N-(2-methoxy-4-morpholinophenyl)formamide | 1578246-48-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: N-(2-methoxy-4-morpholinophenyl)formamide
• 英文别名: N-(2-methoxy-4-morpholin-4-ylphenyl)formamide
• CAS: 1578246-48-6
• 化学式: C₁₂H₁₆N₂O₃
• 分子量: 236.271
• InChiKey: RVHCWNKODCGMBG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  50.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS
  申请人：CANCER REC TECH LTD

  公开号：WO2014037750A1

  公开（公告）日：2014-03-13

  The present invention relates to compounds of formula (I), wherein R, R, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

  本发明涉及式(I)的化合物，其中R、R、Ar、W、X和Z均如本文所定义。本发明的化合物已知可以通过直接或间接地与Mps1激酶本身相互作用来抑制单丝粒体1（Mps1，也称为TTK）激酶的纺锤体检查点功能。具体而言，本发明涉及将这些化合物用作治疗和/或预防增殖性疾病，如癌症的治疗剂。本发明还涉及制备这些化合物的方法，以及包含它们的药物组合物。
• INHIBITOR COMPOUNDS
  申请人：CANCER RESEARCH TECHNOLOGY

  公开号：US20150239884A1

  公开（公告）日：2015-08-27

  The present invention relates to compounds of formula I wherein R 1 , R 4 , Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

  本发明涉及式I的化合物，其中R1、R4、Ar、W、X和Z均如本文所定义。本发明的化合物已知能够直接或间接地通过与Mps1激酶本身的相互作用来抑制单纺锤体1（Mps1，也称为TTK）激酶的纺锤体检查点功能。特别地，本发明涉及使用这些化合物作为治疗和/或预防增生性疾病，如癌症的治疗剂。本发明还涉及制备这些化合物的过程，以及包含它们的药物组合物。
• PYRIDO[3,4-D]PYRIMIDINE DERIVATIVE AND THERAPEUTIC PHARMACEUTIC COMPOSITION COMPRISING SAME
  申请人：Korea Institute of Science and Technology

  公开号：EP4105213A1

  公开（公告）日：2022-12-21

  The present invention relates to a pyrido[[3,4-d]pyrimidine derivative compound showing excellent antiproliferative efficacy against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating, or treating cancer metastasis and proliferative diseases containing the same as an active ingredient, and an anticancer composition for cancer cells. The compound exhibits excellent inhibitory activity and antiproliferative efficacy against cancer cells, and thus the compound is useful not only for inhibiting cancer cells, but also for preventing cancer metastasis and proliferative diseases or for treating cancer.

  本发明涉及一种吡啶并[[3,4-d]嘧啶衍生物化合物，其对癌细胞具有出色的抗增殖功效，以及其药学上可接受的盐、水合物或立体异构体、其生产方法、以该化合物为活性成分的预防、缓解或治疗癌转移和增生性疾病的药物组合物，以及用于癌细胞的抗癌组合物。该化合物表现出优异的抑制活性和抗增殖功效，因此该化合物不仅有助于抑制癌细胞，还可用于预防癌转移和增生性疾病或治疗癌症。
• NOVEL PYRIDO[3,4-D]PYRIMIDIN-8-ONE DERIVATIVE HAVING PROTEIN KINASE INHIBITORY ACTIVITY, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING, ALLEVIATING, OR TREATING CANCER, COMPRISING SAME
  申请人：Korea Institute of Science and Technology

  公开号：EP3929195A1

  公开（公告）日：2021-12-29

  The present disclosure relates to a pyrido[3,4-d]pyrimidin-8-one derivative compound exhibiting excellent anti-proliferative effects against cancer cells, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a stereoisomer thereof, a production method therefor, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative disease containing the same as an active ingredient, and an anticancer composition against cancer cells. The compound exhibits excellent cancer cell inhibitory activity and anti-proliferative effects, and thus is effective in inhibiting cancer cells, preventing cancer metastasis and proliferative diseases or treating cancer.

  本公开涉及一种对癌细胞具有优异抗增殖作用的吡啶并[3,4-d]嘧啶-8-酮衍生物化合物、其药学上可接受的盐、其水合物或其立体异构体、其生产方法、以其为活性成分的用于预防、缓解或治疗癌症转移和增殖性疾病的药物组合物，以及一种针对癌细胞的抗癌组合物。该化合物具有优异的癌细胞抑制活性和抗增殖作用，因此可有效抑制癌细胞、预防癌症转移和增殖性疾病或治疗癌症。
• Compounds that inhibit MPS1 kinase
  申请人：Cancer Research Technology Limited

  公开号：US10479788B2

  公开（公告）日：2019-11-19

  The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

  本发明涉及式 I 的化合物 其中 R1、R4、Ar、W、X 和 Z 均如本文所定义。已知本发明的化合物可直接或间接通过与 Mps1 激酶本身的相互作用抑制 Monospindle 1（Mps1--又称 TTK）激酶的纺锤体检查点功能。特别是，本发明涉及将这些化合物用作治疗和/或预防癌症等增殖性疾病的治疗剂。本发明还涉及这些化合物的制备工艺以及包含这些化合物的药物组合物。