3-(4-amino-1-oxo-1 ,3-dihydroisoindol-2-yl)piperidine-2,6-dione-gallic acid

• 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: 3-(4-amino-1-oxo-1 ,3-dihydroisoindol-2-yl)piperidine-2,6-dione-gallic acid
• 英文别名: gallic acid lenalidomide；3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione;3,4,5-trihydroxybenzoic acid
• 化学式: (x)C₇H₆O₅*C₁₃H₁₃N₃O₃
• 分子量: 429.4
• InChiKey: LIXGHKQWWDTIAE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.53
• 重原子数：
  31
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  191
• 氢给体数：
  6
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  没食子酸 、 来那度胺 以 甲醇 、 水 为溶剂， 反应 24.0h， 生成 3-(4-amino-1-oxo-1 ,3-dihydroisoindol-2-yl)piperidine-2,6-dione-gallic acid
  参考文献：
  名称：

  [EN] SOLID FORMS COMPRISING 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
  [FR] FORMES SOLIDES COMPRENANT DE LA 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISO-INDOL-2-YL)-PIPÉRIDINE-2,6-DIONE ET UN COAGENT DE FORMATION, COMPOSITIONS ET PROCÉDÉS D'UTILISATION CORRESPONDANTS

  摘要：

  本文提供了包含(a) 3-(4-氨基-1-氧代-1,3-二氢异吲哚-2-基)-哌啶-2,6-二酮（来那度胺）和(b) 辅基的固体形式。还披露了包含这些固体形式的药物组合物以及治疗、预防和管理各种疾病的方法。

  公开号：

  WO2014160686A1

文献信息

• Crystalline forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione
  申请人：AMPLIO PHARMA, LLC

  公开号：US10100032B2

  公开（公告）日：2018-10-16

  The invention relates to novel crystalline forms of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.

  本发明涉及 3-(4-氨基-1-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮的新型结晶形式，包括 3-(4-氨基-1-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮的新型脲共晶体；3-(4-氨基-l-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮的新型没食子酸共晶体； 3-(4-氨基-l-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮的新型没食子酸丙酯共晶体；以及 3-(4-氨基-1-氧代-1,3-二氢-异吲哚-2-基)-哌啶-2,6-二酮的新型 L-酒石酸共晶体。本发明描述了根据本发明各种实施方案制备的新型晶体的制备和表征。本发明还涉及含有新型结晶形式的药物组合物以及新型结晶形式的治疗用途。
• [EN] NOVEL CRYSTALLINE FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE<br/>[FR] NOUVELLES FORMES CRISTALLINES DE 3-(4-AMINO-1-OXO-1,3-DIHYDROISOINDOL-2-YL)PIPÉRIDINE-2,6-DIONE
  申请人：AMPLIO PHARMA LLC

  公开号：WO2013012485A3

  公开（公告）日：2013-04-25
• NOVEL CRYSTALLINE FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE
  申请人：AMPLIO PHARMA, LLC

  公开号：US20140296291A1

  公开（公告）日：2014-10-02

  The invention relates to novel crystalline forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.
• US9540341B2
  申请人：——

  公开号：US9540341B2

  公开（公告）日：2017-01-10
• [EN] SOLID FORMS COMPRISING 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF<br/>[FR] FORMES SOLIDES COMPRENANT DE LA 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISO-INDOL-2-YL)-PIPÉRIDINE-2,6-DIONE ET UN COAGENT DE FORMATION, COMPOSITIONS ET PROCÉDÉS D'UTILISATION CORRESPONDANTS
  申请人：CELGENE CORP

  公开号：WO2014160686A1

  公开（公告）日：2014-10-02

  Provided herein are solid forms comprising (a) 3-(4-amino-l-oxo-l,3- dihydro-isoindol-2-yl)-piperidine-2,6-dione (Lenalidomide) and (b) a coformer. Pharmaceutical compositions comprising the solid forms and methods for treating, preventing and managing various disorders are also disclosed.

  本文提供了包含(a) 3-(4-氨基-1-氧代-1,3-二氢异吲哚-2-基)-哌啶-2,6-二酮（来那度胺）和(b) 辅基的固体形式。还披露了包含这些固体形式的药物组合物以及治疗、预防和管理各种疾病的方法。