O-benzyl-N-isopropylhydroxylamine | 136943-84-5

• 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: O-benzyl-N-isopropylhydroxylamine
• 英文别名: N-phenylmethoxypropan-2-amine
• CAS: 136943-84-5
• 化学式: C₁₀H₁₅NO
• 分子量: 165.235
• InChiKey: XWAKWIGFRSCSLI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  O-benzyl-N-isopropylhydroxylamine 在 盐酸 、 sodium nitrite 作用下， 以 乙醇 、 水 为溶剂， 反应 0.5h， 以83%的产率得到N-nitroso-N-isopropyl-O-benzylhydroxylamine
  参考文献：
  名称：

  Bhat, J. Ishwara; Clegg, William; Maskill, Howard, Journal of the Chemical Society. Perkin Transactions 2 (2001), 2000, # 7, p. 1435 - 1446

  摘要：

  DOI：
• 作为产物：
  描述：

  acetone O-benzyloxime 在 甲酸 、 C₁₈H₂₄ClIrN₃⁽¹⁺⁾*Cl^(1-) 、 sodium formate 、 三氟乙酸 作用下， 以 2,2,2-三氟乙醇 为溶剂， 以52 %的产率得到O-benzyl-N-isopropylhydroxylamine
  参考文献：
  名称：

  铱催化肟转移加氢合成N-烷氧基胺和羟胺

  摘要：

  发现阳离子铱（Ir）配合物催化肟的转移加氢以得到N-烷氧基胺和羟胺，并且三氟乙酸加速了反应。该协议的实际应用通过克级转化和杀菌剂 furmecyclox (BAS 389F) 的两步合成得到证明，总产量分别为 92% 和 85%。证明了使用手性 Ir 配合物提供手性N-烷氧基胺的不对称方案，但获得的低产率/ee 表明需要进一步开发。

  DOI：

  10.1039/d2ob01084d

文献信息

• BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
  申请人：Arvinas Operations, Inc.

  公开号：US20190300521A1

  公开（公告）日：2019-10-03

  The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau 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SMARCA2或BRM（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结合Von Hippel-Lindau E3泛素连接酶的配体，另一端结合靶蛋白的双功能化合物，使得靶蛋白与泛素连接酶靠近以实现靶蛋白的降解（和抑制）。本公开展示了与靶蛋白降解/抑制相关的广泛药理活性。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。
• TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
  申请人：Arvinas, Inc.

  公开号：US20180125821A1

  公开（公告）日：2018-05-10

  The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau 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tau蛋白的调节剂具有实用性。具体而言，本公开涉及含有一端结合到E3泛素连接酶的VHL或cereblon配体，另一端结合到tau蛋白的双功能化合物，使得tau蛋白与泛素连接酶靠近，以实现tau蛋白的降解（和抑制）。本公开展示了与tau蛋白降解/抑制相关的广泛药理活性。本公开的化合物和组合物用于治疗或预防由tau蛋白聚集或积累导致的疾病或紊乱。
• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
  申请人：Arvinas, Inc.

  公开号：US20190151295A1

  公开（公告）日：2019-05-23

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the 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, 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，其作为白细胞介素-1受体相关激酶4（IRAK-4；目标蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端结合E3泛素连接酶的Von Hppel-Lindau、cereblon配体的双功能化合物，另一端结合目标蛋白的部分，使得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。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。
• BENZIMIDAZOLE AND IMADAZOPYRIDINE CARBOXIMIDAMIDE COMPOUNDS
  申请人：Gilead Sciences, Inc.

  公开号：US20160333009A1

  公开（公告）日：2016-11-17

  The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R 1 , R 2a , R 2b , R n , R m , and R t are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

  本公开提供了式I的吲哌酮2,3-二氧化酶1（IDOL）抑制剂： 或其药学上可接受的盐，其中X、L、n、m、R 1 、R 2a 、R 2b 、R n 、R m 和R t 如本文所定义，以及包括式I化合物的药物组合物，或其药学上可接受的盐，并使用这些方法来治疗由IDO1介导的疾病。
• [EN] NOVEL COMPOUNDS AS RESPIRATORY STIMULANTS FOR TREATMENT OF BREATHING CONTROL DISORDERS OR DISEASES<br/>[FR] NOUVEAUX COMPOSÉS COMME STIMULANTS RESPIRATOIRES POUR LE TRAITEMENT DE TROUBLES OU DE MALADIES DE CONTRÔLE DE LA RESPIRATION
  申请人：GALLEON PHARMACEUTICALS INC

  公开号：WO2012074999A1

  公开（公告）日：2012-06-07

  The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention, The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.

  本发明涵盖了用于治疗患有呼吸控制疾病或紊乱的受试者的组合物。本发明还包括一种治疗患有呼吸系统疾病或紊乱的受试者的方法，包括向受试者施用本发明的药物配方的治疗有效量。本发明还包括一种预防或稳定患有呼吸节律不稳定的受试者的方法，包括向受试者施用本发明的药物配方的治疗有效量。