4-(5-Chloropyridin-2-yl)piperazine-1-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 4-(5-Chloropyridin-2-yl)piperazine-1-carboxylic acid
• 英文别名: 4-(5-chloropyridin-2-yl)piperazine-1-carboxylic acid
• 化学式: C₁₀H₁₂ClN₃O₂
• 分子量: 241.67
• InChiKey: WYIFRIWAYZSUNF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  56.7
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS<br/>[FR] COMPOSÉS 6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE ET LEUR UTILISATION COMME MODULATEURS ALLOSTÉRIQUES NÉGATIFS DES RÉCEPTEURS MGLUR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2014195311A1

  公开（公告）日：2014-12-11

  The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders.

  本发明涉及一种新型的Formula (I)的6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮衍生物，作为代谢型谷氨酸受体亚型2 ("mGluR2")的负变构调节剂（NAMs）。该发明还涉及包含这些化合物的药物组合物，用于制备这些化合物和组合物的方法，以及用于预防或治疗涉及代谢型受体亚型2的疾病的化合物和组合物的用途，特别是中枢神经系统疾病。
• 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：US20160115169A1

  公开（公告）日：2016-04-28

  The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.

  本发明涉及一种新型的6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮衍生物，作为代谢型谷氨酸受体亚型2（“mGluR2”）的负向变构调节剂（NAMs）。本发明还涉及包含这些化合物的制药组合物、制备这些化合物和组合物的方法，以及使用这些化合物和组合物预防或治疗与代谢型受体亚型2有关的疾病。
• Substituted 6,7-dihydropyrazolo[1,5-a]pyrazines as negative allosteric modulators of mGluR2 receptors
  申请人：Janssen Pharmaceutica NV

  公开号：US10106542B2

  公开（公告）日：2018-10-23

  The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”) useful for the treatment of central nervous system disorders in which the mGluR2 subtype of metabotropic receptors is involved (e.g. mood disorder, schizophrenia, etc.). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for treatment of central nervous system disorders in which the mGluR2 subtype of metabotropic receptors is involved.

  本发明涉及式 (I) 的新型 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮衍生物 作为代谢谷氨酸受体亚型 2（"mGluR2"）的负异位调节剂（NAMs），可用于治疗涉及代谢受体 mGluR2 亚型的中枢神经系统疾病（如情绪障碍、精神分裂症等）。本发明还涉及包含此类化合物的药物组合物、制备此类化合物和组合物的工艺，以及使用此类化合物和组合物治疗涉及mGluR2亚型代谢受体的中枢神经系统疾病。
• 6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP3004107B1

  公开（公告）日：2017-05-10
• SUBSTITUTED 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZINES AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
  申请人：Janssen Pharmaceutica NV

  公开号：US20190055257A1

  公开（公告）日：2019-02-21

  The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.