4-N-(2,2-difluoro-5,5-dimethyl-1,3,6,7,8,8a-hexahydroindolizin-7-yl)-5-fluoro-2-N-phenylpyrimidine-2,4-diamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚里西啶
• 英文名称: 4-N-(2,2-difluoro-5,5-dimethyl-1,3,6,7,8,8a-hexahydroindolizin-7-yl)-5-fluoro-2-N-phenylpyrimidine-2,4-diamine
• 化学式: C₂₀H₂₄F₃N₅
• 分子量: 391.4
• InChiKey: KIGHHHOJQNRNON-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  53.1
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• Protein Kinase C Inhibitors and Uses Thereof
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20160257681A1

  公开（公告）日：2016-09-08

  This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本公开涉及一类化合物，其可用作蛋白激酶C（PKC）的抑制剂，因此可用于治疗通过PKC活性介导或维持的各种疾病和障碍。本公开还涉及包含这些化合物的制药组合物，使用这些化合物治疗各种疾病和障碍的方法，制备这些化合物和在这些过程中有用的中间体的方法。
• Protein kinase C inhibitors and uses thereof
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US10005777B2

  公开（公告）日：2018-06-26

  This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  本公开涉及的化合物可作为蛋白激酶 C (PKC) 的抑制剂，因此可用于治疗通过 PKC 的活性介导或维持的各种疾病和失调。本公开还涉及包含这些化合物的药物组合物、使用这些化合物治疗各种疾病和失调的方法、制备这些化合物的工艺以及在这些工艺中有用的中间体。
• PROTEIN KINASE C INHIBITORS AND USES THEREOF
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：EP2833889B1

  公开（公告）日：2017-11-01
• US20140275055A1
  申请人：——

  公开号：US20140275055A1

  公开（公告）日：2014-09-18
• US9169249B2
  申请人：——

  公开号：US9169249B2

  公开（公告）日：2015-10-27