metformin malonate

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: metformin malonate
• 英文别名: 3-(Diaminomethylidene)-1,1-dimethylguanidine;propanedioic acid；3-(diaminomethylidene)-1,1-dimethylguanidine;propanedioic acid
• 化学式: C₃H₄O₄*C₄H₁₁N₅
• 分子量: 233.227
• InChiKey: LYCRHAJQFPEBMH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  166
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  丙二酸 、 二甲双胍 以 甲醇 、 戊醇 为溶剂， 反应 0.25h， 生成 metformin malonate
  参考文献：
  名称：

  Solid-state landscape and biopharmaceutical implications of novel metformin-based salts

  摘要：

  制备出了三种新的二甲双胍盐，从而优化了该药物的药理特征，并使原料药固态格局更加多样化。

  DOI：

  10.1039/d2nj00453d

文献信息

• N,N-DIMETHYL IMIDODICARBONIMIDIC DIAMIDE DICARBOXYLATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
  申请人：KIM Sung Wuk

  公开号：US20100249241A1

  公开（公告）日：2010-09-30

  Disclosed herein are a novel dicarboxylic acid salt of N,N-dimethylimidodicarbonimidic diamide, a preparation method thereof and a pharmaceutical composition comprising the same. More specifically, disclosed herein are a novel dicarboxylic acid salt of N,N-dimethylimidodicarbonimidic diamide, a crystalline acid addition salt prepared by allowing N,N-dimethylimidodicarbonimidic diamide to react with a specific dicarboxylic acid, which has improved physical and chemical properties including solubility, stability, non-hygroscopicity and anti-adhesive properties, and low toxicity, and thus is very effective in the prevention and treatment of not only diabetes and its complications in patients with so-called metabolic syndromes, in which diabetes, obesity, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndromes, etc. appear in combination, but also p53 gene-deficient cancers, muscular pain, muscle cytotoxicity and rhabdomyolysis, as well as a preparation method thereof and a pharmaceutical composition comprising the same.

  本文披露了一种新型的N,N-二甲基咪唑二碳亚胺二羧酸盐，其制备方法以及包含该盐的药物组成物。更具体地说，本文披露了一种新型的N,N-二甲基咪唑二碳亚胺二羧酸盐，通过让N,N-二甲基咪唑二碳亚胺二羧酸与特定二羧酸反应制备的结晶酸加盐，具有改善的物理和化学性质，包括溶解性、稳定性、不吸湿性和抗粘附性，低毒性，因此在预防和治疗不仅糖尿病及其并发症，还包括所谓的代谢综合征患者中非常有效，这些患者同时出现糖尿病、肥胖、高脂血症、脂肪肝、冠心病、骨质疏松、多囊卵巢综合征等，并且在p53基因缺陷癌症、肌肉疼痛、肌肉细胞毒性和横纹肌溶解症的预防和治疗方面也很有效，同时还提供了其制备方法和包含该盐的药物组成物。
• [EN] N,N-DIMETHYL IMIDODICARBONIMIDIC DIAMIDE DICARBOXYLATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME<br/>[FR] DIAMIDE DICARBOXYLATE N, N- DIMÉTHYL IMIDODICARBONIMIDIQUE, SON PROCÉDÉ DE PRODUCTION ET COMPOSITIONS PHARMACEUTIQUES LE COMPRENANT
  申请人：HANALL PHARMACEUTICAL CO LTD

  公开号：WO2009038396A3

  公开（公告）日：2009-05-14
• PHARMACEUTICAL COMPOSITION COMPRISING METFORMIN AND ROSUVASTATIN
  申请人：Bcworld Pharm. Co. Ltd.

  公开号：EP2519240A2

  公开（公告）日：2012-11-07
• COMPOSITION USING METFORMIN FOR PREVENTING OR TREATING IMMUNE DISEASES INCLUDING LUPUS
  申请人：CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION

  公开号：US20150238445A1

  公开（公告）日：2015-08-27

  The present invention relates to a composition for preventing or treating immune diseases through the suppression of B cell activity induced by metformin. More particularly, the present invention relates to a composition comprising a metformin compound or a pharmaceutically acceptable salt thereof as an active ingredient for preventing or treating immune diseases, wherein the composition is characterized by suppression or reduction of B cell activity which is a cause of disease. The present invention can be valuable in the use thereof for various autoimmune diseases as an immunosuppressant which can prevent or treat immune diseases by suppressing or reducing B cell activity and Th17 cell activity, which are causes of disease, or by promoting or increasing regulatory T cell activity.
• COMPOSITION COMPRISING METFORMIN AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING INFLAMMATORY BOWEL DISEASE
  申请人：CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION

  公开号：US20150196511A1

  公开（公告）日：2015-07-16

  The present invention relates to a composition comprising metformin as an active ingredient for preventing or treating inflammatory bowel disease. The metformin compound or the metformin-etanercept (product name: Enbrel) composite according to the present invention may have excellent effects of maintaining the thickness of the small intestine and length of the large intestine normal, inhibiting or decreasing the activity of IL-17 and TNF-a, and promoting or increasing the activity of IFNr, and therefore can be effectively used as a pharmaceutical composition for preventing or treating autoimmune diseases including inflammatory bowel disease.