amonafide succinate

• 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: amonafide succinate
• 英文别名: 5-Amino-2-[2-(dimethylamino)ethyl]benzo[de]isoquinoline-1,3-dione;butanedioic acid
• 化学式: C₄H₆O₄*C₁₆H₁₇N₃O₂
• 分子量: 401.419
• InChiKey: ALEFKFUOXQZNNR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.52
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  141
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  丁二酸 、 氨萘非特 以 乙醇 、 水 为溶剂， 生成 amonafide succinate
  参考文献：
  名称：

  Amonafide salts

  摘要：

  本发明涉及一种氨酰胺或氨酰胺类似物的盐，其结构式（I）表示为：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烷基或与它们结合的氮原子一起形成非芳香族含氮杂环基；每个R5独立地为—H或C1-C4烷基；R6和R7独立地为H、C1-C4烷基或与它们结合的氮原子一起形成非芳香族含氮杂环基；n为0-3的整数；X−是有机羧酸化合物的羧酸根阴离子。还公开了制备某些结构式（I）所表示的化合物的方法。

  公开号：

  US20030203932A1

文献信息

• Naphthalimide synthesis including amonafide synthesis and pharmaceutical preparations thereof
  申请人：Brown M. Dennis

  公开号：US20050113579A1

  公开（公告）日：2005-05-26

  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，其类似物以及其稳定的液体剂量形式。
• AMONAFIDE SALTS
  申请人：Xanthus Life Sciences, Inc.

  公开号：EP1499595A1

  公开（公告）日：2005-01-26
• COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS INCLUDING SUBSTITUTED NAPHTHALIMIDES SUCH AS AMONAFIDE FOR THE TREATMENT OF IMMUNOLOGICAL, METABOLIC, INFECTIOUS, AND BENIGN OR NEOPLASTIC HYPERPROLIFERATIVE DISEASE CONDITIONS
  申请人：BROWN Dennis M.

  公开号：US20160067241A1

  公开（公告）日：2016-03-10

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.
• [EN] AMONAFIDE SALTS<br/>[FR] SELS D'AMONAFIDE
  申请人：XANTHUS LIFE SCIENCES INC

  公开号：WO2003089415A1

  公开（公告）日：2003-10-30

  Disclosed is a salt of amonafide or amonafide analogs represented Structural Formula (I): R1 is-(CH2)nN+HR3R4 X- or R1 is -(CH2)nN+Hr3r4 X- or -(CH2)nNR3R4 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).
• [EN] COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS INCLUDING SUBSTITUTED NAPHTHALIMIDES SUCH AS AMONAFIDE FOR THE TREATMENT OF IMMUNOLOGICAL, METABOLIC, INFECTIOUS, AND BENIGN OR NEOPLASTIC HYPERPROLIFERATIVE DISEASE CONDITIONS<br/>[FR] COMPOSITIONS ET PROCÉDÉS PERMETTANT D'AMÉLIORER LE BÉNÉFICE THÉRAPEUTIQUE DES COMPOSÉS CHIMIQUES ADMINISTRÉS DE MANIÈRE SUBOPTIMALE COMPRENANT DES NAPHTALIMIDES SUBSTITUÉS TELS QUE L'AMONAFIDE POUR LE TRAITEMENT DES MALADIES IMMUNOLOGIQUES, MÉTABOLIQUES, INFECTIEUSES ET INFECTIEUSES OU HYPERPROLIFÉRATIVES ET NÉOPLASTIQUES.
  申请人：BROWN DENNIS M

  公开号：WO2014179528A2

  公开（公告）日：2014-11-06

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.