histidine methylamide | 86541-64-2

• 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
• 英文名称: histidine methylamide
• 英文别名: N-methyl-N-(histidyl)-amine；2-amino-3-(1H-imidazol-4-yl)-N-methylpropanamide；2-amino-3-(1H-imidazol-5-yl)-N-methylpropanamide
• CAS: 86541-64-2
• 化学式: C₇H₁₂N₄O
• mdl: MFCD20491741
• 分子量: 168.198
• InChiKey: BKNRTJJZMZGFEH-UHFFFAOYSA-N

物化性质

• 熔点：
  127-128 °C
• 沸点：
  531.0±45.0 °C(Predicted)
• 密度：
  1.229±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  83.8
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Derivatives of Amphotericin B
  申请人：Revolution Medicines, Inc.

  公开号：US20160304548A1

  公开（公告）日：2016-10-20

  Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3′-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2′epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.

  披露了与AmB相比具有改善的治疗指数的Amphotericin B（AmB）衍生物。这些AmB衍生物包括根据公式（I）的C16脲、碳酸酯和酰胺；根据公式（II）的C3′-取代的C16脲、碳酸酯和酰胺；根据公式（III）的C16酰基；根据公式（IV）的C2′epi-C16脲、碳酸酯和酰胺；以及根据公式（V）的C16噁唑烷酮衍生物。还披露了包括这些AmB衍生物的药物组合物，以及使用这些AmB衍生物的治疗方法。
• DERIVATIVES OF AMPHOTERICIN B
  申请人：Sfunga Therapeutics, Inc.

  公开号：EP3929203A1

  公开（公告）日：2021-12-29

  Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3'-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2'epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.

  本发明公开了两性霉素 B（AmB）的衍生物，其特点是与 AmB 相比，治疗指数有所提高。这些 AmB 衍生物包括根据式（I）的 C16 脲、氨基甲酸酯和酰胺；根据式（II）的 C3'-取代的 C16 脲、氨基甲酸酯和酰胺；根据式（III）的 C16酰基；根据式（IV）的 C2'表-C16 脲、氨基甲酸酯和酰胺；以及根据式（V）的 C16噁唑烷酮衍生物。还公开了包含 AmB 衍生物的药物组合物，以及使用 AmB 衍生物的治疗方法。
• RUTHENIUM(III) COMPLEXES AS ANTINEOPLASTIC AGENTS
  申请人：BOEHRINGER MANNHEIM ITALIA S.P.A.

  公开号：EP0471709B1

  公开（公告）日：1994-11-30
• DISPERSION DE POLYAMINOACIDES DANS UNE PHASE LIPIDIQUE CONTINUE
  申请人：Flamel Technologies

  公开号：EP2101728A1

  公开（公告）日：2009-09-23
• Dispersion of polyamino acids in a continuous lipid phase
  申请人：POULIQUEN Gauthier

  公开号：US20080152675A1

  公开（公告）日：2008-06-26

  The invention relates to injectable pharmaceutical compositions for the prolonged release of at least one active principle, comprising at least one active principle in an aqueous phase of amphiphilic polymer, said aqueous phase being in the form of a dispersion in a continuous lipid phase. The composition is in the form of a water-in-oil emulsion comprising: a pharmaceutically acceptable, continuous lipid phase, an aqueous disperse phase containing at least one amphiphilic polymer and at least one active principle not covalently bonded to said amphiphilic polymer, and at least one pharmaceutically acceptable surfactant.