[(N¹,N¹-dimethylcarbamimidoyl)guanidino]-4-phenyl-1,3,2-dioxaphosphoramidate | 1108717-25-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: [(N¹,N¹-dimethylcarbamimidoyl)guanidino]-4-phenyl-1,3,2-dioxaphosphoramidate
• 英文别名: [(N1,N1-dimethylcarbamimidoyl)guanidino]-4-phenyl-1,3,2-dioxaphosphoramidate；1,1-dimethyl-2-[N'-(2-oxo-4-phenyl-1,3,2lambda5-dioxaphosphinan-2-yl)carbamimidoyl]guanidine；1,1-dimethyl-2-[N'-(2-oxo-4-phenyl-1,3,2λ5-dioxaphosphinan-2-yl)carbamimidoyl]guanidine
• CAS: 1108717-25-4
• 化学式: C₁₃H₂₀N₅O₃P
• 分子量: 325.307
• InChiKey: OSIJJDOPKHRMEJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  116
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  二甲双胍 、 2r-chloro-4t-phenyl-1,3,2-dioxaphosphorinane 2-oxide 在 N-甲基咪唑 作用下， 以 乙腈 为溶剂， 以165 mg的产率得到[(N¹,N¹-dimethylcarbamimidoyl)guanidino]-4-phenyl-1,3,2-dioxaphosphoramidate
  参考文献：
  名称：

  Towards Metformin Prodrugs

  摘要：

  我们合成了第一批可能的二甲双胍原药，并通过光谱方法对其进行了表征。这五种不同类型的化学性质稳定的原药是由二甲双胍和相应的卤化原基制备的。此外，还确定了不稳定衍生物的产物，并讨论了重排的原因。

  DOI：

  10.1055/s-0028-1083603

文献信息

• TREATMENT OF MUSCLE DISEASE CHARACTERIZED BY INSULIN RESISTANCE
  申请人：Megeney Lynn

  公开号：US20120065176A1

  公开（公告）日：2012-03-15

  It is reported herein that certain muscle diseases and conditions, including forms of muscular dystrophy, are characterized by impaired insulin-dependent signaling in the muscle tissue, in essence, a form of insulin resistance. The present disclosure relates to therapeutic agents, compositions and methods for treating a muscle disease or condition characterized by impaired insulin-dependent signaling by targeting components of the defective insulin signaling pathway. The disease or condition may be treated by administering a therapeutic agent that activates the insulin signaling pathway, in particular, therapeutic agents that act post-insulin receptor to modulate intracellular effector molecules. An exemplary modulator is metformin. Metformin may be administered alone or may be co-administered with another therapeutic agent for treating the muscle disease or condition, such as a corticosteroid.

  本文报道了某些肌肉疾病和状况，包括肌肉萎缩症的形式，其特征是肌肉组织中的胰岛素依赖性信号传导受损，本质上是一种胰岛素抵抗形式。本公开涉及治疗剂、组合物和方法，用于治疗肌肉疾病或状况，其特征是通过靶向缺陷胰岛素信号通路的组分来治疗。可以通过给予激活胰岛素信号通路的治疗剂来治疗该疾病或状况，特别是作用于胰岛素受体后来调节细胞内效应分子的治疗剂。一个示例调节剂是二甲双胍。二甲双胍可以单独给予或与另一种用于治疗肌肉疾病或状况的治疗剂一起给予，例如皮质类固醇。
• Combined Pharmaceutical Preparation for Use in Treating Neuromuscular Disorders
  申请人：Universitäts-Kinderspital beider Basel

  公开号：EP2837390A1

  公开（公告）日：2015-02-18

  The present invention relates to a combined pharmaceutical preparation for use in a method for preventing or treating muscular dystrophy, comprising an activator of neuronal nitric oxide synthase, and a nitric oxide precursor, wherein said nitric oxide precursor is convertible by said nitric oxide synthase to nitric oxide

  本发明涉及一种用于预防或治疗肌肉萎缩症方法的组合药物制剂，包括神经元一氧化氮合酶激活剂和一氧化氮前体，其中所述一氧化氮前体可通过所述一氧化氮合酶转化为一氧化氮
• US8993633B2
  申请人：——

  公开号：US8993633B2

  公开（公告）日：2015-03-31
• [EN] COMBINED PHARMACEUTICAL PREPARATION FOR USE IN TREATING NEUROMUSCULAR DISORDERS<br/>[FR] PRÉPARATION PHARMACEUTIQUE COMBINÉE À UTILISER DANS LE TRAITEMENT DE TROUBLES NEUROMUSCULAIRES
  申请人：UNIVERSITÄTS KINDERSPITAL BEIDER BASEL

  公开号：WO2015022386A1

  公开（公告）日：2015-02-19

  The present invention relates to a pharmaceutical combination product for use in a method for preventing or treating muscular dystrophy, particularly Duchenne muscular dystrophy or Becker muscular dystrophy. The combination product comprises an activator of neuronal nitric oxide synthase, and a nitric oxide precursor, particularly metformin and arginine and/or citrulline.
• Towards Metformin Prodrugs
  作者：Kristiina Huttunen、Jukka Leppänen、Eeva Kemppainen、Piia Palonen、Jarkko Rautio、Tomi Järvinen、Jouko Vepsäläinen

  DOI：10.1055/s-0028-1083603

  日期：2008.11

  The first examples of possible metformin prodrugs have been synthesized and characterized by spectroscopic methods. These five different types of chemically stable prodrugs were prepared from metformin and the corresponding halogenated promoieties. The products from unstable derivatives were also identified and reasons for the rearrangements are discussed.

  我们合成了第一批可能的二甲双胍原药，并通过光谱方法对其进行了表征。这五种不同类型的化学性质稳定的原药是由二甲双胍和相应的卤化原基制备的。此外，还确定了不稳定衍生物的产物，并讨论了重排的原因。