(R)-3-amino-3-methylpiperidine-2,6-dione hydrobromide | 903890-69-7

• 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-amino-3-methylpiperidine-2,6-dione hydrobromide
• 英文别名: (3R)-3-amino-3-methyl-piperidine-2,6-dione hydrobromide；(3S)-3-amino-3-methylpiperidine-2,6-dione hydrobromide；(3R)-3-amino-3-methylpiperidine-2,6-dione;hydron;bromide
• CAS: 903890-69-7
• 化学式: BrH*C₆H₁₀N₂O₂
• 分子量: 223.07
• InChiKey: KLXHHRQZQKDYDC-FYZOBXCZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.74
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  72.2
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-3-amino-3-methylpiperidine-2,6-dione hydrobromide 在 bis(trimethylaluminum)-1,4-diazabicyclo[2.2.2]octane 、 氢气 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 、 甲苯 、 乙腈 为溶剂， 20.0 ℃ 、100.0 kPa 条件下， 反应 54.0h， 生成 tert-butyl (R)-((2-(3-methyl-2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)carbamate
  参考文献：
  名称：

  [EN] LOW MOLECULAR WEIGHT PROTEIN DEGRADERS AND THEIR APPLICATIONS
  [FR] AGENTS DE DÉGRADATION DE PROTÉINES DE FAIBLE POIDS MOLÉCULAIRE ET LEURS APPLICATIONS

  摘要：

  本发明涉及式(Ia)、(Ib)、(Ic)和(II)的化合物及其在治疗癌症方法中的应用。这些化合物可以与已有的抗癌疗法结合使用，以增加其疗效。

  公开号：

  WO2022029138A1
• 作为产物：
  描述：

  (3S)-(3-methyl-2,6-dioxopiperidin-3-yl)-carbamic acid 2-isopropyl-5-methylcyclohexyl ester 在 氢溴酸 作用下， 以 溶剂黄146 为溶剂， 反应 6.5h， 生成 (R)-3-amino-3-methylpiperidine-2,6-dione hydrobromide
  参考文献：
  名称：

  Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma

  摘要：

  Many patients with multiple myeloma (MM) initially respond to treatment with modern combination regimens including immunomodulatory agents (lenalidomide and pomalidomide) and proteasome inhibitors. However, some patients lack an initial response to therapy (i.e., are refractory), and although the mean survival of MM patients has more than doubled in recent years, most patients will eventually relapse. To address this need, we explored the potential of novel cereblon E3 ligase modulators (CELMoDs) for the treatment of patients with relapsed or refractory multiple myeloma (RRMM). We found that optimization beyond potency of degradation, including degradation efficiency and kinetics, could provide efficacy in a lenalidomide-resistant setting. Guided by both phenotypic and protein degradation data, we describe a series of CELMoDs for the treatment of RRMM, culminating in the discovery of CC-92480, a novel protein degrader and the first CELMoD to enter clinical development that was specifically designed for efficient and rapid protein degradation kinetics.

  DOI：

  10.1021/acs.jmedchem.9b01928

文献信息

• [EN] PRPK INHIBITORS<br/>[FR] INHIBITEURS DE PRPK
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2022005961A1

  公开（公告）日：2022-01-06

  This disclosure relates to compounds of formula (I) as defined in the Specification. This disclosure also relates to methods of synthesizing the compound of formula (I) and using the compounds of formula (I) for treating a disease (e.g., cancer).

  本公开涉及到规范中定义的式(I)的化合物。本公开还涉及到合成式(I)化合物的方法以及利用式(I)化合物治疗疾病（例如癌症）的方法。
• 5-Substituted quinazolinone derivatives and compositions comprising and methods of using the same
  申请人：Muller George W.

  公开号：US20080161328A1

  公开（公告）日：2008-07-03

  Provided are 5-substituted quinazolinone compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

  提供了5-取代的喹唑酮化合物，以及其药学上可接受的盐，溶剂化合物，包合物，立体异构体和前药。揭示了这些化合物的使用方法和制药组合物。
• 5-SUBSTITUTED QUINAZOLINONE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME
  申请人：MULLER George W.

  公开号：US20100093774A1

  公开（公告）日：2010-04-15

  Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.

  提供了5-取代的喹唑啉酮化合物，例如式(I)，以及其药学上可接受的盐、溶剂合物、包合物、立体异构体和前药。揭示了用于治疗血管生成或细胞因子相关疾病的使用方法，以及这些化合物的药物组合物。
• 5-substituted quinazolinone derivatives and compositions comprising and methods of using the same
  申请人：Muller George W.

  公开号：US08921385B2

  公开（公告）日：2014-12-30

  Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.

  提供了5-取代的喹唑酮类化合物，例如公式（I）所示的化合物，以及其药学上可接受的盐、溶剂化合物、包合物、立体异构体和前药。还公开了用于治疗血管生成或细胞因子相关疾病的使用方法以及这些化合物的制药组合物。
• 5-substituted quinazolinone derivatives as anti-cancer agents
  申请人：CELGENE CORPORATION

  公开号：EP2420497A1

  公开（公告）日：2012-02-22

  Provided are 5-substituted quinazolinone compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

  本发明提供了 5-取代喹唑啉酮化合物及其药学上可接受的盐、溶液剂、凝胶体、立体异构体和原药。公开了这些化合物的使用方法和药物组合物。