4-[(1S)-1-fluoroethyl]-3-[(4-methoxyphenyl)methyl]-1,3-oxazolidin-2-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 4-[(1S)-1-fluoroethyl]-3-[(4-methoxyphenyl)methyl]-1,3-oxazolidin-2-one
• 化学式: C₁₃H₁₆FNO₃
• 分子量: 253.27
• InChiKey: BNLLBGULBQXZLD-QHGLUPRGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  38.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH<br/>[FR] 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES COMME INHIBITEURS D'IDH MUTANTE
  申请人：NOVARTIS AG

  公开号：WO2014141104A1

  公开（公告）日：2014-09-18

  The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

  这项发明涉及一种式(I)的配方，或其药用可接受的盐，其中R1、R2a、R2b和R3-R7在此处。该发明还涉及含有式(I)化合物的组合物，以及在抑制具有新型活性的突变IDH蛋白中使用这种化合物的用途。该发明还涉及在治疗与这种突变IDH蛋白相关的疾病或紊乱中使用式(I)化合物，包括但不限于细胞增殖紊乱，如癌症。
• 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH
  申请人：NOVARTIS AG

  公开号：US20150152093A1

  公开（公告）日：2015-06-04

  The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2a , R 2b and R 3 -R 7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

  该发明涉及一种公式(I)或其药学上可接受的盐，其中R1、R2a、R2b和R3-R7如下。该发明还涉及含有公式(I)化合物的组合物，并且涉及使用这些化合物来抑制具有新型活性的突变IDH蛋白质。该发明进一步涉及使用公式(I)化合物来治疗与这种突变IDH蛋白质相关的疾病或障碍，包括但不限于细胞增殖障碍，如癌症。
• 2-AMINOPYRIMIDINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
  申请人：Etern Biopharma (Shanghai) Co., Ltd.

  公开号：EP3786166A1

  公开（公告）日：2021-03-03

  The disclosure provides an aminopyrimidine derivative for preventing and treating diseases related to IDH mutation, a preparation method and use thereof. Specifically, the disclosure provides a compound of Formula I, a stereoisomer, racemate thereof, or pharmaceutically acceptable salt thereof. The compound of the general Formula I has isocitrate dehydrogenase 1 (IDH1) inhibitory activity and can treat cancer induced by IDH1 mutation.

  本公开提供了一种用于预防和治疗 IDH 突变相关疾病的氨嘧啶衍生物及其制备方法和用途。具体而言，本公开提供了通式I的化合物、其立体异构体、外消旋体或其药学上可接受的盐。通式I化合物具有异柠檬酸脱氢酶1（IDH1）抑制活性，可治疗IDH1突变诱发的癌症。
• 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
  申请人：NOVARTIS AG

  公开号：US10112931B2

  公开（公告）日：2018-10-30

  The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

  本发明涉及式 (I)： 或其药学上可接受的盐，其中 R1、R2a、R2b 和 R3-R7 在此处。本发明还涉及含有式（I）化合物的组合物，以及此类化合物在抑制具有新变态活性的突变 IDH 蛋白中的用途。本发明进一步涉及式（I）化合物在治疗与此类突变IDH蛋白相关的疾病或紊乱中的用途，包括但不限于细胞增殖紊乱，如癌症。
• Mutant IDH1 inhibitors
  申请人：Eli Lilly and Company

  公开号：US10696665B2

  公开（公告）日：2020-06-30

  The present application provides compounds of Formula I: Formula (I) that are useful as inhibitors of mutant IDH1, pharmaceutical compositions, and uses for the treatment of cancer.

  本申请提供了式 I 的化合物：式 (I) 可用作突变 IDH1 的抑制剂、药物组合物和治疗癌症的用途。