2,3,6,7-tetrahydro-pyrrolo[1,2-a]pyrazine-1,4-dione | 65987-08-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2,3,6,7-tetrahydro-pyrrolo[1,2-a]pyrazine-1,4-dione
• 英文别名: hexahydro-pyrrolo[1,2-a]pyrazine-1,4-dione；2,3,6,7-Tetrahydropyrrolo[1,2-a]pyrazine-1,4-dione
• CAS: 65987-08-8
• 化学式: C₇H₈N₂O₂
• 分子量: 152.153
• InChiKey: SQKSYNMJFDKARV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  49.4
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 6' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
  申请人：Dunn Robert

  公开号：US20080200471A1

  公开（公告）日：2008-08-21

  The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R 1 —R 4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

  本公开提供了具有亲和力的化合物，其对5-HT6受体具有亲和力，其化学式为（I）： 其中R1-R4，A，B，D，E和G如本文所定义。该公开还涉及制备这种化合物的方法，含有这种化合物的组合物，以及这些化合物的使用方法。
• Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
  申请人：Altenbach J. Robert

  公开号：US20050272736A1

  公开（公告）日：2005-12-08

  Compounds of formula (I) wherein R 1 or R 2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, X, X′, Y, Y′, Z, and Z′ are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

  式（I）中R1或R2为含有至少两个杂原子的三环或二环环，其中R1、R2、R3、R3a、R3b、R4、R5、L、X、X′、Y、Y′、Z和Z′如本文所定义，在预防或改善组织胺-3受体配体引起的病症或紊乱方面具有治疗作用。还公开了包含组织胺-3受体配体的药物组合物，使用这类化合物和组合物的方法，以及制备符合式（I）范围内化合物的过程。
• Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands
  申请人：Altenbach J. Robert

  公开号：US20050256309A1

  公开（公告）日：2005-11-17

  Compounds of formula (I) wherein R 1 or R 2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, X, X′, Y, Y′, Z, and Z′ are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

  式（I）中R1或R2为含有至少两个杂原子的三环或二环环，其中R1、R2、R3、R3a、R3b、R4、R5、L、X、X′、Y、Y′、Z和Z′如本文所定义，在预防或改善组织胺-3受体配体引起的病症或紊乱方面具有治疗作用。还公开了包含组织胺-3受体配体的药物组合物，使用这类化合物和组合物的方法，以及制备符合式（I）范围内化合物的方法。
• [EN] SUBSTITUTED HEXAHYDROPYRROLO[1,2-A]PYRAZINES, OCTAHYDROPYRIDO[1,2-A]PYRAZINES AND DECAHYDROPYRAZINO[1,2-A]AZEPINES<br/>[FR] AZEPINES ET PYRAZINES SUBSTITUEES
  申请人：NOVO NORDISK AS

  公开号：WO2003104235A1

  公开（公告）日：2003-12-18

  Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

  小说替代的六氢吡咯并[1,2-a]吡嗪、八氢吡啶并[1,2-a]吡嗪和十氢吡嗪并[1,2-a]氮杂环庚烷，这些化合物作为制药组合物的用途，包含这些化合物的制药组合物，以及利用这些化合物和组合物进行治疗的方法。这些化合物表现出高度和选择性的结合亲和性，表明其具有组胺H3受体拮抗、反向激动活性。因此，这些化合物对于治疗与组胺H3受体相关的疾病和障碍是有用的。
• Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
  申请人：——

  公开号：US20040023946A1

  公开（公告）日：2004-02-05

  Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1 ,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

  这篇文章介绍了一种新型的代替品，包括取代的六氢吡咯并[1,2-a]吡嗪、八氢吡咯并[1,2-a]吡嗪和十氢吡嗪并[1,2-a]氮杂七环，以及这些化合物的药物组成物的使用，包括这些化合物的药物组成物，以及使用这些化合物和组成物的治疗方法。这些化合物表现出对组胺H3受体的高度和选择性结合亲和力，表明具有组胺H3受体拮抗、反向激动剂或激动剂活性。因此，这些化合物可用于治疗与组胺H3受体相关的疾病和障碍。