3-methyl-3-ethoxyazetidine hydrochloride | 1807872-03-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: 3-methyl-3-ethoxyazetidine hydrochloride
• 英文别名: 3-ethoxy-3-methylazetidine hydrochloride；3-Ethoxy-3-methylazetidine HCl；3-ethoxy-3-methylazetidine;hydrochloride
• CAS: 1807872-03-2
• 化学式: C₆H₁₃NO*ClH
• 分子量: 151.636
• InChiKey: CSZSLKOMLADLFF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.81
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-methyl-3-ethoxyazetidine hydrochloride 在 tris-(dibenzylideneacetone)dipalladium(0) 、 水 、 caesium carbonate 、 sodium hydroxide 、 2-二环己基磷-2',6'-二异丙氧基-1,1'-联苯 作用下， 以 1,4-二氧六环 、 甲醇 为溶剂， 反应 3.0h， 生成 6-(3-ethoxy-3-methylazetidin-1-yl)quinoline-4-carboxylic acid
  参考文献：
  名称：

  [EN] N-(2-(4-CYANOTHIAZOLIDIN-3-YL)-2-OXOETHYL)- QUINOLINE-4-CARBOXAMIDES
  [FR] N-(2-(4-CYANOTHIAZOLIDIN-3-YL)-2-OXOÉTHYL)-QUINOLÉINE-4-CARBOXAMIDES

  摘要：

  具有公式（I）结构及其药学上可接受的盐的化合物，其中X1，R1，R2，R3，R4，R5和R6如规范中所定义; 包括此类化合物和盐的制药组合物; 使用此类化合物和盐来治疗或预防脯氨酰内切酶成纤维细胞激活蛋白（FAP）介导的疾病; 包含此类化合物和盐的试剂盒; 以及制造此类化合物和盐的方法。

  公开号：

  WO2022130270A1

文献信息

• N2-phenyl-pyrido[3,4-D]pyrimidine-2, 8-diamine derivatives and their use as Mps1 inhibitors
  申请人：Cancer Research Technology Limited

  公开号：US10399974B2

  公开（公告）日：2019-09-03

  The present invention relates to compounds of formula I: wherein R1, R2, R3 and R4 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、R2、R3 和 R4 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。
• N2-PHENYL-PYRIDO[3,4-D]PYRIMIDINE-2,8-DIAMINE DERIVATIVES AND THEIR USE AS MPS1 INHIBITORS
  申请人：Cancer Research Technology Ltd

  公开号：EP3110816B1

  公开（公告）日：2019-06-19
• N2-PHENYL-PYRIDO[3,4-D]PYRIMIDINE-2, 8-DIAMINE DERIVATIVES AND THEIR USE AS MPS1 INHIBITORS
  申请人：CANCER RESEARCH TECHNOLOGY LIMITED

  公开号：US20160362409A1

  公开（公告）日：2016-12-15

  The present invention relates to compounds of formula I: wherein R 1 , R 2 , R 3 and R 4 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.
• N2-PHENYL-PYRIDO[3,4- D]PYRIMIDINE-2, 8-DIAMINE DERIVATIVES AND THEIR USE AS MPS1 INHIBITORS
  申请人：Cancer Research Technology Limited

  公开号：US20180194761A1

  公开（公告）日：2018-07-12

  The present invention relates to compounds of formula I: wherein R 1 , R 2 , R 3 and R 4 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.
• US9902721B2
  申请人：——

  公开号：US9902721B2

  公开（公告）日：2018-02-27