2-[4-(4-bromophenoxy)phenyl]propan-2-ol | 1128150-10-6

• 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-(4-bromophenoxy)phenyl]propan-2-ol
• 英文别名: 2-[4-(4-Bromo-phenoxy)-phenyl]-propan-2-ol
• CAS: 1128150-10-6
• 化学式: C₁₅H₁₅BrO₂
• 分子量: 307.187
• InChiKey: DVDXSFVJGQRUGM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1-(4-(4-溴苯氧基)苯基)乙酮 、 甲基溴化镁 在 水 、 氯化铵 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 以75%的产率得到2-[4-(4-bromophenoxy)phenyl]propan-2-ol
  参考文献：
  名称：

  [EN] 1,3-DISUBSTITUTED 4-(ARYL-X-PHENYL)-1H-PYRIDIN-2-ONES
  [FR] 4-(ARYL-X-PHÉNYL)-1H-PYRIDINE-2-ONES 1,3-DISUBSTITUÉES

  摘要：

  本发明涉及新化合物，特别是根据式（I）的新吡啶酮衍生物，其中所有基团如申请和索赔中所定义。根据本发明的化合物是代谢型受体-亚型2（'mGluR2'）的阳性别构调节剂，对与谷氨酸功能障碍相关的神经系统和精神障碍以及涉及代谢型受体亚型mGluR2的疾病的治疗或预防是有用的。具体来说，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等疾病组中选择的中枢神经系统疾病。该发明还涉及制备这种化合物和组合物的药物组合物和方法，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病。

  公开号：

  WO2009033702A1

文献信息

• 1,3-DISUBSTITUTED 4-(ARYL-X-PHENYL)-1H-PYRIDIN-2-ONES
  申请人：DUVEY Guillaume Albert Jacques

  公开号：US20120309793A1

  公开（公告）日：2012-12-06

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新颖化合物，特别是公式（I）中定义的新型吡啶酮衍生物，其中所有基团均如申请和权利要求中所定义。本发明的化合物是代谢型受体-亚型2（“mGluR2”）的正变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体mGluR2亚型的疾病。特别是，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病组中选择的。本发明还涉及制备这样的化合物和组合物的制药组合物和过程，以及使用这些化合物预防和治疗涉及mGluR2的这些疾病。
• 1,3-disubstituted 4-(aryl-X-phenyl)-1H-pyridin-2-ones
  申请人：Janssen Pharmaceuticals, Inc.

  公开号：US08252937B2

  公开（公告）日：2012-08-28

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是公式（I）中定义的新型吡啶酮衍生物，其中所有基团均如本申请和权利要求所定义。本发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。特别是，这些疾病是选自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的一组。本发明还涉及制备这些化合物和组合物的制药组合物和过程，以及将这些化合物用于预防和治疗涉及mGluR2的这些疾病的用途。
• US8252937B2
  申请人：——

  公开号：US8252937B2

  公开（公告）日：2012-08-28
• US8748621B2
  申请人：——

  公开号：US8748621B2

  公开（公告）日：2014-06-10
• [EN] 1,3-DISUBSTITUTED 4-(ARYL-X-PHENYL)-1H-PYRIDIN-2-ONES<br/>[FR] 4-(ARYL-X-PHÉNYL)-1H-PYRIDINE-2-ONES 1,3-DISUBSTITUÉES
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2009033702A1

  公开（公告）日：2009-03-19

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I), wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors - subtype 2 ('mGluR2') which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新化合物，特别是根据式（I）的新吡啶酮衍生物，其中所有基团如申请和索赔中所定义。根据本发明的化合物是代谢型受体-亚型2（'mGluR2'）的阳性别构调节剂，对与谷氨酸功能障碍相关的神经系统和精神障碍以及涉及代谢型受体亚型mGluR2的疾病的治疗或预防是有用的。具体来说，这些疾病是从焦虑、精神分裂症、偏头痛、抑郁症和癫痫等疾病组中选择的中枢神经系统疾病。该发明还涉及制备这种化合物和组合物的药物组合物和方法，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病。