N,N'-bis-[2-(1H-imidazol-4-yl)ethyl]ethanediamide

• 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: N,N'-bis-[2-(1H-imidazol-4-yl)ethyl]ethanediamide
• 英文别名: bis-1,2-(N^β-histaminyl)oxalic acid；US11845740, No I；N,N'-bis[2-(1H-imidazol-5-yl)ethyl]oxamide
• 化学式: C₁₂H₁₆N₆O₂
• 分子量: 276.298
• InChiKey: SRJWMAXOCIEGRK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  20
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  116
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  组胺 、 草酸二乙酯 以 异戊醇 为溶剂， 反应 4.0h， 以72%的产率得到N,N'-bis-[2-(1H-imidazol-4-yl)ethyl]ethanediamide
  参考文献：
  名称：

  DICARBOXYLIC ACID BISAMIDE DERIVATIVES, USE THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON AND METHODS FOR PRODUCING DICARBOXYLIC ACID BISAMIDE DERIVATIVES

  摘要：

  本发明涉及一种新型生物活性化合物，特别是一般式I的二羧酸双酰胺衍生物，或其药学上可接受的盐，能够与金属离子形成络合物或螯合物。该发明还涉及所述化合物作为预防和/或治疗心血管、病毒性、癌症、神经退行性和炎症性疾病、糖尿病、与年龄相关的疾病、微生物毒素引起的疾病、酗酒和酒精性肝硬化、贫血、皮肤坏疽性卟啉病和过渡金属盐中毒的药剂。本发明还涉及制备一般式I的二羧酸双酰胺衍生物的新方法。

  公开号：

  US20160031858A1

文献信息

• NOVEL GLUTAMINYL CYCLASE INHIBITORS AND THE USE THEREOF IN TREATMENT OF VARIOUS DISEASES
  申请人：Obschestvo S Ogranichennoi Otvetstvennostiyu "Pharmenterprises"

  公开号：EP3632433A1

  公开（公告）日：2020-04-08

  The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) wherein R1 is -C(O)-R2-C(O)- or -R2-C(O)- group, where R2 is -(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl, n is an integer from 0 to 4; wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system. This invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compounds of formula (A) as defined above.

  本发明涉及有机物化学、药理学和医学，通过使用式 (A) 化合物治疗与免疫系统细胞异常活动有关的疾病，特别是治疗肺部、呼吸道和腹部疾病、放射病和疼痛综合征以及其他疾病。 其中 R1 是-C(O)-R2-C(O)-或-R2-C(O)-基团，其中 R2 是任选被一个或两个 C1-C6 烷基或苯基取代的-(CH2)n-基团、 n 是 0 至 4 的整数； 其中化合物选自描述中所列的化合物组。这些化合物及其药学上可接受的盐类在抑制谷氨酰胺环化酶方面非常有效，谷氨酰胺环化酶尤其参与趋化因子的翻译后修饰过程以及单核细胞、巨噬细胞和免疫系统其他细胞的趋化过程。本发明还涉及药物组合物，其中包含治疗有效量的如上定义的式 (A) 化合物。
• DICARBOXYLIC ACID BISAMIDE DERIVATIVES, USE THEREOF, PHARMACEUTICAL COMPOSITION BASED THEREON AND METHODS FOR PRODUCING DICARBOXYLIC ACID BISAMIDE DERIVATIVES
  申请人：OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"

  公开号：US20160031858A1

  公开（公告）日：2016-02-04

  The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I: or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.

  本发明涉及一种新型生物活性化合物，特别是一般式I的二羧酸双酰胺衍生物，或其药学上可接受的盐，能够与金属离子形成络合物或螯合物。该发明还涉及所述化合物作为预防和/或治疗心血管、病毒性、癌症、神经退行性和炎症性疾病、糖尿病、与年龄相关的疾病、微生物毒素引起的疾病、酗酒和酒精性肝硬化、贫血、皮肤坏疽性卟啉病和过渡金属盐中毒的药剂。本发明还涉及制备一般式I的二羧酸双酰胺衍生物的新方法。