(E)-4-吗啉酮-2-烯酸盐酸盐 | 1419865-05-6

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 中文名称: (E)-4-吗啉酮-2-烯酸盐酸盐
• 英文名称: 4-Morpholin-4-yl-but-2-enoic acid hydrochloride
• 英文别名: (E)-4-morpholin-4-ylbut-2-enoic acid;hydrochloride
• CAS: 1419865-05-6；1807940-64-2
• 化学式: C8H14ClNO3
• 分子量: 207.65
• InChiKey: DQELLWQXAROXTC-TYYBGVCCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.38
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  49.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
  申请人：ANCUREALL PHARMACEUTICAL (SHANGHAI) CO., LTD.

  公开号：US20190345139A1

  公开（公告）日：2019-11-14

  The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and a use thereof as a histone methyltransferase EZH2 inhibitor for treating diseases associated with the histone methyltransferase EZH2, especially cancer. The definition of each substituents in the general formula (I) is same as the definition in the specification.

  这项发明涉及一种组蛋白甲基转移酶EZH2抑制剂，其制备方法和药用。具体而言，该发明涉及一种由通式（I）表示的化合物，其制备方法，含有该化合物的药物组合物，以及将其用作组蛋白甲基转移酶EZH2抑制剂治疗与组蛋白甲基转移酶EZH2相关的疾病，特别是癌症。通式（I）中每个取代基的定义与规范中的定义相同。
• [EN] HETEROCYCLYL SUBSTITUTED PYRROLOPYRIDINES THAT ARE INHIBITORS OF THE CDK12 KINASE<br/>[FR] PYRROLOPYRIDINES À SUBSTITUTION HÉTÉROCYCLYLE UTILISÉES EN TANT QU'INHIBITEURS DE LA KINASE CDK12
  申请人：UNIV NOTTINGHAM

  公开号：WO2019058132A1

  公开（公告）日：2019-03-28

  This invention relates to compounds that are inhibitors of the CDK12 kinase. The compounds are useful in the treatment of disorders mediated by CDK12 kinase including myotonic dystrophy type 1 (DM1) and other disorders caused by the generation of RNA repeat expansion transcripts. In particular,the invention relates to compounds of the formula (I), or a pharmaceutically acceptable salts or N-oxides thereof, wherein R1a, R2, R3, R4a, R4b and R4c are as defined herein.

  这项发明涉及抑制CDK12激酶的化合物。这些化合物可用于治疗由CDK12激酶介导的疾病，包括1型肌强直性营养不良（DM1）和其他由RNA重复扩展转录物引起的疾病。特别是，该发明涉及公式（I）的化合物，或其药用可接受的盐或N-氧化物，其中R1a, R2, R3, R4a, R4b和R4c按本文定义。
• Histone methyltransferase EZH2 inhibitor, preparation method and pharmaceutical use thereof
  申请人：ANCUREALL PHARMACEUTICAL (SHANGHAI) CO., LTD.

  公开号：US11214561B2

  公开（公告）日：2022-01-04

  The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and a use thereof as a histone methyltransferase EZH2 inhibitor for treating diseases associated with the histone methyltransferase EZH2, especially cancer. The definition of each substituents in the general formula (I) is same as the definition in the specification.

  本发明涉及一种组蛋白甲基转移酶EZH2抑制剂、其制备方法和药物用途。特别是，本发明涉及通式（I）代表的化合物、其制备方法、含有该化合物的药物组合物，以及其作为组蛋白甲基转移酶EZH2抑制剂用于治疗与组蛋白甲基转移酶EZH2相关的疾病，特别是癌症的用途。通式（I）中各取代基的定义与说明书中的定义相同。
• HETEROCYCLYL SUBSTITUTED PYRROLOPYRIDINES THAT ARE INHIBITORS OF THE CDK12 KINASE
  申请人：The University of Nottingham

  公开号：EP3684776A1

  公开（公告）日：2020-07-29