US10202370, Example 046

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: US10202370, Example 046
• 英文别名: N-[6-methyl-2-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-1H-benzimidazol-5-yl]-4-pyridin-4-yl-1,3-thiazol-2-amine
• 化学式: C₂₈H₂₉N₇S
• 分子量: 495.6
• InChiKey: PXLWFWUOFKTKDA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  36
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• BENZIMIDAZOLE DERIVATIVES AS SELECTIVE PROTEINE KINASE INHIBITORS
  申请人：AB SCIENCE

  公开号：US20160152608A1

  公开（公告）日：2016-06-02

  Disclosed are compounds of formula I or pharmaceutically acceptable salts thereof: Wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , A, Q and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.

  公开了式I的化合物或其药学上可接受的盐：其中n，R1，R2，R3，R4，R5，A，Q和X如描述中所定义。这些化合物可以选择性地调节、调控和/或抑制某些与细胞增殖、代谢、过敏和退行性疾病有关的天然和/或突变蛋白激酶介导的信号转导。更具体地说，这些化合物是有效且选择性的天然和/或突变c-kit抑制剂。
• Benzimidazole derivatives as selective proteine kinase inhibitors
  申请人：AB SCIENCE

  公开号：US10202370B2

  公开（公告）日：2019-02-12

  Disclosed are compounds of formula I or pharmaceutically acceptable salts thereof: Wherein n, R1, R2, R3, R4, R5, A, Q and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.

  所公开的是式 I 化合物或其药学上可接受的盐类： 其中 n、R1、R2、R3、R4、R5、A、Q 和 X 如描述中所定义。这些化合物可选择性地调节、调节和/或抑制由某些原生和/或突变蛋白激酶介导的信号转导，这些信号转导与多种人类和动物疾病有关，如细胞增殖性疾病、代谢性疾病、过敏性疾病和退行性疾病。更特别的是，这些化合物是强效和选择性的原生和/或突变 c-kit 抑制剂。
• BENZIMIDAZOLE DERIVATIVES AS SELECTIVE PROTEIN KINASE INHIBITORS
  申请人：AB Science

  公开号：EP3010906B1

  公开（公告）日：2019-06-12