N-[2-[(E)-1-aminoethylideneamino]oxyethyl]-2-[3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxopyrazin-1-yl]acetamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: N-[2-[(E)-1-aminoethylideneamino]oxyethyl]-2-[3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxopyrazin-1-yl]acetamide
• 化学式: C₁₉H₂₄F₂N₆O₃
• 分子量: 422.4
• InChiKey: MVTKCLQDNRFSFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  30
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  121
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• N-[2-[[(DIAMINOMETHYLENE)AMINO]OXY]ETHYL]-3-[(2,2-DIFLUORO-2-PHENYLETHYL)AMINO]-6-METHYL-2-OXO-1(2H)-PYRAZINEACETAMIDE
  申请人：Patel N. Mitul

  公开号：US20080021044A1

  公开（公告）日：2008-01-24

  The present invention is directed to N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-s-oxo-1(2H)-pyrazineacetamide, pharmaceutical compositions containing said compound and methods of treatment comprising inhibiting a serine protease using said compound. The present invention is further directed to a process for the preparation of the N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide as a free base. The present invention is further directed to a process for the preparation of pharmaceutically acceptable salts of N-[2-[[(aminoiminomethyl)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2H)-pyrazineacetamide.

  本发明涉及一种N-[2-[[(二氨基甲基)氨基]氧基]乙基]-3-[(2,2-二氟-2-苯乙基)氨基]-6-甲基-2-氧代-1(2H)-吡嗪乙酰胺化合物，含有该化合物的制药组合物以及使用该化合物抑制丝氨酸蛋白酶的治疗方法。本发明还涉及一种制备N-[2-[[(二氨基甲基)氨基]氧基]乙基]-3-[(2,2-二氟-2-苯乙基)氨基]-6-甲基-2-氧代-1(2H)-吡嗪乙酰胺自由碱的方法。本发明还涉及一种制备N-[2-[[(氨基亚甲基)氨基]氧基]乙基]-3-[(2,2-二氟-2-苯乙基)氨基]-6-甲基-2-氧代-1(2H)-吡嗪乙酰胺药用可接受盐的方法。
• GASTRORETENTIVE SUSTAINED RELEASE FORMULATIONS
  申请人：Wang W. Wenhua

  公开号：US20070269512A1

  公开（公告）日：2007-11-22

  The present invention is directed to a gastroretentive sustained release formulation, processes for preparing said gastroretentive sustained release formulation and the use thereof.