛的药理活性，与雄激素受体的降解/抑制一致。
• Galactose Derivative, Drug Carrier and Medicinal Composition
  申请人：Ohgi Tadaaki

  公开号：US20070244058A1

  公开（公告）日：2007-10-18

  The present invention relates to a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention also relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, or an oligo nucleic acid).

  本发明涉及一种新颖且有用的半乳糖衍生物，该衍生物构成了一种药物载体，可以有效地将药物转运到肝脏，包括该衍生物的药物载体以及包含该载体和药物的制药组合物。本发明还涉及由半乳糖、适当的间隔物和某种脂质组成的半乳糖衍生物，该衍生物构成了一种药物载体，包括该衍生物和阳离子脂质的药物载体，以及包含该载体和药物（优选为双链RNA、双链DNA或寡核苷酸）的制药组合物。
• Compounds and methods for the targeted degradation of androgen receptor
  申请人：Arvinas, Inc.

  公开号：US10584101B2

  公开（公告）日：2020-03-10

  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。