(S)-4-{2-[4-(1-hydroxymethyl-2-phenyl-ethylamino)-2-oxo-1,2-dihydro-pyridin-3-yl]-7-methyl-3H-benzimidazol-5-yl}-piperazine-1-carboxylic acid ethylamide | 468734-77-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (S)-4-{2-[4-(1-hydroxymethyl-2-phenyl-ethylamino)-2-oxo-1,2-dihydro-pyridin-3-yl]-7-methyl-3H-benzimidazol-5-yl}-piperazine-1-carboxylic acid ethylamide
• 英文别名: N-ethyl-4-[2-[4-[[(2S)-1-hydroxy-3-phenylpropan-2-yl]amino]-2-oxo-1H-pyridin-3-yl]-7-methyl-3H-benzimidazol-5-yl]piperazine-1-carboxamide
• CAS: 468734-77-2
• 化学式: C₂₉H₃₅N₇O₃
• 分子量: 529.642
• InChiKey: PXTIZCPXMSUJIH-NRFANRHFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  39
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  126
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• Novel tyrosine kinase inhibitors
  申请人：——

  公开号：US20040044203A1

  公开（公告）日：2004-03-04

  The present invention provides compounds of formula I 1 and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.

  本发明提供了公式I1的化合物及其药用盐。公式I化合物抑制酪氨酸激酶酶，因此可用作抗癌剂。公式I化合物还可用于治疗其他可以通过抑制酪氨酸激酶酶来治疗的疾病。
• Synergistic methods and compositions for treating cancer
  申请人：——

  公开号：US20040209930A1

  公开（公告）日：2004-10-21

  Combination therapies using IGF1R inhibitors in combination with additional kinase inhibitors are described for the synergistic treatment of cancer.

  描述了使用IGF1R抑制剂与其他激酶抑制剂结合的联合疗法，用于癌症的协同治疗。
• Inhibition of intestinal apical membrane Na/phosphate co-transportation in humans
  申请人：——

  公开号：US20030162753A1

  公开（公告）日：2003-08-28

  The compounds of formula (I) are hydrophilic aryl phosphate, thiophosphate, and aminophosphate intestinal apical membrane Na-mediated phosphate co-transportation inhibitors. The compounds can be administered orally, where they act to inhibit Na-dependent phosphate uptake in the intestines, or internally, where they interact with the phosphate control functions of the kidneys and parathyroid. They are useful for inhibiting sodium-mediated phosphate uptake, reducing serum PTH, calcium, calcitriol, and phosphate, and treating renal disease in an animal, including a human.

  化合物的化学式（I）为亲水性芳基磷酸酯、硫代磷酸酯和氨基磷酸酯，是肠道顶端膜Na介导的磷酸盐共同运输抑制剂。这些化合物可以经口服给药，在肠道中起到抑制Na依赖性磷酸盐摄取的作用，或者内部给药，在肾脏和甲状旁腺的磷酸盐控制功能中发挥作用。它们可用于抑制钠介导的磷酸盐摄取，降低血清PTH、钙、钙三醇和磷酸盐，治疗动物（包括人类）的肾脏疾病。
• [EN] NOVEL TYROSINE KINASE INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE LA TYROSINE KINASE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2002079192A1

  公开（公告）日：2002-10-10

  The present invention provides compounds of formula I[ ] and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.

  本发明提供了I[ ]式化合物及其药学上可接受的盐。I式化合物抑制酪氨酸激酶酶，因此可用作抗癌剂。I式化合物也可用于治疗其他可以通过抑制酪氨酸激酶酶来治疗的疾病。
• Methods for treating IGF1R-inhibitor induced hyperglycemia
  申请人：Carboni M. Joan

  公开号：US20050075358A1

  公开（公告）日：2005-04-07

  Methods for treating cancer using IGF1R inhibitors in combination with insulin sensitizers are provided for the treatment or prevention of hyperglycemia.

  提供了使用 IGF1R 抑制剂与胰岛素增敏剂联合治疗癌症的方法，以治疗或预防高血糖症。