1-(2,4-difluorobenzyl)-5-(benzofuran-2-yl)pyridin-2(1H)-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并呋喃
• 英文名称: 1-(2,4-difluorobenzyl)-5-(benzofuran-2-yl)pyridin-2(1H)-one
• 英文别名: 5-(1-Benzofuran-2-yl)-1-[(2,4-difluorophenyl)methyl]pyridin-2-one
• 化学式: C₂₀H₁₃F₂NO₂
• 分子量: 337.326
• InChiKey: MRIHTNBBGHKTEL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  33.4
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• NOVEL PYRIDINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS
  申请人：Imogai Julien Hassan

  公开号：US20070213323A1

  公开（公告）日：2007-09-13

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) X R1 N Y (I) R2 R3 wherein all radicals are defined in the application. 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，特别是按照公式（I）X R1 N Y（I）R2 R3定义的新型吡啶酮衍生物。该发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，适用于治疗或预防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2的疾病。特别是，这些疾病是选择自焦虑、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种化合物和组合物的制药组合物和制备过程，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病的用途。
• US8399493B2
  申请人：——

  公开号：US8399493B2

  公开（公告）日：2013-03-19