(+/-)-2-[4-[1-amino-ethyl]-3-fluoro-phenyl]-propan-2-ol | 353282-72-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (+/-)-2-[4-[1-amino-ethyl]-3-fluoro-phenyl]-propan-2-ol
• 英文别名: 2-[4-(1-aminoethyl)-3-fluorophenyl]propan-2-ol
• CAS: 353282-72-1
• 化学式: C₁₁H₁₆FNO
• 分子量: 197.253
• InChiKey: XXDNNODEUGVVFV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (+/-)-2-[1-[2-fluoro-4-[1-hydroxy-1-methyl-ethyl]-phenyl]-ethyl]-isoindole-1,3-dione 在 一水合肼 作用下， 以 甲醇 为溶剂， 生成 (+/-)-2-[4-[1-amino-ethyl]-3-fluoro-phenyl]-propan-2-ol
  参考文献：
  名称：

  Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of pde4 isozymes

  摘要：

  在治疗由嗜酸性粒细胞的激活和脱颗粒调节的疾病，特别是哮喘、慢性支气管炎和慢性阻塞性肺病中作为PDE4抑制剂有用的化合物，其化学式为（1.0.0）： 其中R5和R6一起取代形成部分化学式（1.1.1）至（1.1.5）的基团， 或其药用可接受的盐。

  公开号：

  US20030186989A1

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。
• Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of PDE4 isozymes
  申请人：Pfizer Products Inc.

  公开号：US07354941B2

  公开（公告）日：2008-04-08

  Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of Formula (1.0.0): wherein R5 and R6 are taken together to form a moiety of partial Formulas (1.1.1) through (1.1.5): or a pharmaceutically acceptable salt thereof.

  本发明涉及一种化合物，其在治疗由嗜酸性粒细胞的激活和脱颗粒调节的疾病中，特别是哮喘、慢性支气管炎和慢性阻塞性肺疾病中作为PDE4抑制剂有用。该化合物的化学式为(1.0.0)，其中R5和R6共同形成部分化学式(1.1.1)至(1.1.5)中的一个，或其药学上可接受的盐。
• 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。
• NICOTINAMIDE BENZOFUSED-HETEROCYCLYL DERIVATIVES USEFUL AS SELECTIVE INHIBITORS OF PDE4 ISOZYMES
  申请人：Pfizer Products Inc.

  公开号：EP1252158A1

  公开（公告）日：2002-10-30