metformin malate

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: metformin malate
• 英文别名: metformin malate (2:1)；3-(Diaminomethylidene)-1,1-dimethylguanidine;2-hydroxybutanedioic acid
• 化学式: C₄H₆O₅*2C₄H₁₁N₅
• 分子量: 392.418
• InChiKey: GEKDIAKUBDADFU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.34
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  186
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  盐酸二甲双胍 以 水 为溶剂， 以60.4%的产率得到metformin malate
  参考文献：
  名称：

  [EN] N,N-DIMETHYL IMIDODICARBONIMIDIC DIAMIDE DICARBOXYLATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
  [FR] DIAMIDE DICARBOXYLATE N, N- DIMÉTHYL IMIDODICARBONIMIDIQUE, SON PROCÉDÉ DE PRODUCTION ET COMPOSITIONS PHARMACEUTIQUES LE COMPRENANT

  摘要：

  公开号：

  WO2009038396A3

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。
• A NEW METFORMIN GLYCINATE SALT FOR BLOOD GLUCOSE CONTROL
  申请人：Laboratorios Silanes, S.A. de C.V.

  公开号：EP2303838A1

  公开（公告）日：2011-04-06
• METFORMIN AMINO ACID COMPOUNDS AND METHODS OF USING THE SAME
  申请人：Laboratorios Silanes S.A. DE C.V.

  公开号：US20200222343A1

  公开（公告）日：2020-07-16

  The present invention relates to metformin amino acid compounds (SLNs), pharmaceutical compositions thereof, and methods of using them for the treatment of hyperglycemia, diabetes, and Type 2 diabetes. The compounds can be synthesized using the processes disclosed herein.
• US8076377B2
  申请人：——

  公开号：US8076377B2

  公开（公告）日：2011-12-13
• [EN] A NEW METFORMIN GLYCINATE SALT FOR BLOOD GLUCOSE CONTROL<br/>[FR] NOUVEAU SEL DE METFORMINE GLYCINATE POUR RÉGULATION DE LA GLYCÉMIE
  申请人：SILANES SA DE CV LAB

  公开号：WO2009144527A1

  公开（公告）日：2009-12-03

  In this invention, a new 1,1 -dimethylbiguanide Glycinate salt was synthesised, called metformin Glycinate. This salt exhibits advantages over other metformin salts. These advantages are due, in the first place, to the fact that the glycine counterion exhibits hypoglycaemic effects by itself. Moreover, this salt exhibits more rapid absorption, reaching higher plasma concentrations than those produced with metformin hydrochloride. The synthesis was synthesised from the Metformin Hydrochloride salt, where free Metformin was produced by releasing the hydrochloride counterion, using an ion-exchange column for this purpose; the metformin base released was dissolved in an aqueous medium and, subsequently, glycine was added at ambient temperature under constant stirring; subsequently, the resulting product is heated until a concentrated solution is produced, an organic solvent is added which does not react with the components present and wherein glycine is insoluble in order to create insolubility in the medium and favour crystallisation of the saturated medium; all this in order to precipitate the excess glycine and then separate it by filtering; the filtrate was concentrated again until precipitation of the metformin glycinate salt was achieved.