2HCl amonafide | 135862-48-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: 2HCl amonafide
• 英文别名: amonafide hydrochloride；amonafide monohydrochloride；5-amino-2-[2-(dimethylamino)ethyl]benzo[de]isoquinoline-1,3-dione;hydrochloride
• CAS: 135862-48-5
• 化学式: C₁₆H₁₇N₃O₂*ClH
• 分子量: 319.791
• InChiKey: DFXVLDIRUFRLAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.0
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  66.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  氨萘非特 在 盐酸 作用下， 以 四氢呋喃 为溶剂， 生成 2HCl amonafide
  参考文献：
  名称：

  [EN] NAPHTHALIMIDE SYNTHESIS INCLUDING AMONAFIDE SYNTHESIS AND PHARMACEUTICAL PREPARATIONS THEREOF
  [FR] SYNTHESE DE NAPHTALIMIDES, Y COMPRIS D'AMONAFIDES, ET PREPARATIONS PHARMACEUTIQUES LES CONTENANT

  摘要：

  本发明涉及一种合成萘酰亚胺和米托那菲类似物及其盐的新方法。还包括新的组合物，包括萘酰亚胺和萘酰亚胺盐、类似物及其稳定的液态剂型。

  公开号：

  WO2004004716A1

文献信息

• Naphthalimide synthesis including amonafide synthesis and pharmaceutical preparations thereof
  申请人：ChemGenex Therapeutics, Inc.

  公开号：US20040082788A1

  公开（公告）日：2004-04-29

  The present invention concerns novel methods for the synthesis of naphthalimides and mitonafide analogs, as well as salts thereof. Also included are novel compositions, including naphthalimides and naphthalimide salts, analogs thereof, as well as stable liquid dosage forms thereof.

  本发明涉及一种合成萘酰亚胺和mitonafide类似物及其盐的新方法。还包括新的组合物，包括萘酰亚胺和萘酰亚胺盐，类似物以及其稳定的液态剂量形式。
• Amonafide salts
  申请人：Xanthus Life Sciences, Inc.

  公开号：US20040132763A1

  公开（公告）日：2004-07-08

  Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): 1 R1 is —(CH 2 ) n N + HR3R4 X − or R1 is —(CH 2 ) n N + HR3R4 X − or —(CH 2 ) n NR3R4 when R2 is —N + HR6R7. R2 is —OR5, halogen, —NR6R7, —N + HR6R7 X −, sulphonic acid, nitro, —NR5COOR5, —NR5COR5 or —OCOR5; R3 and R4 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; each R5 is independently —H or a C1-C4 alkyl group; R6 and R7 are independently H, C1-C4 alkyl group or, taken together with the nitrogen atom to which they are bonded, a non-aromatic nitrogen-containing heterocyclic group; n is an integer from 0-3; and X − is the carboxylate anion of an organic carboxylic acid compound. Also disclosed are methods of preparing certain compounds represented by Structural Formula (I).

  本文揭示了一种氨咪非德盐或氨咪非德类似物的盐，其结构式表示为（I）：其中1R1为—（CH2）nN+HR3R4 X−或R1为—（CH2）nN+HR3R4 X−或—（CH2）nNR3R4，当R2为—N+HR6R7时。R2为—OR5，卤素，—NR6R7，—N+HR6R7 X−，磺酸，硝基，—NR5COOR5，—NR5COR5或—OCOR5；R3和R4独立地为H，C1-C4烷基或与它们连接的氮原子一起形成非芳香氮杂环基团；每个R5独立地为—H或C1-C4烷基；R6和R7独立地为H，C1-C4烷基或与它们连接的氮原子一起形成非芳香氮杂环基团；n为0-3的整数；X−是有机羧酸化合物的羧酸根阴离子。本文还揭示了制备某些结构式（I）化合物的方法。
• Amonafide salts and compositions comprising same
  申请人：ChemGenex Pharmaceuticals, Inc.

  公开号：EP2305257A1

  公开（公告）日：2011-04-06

  The present invention concerns novel methods for the synthesis of napthalimides and mitonafide analogs, as well as salts thereof. Also included are novel compositions, including napthalimides and napthalimide salts, analogs thereof, as well as stable liquid dosage forms thereof.

  本发明涉及合成萘啶酰亚胺和螨酰亚胺类似物及其盐类的新方法。本发明还包括新型组合物，包括萘啶酰亚胺和萘啶酰亚胺盐、其类似物及其稳定的液体剂型。
• Naphthalimide dosing by N-acetyl transferase genotyping
  申请人：Brown M. Dennis

  公开号：US20050192312A1

  公开（公告）日：2005-09-01

  The present invention provides methods for dosing patients with naphthalimides, including amonafide, amonafide salts, and analogs thereof based on N-acetyl transferase genotyping. The invention also provides methods for dosing the amount of granulocyte colony stimulating factor (GCSF) used in combination with naphthalimide to prevent or modulate leukocytopenia.

  本发明提供了基于N-乙酰转移酶基因分型的萘啶酰亚胺类药物（包括氨酰胺、氨酰胺盐及其类似物）的患者用药方法。本发明还提供了粒细胞集落刺激因子（GCSF）与萘酞酰亚胺联合使用以预防或调节白细胞减少症的剂量方法。
• Methods of treating cellular proliferative disease using naphthalimide and PARP-1 inhibitors
  申请人：Brown M. Dennis

  公开号：US20050288310A1

  公开（公告）日：2005-12-29

  A method of treating a cellular proliferative in a patient through the use of a naphthalimide and a PARP-1 inhibitor is disclosed. In a one embodiment, the naphthalimide is amonafide or an analog thereof.

  本发明公开了一种通过使用萘啶酰亚胺和 PARP-1 抑制剂治疗患者细胞增生的方法。在一个实施方案中，萘啶酰亚胺是氨酰亚胺或其类似物。