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

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N,N'-bis-[2-(1H-imidazol-4-yl)ethyl]propanediamide
• 英文别名: bis-1,3-(N^β-histaminyl)malonic acid；US11845740, No IV；N,N'-bis[2-(1H-imidazol-5-yl)ethyl]propanediamide
• 化学式: C₁₃H₁₈N₆O₂
• 分子量: 290.325
• InChiKey: MWORBFIKQWWKQH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  21
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 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 、 丙二酸二乙酯 以44%的产率得到N,N'-bis-[2-(1H-imidazol-4-yl)ethyl]propanediamide
  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

• ATTENUATED INFLUENZA VECTORS FOR THE PREVENTION AND/OR TREATMENT OF INFECTIOUS DISEASES AND FOR THE TREATMENT OF ONCOLOGICAL DISEASES
  申请人：«PHARMENTERPRISES BIOTECH» LIMITED LIABILITY COMPANY

  公开号：EP3382010A2

  公开（公告）日：2018-10-03

  The present invention relates to the field of medicine and virology. An attenuated influenza A virus, an influenza virus vector based thereon, and a pharmaceutical composition comprising thereof are provided, which can be used for the prevention and/or treatment of an infectious disease. In addition, the present invention relates to an attenuated influenza A virus, an influenza virus vector based thereon, and a pharmaceutical composition comprising thereof, which can be used for the treatment of oncological diseases.

  本发明涉及医学和病毒学领域。本发明提供了一种减毒甲型流感病毒、以其为基础的流感病毒载体以及由其组成的药物组合物，可用于预防和/或治疗传染病。此外，本发明还涉及一种可用于治疗肿瘤疾病的减毒甲型流感病毒、以其为基础的流感病毒载体以及由其组成的药物组合物。
• 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。
• Attenuated influenza vectors for the prevention and/or treatment of infectious diseases and for the treatment of oncological diseases
  申请人：PHARMENTERPRISES BIOTECH Limited Liability Company

  公开号：US10392604B2

  公开（公告）日：2019-08-27

  The present invention relates to the field of medicine and virology. An attenuated influenza A virus, an influenza virus vector based thereon, and a pharmaceutical composition comprising thereof are provided, which can be used for the prevention and/or treatment of an infectious disease. In addition, the present invention relates to an attenuated influenza A virus, an influenza virus vector based thereon, and a pharmaceutical composition comprising thereof, which can be used for the treatment of oncological diseases.

  本发明涉及医学和病毒学领域。本发明提供了一种减毒甲型流感病毒、以其为基础的流感病毒载体以及由其组成的药物组合物，可用于预防和/或治疗传染病。此外，本发明还涉及一种可用于治疗肿瘤疾病的减毒甲型流感病毒、以其为基础的流感病毒载体以及由其组成的药物组合物。
• USE OF A BISAMIDE DERIVATIVE OF MALONIC ACID FOR TREATING ALLERGIC AND OTHER DISEASES IN HUMANS AND ANIMALS
  申请人：PHARMENTERPRISES ALLERGY LLC

  公开号：US20210361624A1

  公开（公告）日：2021-11-25

  The invention relates to the therapy of diseases associated with the activity of histamine receptors, in particular for the treatment of allergic diseases, preferably the therapy of perennial and persistent allergic rhinitis, itch, as well as a number of other diseases associated with the activity of histamine receptor type 3 and/or 4, using compound N,N′-bis(2-(1H-imidazol-5-yl)ethyl)malonamide. This compound, as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, is an antagonist of histamine receptor type 3 and/or 4. The invention also relates to pharmaceutical compositions containing a therapeutically effective amount of Compound I.
• [EN] NOVEL METHOD FOR PRODUCING N,N'-BIS[2-(1Н-IMIDAZOL-4-YL)ETHYL]MALONAMIDE<br/>[FR] NOUVEAU PROCÉDÉ DE PRODUCTION DE N,N'-BIS[2-(1H-IMIDAZOL-4-IL)ÉTHYL]MALONAMIDE<br/>[RU] НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ N,N'-БИС[2-(1Н-ИМИДАЗОЛ-4-ИЛ)ЭТИЛ]МАЛОНАМИДА
  申请人：OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU PHARMENTERPRISES

  公开号：WO2020091632A1

  公开（公告）日：2020-05-07

  Способ получения N,N'-бис[2-(1Н-имидазол-4-ил)этил]малонамида формулы (I) реакцией диметилмалоната с гистамином в полярном органическом 5 растворителе при температуре 85-120°С, включающий стадию кристаллизации из воды и/или полярного органического растворителя. Способ позволяет получать продукт чистотой от 99, 0 мас% и пригоден для получения субстанции в фармацевтической промышленности.