1-(二硫代羧基)-L-脯氨酸 | 7250-31-9

• 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
• 中文名称: 1-(二硫代羧基)-L-脯氨酸
• 英文名称: Proline dithiocarbamate
• 英文别名: carbamodithioic acid;(2S)-pyrrolidine-2-carboxylic acid
• CAS: 7250-31-9
• 化学式: C6H12N2O2S2
• 分子量: 208.3
• InChiKey: SDHWCDDSZTZOQC-WCCKRBBISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.02
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  108
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• Therapeutic methods employing disulfide derivatives of dithiocarbamates and compositions useful therefor
  申请人：Medinox, Inc.

  公开号：US20030181495A1

  公开（公告）日：2003-09-25

  The present invention provides novel combinations of dithiocarbamate disulfide dimers with other active agents. In one method, the disulfide derivative of a dithiocarbamate is coadministered with a thiazolidinedione for the treatment of diabetes. In another embodiment, In another embodiment, invention combinations further comprise additional active agents such as, for example, metformin, insulin, sulfonylureas, and the like. In another embodiment, the present invention relates to compositions and formulations useful in such therapeutic methods.

  本发明提供了二硫代氨基甲酸盐二硫化二聚体与其他活性药剂的新组合。在一种方法中，二硫代氨基甲酸盐的二硫化衍生物与噻唑烷二酮联合用于治疗糖尿病。在另一实施例中，该发明的组合进一步包括额外的活性药剂，例如二甲双胍、胰岛素、磺酰脲类药物等。在另一实施例中，本发明涉及用于这种治疗方法的组合物和配方。
• [EN] METHOD FOR PREPARATION OF PHARMACEUTICAL-GRADE DISULFIDE OF DITHIOCARBAMATES<br/>[FR] PROCEDE PERMETTANT LA PREPARATION DE DERIVES DISULFURE DE CLASSE PHARMACEUTIQUE DE DITHIOCARBAMATES
  申请人：MEDINOX INC

  公开号：WO2003099784A1

  公开（公告）日：2003-12-04

  In accordance with the present invention, there are provided methods for producing pharmaceutical-grade dithiocarbamates and disulfide derivatives thereof. Invention methods are preferably conducted under sterile conditions, thereby producing a sterile pharmaceutical-grade disulfide derivative of a dithiocarbamate. In one embodiment, the invention method comprises vigorously contacting a mixture of carbon disulfide, at least one secondary amine, and a pharmaceutically acceptable diluent in a mixing zone under an inert gas atmosphere, wherein the diluent is a solvent for the carbon disulfide, but not for the dithiocarbamate. The invention method further comprises contracting the resulting reaction mixture with an oxidizing agent under conditions suitable to convert dithiocarbamate into the disulfide derivative thereof.

  根据本发明，提供了生产药品级二硫代氨基甲酸盐及其二硫化物衍生物的方法。发明方法最好在无菌条件下进行，从而产生一种无菌的药品级二硫化物衍生物。在一种实施例中，本发明方法包括在惰性气氛下，在混合区中强烈接触碳二硫化物、至少一种二级胺和药用可接受稀释剂的混合物中，其中稀释剂是碳二硫化物的溶剂，但不是二硫代氨基甲酸盐的溶剂。本发明方法还包括在适宜的条件下，将反应产物与氧化剂接触，以将二硫代氨基甲酸盐转化为其二硫化物衍生物。
• Use of nitric oxide scavengers to treat side effects caused by therapeutic administration of sources of nitric oxide
  申请人：——

  公开号：US20010056108A1

  公开（公告）日：2001-12-27

  Nitric oxide scavengers, such as dithiocarbamate-containing compounds, are used to reduce side effects caused by therapeutic administration of nitric oxide sources by administering the nitric oxide scavenger(s) to the subject after the therapeutic effect of the nitric oxide source has been achieved. For example, the nitric oxide source can be coadministered with the nitric oxide scavenger, with the latter formulated in a time release vehicle selected to delay release of the scavenger for a period of time sufficient to ensure that the therapeutic goal of the nitric oxide source has been achieved before release of the scavenger. Formulations and kits, including a bubble pack with pairwise arrangement of unit doses of a desired nitric oxide source and nitric oxide scavenger, are also provided. The side effects of sildenafil citrate (Viagra®), or of simultaneous administration of such a nitric oxide source in combination with another, such as nitroglycerin, are effectively controlled by the methods, formulations and kits of the invention.

  一氧化氮清除剂，如含二硫代氨基甲酸盐的化合物，可用于减少一氧化氮源治疗给药引起的副作用，方法是在一氧化氮源的治疗效果达到后再给受试者使用一氧化氮清除剂。例如，可以将一氧化氮源与一氧化氮清除剂联合给药，后者配制在一种经选择的定时释放载体中，以将清除剂的释放延迟一段时间，足以确保在清除剂释放之前一氧化氮源的治疗目标已经实现。此外，还提供了配方和试剂盒，包括将所需一氧化氮源和一氧化氮清除剂的单位剂量成对排列的气泡袋。本发明的方法、制剂和试剂盒可有效控制枸橼酸西地那非（万艾可®）的副作用，或同时服用这种一氧化氮源和另一种一氧化氮源（如硝酸甘油）的副作用。
• Conjugates of dithiocarbamates with pharmacologically active agents and uses therefor
  申请人：Medinox, Inc.

  公开号：US20030087840A1

  公开（公告）日：2003-05-08

  In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.

  根据本发明，提供了一氧化氮清除剂（如二硫代氨基甲酸盐或 "DC"）和药理活性剂（如非甾体抗炎药）的共轭物。本发明共轭物提供了一类新的药理活性制剂（如消炎药），由于本文所述对药理活性制剂的改性所带来的保护作用，其副作用发生率大大降低。此外，本发明共轭物比未经改性的药理活性剂更有效，因为当本发明共轭物被裂解时，除了游离的药理活性剂外，一氧化氮清除剂（如二硫代氨基甲酸盐）也会同时产生，从而保护与药理活性剂接触的细胞和组织免受一氧化氮过量产生的潜在破坏作用。
• CONJUGATES OF DITHIOCARBAMATES WITH PHARMACOLOGICALLY ACTIVE AGENTS AND USES THEREFOR
  申请人：Medinox, Inc.

  公开号：EP1001932A1

  公开（公告）日：2000-05-24