(NE)-N-[[1-(4-chlorophenyl)imidazol-4-yl]methylidene]-2-methylpropane-2-sulfinamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: (NE)-N-[[1-(4-chlorophenyl)imidazol-4-yl]methylidene]-2-methylpropane-2-sulfinamide
• 化学式: C₁₄H₁₆ClN₃OS
• 分子量: 309.8
• InChiKey: TVMCNUCMJIGQOU-CAOOACKPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  66.5
• 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。
• HETEROCYCLIC COMPOUNDS AS MUTANT IDH INHIBITORS
  申请人：INTEGRAL BIOSCIENCES PRIVATE LIMITED

  公开号：US20200206233A1

  公开（公告）日：2020-07-02

  The present disclosure relates generally to compounds useful in treatment of conditions associated with mutant isocitrate dehydrogenase (mt-IDH), particularly mutant IDH1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against mutant IDH1 enzymes. Method of treating conditions associated with excessive activity of mutant IDH1 enzymes with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.

  本公开涉及一般用于治疗与突变异柠檬酸脱氢酶（mt-IDH）相关的疾病的化合物，特别是突变IDH1酶。具体地，本发明揭示了式（IA）的化合物，该化合物对突变IDH1酶表现出抑制活性。还公开了使用该化合物治疗与突变IDH1酶过度活性相关的疾病的方法。此外，还公开了其用途、药物组合物和试剂盒。
• [EN] 1-(2-(ETHYLAMINO)PYRIMIDIN-4-YL)PYRROLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH<br/>[FR] 1-(2-(ÉTHYLAMINO)PYRIMIDIN-4-YL)PYRROLIDIN-2-ONES EN TANT QU'INHIBITEURS DU MUTANT IDH
  申请人：NOVARTIS AG

  公开号：WO2014147586A1

  公开（公告）日：2014-09-25

  The invention is directed to a formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a–R1f, R2, R3 and R4 are described 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.

  该发明涉及一种化合物(I)的公式：(I)或其药学上可接受的盐，其中R1a-R1f，R2，R3和R4如本文所述。该发明还涉及含有化合物(I)的组合物，以及利用这些化合物抑制具有新型活性的突变IDH蛋白。该发明还涉及利用化合物(I)治疗与这些突变IDH蛋白相关的疾病或疾病，包括但不限于细胞增殖异常，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。
• 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。