6-Chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1,2-benzoxazin-3-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: 6-Chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1,2-benzoxazin-3-one
• 英文别名: 6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1,2-benzoxazin-3-one
• 化学式: C₁₄H₉ClF₃NO₂
• 分子量: 315.67
• InChiKey: GUXQGDFVDWQJQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• HIGHLY LOADED AMORPHOUS EFAVIRENZ COMPOSITION AND PROCESS FOR PREPARING THE SAME
  申请人：ISP Investments Inc.

  公开号：US20140148449A1

  公开（公告）日：2014-05-29

  A stable and high loading ternary solid dispersion composition comprising (a) about 50% wt. to about 90% wt. of amorphous Efavirenz; (b) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone (PVP), a first polymer; (c) about 1% wt. to about 30% wt. of a water-soluble second polymer; and (d) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Also discloses a high loading ternary composition comprising (a) a solid dispersion composition comprising (i) about 50% wt. to about 90% wt. of amorphous Efavirenz; (ii) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone, a first polymer; (b) about 1% wt. to about 30% wt. of a water-soluble second polymer blended with solid dispersion of composition of (a); and (c) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Additionally discloses a method for preparing solid dosage forms comprising (i) amorphous Efavirenz and (ii) polyvinyl pyrrolidone (PVP), a first polymer; (iii) a water-soluble second polymer; and (iv) optionally, at least one pharmaceutical excipients.
• US9114170B2
  申请人：——

  公开号：US9114170B2

  公开（公告）日：2015-08-25