1-Fluoro-4-methyl-1,1-diphenylpentan-2-amine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-Fluoro-4-methyl-1,1-diphenylpentan-2-amine
• 化学式: C₁₈H₂₂FN
• 分子量: 271.4
• InChiKey: PDTGGQHFGXMDGP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX
  申请人：THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

  公开号：US20160215012A1

  公开（公告）日：2016-07-28

  Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

  提供了一些特定的两性霉素B（AmB）衍生物，其具有降低毒性和保留抗真菌活性的特点。其中一些衍生物是AmB的C16脲衍生物。其中一些衍生物是AmB的C3、C5、C8、C9、C11、C13或C15去氧衍生物。其中一些衍生物包括对AmB的甲氨葡萄糖胺附属物的C3′或C4′修饰。还提供了制备该发明的AmB衍生物的方法，包括该发明的AmB衍生物的药物组合物，以及该发明的AmB衍生物的使用方法。
• [EN] CONCISE SYNTHESIS OF UREA DERIVATIVES OF AMPHOTERICIN B<br/>[FR] SYNTHÈSE CONCISE DE DÉRIVÉS D'URÉE D'AMPHOTÉRICINE B
  申请人：UNIV ILLINOIS

  公开号：WO2016112260A1

  公开（公告）日：2016-07-14

  Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti -fungal activity. Certain of the derivatives are C16 urea derivatives and C16 carbamate derivatives of AmB. Also provided are methods of making the AmB derivatives.

  提供了某些特征为降低毒性并保留抗真菌活性的两性霉素B（AmB）衍生物。其中某些衍生物是AmB的C16脲衍生物和C16氨基甲酸酯衍生物。还提供了制备AmB衍生物的方法。
• Amphotericin B derivatives with improved therapeutic index
  申请人：The Board of Trustees of the University of Illinois

  公开号：US10323057B2

  公开（公告）日：2019-06-18

  Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

  本文提供了两性霉素 B（AmB）的某些衍生物，其特点是毒性降低，抗真菌活性保持不变。其中某些衍生物是 AmB 的 C16 脲衍生物。某些衍生物是 AmB 的 C3、C5、C8、C9、C11、C13 或 C15 脱氧核衍生物。某些衍生物包括 AmB 的霉菌胺附属物的 C3′或 C4′修饰。此外，还提供了制造本发明AmB衍生物的方法、包含本发明AmB衍生物的药物组合物以及本发明AmB衍生物的使用方法。
• CONCISE SYNTHESIS OF UREA DERIVATIVES OF AMPHOTERICIN B
  申请人：The Board of Trustees of the University of Illinois

  公开号：EP3242554A1

  公开（公告）日：2017-11-15
• [EN] AMPHOTERICIN B DERIVATIVES WITH IMPROVED THERAPEUTIC INDEX<br/>[FR] DÉRIVÉS D'AMPHOTÉRICINE B AYANT UN INDICE THÉRAPEUTIQUE AMÉLIORÉ
  申请人：UNIV ILLINOIS

  公开号：WO2015054148A1

  公开（公告）日：2015-04-16

  Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3' or C4' modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.