(R)-3-aminopiperidine-2,6-dione hydrochloride | 1801140-47-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (R)-3-aminopiperidine-2,6-dione hydrochloride
• 英文别名: (3R)-3-aminopiperidine-2,6-dione hydrochloride；(R)-3-Amino-piperidine-2,6-dione hydrochloride；(3R)-3-aminopiperidine-2,6-dione;hydrochloride
• CAS: 1801140-47-5
• 化学式: C₅H₈N₂O₂*ClH
• 分子量: 164.592
• InChiKey: YCPULGHBTPQLRH-AENDTGMFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.83
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  72.2
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  BOC-L-苯丙氨酸 、 (R)-3-aminopiperidine-2,6-dione hydrochloride 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以91%的产率得到(3R,2’S)-3-(N-tert-butoxycarbonylphenylalanylamino)piperidine-2,6-dione
  参考文献：
  名称：

  Synthesis of New Hydantoins Bearing Glutarimide or Succinimide Moiety and Their Evaluation for Cell Differentiation-inducing and Anti-angiogenic Activities

  摘要：

  Several derivatives of hydantoin containing glutarimide or succinimide at the 3-position were synthesized. The new hydantoin derivatives had a structure similar to that of thalidomide, and so may possess activity similar to that of thalidomide and/or its analogs, such as effects on cell differentiation and angiogenesis. Some hydantoins showed enhancing effects on all-trans retinoic acid (ATRA)-induced cell differentiation of human leukemia cell line HL-60 and anti-angiogenic activity on human umbilical vein endothelial cells (HUVEC). These new hydantoin derivatives were more effective than thalidomide in cell differentiation-inducing activity on HL-60 and anti-angiogenic activity on HUVEC.

  DOI：

  10.3987/com-15-13184
• 作为产物：
  描述：

  (R)-3-(tert-butoxycarbonylamino)piperidine-2,6-dione 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 1.0h， 以69%的产率得到(R)-3-aminopiperidine-2,6-dione hydrochloride
  参考文献：
  名称：

  Synthesis of New Hydantoins Bearing Glutarimide or Succinimide Moiety and Their Evaluation for Cell Differentiation-inducing and Anti-angiogenic Activities

  摘要：

  Several derivatives of hydantoin containing glutarimide or succinimide at the 3-position were synthesized. The new hydantoin derivatives had a structure similar to that of thalidomide, and so may possess activity similar to that of thalidomide and/or its analogs, such as effects on cell differentiation and angiogenesis. Some hydantoins showed enhancing effects on all-trans retinoic acid (ATRA)-induced cell differentiation of human leukemia cell line HL-60 and anti-angiogenic activity on human umbilical vein endothelial cells (HUVEC). These new hydantoin derivatives were more effective than thalidomide in cell differentiation-inducing activity on HL-60 and anti-angiogenic activity on HUVEC.

  DOI：

  10.3987/com-15-13184

文献信息

• [EN] BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY<br/>[FR] COMPOSÉS BIFONCTIONNELS POUR LA DÉGRADATION DE LA BTK PAR L'INTERMÉDIAIRE DE LA VOIE DE L'UBIQUITINE-PROTÉOSOME
  申请人：NURIX THERAPEUTICS INC

  公开号：WO2021113557A1

  公开（公告）日：2021-06-10

  This disclosure relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The description also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

  本公开涉及通过泛素蛋白酶途径降解BTK的化合物。描述还提供了包括这些化合物的药学上可接受的组合物，以及使用这些组合物治疗各种疾病、状况或障碍的方法。
• [EN] GLUTARIMIDE<br/>[FR] GLUTARIMIDE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2019043214A1

  公开（公告）日：2019-03-07

  The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

  本发明提供了一种与广泛表达的E3连接酶蛋白Cereblon（CRBN）结合并改变CRBN E3泛素连接酶复合物底物特异性的化合物，导致内在下游蛋白的降解。因此，目前的化合物对于治疗各种癌症是有用的。
• [EN] BTK INHIBITOR RING DERIVATIVE, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL APPLICATION THEREOF<br/>[FR] DÉRIVÉ DE CYCLE INHIBITEUR DE BTK, SON PROCÉDÉ DE PRÉPARATION ET SON APPLICATION PHARMACEUTIQUE<br/>[ZH] 一种BTK抑制剂环衍生物及其制备方法和药学上的应用
  申请人：SICHUAN HAISCO PHARMACEUTICAL CO LTD

  公开号：WO2020239103A1

  公开（公告）日：2020-12-03

  涉及一种BTK抑制剂环衍生物及其制备方法和药学上的应用，所述BTK抑制剂环衍生物为通式(I)所述的化合物或者其立体异构体、溶剂化物、前药、代谢产物、药学上可接受的盐或共晶，所述BTK抑制剂环衍生物用于治疗与BTK相关疾病如肿瘤或自身免疫系统疾病。
• EP3978496
  申请人：——

  公开号：——

  公开（公告）日：——
• BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
  申请人：Nurix Therapeutics, Inc.

  公开号：US20210198280A1

  公开（公告）日：2021-07-01

  This disclosure relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The description also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.