3-((2,2-dimethylpiperidin-1-yl)methyl)-N-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)isothiazol-5-amine | 1094070-27-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡嗪类
• 英文名称: 3-((2,2-dimethylpiperidin-1-yl)methyl)-N-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)isothiazol-5-amine
• 英文别名: 3-[(2,2-dimethylpiperidin-1-yl)methyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
• CAS: 1094070-27-5
• 化学式: C₂₁H₂₆N₈S
• 分子量: 422.557
• InChiKey: VNVLNNHKVAWQGQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  115
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  在 盐酸 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 生成 3-((2,2-dimethylpiperidin-1-yl)methyl)-N-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)isothiazol-5-amine
  参考文献：
  名称：

  Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors

  摘要：

  We report a series of potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Optimization of the solvent accessible 8-position led to improvements in both oral bioavailability and off-target kinase inhibition. Compound 25 demonstrates anti-tumor activity in an A2780 ovarian tumor xenograft model. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.08.140

文献信息

• Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer
  申请人：Wang Yaolin

  公开号：US20110129456A1

  公开（公告）日：2011-06-02

  The present invention relates to the sequential administration of a cytotoxic agent followed by an IGF1R antagonist (e.g., an antibody) for the treatment of hyperproliferative disorders including cancer.

  本发明涉及采用细胞毒性药物后接IGF1R拮抗剂（例如抗体）的顺序治疗高增殖性疾病，包括癌症。
• [EN] SEQUENTIAL ADMINISTRATION OF CHEMOTHERAPEUTIC AGENTS FOR TREATMENT OF CANCER<br/>[FR] ADMINISTRATION SÉQUENTIELLE D'AGENTS DE CHIMIOTHÉRAPIE POUR LE TRAITEMENT DU CANCER
  申请人：SCHERING CORP

  公开号：WO2009137378A2

  公开（公告）日：2009-11-12

  The present invention relates to the sequential administration of a cytotoxic agent followed by an IGF1R antagonist (e.g., an antibody) for the treatment of hyperproliferative disorders including cancer.