N-(2-oxo-1-propan-2-ylpyrimidin-4-yl)acetamide

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-(2-oxo-1-propan-2-ylpyrimidin-4-yl)acetamide
• 化学式: C₉H₁₃N₃O₂
• 分子量: 195.22
• InChiKey: SZPZGPOEUSKUOR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  61.8
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 2'-AZIDO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
  申请人：Girijavallabhan Vinay

  公开号：US20140206640A1

  公开（公告）日：2014-07-24

  The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

  本发明涉及式(I)的2'-叠氮基取代核苷衍生物及其药学上可接受的盐，其中B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-叠氮基取代核苷衍生物的组合物，以及使用这些2'-叠氮基取代核苷衍生物治疗或预防患者HCV感染的方法。
• 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES
  申请人：Girijavallabhan Vinay

  公开号：US20140161770A1

  公开（公告）日：2014-06-12

  The present invention relates to 2′-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Cyano Substituted Nucleoside Derivative, and methods of using the 2′-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

  本发明涉及式(I)的2'-氰基取代核苷衍生物及其药学上可接受的盐，其中B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-氰基取代核苷衍生物的组合物，以及使用这些2'-氰基取代核苷衍生物治疗或预防患者HCV感染的方法。
• Novel Use
  申请人：Nuclera Nucleics Ltd.

  公开号：US20190144905A1

  公开（公告）日：2019-05-16

  The invention relates to the use of an amine masked moiety in a method of enzymatic nucleic acid synthesis. The invention also relates to said amine masked moieties per se and a process for preparing nucleotide triphosphates comprising said amine masked moieties.

  该发明涉及在酶催化核酸合成方法中使用胺掩蔽基团。该发明还涉及该胺掩蔽基团本身以及制备包含该胺掩蔽基团的核苷酸三磷酸盐的方法。
• Nucleotides for the treatment of cancer
  申请人：IDENIX PHARMACEUTICALS LLC

  公开号：US10766917B2

  公开（公告）日：2020-09-08

  The present invention relates to novel nucleoside derivatives, pharmaceutical compositions comprising the compounds, processes of preparation thereof, and methods of use thereof for treating cancer.

  本发明涉及新型核苷衍生物、包含这些化合物的药物组合物、其制备工艺以及用于治疗癌症的方法。
• Synthesis of backbone modified morpholino oligonucleotides and chimeras using phosphoramidite chemistry
  申请人：THE REGENTS OF THE UNIVERSITY OF COLORADO

  公开号：US11230565B2

  公开（公告）日：2022-01-25

  Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

  除了经典的 N,N-二甲基氨基 PMO 类似物之外，本研究还提供了胺取代的吗啉寡核苷酸，以及高效高产合成这些寡核苷酸的方法。具有硫代磷酰胺、磷酰胺和烷基磷酰胺连接体的吗啉寡核苷酸。可以制备含有未修饰 DNA/RNA 和其他 DNA/RNA 类似物的嵌合体。这些寡核苷酸与互补 DNA 或 RNA 形成双链，比天然 DNA 或 DNA/RNA 复合物更稳定，对 RNAse H1 有活性，可使用标准脂质试剂转染细胞。因此，这些类似物可用于多种用途。