methyl 2,2-difluoro-2-(quinolin-6-yl)acetate | 943541-38-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: methyl 2,2-difluoro-2-(quinolin-6-yl)acetate
• 英文别名: methyl 2,2-difluoro-2-quinolin-6-ylacetate
• CAS: 943541-38-6
• 化学式: C₁₂H₉F₂NO₂
• 分子量: 237.206
• InChiKey: GLRLRHVXCLJGTB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  39.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  methyl 2,2-difluoro-2-(quinolin-6-yl)acetate 在 肼 作用下， 以 甲醇 为溶剂， 反应 2.0h， 以100%的产率得到2,2-二氟-2-(喹啉-6-基)乙酸肼
  参考文献：
  名称：

  WO2007/75567

  摘要：

  公开号：
• 作为产物：
  描述：

  oxo-quinolin-6-ylacetic acid methyl ester 在 二甲氨基三氟化硫 作用下， 以 二氯甲烷 为溶剂， 反应 48.0h， 以87%的产率得到methyl 2,2-difluoro-2-(quinolin-6-yl)acetate
  参考文献：
  名称：

  WO2007/75567

  摘要：

  公开号：

文献信息

• Fused heterocyclic derivatives and methods of use
  申请人：Albrecht Brian K.

  公开号：US20090124612A1

  公开（公告）日：2009-05-14

  Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  所选化合物对于预防和治疗疾病，如HGF介导的疾病具有有效性。本发明包括新颖的化合物、类似物、前药和其药学上可接受的盐、药物组合物和预防和治疗涉及癌症等疾病和其他疾病或病况的方法。该发明还涉及制备这样的化合物的过程，以及在这样的过程中有用的中间体。
• TRIAZOLOPYRIDAZINES AS KINASE MODULATORS
  申请人：Lu Tianbao

  公开号：US20090098181A1

  公开（公告）日：2009-04-16

  The invention is directed to triazolopyridazine compounds of Formula I: where R 1 , R 5 , R 6 , R 7 , R 8 , and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

  本发明涉及式I的三唑并吡嗪化合物：其中R1、R5、R6、R7、R8和A如本文所定义，使用这种化合物作为蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂，并使用这种化合物来减少或抑制细胞或受体中c-Met的激酶活性，调节细胞或受体中c-Met的表达，并使用这种化合物预防或治疗细胞增殖性疾病和/或与c-Met相关的疾病。本发明还涉及包含本发明化合物的制药组合物以及治疗癌症和其他细胞增殖性疾病的方法。
• FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE
  申请人：ALBRECHT Brian K.

  公开号：US20120148531A1

  公开（公告）日：2012-06-14

  Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的化合物对于预防和治疗疾病，如HGF介导的疾病，具有有效性。该发明涵盖了新颖的化合物、类似物、前药和其药学上可接受的盐、制药组合物以及用于预防和治疗涉及癌症等疾病和其他疾病或病情的方法。该发明还涉及制备这种化合物的过程以及在这种过程中有用的中间体。
• Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring <i>MET</i> Gene Alteration Treatment
  作者：Chaofan Wang、Jie Li、Lingzhi Qu、Xia Tang、Xiaojuan Song、Fang Yang、Xiaojuan Chen、Qianmeng Lin、Weibin Lin、Yang Zhou、ZhengChao Tu、Yongheng Chen、Zhang Zhang、Xiaoyun Lu

  DOI：10.1021/acs.jmedchem.2c00981

  日期：2022.11.24

  and gastric cancers. The c-Met inhibitors, capmatinib, tepotinib, and savolitinib, are only approved for the treatment of NSCLC harboring exon 14 skipping mutant MET. We used a molecular hybridization in conjunction with macrocyclization strategy for structural optimization to obtain a series of 2-(2-(quinolin-6-yl)ethyl)pyridazin-3(2H)-one derivatives as new c-Met inhibitors. One of the macrocyclic

  MET改变已被验证为 NSCLC 和胃癌的驱动因素。c-Met 抑制剂 capmatinib、tepotinib 和 savolitinib 仅被批准用于治疗携带外显子 14 跳跃突变 MET 的 NSCLC。我们使用分子杂交结合大环化策略进行结构优化，获得了一系列 2-(2-(quinolin-6-yl)ethyl)pyridazin-3(2 H )-one 衍生物作为新的 c-Met 抑制剂。其中一种大环化合物 D6808 有效抑制 c-Met 激酶和MET扩增的 Hs746T 胃癌细胞，IC 50值分别为 2.9 和 0.7 nM。它还用 IC 强烈抑制具有抗性相关突变 (F1200L/M1250T/H1094Y/F1200I/L1195V) 的 Ba/F3-Tpr-Met 细胞50 个值分别为 4.2、3.2、1.0、39.0 和 33.4 nM。此外，D6808 在针对 373
• [1,2,4]TRIAZOLO[4,3-A]PYRIDINE DERIVATIVES USEFUL AS INHIBITORS OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR
  申请人：Amgen, Inc

  公开号：EP3093289A1

  公开（公告）日：2016-11-16

  Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  所选化合物可有效预防和治疗疾病，如 HGF 介导的疾病。本发明包括新型化合物、类似物、原药及其药学上可接受的盐、药物组合物以及用于预防和治疗涉及癌症等疾病和其他弊病或病症的方法。本发明还涉及制造此类化合物的工艺以及在此类工艺中有用的中间体。