N-[2-methoxy-5-(4-methyl-6-morpholin-4-ylpyrimidin-5-ylethynyl)-pyridin-3-yl]-methylsulfonamide | 1391978-97-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-[2-methoxy-5-(4-methyl-6-morpholin-4-ylpyrimidin-5-ylethynyl)-pyridin-3-yl]-methylsulfonamide
• 英文别名: N-[2-methoxy-5-(4-methyl-6-morpholin-4-yl-pyrimidin-5-ylethynyl)-pyridin-3-yl]-methylsulfonamide；N-[2-methoxy-5-[2-(4-methyl-6-morpholin-4-ylpyrimidin-5-yl)ethynyl]pyridin-3-yl]methanesulfonamide
• CAS: 1391978-97-4
• 化学式: C₁₈H₂₁N₅O₄S
• 分子量: 403.462
• InChiKey: CIFIUOLPDLVUBV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  115
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  5-溴-2-氯-3-硝基吡啶 在 吡啶 、 bis-triphenylphosphine-palladium(II) chloride 、 copper(l) iodide 、 tin(II) chloride dihydrate 、 三乙胺 作用下， 以 甲醇 、 二氯甲烷 、 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 N-[2-methoxy-5-(4-methyl-6-morpholin-4-ylpyrimidin-5-ylethynyl)-pyridin-3-yl]-methylsulfonamide
  参考文献：
  名称：

  5-Alkynyl-pyridines

  摘要：

  这项发明涉及一般式(I)的5-炔基吡啶 它们作为PI3Kα活性抑制剂的用途，含有它们的药物组合物，以及它们作为治疗和/或预防由细胞过度或异常增殖引起的疾病及相关症状（如癌症）的药物的用途。 R1到R6和n的含义如权利要求和说明书中所述。

  公开号：

  EP2546249A1

文献信息

• [EN] NEW 5-ALKYNYL-PYRIDINES<br/>[FR] NOUVELLES 5-ALKYNYL-PYRIDINES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012101186A1

  公开（公告）日：2012-08-02

  This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of P13Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.

  这项发明涉及一般式(I)的5-炔基吡啶，它们作为P13Kalpha活性抑制剂的用途，含有它们的药物组合物，以及它们作为治疗和/或预防由过度或异常细胞增殖和相关疾病条件（如癌症）所特征的疾病的药物的用途。R1到R6和n的含义如索赔和说明书中所述。
• 5-ALKYNYL-PYRIDINES
  申请人：WUNBERG Tobias

  公开号：US20130023519A1

  公开（公告）日：2013-01-24

  5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R 1 to R 6 and n have the meanings given in the claims and in the specification.

  通式（I）的5-炔基吡啶，其作为PI3Kα活性抑制剂的用途，包含它们的制药组合物，以及它们作为治疗和/或预防由过度或异常细胞增殖所特征化的疾病及相关病症（如癌症）的药物的用途。其中，基团R1至R6和n的含义在权利要求和说明书中给出。
• ARYLOXYANILIDE IMAGING AGENTS
  申请人：GE HEALTHCARE LIMITED

  公开号：US20140288317A1

  公开（公告）日：2014-09-25

  The present invention provides a novel radiolabelled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.

  本发明提供了一种新型放射性标记的芳氧基丙氨酸衍生物，适合用于体内成像。与已知的芳氧基丙氨酸衍生物体内成像剂相比，本发明的体内成像剂具有更好的体内成像性能。本发明的体内成像剂在给予受试者后表现出良好的选择性结合外周苯二氮平受体（PBR），以及良好的大脑摄取和体内动力学。
• 5-alkynyl-pyridines
  申请人：Wunberg Tobias

  公开号：US08598157B2

  公开（公告）日：2013-12-03

  5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.

  通式为(I)的5-炔基吡啶，其作为PI3Kalpha活性抑制剂的用途，含有它们的制药组合物，以及它们作为治疗和/或预防由过度或异常细胞增殖引起的疾病及相关病症，如癌症的药物的用途。其中，基团R1至R6和n的含义在权利要求书和规范中给出。
• NEW 5-ALKYNYL-PYRIDINES
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2668179A1

  公开（公告）日：2013-12-04