(4-Bromo-2-trifluoromethyl-phenyl)-(tetrahydro-pyran-4-yl)-amine | 1056465-05-4

• 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: (4-Bromo-2-trifluoromethyl-phenyl)-(tetrahydro-pyran-4-yl)-amine
• 英文别名: N-[4-bromo-2-(trifluoromethyl)phenyl]oxan-4-amine
• CAS: 1056465-05-4
• 化学式: C₁₂H₁₃BrF₃NO
• 分子量: 324.14
• InChiKey: BJOPFEPSTFSUFJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-氨基-5-溴三氟甲苯 、 四氢吡喃酮 、 三乙酰氧基硼氢化钠 在 二氯甲烷 、 碳酸氢钠 、 Sodium sulfate-III 、 crude product 、 silica gel 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 72.0h， 以to yield intermediate 13 as a yellow oil (1.11 g, 99%)的产率得到(4-Bromo-2-trifluoromethyl-phenyl)-(tetrahydro-pyran-4-yl)-amine
  参考文献：
  名称：

  3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES

  摘要：

  本发明涉及新型化合物，特别是根据公式（I）的新型吡啶酮衍生物，包括其任何立体化异构体形式，或其药学上可接受的盐或其溶剂化物，其中所有基团在申请和权利要求中均有定义。本发明的化合物是代谢型谷氨酸受体亚型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相关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。特别地，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。本发明还涉及制备这些化合物及其制剂的制药组合物和方法，以及使用这些化合物预防和治疗涉及mGluR2的这些疾病。

  公开号：

  US20100087487A1

文献信息

• 3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES
  申请人：Cid-Núñez José Maria

  公开号：US20100087487A1

  公开（公告）日：2010-04-08

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate 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 such 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，特别是根据公式（I）的新型吡啶酮衍生物，包括其任何立体化异构体形式，或其药学上可接受的盐或其溶剂化物，其中所有基团在申请和权利要求中均有定义。本发明的化合物是代谢型谷氨酸受体亚型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相关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。特别地，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。本发明还涉及制备这些化合物及其制剂的制药组合物和方法，以及使用这些化合物预防和治疗涉及mGluR2的这些疾病。
• US8796311B2
  申请人：——

  公开号：US8796311B2

  公开（公告）日：2014-08-05
• US8906939B2
  申请人：——

  公开号：US8906939B2

  公开（公告）日：2014-12-09
• [EN] 3-CYANO-4-(4-TETRAHYDROPYRAN-PHENYL)-PYRIDIN-2-ONE DERIVATIVES<br/>[FR] DÉRIVÉS DE 3-CYANO-4-(4-TÉTRAHYDROPYRANE-PHÉNYL)-PYRIDIN-2-ONE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2008107481A1

  公开（公告）日：2008-09-12

  [EN] The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate 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 centralnervous 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 such compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
  [FR] La présente invention porte sur de nouveaux composés, en particulier de nouveaux dérivés de pyridinone selon la Formule (I) comprenant n'importe quelle forme stéréochimiquement isomère de ceux-ci, ou sur un sel pharmaceutiquement acceptable de ceux-ci ou un solvate de ceux-ci, où tous les radicaux sont définis dans la description et les revendications. Les composés selon l'invention sont des modulateurs allostériques positifs de récepteurs métabotropiques du glutamate sous-type 2 (= mGluR2 =) utiles dans le traitement ou la prévention de troubles neurologiques et psychiatriques associés au dysfonctionnement du glutamate et de maladies dans lesquelles le sous-type mGluR2 des récepteurs métabotropiques est mis en jeu, en particulier des troubles du système nerveux central dont l'anxiété, la schizophrénie, la migraine, la dépression et l'épilepsie. L'invention porte également sur des compositions pharmaceutiques et des procédés pour préparer de tels composés et de telles compositions, ainsi que sur l'utilisation de tels composés pour la prévention et le traitement de maladies dans lesquelles mGluR2 est mis en jeu.
• 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
  申请人：Cid-Nunez Jose Maria

  公开号：US08796311B2

  公开（公告）日：2014-08-05

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate 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 such 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，特别是根据式（I）的新型吡啶酮衍生物，包括其任何立体化异构体形式、药学上可接受的盐或其溶剂化物，其中所有基团在申请和权利要求中都有定义。本发明的化合物是代谢型谷氨酸受体亚型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相关的神经和精神障碍以及mGluR2代谢型受体参与的疾病。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中选择的。本发明还涉及制备这种化合物和这种组合物的制药组合物和过程，以及利用这种化合物预防和治疗mGluR2参与的这种疾病。