S-2-(3-Aminopropylamino)-2-methylpropyldihydrogenphosphorthioat | 23545-68-8

• 分子结构分类: 有机化合物 - 有机硫化合物
• 英文名称: S-2-(3-Aminopropylamino)-2-methylpropyldihydrogenphosphorthioat
• 英文别名: S-2-(3-Amino-propylamino)-2-methyl-propyl-dihydrogenphosphorothioat；[2-(3-Aminopropylamino)-2-methylpropyl]sulfanylphosphonic acid
• CAS: 23545-68-8
• 化学式: C₇H₁₉N₂O₃PS
• 分子量: 242.279
• InChiKey: BIQVLUUDYJRKIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.8
• 重原子数：
  14
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  121
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  N¹-(2-Bromo-1,1-dimethyl-ethyl)-propane-1,3-diamine; hydrobromide 生成 S-2-(3-Aminopropylamino)-2-methylpropyldihydrogenphosphorthioat
  参考文献：
  名称：

  S-2-（ω-氨基烷基氨基）乙基二氢硫代磷酸酯和相关化合物作为潜在的抗辐射剂。

  摘要：

  DOI：

  10.1021/jm00302a010

文献信息

• [EN] CRYSTALLINE AMIFOSTINE COMPOSITIONS AND METHODS FOR THE PREPARATION AND USE OF SAME<br/>[FR] COMPOSITIONS D'AMIFOSTINE CRISTALLINE ET LEURS PROCEDES DE PREPARATION ET D'UTILISATION
  申请人：U.S. BIOSCIENCE, INC.

  公开号：WO1994003179A1

  公开（公告）日：1994-02-17

  (EN) The present invention relates to a sterile, stable vacuum dried crystalline amifostine composition and, optionally, pharmaceutically acceptable excipient(s). Typically, the crystalline compositions of the present invention exhibit enhanced stability at temperatures ranging from about 4 °C to about ambient temperature for a period of at least 2 years relative to existing solid vacuum dried amorphous amifostine preparations. The reconstituted compositions of the present invention are suitable for administration to humans as a radio- or chemoprotecting agent.(FR) L'invention concerne une composition d'amifostine cristalline stérile stable séchée sous vide et, éventuellement, un(des) excipient(s) pharmaceutiquement acceptables. Les compositions cristallines selon l'invention présentent une stabilité supérieure à des températures variant entre environ 4 °C et la température ambiante pendant au moins deux ans par rapport aux préparations d'amifostine amorphes solides séchées sous vide. Les compositions reconstituées selon l'invention peuvent être administrées à l'homme et utilisées en tant qu'agent radio- ou chimioprotecteur.

  本发明涉及一种无菌、稳定的真空干燥结晶阿米福斯汀组合物，以及可能的药用辅料。通常，本发明的结晶组合物在温度从约4°C到大约常温的范围内，相对于现有的固体真空干燥非晶态阿米福斯汀制剂，展现出至少2年的增强稳定性。本发明的重新制备组合物适合作为放射性或化学保护剂用于人类的给药。
• Crystalline amifostine compositions and methods for the preparation and use of same
  申请人：Medimmune Oncology, Inc.

  公开号：EP1243272A2

  公开（公告）日：2002-09-25

  The present invention relates to a sterile, stable vacuum dried crystalline amifostine composition and, optionally, pharmaceutically acceptable excipient(s). Typically, the crystalline compositions of the present invention exhibit enhanced stability at temperatures ranging from about 4°C to about ambient temperature for a period of at least 2 years relative to existing solid vacuum dried amorphous amifostine preparations. The reconstituted compositions of the present invention are suitable for administration to humans as a radio- or chemoprotecting agent.

  本发明涉及一种无菌、稳定的真空干燥结晶阿米福星组合物，以及可选的药学上可接受的赋形剂。通常，相对于现有的固体真空干燥无定形阿米福斯汀制剂，本发明的结晶组合物在从约 4°C 到约环境温度的温度范围内显示出至少 2 年的稳定性。本发明的重构组合物适合作为放射或化学保护剂给人类使用。
• Use of aminothiol compounds for the treatment xerostomia caused by therapeutic agents or radiation
  申请人：Medimmune Oncology, Inc.

  公开号：EP1537861A2

  公开（公告）日：2005-06-08

  The present invention relates to new uses of S-2(3-aminopropylamino)ethyl dihydrogen phosphorothioate (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, or radiation treatment. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.

  本发明涉及 S-2(3-氨丙基氨基)乙基二氢硫代磷酸酯（氨磷汀）和其他氨硫醇化合物在治疗和逆转由治疗剂或放射治疗引起的毒性方面的新用途。特别是，本发明提供了一种治疗与施用化疗药物有关的神经毒性和肾毒性的方法。
• STABLE AMORPHOUS AMIFOSTINE COMPOSITIONS AND DOSAGE FORM
  申请人：——

  公开号：US20020010357A1

  公开（公告）日：2002-01-24

  The present invention relates to a sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and of amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous amifostine.

  本发明涉及一种无菌、稳定的剂型，适用于对患者进行复溶和肠外给药，所述剂型包括无定形氨基烷基二氢硫代磷酸酯，尤其是阿米福斯汀的无定形氨基烷基二氢硫代磷酸酯。本发明还涉及一种制备这种剂型的方法，与现有的真空干燥无定形氨磷汀相比，这种剂型通常具有更强的热稳定性。
• Methods for treatment of neuro- and nephro- disorders and therapeutic toxicities using aminothiol compounds
  申请人：U.S. Bioscience, Inc.

  公开号：US20020132795A1

  公开（公告）日：2002-09-19

  The present invention relates to new uses of S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, radiation treatment or diabetes. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.

  本发明涉及 S-2-(3-氨基丙基氨基)乙基二氢硫代磷酸酯（氨磷汀）和其他氨硫醇化合物治疗和逆转由治疗剂、放射治疗或糖尿病引起的毒性的新用途。特别是，本发明提供了一种治疗与施用化疗药物有关的神经毒性和肾毒性的方法。